Journal articles on the topic 'Bioactive gla'
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Zhu, Weidong, Yi Zhang, Yueshan Li, and Hao Wu. "Glaucocalyxin A Attenuates IL-1β-Induced Inflammatory Response and Cartilage Degradation in Osteoarthritis Chondrocytes via Inhibiting the Activation of NF-κB Signaling Pathway." Disease Markers 2022 (February 26, 2022): 1–9. http://dx.doi.org/10.1155/2022/6516246.
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Glaucocalyxin A (GLA) is a bioactive natural compound with anti-inflammatory activity. Herein, the role of GLA in osteoarthritis (OA) was evaluated. Our results demonstrated that the IL-1β-induced inducible nitric oxide synthase (iNOS) and cyclooygenase-2 (COX-2) expression, two enzymes resulting in the release of nitric oxide (NO) and PGE2, were also prevented by GLA in chondrocytes. Moreover, GLA suppressed inflammatory cytokines production in chondrocytes. In addition, the elevated expressions of MMPs and ADAMTSs and the degradation of aggrecan and collagen II were reversed by GLA in chondrocytes. Furthermore, GLA decreased p-p65 level and suppressed the nuclear p65 accumulation in the nucleus of chondrocytes. Collectively, we concluded that GLA attenuated inflammatory response in chondrocytes via NF-κB pathway. These findings suggested that GLA might become an effective agent for OA treatment.
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González-Fernández, María José, Ignacio Ortea, and José Luis Guil-Guerrero. "α-Linolenic and γ-linolenic acids exercise differential antitumor effects on HT-29 human colorectal cancer cells." Toxicology Research 9, no. 4 (July 2020): 474–83. http://dx.doi.org/10.1093/toxres/tfaa046.
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Abstract α-Linolenic acid (ALA, 18:3n-3) and γ-gamma linolenic acid (GLA, 18:3n-6) are polyunsaturated fatty acids (PUFA) that improve the human health. The present study focused on testing the in vitro antitumor actions of pure ALA and GLA on the HT-29 human colorectal cancer cell line. Cell viability was checked by MTT ((3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) test, cell membrane damage by the lactate dehydrogenase assay, apoptosis was tested by both caspase-3 activity trial and transmission electron microscopy images, and protein composition was analyzed by quantitative proteomics analysis. MTT test revealed IC50 values of 230 and 255 μM for ALA and GLA, respectively, at 72 h. After 24 h of incubation, both ALA and GLA induced apoptosis on HT-29 colorectal cancer cells according to the caspase-3 assay and microscopy images. SWATH/MS analysis evidenced that ALA significantly affected the mitochondrial protein import pathway and the citric acid cycle pathway, while GLA did not significantly affect any particular pathway. In summary, both ALA and GLA showed concentration-dependent inhibitory effects on HT-29 cells viability and induced cell death by apoptosis. ALA significantly affected cellular pathways, while GLA does not have specific actions on either pathway. Both n-3 and n-6 C18 PUFA are bioactive food components useful in the colorectal cancer prevention.
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Das, Undurti N. "“Cell Membrane Theory of Senescence” and the Role of Bioactive Lipids in Aging, and Aging Associated Diseases and Their Therapeutic Implications." Biomolecules 11, no. 2 (February 8, 2021): 241. http://dx.doi.org/10.3390/biom11020241.
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Lipids are an essential constituent of the cell membrane of which polyunsaturated fatty acids (PUFAs) are the most important component. Activation of phospholipase A2 (PLA2) induces the release of PUFAs from the cell membrane that form precursors to both pro- and ant-inflammatory bioactive lipids that participate in several cellular processes. PUFAs GLA (gamma-linolenic acid), DGLA (dihomo-GLA), AA (arachidonic acid), EPA (eicosapentaenoic acid) and DHA (docosahexaenoic acid) are derived from dietary linoleic acid (LA) and alpha-linolenic acid (ALA) by the action of desaturases whose activity declines with age. Consequently, aged cells are deficient in GLA, DGLA, AA, AA, EPA and DHA and their metabolites. LA, ALA, AA, EPA and DHA can also be obtained direct from diet and their deficiency (fatty acids) may indicate malnutrition and deficiency of several minerals, trace elements and vitamins some of which are also much needed co-factors for the normal activity of desaturases. In many instances (patients) the plasma and tissue levels of GLA, DGLA, AA, EPA and DHA are low (as seen in patients with hypertension, type 2 diabetes mellitus) but they do not have deficiency of other nutrients. Hence, it is reasonable to consider that the deficiency of GLA, DGLA, AA, EPA and DHA noted in these conditions are due to the decreased activity of desaturases and elongases. PUFAs stimulate SIRT1 through protein kinase A-dependent activation of SIRT1-PGC1α complex and thus, increase rates of fatty acid oxidation and prevent lipid dysregulation associated with aging. SIRT1 activation prevents aging. Of all the SIRTs, SIRT6 is critical for intermediary metabolism and genomic stability. SIRT6-deficient mice show shortened lifespan, defects in DNA repair and have a high incidence of cancer due to oncogene activation. SIRT6 overexpression lowers LDL and triglyceride level, improves glucose tolerance, and increases lifespan of mice in addition to its anti-inflammatory effects at the transcriptional level. PUFAs and their anti-inflammatory metabolites influence the activity of SIRT6 and other SIRTs and thus, bring about their actions on metabolism, inflammation, and genome maintenance. GLA, DGLA, AA, EPA and DHA and prostaglandin E2 (PGE2), lipoxin A4 (LXA4) (pro- and anti-inflammatory metabolites of AA respectively) activate/suppress various SIRTs (SIRt1 SIRT2, SIRT3, SIRT4, SIRT5, SIRT6), PPAR-γ, PARP, p53, SREBP1, intracellular cAMP content, PKA activity and peroxisome proliferator-activated receptor γ coactivator 1-α (PGC1-α). This implies that changes in the metabolism of bioactive lipids as a result of altered activities of desaturases, COX-2 and 5-, 12-, 15-LOX (cyclo-oxygenase and lipoxygenases respectively) may have a critical role in determining cell age and development of several aging associated diseases and genomic stability and gene and oncogene activation. Thus, methods designed to maintain homeostasis of bioactive lipids (GLA, DGLA, AA, EPA, DHA, PGE2, LXA4) may arrest aging process and associated metabolic abnormalities.
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Ciganović, Petar, Katarzyna Jakimiuk, Michał Tomczyk, and Marijana Zovko Končić. "Glycerolic Licorice Extracts as Active Cosmeceutical Ingredients: Extraction Optimization, Chemical Characterization, and Biological Activity." Antioxidants 8, no. 10 (October 1, 2019): 445. http://dx.doi.org/10.3390/antiox8100445.
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A green ultrasound-assisted extraction (UAE) method using glycerol/water mixtures for extraction of licorice (Glycyrrhiza glabra) bioactive constituents was developed in this study. The response surface method, according to the Box-Behnken design, was employed to optimize the extraction parameters: glycerol concentration (X1), temperature (X2), and the amount of herbal drug used in the production (X3). The responses were content of total phenols (TP), TP extraction efficiency (TPy) and the content of licorice characteristic constituents, glabridin (Gla) and isoliquiritigenin (Iso). Response surface analysis predicted the optimal extraction conditions for maximized amounts of TP, Tpy, Gla, and Iso. The extracts were prepared using the calculated conditions. The analysis of the selected constituents confirmed the validity of the model. Furthermore, biological activity of the extracts was tested. The results demonstrate that UAE using glycerol is a fast and efficient method for preparation of extracts with excellent radical scavenging, Fe2+ chelating and antioxidant activity. Furthermore, the observed notable tyrosinase and elastase inhibitory activity of the extracts, as well as their anti-inflammatory activity, indicate the anti-aging properties of the investigated extracts. The fact that the extracts were prepared using the safe, cosmetically active solvent, glycerol, makes them suitable for direct use in specialized cosmeceutical formulations.
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Ørnsrud, R., E. J. Lock, C. N. Glover, and G. Flik. "Retinoic acid cross-talk with calcitriol activity in Atlantic salmon (Salmo salar)." Journal of Endocrinology 202, no. 3 (June 16, 2009): 473–82. http://dx.doi.org/10.1677/joe-09-0199.
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Vitamins A (VA) and D (VD) are metabolised by vertebrates to bioactive retinoic acid (RA) and calcitriol (CTR). RA and CTR involvement in bone metabolism requires fine-tuned regulation of their synthesis and breakdown. In mammals antagonism of VA and VD is observed, but the mechanism of interaction is unknown. We investigated VA–VD interactions in Atlantic salmon (Salmo salar L.) following i.p. injection of RA and/or CTR. VA metabolites, CTR, calcium (Ca), magnesium (Mg) and phosphorus (P) were determined in plasma. Expression of bone matrix Gla protein (mgp), collagen 1 alpha2 chain (col1a2) and alkaline phosphatase (alp) mRNA was quantified to reflect osteogenesis. Branchial epithelial Ca channel (ecac listed as trpv6 in ZFIN Database) mRNA levels and intestinal Ca and P influx were determined to study Ca/P handling targets of RA and CTR. RA-injection (with or without CTR) decreased plasma CTR-levels three- to sixfold. CTR injection did not affect RA metabolites, but lowered CTR in plasma 3 and 5 days after injection. Lowered plasma CTR correlated with decreased mgp and col1a2 expression in all groups and with decreased alp in CTR-injected fish. RA-treated salmon had enhanced alp expression, irrespective of reduced plasma CTR. Expression of ecac and unidirectional intestinal influx of Ca were stimulated following RA–CTR treatment. Plasma Ca, Mg and P were not affected by any treatment. The results suggest cross-talk of RA with the VD endocrine system in Atlantic salmon. Enhanced Ca flux and osteogenesis (alp transcription) in RA-treated fish and inhibition of mgp expression revealed unprecedented disturbance of Ca physiology in hypervitaminosis A.
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El Baky, Hanaa H. Abd, Gamal S. El Baroty, and Enas M. Mostafa. "Optimization Growth of Spirulina (Arthrospira) Platensis in Photobioreactor Under Varied Nitrogen Concentration for Maximized Biomass, Carotenoids and Lipid Contents." Recent Patents on Food, Nutrition & Agriculture 11, no. 1 (April 29, 2020): 40–48. http://dx.doi.org/10.2174/2212798410666181227125229.
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Aims and Background: Spirulina (Arthrospira) platensis (SP) microalgae were cultured in Zarrouk Medium (ZM), containing three nitrogen concentrations (N-limited, N-optimal and Nrich medium) in ten liter-photo-bioreactor (10 L PBR) for 15-days, in order to study changes in lipid compounds (total carotenoids and total lipids and their effect on fatty acid profile). Based on US patent, the yield of bioactive compounds (such as gamma-linolenic acid GLA, C18:3) extracted from microalgae biomass, mainly depends on the extraction processes (1). GLA has much attention with respect to its therapeutic properties such as its ability to decrease blood cholesterol levels. Methods: The impact of the addition of N in cultures of S. platensis in terms of growth, biomasses and induced lipid compounds (total carotenoids and total lipid contents and its fatty acid profile), as well as the Sonication (SON) and Microwave (MIC) process as aiding techniques for lipid extraction compared with a Cold Condition (COL), was examined. GC/MS method was used to determine the fatty acid profile of lipid extract of SP cultures. Results: In all S. platensis tested culture, the SP was growing successfully, with varying degrees. In N-rich media, the highest cell growth rate and biomass yield were obtained compared with that recorded in other cultures. Under an N-limited condition, SP had higher Total Carotenoids (TCAR, 45.54 mg/g dw) and total lipid contents (TL, 29.51%± 1.92 g/100g dw) compared with that recorded either in N-rich (11.2 mg/g dw) or in N-optimal (6.23 mg/g dw) cultures. Thus, SP copes with the N -stress by altering the metabolic pathways towards inducing lipid biosynthesis. To maximize the TL and TCAR extraction yields, from N-limited cultures, a set of operating process was applied including the Sonication (SON) and Microwave (MIC), which were used as aiding techniques for lipid extraction compared with the Cold Condition (COL) techniques. The results showed that the extraction efficiency of the S. platensis TL increased in the following order: MIC (29.51%± 1.92) > SON (25.46% ± 1.65> COL (20.43% ±1.43). In a comparative study for its fatty acid profiles (FAPs) among all SP cultures, lipids were analyzed by GC/MS. The predominant fatty acids (>10%, of total FA) were found to be myristic acid (C14:0, MA), palmitic acid (C16:0, PA) and oleic acid (C18:1). Conclusion: The study concluded that the N-limited condition was found to have a strong influence on biomass dry weight and lipid contents and total carotenoids in SP cells compared to either Nrich or N-optimal conditions. The use of sonication and the microwave techniques lead to a great increase in the extraction of lipid contents and in high amount Polyunsaturated Fatty Acids (PUFAs) in N-limited cultures, in particular, the omega-6 (ω 6) and omega-3 (ω 3) of the essential C18 fatty acids. It seems that the SP rich in lipid content with a high amount of GLC produced under nitrogen limitation in PBR conditions can be used as a food additive or as a nutritional supplement.
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Chang, Te-Sheng, Horng-Huey Ko, Tzi-Yuan Wang, Chun-Hsien Lee, and Jiumn-Yih Wu. "Biotransformation of Ganoderic Acid A to 3-O-Acetyl Ganoderic Acid A by Soil-isolated Streptomyces sp." Fermentation 4, no. 4 (December 1, 2018): 101. http://dx.doi.org/10.3390/fermentation4040101.
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The medicinal fungus Ganoderma lucidum contains many bioactive triterpenoids, ganoderic acid A (GAA) being one of the major ones. The present study explored the microbial biotransformation of GAA, isolating 283 strains of soil actinomycetes and determining their abilities to biotransform GAA with ultra-performance liquid chromatography analysis. One positive strain, AI 045, was selected to validate the biotransformation activity. The strain was identified as Streptomyces sp. based on the sequenced 16S rRNA gene. The produced compound obtained from the biotransformation of GAA was purified with the preparative high-performance liquid chromatography method and identified as 3-O-acetyl GAA based on mass and nuclear magnetic resonance spectral data. The present study is the first report that bacteria have the novel ability to biotransform the triterpenoids of fungus G. lucidum. Moreover, the identified 3-O-acetyl GAA is a new triterpenoid product discovered in microbes.
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Carlsen, Sandra C. K., Hans A. Pedersen, Niels H. Spliid, and Inge S. Fomsgaard. "Fate in Soil of Flavonoids Released from White Clover (Trifolium repensL.)." Applied and Environmental Soil Science 2012 (2012): 1–10. http://dx.doi.org/10.1155/2012/743413.
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White clover is frequently used as a leguminous cover crop, serving as green manure, and is also included with grasses in cattle feed mixtures. Numerous biological effects reported for clover cultivation have been attributed to the production of bioactive secondary metabolites. Thus far the presence in soil of bioactive secondary metabolites from clover has received limited attention. In this paper we examine for the first time the release of flavonoids both from field-grown white clover and from soil-incorporated white clover plants of flavonoids, as analyzed by LC-MS/MS. The dominant flavonoid aglycones were formononetin, medicarpin, and kaempferol. Soil-incorporated white clover plants generated high concentrations of the glycosides kaempferol-Rha-Xyl-Gal and quercetin-Xyl-Gal. Substantial amounts of kaempferol persisted in the soil for days while the other compounds were degraded faster. These compounds should be considered in future studies of soil fatigue, allelopathic activity, and possible environmental risks from extended clover cultivation.
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Bhunia, Anirban, Oliver Schwardt, Heiko Gäthje, Gan-Pan Gao, Soerge Kelm, Andrew J. Benie, Milos Hricovini, Thomas Peters, and Beat Ernst. "Consistent Bioactive Conformation of the Neu5Acα(2→3)Gal Epitope Upon Lectin Binding." ChemBioChem 9, no. 18 (December 15, 2008): 2941–45. http://dx.doi.org/10.1002/cbic.200800458.
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Jiayi, Ma, Ingrid Melinda Gyalai, and Ferenc Lantos. "Investigation of water soluble sugar content and flavour evaluation of Gala Must, Royal Gala and Pinova apple varieties." Review on Agriculture and Rural Development 10, no. 1-2 (January 3, 2022): 169–75. http://dx.doi.org/10.14232/rard.2021.1-2.169-175.
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Humankind has known regular consumption of apple since ancient times. The fruits contain several bioactive compounds for human. Nowadays, a lot of breeded varieties are in cultivation on the world. There are more than 7,500 known cultivars of apples, resulting in a wide range of desired characteristics. The Gala series apples are one of the most popular and common apples in Hungary in the 21st century. Gala Must was used as the subject of a study to compare the fruit quality of Hungarian Gala Must with Pinova and commercially available Royal Gala apples. By studying the data recorded and samples collected in the orchard, the following points were studied and its cultivation in the Szentes region of Hungary is described: total sugar concentration, firmness, colour of fruits in biological ripening status and opinion of consumers. Based our results the water soluble sugar content of Gala Must 15; Pinova 13.8; Royal Gala 14.1 BRIX%
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Sawicka, Monika, Piotr Latocha, and Barbara Łata. "Peel to Flesh Bioactive Compounds Ratio Affect Apple Antioxidant Potential and Cultivar Functional Properties." Agriculture 13, no. 2 (February 16, 2023): 478. http://dx.doi.org/10.3390/agriculture13020478.
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More than ten thousand apple cultivars with high variability in the quality traits and year-round availability place apples at the forefront of consumed fruits. Yet consumers and producers alike are still looking for new apple cultivars with specific quality attributes such as plant resistance to biotic and abiotic stresses as well as a high health-promoting potential. The model plants were three cultivars: a new ‘Chopin’ and an old ‘Granny Smith’, scab resistant cultivars with green peel, and a red-skinned cultivar ‘Gala Schniga’. Apple peel and flesh were analyzed separately during two growing seasons: 2016 and 2017. The total ascorbate and phenolics as well as individual phenolic compounds, such as (+)-catechin, (−)-epicatechin, chlorogenic acid, phloridzin, and rutin concentrations, proved to be highly tissue-type and cultivar dependent. The apple of the ‘Chopin’ and ‘Granny Smith’ cultivars expressed much lower skin-to-flesh antioxidant potential differences as compared to ‘Gala Schniga’. The lowest differences between tissue types were observed in the case of chlorogenic acid and flavan-3-ols, followed by total phenolics and ascorbate concentrations. Except for phloridzin, ‘Gala Schniga’ exhibited the highest differences in global and individual phenolic compound concentrations as well as total antioxidant capacity between the apple peel and flesh. ‘Chopin’ was definitely distinguished by the highest concentration of ascorbate in both the peel and the flesh and expressed a higher concentration of flavanols, especially compared to ‘Granny Smith’. In contrast to ‘Gala Schniga’, ‘Chopin’ was richer in chlorogenic acid, (+)-catechin, and (−)-epicatechin in the flesh. The total antioxidant capacity of the green-peel apple cultivars was similar to that of the red-peel one. A narrower range of differences between the concentration of antioxidants in apple peel and flesh could mean better health-promoting properties and might be related to a greater resistance to environmental stress factors.
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Chang, Te-Sheng, Chien-Min Chiang, Tzi-Yuan Wang, Yu-Li Tsai, Yu-Wei Wu, Huei-Ju Ting, and Jiumn-Yih Wu. "One-Pot Bi-Enzymatic Cascade Synthesis of Novel Ganoderma Triterpenoid Saponins." Catalysts 11, no. 5 (April 30, 2021): 580. http://dx.doi.org/10.3390/catal11050580.
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Ganoderma lucidum is a medicinal fungus whose numerous triterpenoids are its main bioactive constituents. Although hundreds of Ganoderma triterpenoids have been identified, Ganoderma triterpenoid glycosides, also named triterpenoid saponins, have been rarely found. Ganoderic acid A (GAA), a major Ganoderma triterpenoid, was synthetically cascaded to form GAA-15-O-β-glucopyranoside (GAA-15-G) by glycosyltransferase (BtGT_16345) from Bacillus thuringiensis GA A07 and subsequently biotransformed into a series of GAA glucosides by cyclodextrin glucanotransferase (Toruzyme® 3.0 L) from Thermoanaerobacter sp. The optimal reaction conditions for the second-step biotransformation of GAA-15-G were found to be 20% of maltose; pH 5; 60 °C. A series of GAA glucosides (GAA-G2, GAA-G3, and GAA-G4) could be purified with preparative high-performance liquid chromatography (HPLC) and identified by mass and nucleic magnetic resonance (NMR) spectral analysis. The major product, GAA-15-O-[α-glucopyranosyl-(1→4)-β-glucopyranoside] (GAA-G2), showed over 4554-fold higher aqueous solubility than GAA. The present study demonstrated that multiple Ganoderma triterpenoid saponins could be produced by sequential actions of BtGT_16345 and Toruzyme®, and the synthetic strategy that we proposed might be applied to many other Ganoderma triterpenoids to produce numerous novel Ganoderma triterpenoid saponins in the future.
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Yang, Li V., Caius G. Radu, Li Wang, Mireille Riedinger, and Owen N. Witte. "Gi-independent macrophage chemotaxis to lysophosphatidylcholine via the immunoregulatory GPCR G2A." Blood 105, no. 3 (February 1, 2005): 1127–34. http://dx.doi.org/10.1182/blood-2004-05-1916.
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Abstract G2A is a G-protein–coupled receptor (GPCR) involved in immune regulation. Previous studies have shown that lysophosphatidylcholine (LPC), a bioactive lipid associated with atherosclerosis and autoimmunity, acts through G2A to induce diverse biologic effects. Production of LPC during cell apoptosis serves as a chemotactic signal for macrophage recruitment. Here we demonstrate that macrophage chemotaxis to LPC is dependent on G2A function. Wild-type but not G2A-deficient mouse peritoneal macrophages migrated toward LPC. RNAi-mediated knockdown of G2A in J774A.1 macrophages abolished LPC-induced chemotaxis, whereas overexpression of G2A significantly enhanced this process. Mutation of the conserved DRY motif of G2A resulted in loss of chemotaxis to LPC, suggesting a requirement for G-protein signaling. Unlike most GPCRs, including the chemokine receptors, coupling to Gi is not required for LPC/G2A-mediated chemotaxis, but coupling to Gq/11 and G12/13 is necessary as judged by inhibition with dominant negative forms of these alpha subunits or with regulators of G-protein signaling (RGS) constructs. Collectively, these data establish that pertussis toxin–insensitive G2A signaling regulates macrophage chemotaxis to LPC. Defects in this signaling pathway may be related to the pathogenesis of systemic autoimmune disease.
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Ma, Zhe, Lin Peng, Wenhui Chu, Pan Wang, and Yongqian Fu. "Osthole Alleviates D-Galactose-Induced Liver Injury In Vivo via the TLR4/MAPK/NF-κB Pathways." Molecules 28, no. 1 (January 3, 2023): 443. http://dx.doi.org/10.3390/molecules28010443.
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Osthole, a coumarin derivative, is found in several medicinal herbs. However, the protective effects of osthole against D-galactose (D-Gal)-induced liver injury still remain unclear. In this study, osthole treatment effectively reversed D-Gal-induced liver injury, according to the results of liver HE staining, and improved ALT and AST activities. Feeding with D-Gal significantly increased MDA content, and reduced the level or activity of SOD, CAT and GSH-Px, which were all alleviated by osthole intervention. Meanwhile, osthole treatment significantly inhibited the D-Gal-induced secretion of pro-inflammatory cytokines, such as TNF-α, IL-1β and IL-6, in both serum and liver tissue. Investigations revealed that osthole ameliorated the D-Gal-induced activation of TLR4, MYD88 and its downstream signaling pathways of MAPK (p38 and JNK) and NF-κB (nucleus p65). Therefore, osthole mediates a protective effect against D-Gal-induced liver injury via the TLR4/MAPK/NF-κB pathways, and this coumarin derivative could be developed as a candidate bioactive component for functional food.
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Puschmann, Till B., Carl Zandén, Yolanda De Pablo, Frank Kirchhoff, Marcela Pekna, Johan Liu, and Milos Pekny. "Bioactive 3D cell culture system minimizes cellular stress and maintains thein vivo-like morphological complexity of astroglial cells." Glia 61, no. 3 (January 7, 2013): 432–40. http://dx.doi.org/10.1002/glia.22446.
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G, Tamaddon. "Apoptosis Induction of Ganoderic Acid-A by Downregulating miR- 125b and miR-365a-3p in Nalm-6 cells." Haematology International Journal 6, no. 2 (2022): 1–10. http://dx.doi.org/10.23880/hij-16000201.
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Acute lymphoblastic leukemia is the most common leukemia in children, which is associated with a high relapse rate despite prevalent therapies. Ganoderic acid-A (GAA) is one of the bioactive compounds of Ganoderma lucidum, which possesses potential antileukemic properties. This study aimed to investigate the effect of the GAA extract on the expression of microRNA and the apoptosis induction in the BCP-ALL cell line. In this case-control study, NALM-6 Cells were treated with the GAA extract and L-asparaginase separately. The cell viability and apoptosis rates were examined using MTT and flow cytometry, respectively. Moreover, the effect of the GAA on the expression of miR-125b and miR-365a-3p, in comparison to L-asparaginase, was studied using RT-PCR. The GAA extract inhibited the cell growth in a dose- and time-dependent manner. Moreover, the GAA extract significantly induced apoptosis compared to L-asparaginase (P=0.0021 vs. P=0.0112). The results showed that the treatment of Nalm-6 cells with GAA significantly reduced the expression of miR-125b (P< 0.0001) and miR-365a-3p (P= 0.0001). Furthermore, it was demonstrated that the downregulation of miR-125b and miR-365a-3p was surprisingly higher in the GA-treated Nalm-6 cells than in L-asparaginase-treated Nalm-6 cells. According to the findings, the GAA extract has antileukemic effects and can be used as a promising agent with fewer side effects in all treatments.
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Chang, Te-Sheng, Chien-Min Chiang, Yu-Han Kao, Jiumn-Yih Wu, Yu-Wei Wu, and Tzi-Yuan Wang. "A New Triterpenoid Glucoside from a Novel Acidic Glycosylation of Ganoderic Acid A via Recombinant Glycosyltransferase of Bacillus subtilis." Molecules 24, no. 19 (September 24, 2019): 3457. http://dx.doi.org/10.3390/molecules24193457.
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Ganoderic acid A (GAA) is a bioactive triterpenoid isolated from the medicinal fungus Ganoderma lucidum. Our previous study showed that the Bacillus subtilis ATCC (American type culture collection) 6633 strain could biotransform GAA into compound (1), GAA-15-O-β-glucoside, and compound (2). Even though we identified two glycosyltransferases (GT) to catalyze the synthesis of GAA-15-O-β-glucoside, the chemical structure of compound (2) and its corresponding enzyme remain elusive. In the present study, we identified BsGT110, a GT from the same B. subtilis strain, for the biotransformation of GAA into compound (2) through acidic glycosylation. BsGT110 showed an optimal glycosylation activity toward GAA at pH 6 but lost most of its activity at pH 8. Through a scaled-up production, compound (2) was successfully isolated using preparative high-performance liquid chromatography and identified to be a new triterpenoid glucoside (GAA-26-O-β-glucoside) by mass and nuclear magnetic resonance spectroscopy. The results of kinetic experiments showed that the turnover number (kcat) of BsGT110 toward GAA at pH 6 (kcat = 11.2 min−1) was 3-fold higher than that at pH 7 (kcat = 3.8 min−1), indicating that the glycosylation activity of BsGT110 toward GAA was more active at acidic pH 6. In short, we determined that BsGT110 is a unique GT that plays a role in the glycosylation of triterpenoid at the C-26 position under acidic conditions, but loses most of this activity under alkaline ones, suggesting that acidic solutions may enhance the catalytic activity of this and similar types of GTs toward triterpenoids.
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Aureli, Anna, Manuela Del Cornò, Beatrice Marziani, Sandra Gessani, and Lucia Conti. "Highlights on the Role of Galectin-3 in Colorectal Cancer and the Preventive/Therapeutic Potential of Food-Derived Inhibitors." Cancers 15, no. 1 (December 22, 2022): 52. http://dx.doi.org/10.3390/cancers15010052.
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Colorectal cancer (CRC) is a leading cause of death worldwide. Despite advances in surgical and therapeutic management, tumor metastases and resistance to therapy still represent major hurdles. CRC risk is highly modifiable by lifestyle factors, including diet, which strongly influences both cancer incidence and related mortality. Galectin-3 (Gal-3) is a multifaceted protein involved in multiple pathophysiological pathways underlying chronic inflammation and cancer. Its versatility is given by the ability to participate in a wide range of tumor-promoting processes, including cell–cell/cell–matrix interactions, cell growth regulation and apoptosis, and the immunosuppressive tumor microenvironment. This review provides an updated summary of preclinical and observational human studies investigating the pathogenetic role of Gal-3 in intestinal inflammation and CRC, as well as the potential of Gal-3 activity inhibition by plant-source food-derived bioactive compounds to control CRC onset/growth. These studies highlight both direct and immuno-mediated effects of Gal-3 on tumor growth and invasiveness and its potential role as a CRC prognostic biomarker. Substantial evidence indicates natural food-derived Gal-3 inhibitors as promising candidates for CRC prevention and therapy. However, critical issues, such as their bioavailability and efficacy, in controlled human studies need to be addressed to translate research progress into clinical applications.
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Falk, Shaun P., Andrew T. Ulijasz, and Bernard Weisblum. "Differential Assay for High-Throughput Screening of Antibacterial Compounds." Journal of Biomolecular Screening 12, no. 8 (December 2007): 1102–8. http://dx.doi.org/10.1177/1087057107308161.
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The previously described Bacillus subtilis reporter strain BAU-102 is capable of detecting cell wall synthesis inhibitors that act at all stages of the cell wall synthesis pathway. In addition, this strain is capable of detecting compounds with hydrophobic/ surfactant activity and alternative mechanisms of cell wall disruption. BAU-102 sequesters preformed β-gal in the periplasm, suggesting leakage of β-gal as the means by which this assay detects compound activities. A model is proposed according to which β-gal release by BAU-102 reflects activation of pathways leading to autolysis. The authors also report a simplified high-throughput assay using BAU-102 combined with the fluorogenic substrate N-methylumbelliferyl-β-D-galactoside as a single reagent. Cell wall inhibitors release β-gal consistently only after 60 min of incubation, whereas compounds with surfactant activity show an almost immediate release. A high-throughput screen of a 480-compound library of known bioactives yielded 8 compounds that cause β-gal release. These results validate the BAU-102 assay as an effective tool in antimicrobial drug discovery. ( Journal of Biomolecular Screening 2007:1102-1108)
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Odun-Ayo, Frederick, and Lalini Reddy. "Potential Roles of Modified Pectin Targeting Galectin-3 against Severe Acute Respiratory Syndrome Coronavirus-2." J 4, no. 4 (November 29, 2021): 824–37. http://dx.doi.org/10.3390/j4040056.
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Modified pectin (MP) is a bioactive complex polysaccharide that is broken down into smaller fragments of units and used as an oral dietary supplement for cell proliferation. MP is safe and non-toxic with promising therapeutic properties with regard to targeting galectin-3 (GAL-3) toward the prevention and inhibition of viral infections through the modulation of the immune response and anti-inflammatory cytokine effects. This effect of MP as a GAL-3 antagonism, which has shown benefits in preclinical and clinical models, may be of relevance to the progression of the novel severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) in coronavirus disease 2019 patients. The outbreak of emerging infectious diseases continues to pose a threat to human health. Further to the circulation of multiple variants of SARS-CoV-2, an effective and alternative therapeutic approach to combat it has become pertinent. The use of MP as a GAL-3 inhibitor could serve as an antiviral agent blocking against the SARS-CoV-2-binding spike protein. This review highlights the potential effects of MP in viral infections, its proposed role as a GAL-3 inhibitor, and the associated function concerning a SARS-CoV-2 infection.
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Gustavo Sganzerla, William, Mayeve Didomenico Melo, Jocleita Peruzzo Ferrareze, Ana Paula de Lima Veeck, Paula Iaschitzki Ferreira, and César Luis Girardi. "Postharvest treatment with 1-MCP in apple ‘Gala’ mutants: physicochemical characterization, bioactive compounds and antioxidant activity." Communications in Plant Sciences 8, no. 1 (2018): 40–47. http://dx.doi.org/10.26814/cps2018006.
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Mendes, Luana Guabiraba, Francisco Rogênio da Silva Mendes, Roselayne Ferro Furtado, Gabrielle Albuquerque Freire, Gleilton Weyne Passos Sales, José Maria Correia da Costa, Nádia Accioly Pinto Nogueira, Ana Cristina de Oliveira Monteiro-Moreira, and Renato de Azevedo Moreira. "Use of cashew gum combined with galactomannan for encapsulation of Rosmarinus officinalis essential oil." Journal of Environmental Analysis and Progress 5, no. 4 (October 28, 2020): 369–80. http://dx.doi.org/10.24221/jeap.5.4.2020.2748.369-380.
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Encapsulating matrices are important to maintain the properties, promote the low and controlled release, and avoid these bioactive compounds' undesirable reactions. This study's objective was to evaluate cashew gum (CG) use combined with galactomannan (GAL) in the rosemary essential oil encapsulation by atomization. During the emulsification, the polysaccharides were crosslinked with sodium trimetaphosphate. The particles obtained after encapsulation were evaluated for moisture, solubility, particle size, encapsulation efficiency, morphology, antimicrobial activity, and chemical composition of the essential oil volatiles. GAL/CG blend showed higher encapsulation efficiency and lower oil release than the cashew gum matrix. Undoubtedly, galactomannan combined with cashew gum improved the microparticles' characteristics due to the galactomannan's high emulsifying property even in low concentration. Essential oil maintained its antimicrobial and chemical properties practically after the encapsulation procedure.
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Walkowiak-Tomczak, Dorota, Natalia Idaszewska, Grzegorz P. Łysiak, and Krzysztof Bieńczak. "The Effect of Mechanical Vibration during Transport under Model Conditions on the Shelf-Life, Quality and Physico-Chemical Parameters of Four Apple Cultivars." Agronomy 11, no. 1 (January 2, 2021): 81. http://dx.doi.org/10.3390/agronomy11010081.
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The study assessed the changes in the quality and physical and chemical parameters of apples of four cultivars (‘Gala’, ‘Idared’, ‘Topaz’, ‘Red Prince’) subjected to mechanical vibration during transport under model conditions and after storage (shelf-life). Quality changes in apples were evaluated based on skin and flesh colour, total soluble solids, dry matter, firmness, titratable acidity, pH value, total polyphenol content, and antioxidant capacity. The vibration applied at a frequency of 28 Hz caused changes in the above parameters, which were visible also after storage and depended on the cultivar, but often did not show any clear trend or direction or were not statistically significant. The values of the total colour difference factor ΔE showed considerable variations in the skin colour but only small variations in the flesh colour of individual cultivars. Vibration resulted in a decrease in firmness. Variations in dry matter, total soluble solids, pH, and titratable acidity were small, often insignificant. Mechanical vibration and storage led to an increase in the polyphenol content and antioxidant capacity of all studied cultivars. The greatest stability of quality parameters, relatively high content of bioactive compounds, and antioxidant capacity were observed for ‘Red Prince’. The lowest quality parameters were noted for ‘Gala’. The analysed cultivars continued to show a high level of antioxidant capacity after treatment, which allows the conclusion that they remain a good source of bioactive compounds after transport and short-term storage.
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Aladaileh, Abukhalil, Saghir, Hanieh, Alfwuaires, Almaiman, Bin-Jumah, and Mahmoud. "Galangin Activates Nrf2 Signaling and Attenuates Oxidative Damage, Inflammation, and Apoptosis in a Rat Model of Cyclophosphamide-Induced Hepatotoxicity." Biomolecules 9, no. 8 (August 5, 2019): 346. http://dx.doi.org/10.3390/biom9080346.
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Cyclophosphamide (CP) is a widely used chemotherapeutic agent; however, its clinical application is limited because of its multi-organ toxicity. Galangin (Gal) is a bioactive flavonoid with promising biological activities. This study investigated the hepatoprotective effect of Gal in CP-induced rats. Rats received Gal (15, 30 and 60 mg/kg/day) for 15 days followed by a single dose of CP at day 16. Cyclophosphamide triggered liver injury characterized by elevated serum transaminases, alkaline phosphatase (ALP) and lactate dehydrogenase (LDH), and histopathological manifestations. Increased hepatic reactive oxygen species, malondialdehyde, nitric oxide, and oxidative DNA damage along with declined glutathione and antioxidant enzymes were demonstrated in CP-administered rats. CP provoked hepatic nuclear factor-kappaB (NF-κB) phosphorylation and increased mRNA abundance of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β) both expression and serum levels. Gal prevented CP-induced liver injury, boosted antioxidants and suppressed oxidative stress, DNA damage, NF-κB phosphorylation and pro-inflammatory mediators. Gal diminished Bax and caspase-3, and increased B-cell lymphoma-2 (Bcl-2) in liver of CP-administered rats. In addition, Gal increased peroxisome proliferator-activated receptor gamma (PPARγ) expression and activated hepatic nuclear factor erythroid 2-related factor 2 (Nrf2) signaling showed by the increase in Nrf2, NAD(P)H: quinone acceptor oxidoreductase-1 (NQO-1) and heme oxygenase 1 (HO-1) in CP-administered rats. These findings suggest that Gal prevents CP hepatotoxicity through activation of Nrf2/HO-1 signaling and attenuation of oxidative damage, inflammation and cell death. Therefore, Gal might represent a promising adjuvant therapy to prevent hepatotoxicity in patients on CP treatment.
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Miller, Michelle C., Irina V. Nesmelova, Vladimir A. Daragan, Hans Ippel, Malwina Michalak, Aurelio Dregni, Herbert Kaltner, Jürgen Kopitz, Hans-Joachim Gabius, and Kevin H. Mayo. "Pro4 prolyl peptide bond isomerization in human galectin-7 modulates the monomer-dimer equilibrum to affect function." Biochemical Journal 477, no. 17 (September 4, 2020): 3147–65. http://dx.doi.org/10.1042/bcj20200499.
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Human galectin-7 (Gal-7; also termed p53-induced gene 1 product) is a multifunctional effector by productive pairing with distinct glycoconjugates and protein counter-receptors in the cytoplasm and nucleus, as well as on the cell surface. Its structural analysis by NMR spectroscopy detected doubling of a set of particular resonances, an indicator of Gal-7 existing in two conformational states in slow exchange on the chemical shift time scale. Structural positioning of this set of amino acids around the P4 residue and loss of this phenomenon in the bioactive P4L mutant indicated cis–trans isomerization at this site. Respective resonance assignments confirmed our proposal of two Gal-7 conformers. Mapping hydrogen bonds and considering van der Waals interactions in molecular dynamics simulations revealed a structural difference for the N-terminal peptide, with the trans-state being more exposed to solvent and more mobile than the cis-state. Affinity for lactose or glycan-inhibitable neuroblastoma cell surface contact formation was not affected, because both conformers associated with an overall increase in order parameters (S2). At low µM concentrations, homodimer dissociation is more favored for the cis-state of the protein than its trans-state. These findings give direction to mapping binding sites for protein counter-receptors of Gal-7, such as Bcl-2, JNK1, p53 or Smad3, and to run functional assays at low concentration to test the hypothesis that this isomerization process provides a (patho)physiologically important molecular switch for Gal-7.
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Shiwakoti, Saugat, Deepak Adhikari, Jeong Pyo Lee, Ki-Woon Kang, Ik-Soo Lee, Hyun Jung Kim, and Min-Ho Oak. "Prevention of Fine Dust-Induced Vascular Senescence by Humulus lupulus Extract and Its Major Bioactive Compounds." Antioxidants 9, no. 12 (December 7, 2020): 1243. http://dx.doi.org/10.3390/antiox9121243.
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Both short- and long-term exposure to fine dust (FD) from air pollution has been linked to various cardiovascular diseases (CVDs). Endothelial cell (EC) senescence is an important risk factor for CVDs, and recent evidence suggests that FD-induced premature EC senescence increases oxidative stress levels. Hop plant (Humulus lupulus) is a very rich source of polyphenols known to have nutritional and therapeutic properties, including antioxidant behavior. The aims of this study were to evaluate whether Humulus lupulus extract prevents FD-induced vascular senescence and dysfunction and, if so, to characterize the underlying mechanisms and active components. Porcine coronary arteries and endothelial cells were treated with FD in the presence or absence of hop extract (HOP), and the senescence-associated-beta galactosidase (SA-β-gal) activity, cell-cycle progression, expression of senescence markers, oxidative stress level, and vascular function were evaluated. Results indicated that HOP inhibited FD-induced SA-β-gal activity, cell-cycle arrest, and oxidative stress, suggesting that HOP prevents premature induction of senescence by FD. HOP also ameliorated FD-induced vascular dysfunction. Additionally, xanthohumol (XN) and isoxanthohumol (IX) were found to produce the protective effects of HOP. Treatment with HOP and its primary active components XN and IX downregulated the expression of p22phox, p53, and angiotensin type 1 receptor, which all are known FD-induced redox-sensitive EC senescence inducers. Taken together, HOP and its active components protect against FD-induced endothelial senescence most likely via antioxidant activity and may be a potential therapeutic agent for preventing and/or treating air-pollution-associated CVDs.
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Seweryn, Ewa, Emilia Królewicz, Kamilla Stach, and Irena Kustrzeba-Wójcicka. "Nutritional and allergenic properties of hen eggs." Postępy Higieny i Medycyny Doświadczalnej 72 (April 6, 2018): 205–14. http://dx.doi.org/10.5604/01.3001.0011.7339.
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Chicken eggs, along with cow milk, are the most important source of proteins and other valuable nutrients that are introduced to a baby`s diet. Certain components of eggs, besides nutritional, also have other biological functions. Both proteins, phospholipids or carotenoids, are bioactive components which affect the physiological processes in the human body. Regular consumption of chicken eggs rich in substances with antibacterial, anti-inflammatory, immunomodulatory and antioxidant properties may contribute to reducing the incidence of certain lifestyle diseases. Ovomucoid, as a glycoprotein which inhibits bacterial protease, is a component of eggs with bactericidal properties. Similarly, the ovotransferrin protein has a bacteriostatic effect on the Escherichia coli strain or Streptococcus mutans. Due to the strong antioxidant properties, phospholipids, vitamin E and folic acid are extremely valuable egg components. It is believed that the high antioxidant potential of these compounds is important in preventing the development of atherosclerosis and other metabolic syndromes. It is also worth mentioning lutein and zeaxanthin, which are dyes that form a protective barrier against the degeneration of the macula of the human eye. An extremely important function for the human immune system is also met by lysozyme, which stimulates the synthesis of interferon, stimulating the immune response. Unfortunately, hypersensitivity to chicken eggs is one of the most common food allergies in children and affects 0.5-9% of the population. The major egg allergens (Gallus spp.): ovomucoid (Gal d 1), ovalbumin (Gal d 2), conalbumin (Gal d 3) and lysozyme (Gal d 4) are present in egg white and most often cause allergic reactions in children. Minor allergens: serum albumin (Gal d 5) and YGP42 protein (Gal d 6) are found in the egg yolk and are more likely to sensitize adults.
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Gottlieb, Otto R., Maria Renata de M. B. Borin, and Nei Regis S. de Brito. "Quantitative chemobiology." Pure and Applied Chemistry 73, no. 3 (January 1, 2001): 583–88. http://dx.doi.org/10.1351/pac200173030583.
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One of the mysteries of man's contact with nature concerns the question why shamanism and science so often lead to consistent results in the search for useful natural products. To find clues toward an answer via a coherent chemobiological language, structural and functional information is taken into account. The functional information, given by ethnobotanical codes based on traditional knowledge (via number of useful dicotyledon species), is confronted with the structural information, given by metabolic codes based on micromolecular diversification (via number of occurrences in dicotyledons). The challenge to integrate these databases implies in the development of qualitative (via dahlgrenograms) and quantitative (via Sporne indices) models into an evolutionary framework. The follow-up of ethnobotanical qualifications reveals systematic and evolutionary patterns, susceptible to juxtaposition into a phytochemical background based on gallates (GAL) and caffeates (CAF), regulators of intermediate metabolism. Comparison of the two models of information suggests that the "spectral" features of the GAL and CAF-models are coincident with the ethnobotany-guided food- and medicine-plants respectively. Hence, the complementary nature of food and medicine species can be rationalized by oscillations between GAL/CAF. Analyses of these indicators of toxicity would allow advances in the understanding of mechanisms regulating the production of bioactive products.
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Park, Yoonseong, Donghun Kim, Gunavanthi Boorgula, Kristof De Schutter, Guy Smagghe, Ladislav Šimo, Stephanie Archer-Hartmann, and Parastoo Azadi. "Alpha-Gal and Cross-Reactive Carbohydrate Determinants in the N-Glycans of Salivary Glands in the Lone Star Tick, Amblyomma americanum." Vaccines 8, no. 1 (January 9, 2020): 18. http://dx.doi.org/10.3390/vaccines8010018.
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Ticks are important ectoparasites and vectors of numerous human and animal pathogens. Ticks secrete saliva that contains various bioactive materials to evade the host defense system, and often facilitates the pathogen transmission. In addition, the Lone star tick saliva is thought to be the sensitizer in red meat allergy that is characterized by an allergic reaction to glycan moieties carrying terminal galactose-alpha-1,3-galactose (aGal). To assess N-glycome of Amblyomma americanum, we examined the N-glycan structures in male and female salivary glands at three different feeding stages and in carcasses of partially fed lone star ticks. We also surveyed the genes involved in the N-glycosylation in the tick species. The aGal epitopes and cross-reactive carbohydrate determinants (CCD) increases over time after the onset of blood feeding in both male and female A. americanum. These CCDs include xylosylation of the core mannose, 1,3-mono and 1,3- and 1,6-difucosylations of the basal GlcNac and mono- or diantennary aGal. Combinations of both xylosylation and aGal and fucosylation and aGal were also found on the N-glycan structures. While the enzymes required for the early steps of the N-glycosylation pathway are quite conserved, the enzymes involved in the later stages of N-glycan maturation in the Golgi apparatus are highly diverged from those of insects. Most of all, we propose that the aGal serves as a molecular mimicry of bioactive proteins during tick feedings on mammalian hosts, while it contributes as a sensitizer of allergy in atypical host human.
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Wang, Shanshan, France Moreau, and Kris Chadee. "The colonic pathogen Entamoeba histolytica activates caspase-4/1 that cleaves the pore-forming protein gasdermin D to regulate IL-1β secretion." PLOS Pathogens 18, no. 3 (March 18, 2022): e1010415. http://dx.doi.org/10.1371/journal.ppat.1010415.
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A hallmark of Entamoeba histolytica (Eh) invasion in the gut is acute inflammation dominated by the secretion of pro-inflammatory cytokines TNF-α and IL-1β. This is initiated when Eh in contact with macrophages in the lamina propria activates caspase-1 by recruiting the NLRP3 inflammasome complex in a Gal-lectin and EhCP-A5-dependent manner resulting in the maturation and secretion of IL-1β and IL-18. Here, we interrogated the requirements and mechanisms for Eh-induced caspase-4/1 activation in the cleavage of gasdermin D (GSDMD) to regulate bioactive IL-1β release in the absence of cell death in human macrophages. Unlike caspase-1, caspase-4 activation occurred as early as 10 min that was dependent on Eh Gal-lectin and EhCP-A5 binding to macrophages. By utilizing CRISPR-Cas9 gene edited CASP4/1, NLRP3 KO and ASC-def cells, caspase-4 activation was found to be independent of the canonical NLRP3 inflammasomes. In CRISPR-Cas9 gene edited CASP1 macrophages, caspase-4 activation was significantly up regulated that enhanced the enzymatic cleavage of GSDMD at the same cleavage site as caspase-1 to induce GSDMD pore formation and sustained bioactive IL-1β secretion. Eh-induced IL-1β secretion was independent of pyroptosis as revealed by pharmacological blockade of GSDMD pore formation and in CRISPR-Cas9 gene edited GSDMD KO macrophages. This was in marked contrast to the potent positive control, lipopolysaccharide + Nigericin that induced high expression of predominantly caspase-1 that efficiently cleaved GSDMD with high IL-1β secretion/release associated with massive cell pyroptosis. These results reveal that Eh triggered “hyperactivated macrophages” allowed caspase-4 dependent cleavage of GSDMD and IL-1β secretion to occur in the absence of pyroptosis that may play an important role in disease pathogenesis.
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Hwang, Ki Cheol, Hyun Young Shin, Woo Jung Kim, Mi Suk Seo, and Hoon Kim. "Effects of a High-Molecular-Weight Polysaccharides Isolated from Korean Persimmon on the Antioxidant, Anti-Inflammatory, and Antiwrinkle Activity." Molecules 26, no. 6 (March 13, 2021): 1600. http://dx.doi.org/10.3390/molecules26061600.
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Persimmon (Diospyros kaki), a familiar and widespread fruit worldwide, is known to exhibit several physiological effects because of the presence of pharmacologically active compounds called phytochemicals. However, its high-molecular-weight compounds, particularly polysaccharides, have not been extensively studied. In this study, D. kaki extract (DK) was fractionated into low- and high-molecular-weight fractions (DK-L and DK-H, respectively) through ethanol fractionation, and their effects on antioxidant, anti-inflammatory, and antiwrinkle activities were investigated by an in vitro system. DK-H contained significantly higher contents of neutral sugar, uronic acid, and polyphenols compared to DK and DK-L. Furthermore, DK-H exhibited significantly improved pharmacological activities, such as antioxidant, anti-inflammatory, and antiwrinkle properties, compared to those of DK and DK-L, demonstrating that DK-H may play an important role in mediating the beneficial effects of persimmon. Sugar composition analysis and molecular characterization indicated that DK-H consisted of a galacturonic acid (GalA)-rich polysaccharide with a molecular weight of >345 kDa that mainly comprised GalA and small amounts of neutral sugar and polyphenol residues. These results suggest that the bioactive fraction DK-H is likely to be a GalA-rich pectic polysaccharide containing a small number of polyphenol residues, which may be a novel candidate in the pharmaceutical and cosmeceutical industries.
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Mikołajczyk, Anita, and Dagmara Złotkowska. "Subclinical Lipopolysaccharide from Salmonella Enteritidis Induces Dysregulation of Bioactive Substances from Selected Brain Sections and Glands of Neuroendocrine Axes." Toxins 11, no. 2 (February 2, 2019): 91. http://dx.doi.org/10.3390/toxins11020091.
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Bacterial lipopolysaccharide (LPS) can contribute to the pathogenesis and the clinical symptoms of many diseases such as cancer, mental disorders, neurodegenerative as well as metabolic diseases. The asymptomatic carrier state of Salmonella spp. is a very important public health problem. A subclinical single dose of LPS obtained from S. Enteritidis (5 μg/kg, i.v.) was administered to discern the consequences of changes of various brain peptides such as corticotropin-releasing hormone (CRH), gonadotropin-releasing hormone (GnRH), thyrotropin-releasing hormone (TRH), galanin (GAL), neuropeptide Y (NPY), somatostatin (SOM), substance P (SP), and vasoactive intestinal polypeptide (VIP) in selected clinically important brain sections and endocrine glands of the hypothalamic-pituitary-adrenal (HPA), -thyroid (HPT), -ovarian (HPO) axes. The study was conducted on ten immature crossbred female pigs. The brain peptides were extracted from the hypothalamus (medial basal hypothalamus, preoptic area, lateral hypothalamic area, mammillary bodies, and the stalk median eminence), and pituitary gland (adenohypophysis and neurohypophysis) sections and from the ovaries and adrenal and thyroid glands. There was no difference in health status between LPS and the control groups during the period of the experiment. Nevertheless, even a low single dose of LPS from S. Enteritidis that did not result in any clinical symptoms of disease induced dysregulation of various brain peptides, such as CRH, GnRH, TRH, GAL, NPY, SOM, SP, and VIP in selected brain sections of hypothalamus, pituitary gland and in the endocrine glands of the HPA, HPO, and HPT axes. In conclusion, the obtained results clearly show that subclinical LPS from S. Enteritidis can affect the brain chemistry structure and dysregulate bioactive substance from selected brain sections and glands of the neuroendocrine axes. The exact mechanisms by which LPS can influence major neuroendocrine axes are not fully understood and require further studies.
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Cao, Jun, Huimin Wang, Wei Zhang, Fuliang Cao, Geli Ma, and Erzheng Su. "Tailor-Made Deep Eutectic Solvents for Simultaneous Extraction of Five Aromatic Acids from Ginkgo biloba Leaves." Molecules 23, no. 12 (December 5, 2018): 3214. http://dx.doi.org/10.3390/molecules23123214.
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Ginkgo biloba leaves have various health benefits due to the presence of bioactive compounds such as polyprenyl acetates, flavonoids, and terpene trilactones. However, there is little literature reported on the aromatic acids in Ginkgo biloba leaves. In this work, five aromatic acids including shikimic acid (SA), 6-hydroxykynurenic acid (6-HKA), protocatechuic acid (PA), gallic acid (GAA), and p-hydroxybenzoic acid (PHBA) were simultaneously extracted from Ginkgo biloba leaves by employing the green deep eutectic solvents (DESs). A DES tailor-made from xylitol, glycolic acid and 1,5-pentanedioic acid at a molar ratio of 1:3:1 with 50% (w/w) water addition, named as NGG50, gave higher extraction yields for the five aromatic acids. Main factors affecting the extraction process were further optimized. The highest extraction yields of SA, GAA, 6-HKA, PA, and PHBA were 94.15 ± 0.96 mg/g, 332.69 ± 5.19 μg/g, 25.90 ± 0.61 μg/g, 429.89 ± 11.47 μg/g and 67.94 ± 0.37 μg/g, respectively. The NGG50-based extraction process developed here was a successful attempt of simultaneously extracting five aromatic acids from Ginkgo biloba leaves for the first time, which could provide a new exploitation direction of Ginkgo biloba leaves.
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Shaw, Chris, and T. Chen. "Helokinestatins: A novel family of bioactive peptides with drug-lead potential from the venom of the Gila Monster (Heloderma suspectum)." Regulatory Peptides 164, no. 1 (September 2010): 23–24. http://dx.doi.org/10.1016/j.regpep.2010.07.148.
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Huh, Sora, Seulki Lee, Su Jin Choi, Zhexue Wu, Jae-Han Cho, Lina Kim, Yu Su Shin, et al. "Quercetin Synergistically Inhibit EBV-Associated Gastric Carcinoma with Ganoderma lucidum Extracts." Molecules 24, no. 21 (October 24, 2019): 3834. http://dx.doi.org/10.3390/molecules24213834.
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Mycotherapy has been shown to improve the overall response rate during cancer treatment and reduce some chemotherapy-related adverse events. Ganoderma lucidum is a traditional mushroom used for pharmaceutical purposes. G. lucidum extracts (GLE) showed potential antitumor activities against several cancers. These tumor inhibitory effects of GLE were attributed to the suppression of the proliferation and metastasis of cancer cells. Epstein-Barr virus (EBV)-associated gastric carcinoma (EBVaGC) is defined as the monoclonal proliferation of carcinoma cells with latent EBV infection. The inhibitory effects of GLE against EBVaGC are questionable. The aim of this study was to investigate GLE as potential antitumor agents and a counterpart of quercetin (QCT) for the cotreatment in suppressing EBVaGC development. Therefore, this study conducted antitumor assays using a EBVaGC xenograft mice model and found that GLE could suppress tumor development. These inhibitory effects were significantly augmented by the low concentration of the quercetin (QCT) cotreatment in the xenograft mice. The addition of GLE in low concentrations synergistically reinforced QCT-induced apoptosis and EBV lytic reactivation. GLE contains various polysaccharides and triterpenes, such as ganoderic acid. Interestingly, the addition of ganoderic acid A (GAA) could produce similar bioactive effects like GLE in QCT-mediated antitumor activity. The GAA addition in low concentrations synergistically reinforced QCT-induced apoptosis and EBV lytic reactivation. GAA was sufficiently effective as much as GLE. Therefore, our results suggested that QCT-supplemented GLE could be a potential food adjunct for the prevention of EBVaGC development.
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Di Pietro, Paola, Rosario Lizio, Carmine Izzo, Valeria Visco, Antonio Damato, Eleonora Venturini, Massimiliano De Lucia, et al. "A Novel Combination of High-Load Omega-3 Lysine Complex (AvailOm®) and Anthocyanins Exerts Beneficial Cardiovascular Effects." Antioxidants 11, no. 5 (April 30, 2022): 896. http://dx.doi.org/10.3390/antiox11050896.
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Omega-3 fatty acids have been shown to exert several beneficial effects in the prevention of cardiovascular and cerebrovascular diseases. The objective of the present study was to analyze the effects of a novel high-load omega-3 lysine complex, AvailOm®, its related constituents and a novel mixture of AvailOm® with specific vasoactive anthocyanins on vascular function in mice resistance artery. Pressure myograph was used to perform vascular reactivity studies. Nitric oxide and oxidative stress were assessed by difluorofluorescein diacetate and dihydroethidium, respectively. Increasing doses of AvailOm® exerted a dose-response vasorelaxation via AMPK-eNOS-mediated signaling. Omega-3 Ethyl Ester was identified as the main bioactive derivative of AvailOm®, being capable of inducing vasorelaxant action to the same extent of entire product. The combination of AvailOm® with a mix of potent vasoactive anthocyanins (C3-glu + DP3-glu + Mal3-glu + Mal3-gal + PEO3-gal), strongly protected mesenteric arteries from vascular dysfunction and oxidative stress evoked by oxidized-LDL. These data demonstrate for the first time the direct effects of AvailOm® on resistance arteries. The evidence that the combination of specific vasoactive anthocyanins and AvailOm® further enhanced the vasculoprotective properties of these compounds, may offer new promising perspectives for preventing the onset of cardiovascular and cerebrovascular events.
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Kusnandar, Feri, Asep Safari, and Elvira Syamsir. "Perubahan Karakteristik Fisik Model Minuman Biji Chia Akibat Proses Pemanasan, Perubahan pH, Penambahan Gula dan Garam." Jurnal Mutu Pangan : Indonesian Journal of Food Quality 7, no. 1 (April 30, 2020): 21–29. http://dx.doi.org/10.29244/jmpi.2020.7.1.21.
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Chia seed is rich in protein, lipid, and carbohydrates as well as bioactive compounds such as phenol. The outer layer of chia seed is made of insoluble polysaccharide (mucilage) which is able to absorb water. For this reason, chia seed is potentially used as a functional ingredient in beverages. This study aimed to evaluate the changes of physical characteristics of chia seeds in beverage models (water absorption capacity or WAC and capsule thickness of chia seeds, and viscosity of beverage model) as the effect of heating temperatures (70, 90oC) and heating times (1, 2 hours), pH changes (3, 5, 7), the addition of sugar (0, 15%) and salts (1% KCl and 1% CaCl2) at 3% and 5% chia seeds. The results showed that the pH of the beverage models affected the WAC, viscosity and capsule thickness. The higher the pH, the greater the WAC, viscosity, and capsule thickness. Sugar concentration and heating time did not affect the physical charac-teristics of chia seeds, whereas the heating temperature only showed a significant effect at pH 3. Addition of CaCl2 1% caused the increase of WAC for approximately twice compared to that of KCl 1%.
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Mehra, Lalita, Smritee Mehra, Nidhi Tiwari, Thakuri Singh, Harish Rawat, Shreeshail Belagavi, Abhinav Jaimini, and Gaurav Mittal. "Fabrication, characterization and evaluation of the efficacy of gelatin/hyaluronic acid microporous scaffolds suffused with aloe-vera in a rat burn model." Journal of Biomaterials Applications 36, no. 8 (December 7, 2021): 1346–58. http://dx.doi.org/10.1177/08853282211061821.
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Burn induced injuries are commonly encountered in civilian and military settings, leading to severe morbidity and mortality. Objective of this study was to construct microporous bioactive scaffolds of gelatin-hyaluronic acid suffused with aloe-vera gel (Gela/HA/AvG), and to evaluate their efficacy in healing partial-thickness burn wounds. Scaffolds were characterized using Fourier transform-infrared spectroscopy, Scanning electron microscopy, and Thermo-gravimetric analysis to understand intermolecular interactions and morphological characteristics. In-vitro fluid uptake ability and hemolytic index of test scaffolds were also determined. In-vitro collagenase digestion was done to assess biodegradability of scaffolds. Wound retraction studies were carried out in Sprague Dawley rats inflicted with partial-thickness burn wounds to assess and compare efficacy of optimized scaffolds with respect to negative and positive control groups. In-vivo gamma scintigraphy using Technetium-99m labeled Immunoglobulin-G ( 99m Tc-IgG) as imaging agent was also performed to validate efficacy results. Histological and immunohistochemical comparison between groups was also made. Scaffolds exhibited mircoporous structure, with pore size getting reduced from 41.3 ± 4.3 µm to 30.49 ± 5.7 µm when gelatin conc. was varied from 1% to 5%. Optimized test scaffolds showed sustained in-vitro swelling behavior, were biodegradable and showed hemolytic index in range of 2.4–4.3%. Wound retraction study along with in-vivo gamma scintigraphy indicated that Gela/HA/AvG scaffolds were not only able to reduce local inflammation faster but also accelerated dermis regeneration. Immunohistochemical analysis, in terms of expression levels of epidermal growth factor and fibroblast growth factor-2 also corroborated in-vivo efficacy findings. Gela/HA/AvG scaffolds, therefore, can potentially be developed into an effective dermal regeneration template for partial-thickness burn wounds.
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Reche, Juana, Maria Soledad Almansa, Francisca Hernández, Asunción Amorós, and Pilar Legua. "Physicochemical and Antioxidant Capacity of Jujube (Ziziphus jujuba Mill.) at Different Maturation Stages." Agronomy 11, no. 1 (January 12, 2021): 132. http://dx.doi.org/10.3390/agronomy11010132.
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Jujube is a crop very resistant to drought and salinity, making it an interesting growing alternative in southeastern Spain. The characteristics of five different cultivars of the jujube fruit have been evaluated and classified into four different maturation stages according to the color of the peel, ranging from green in its most immature stage, to white, yellow, and red in its last, more mature stage. This is due in part to the amount of carotenoids and chlorophylls studied, which vary as the fruit matures. The cultivars ‘GAL-E’ and ‘GAL-T’ are the largest in size and weight, followed by ‘MSI’, ‘PSI’, and ‘DAT’, which are the smallest cultivars. The content of phenolic compounds was also analyzed. The antioxidant activity, which was studied by different methods, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP), showed the highest activity in stages 3 and 4 of jujube fruit. The antioxidant activity studied in the hydrophilic and lipophilic fraction by the ABTS method showed the highest peak in stages 1 and 2. This is an important information to know promising cultivars to be used in future breeding programs. Moreover, the maturation stage is relevant to obtain fruit with a high content of bioactive compounds as well as interesting organoleptic properties.
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Kindahl, Lill, Corine Sandström, A. Grey Craig, Thomas Norberg, and Lennart Kenne. "1H NMR studies on the solution conformation of contulakin-G and analogues." Canadian Journal of Chemistry 80, no. 8 (August 1, 2002): 1022–31. http://dx.doi.org/10.1139/v02-115.
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The conformation of contulakin-G, a bioactive 16 amino acid O-linked glycopeptide (ZSEEGGSNAT*KKPYIL) with the disaccharide β-D-Gal(1[Formula: see text]3)α-D-GalNAc attached to the threonine residue in position 10, has been investigated by 1H NMR spectroscopy. The 1H NMR data for the non-glycosylated peptide and for two glycopeptide analogues, one with the monosaccharide α-D-GalNAc at Thr10 and one with the disaccharide β-D-Gal(1–>3)α-D-GalNAc at Ser7, all of lower bioactivity than contulakin-G, have also been collected. The chemical shifts, NOEs, temperature coefficients of amide protons, and 3JNH,αH-values suggest that all four compounds exist mainly in random coil conformations. Some transient populations of folded conformations are also present in the glycopeptides and turns, probably induced by the sugars, are present in the peptide chain around the site of glycosylation. In the two peptides O-glycosylated at Thr10, the rotation of α-D-GalNAc around the linkage between the sugar and the peptide is restricted. There is evidence for a hydrogen bond between the amide proton of α-D-GalNAc and the peptide chain that could contribute to this torsional rigidity. An intramolecular hydrogen bond between the carbohydrate and the peptide chain does not exist in the peptide O-glycosylated at the Ser7 residue. Key words: conformation, contulakin-G, NMR, O-linked glycopeptide.
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Du, Tian-Ye, Samantha C. Karunarathna, Xian Zhang, Dong-Qin Dai, Ausana Mapook, Nakarin Suwannarach, Jian-Chu Xu, et al. "Endophytic Fungi Associated with Aquilaria sinensis (Agarwood) from China Show Antagonism against Bacterial and Fungal Pathogens." Journal of Fungi 8, no. 11 (November 14, 2022): 1197. http://dx.doi.org/10.3390/jof8111197.
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Agarwood is the most expensive non-construction wood product in the world. As a therapeutic agent, agarwood can cure some diseases, but few studies have been carried out on the antagonistic abilities of endophytic fungi associated with agarwood. Agarwood is mainly found in the genus Aquiaria. The objectives of this study are to understand the antimicrobial activities and their potential as biocontrol agents of the endophytic fungi of Aquilaria sinensis. First, fresh samples of A. sinensis were collected from Yunnan and Guangdong Provinces in 2020–2021, and the endophytic fungi were isolated and identified to genus level based on the phylogenetic analyses of the Internal Transcribed Spacer (ITS) region. In this bioassay, 47 endophytic strains were selected to check their bioactivities against three bacterial pathogens viz. Erwinia amylovora, Pseudomonas syringae, and Salmonella enterica; and three fungal pathogens viz. Alternaria alternata, Botrytis cinerea, and Penicillium digitatum. The antibiosis test was carried out by the dual culture assay (10 days), and among the 47 strains selected, 40 strains belong to 18 genera viz. Alternaria, Annulohypoxylon, Aspergillus, Botryosphaeria, Colletotrichum, Corynespora, Curvularia, Daldinia, Diaporthe, Fusarium, Lasiodiplodia, Neofusicoccum, Neopestalotiopsis, Nigrospora, Paracamarosporium, Pseudopithomyces, Trichoderma, Trichosporon and one strain belongs to Xylariaceae had antimicrobial activities. In particular, Lasiodiplodia sp. (YNA-D3) showed the inhibition of all the bacterial and fungal pathogens with a significant inhibition rate. In addition, the strains viz; Curvularia sp. (GDA-3A9), Diaporthe sp. (GDA-2A1), Lasiodiplodia sp. (YNA-D3), Neofusicoccum sp. (YNA-1C3), Nigrospora sp. (GDA-4C1), and Trichoderma sp. (YNA-1C1) showed significant antimicrobial activities and are considered worthy of further studies to identify individual fungal species and their bioactive compounds. This study enriches the diversity of endophytic fungi associated with agarwood, and their potential antagonistic effects against bacterial and fungal pathogens.
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Lu, Mengji, Masanori Isogawa, Yang Xu, and Gero Hilken. "Immunization with the Gene Expressing Woodchuck Hepatitis Virus Nucleocapsid Protein Fused to Cytotoxic-T-Lymphocyte-Associated Antigen 4 Leads to Enhanced Specific Immune Responses in Mice and Woodchucks." Journal of Virology 79, no. 10 (May 15, 2005): 6368–76. http://dx.doi.org/10.1128/jvi.79.10.6368-6376.2005.
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ABSTRACT A number of options are available to modify and improve DNA vaccines. An interesting approach to improve DNA vaccines is to fuse bioactive domains, like cytotoxic-T-lymphocyte-associated protein 4 (CTLA-4), to an antigen. Such fusion antigens are expressed in vivo and directed to immune cells by the specific bioactive domain and therefore possess great potential to induce and modulate antigen-specific immune responses. In the present study, we tested this new approach for immunomodulation against hepadnavirus infection in the woodchuck model. Plasmids expressing the nucleocapsid protein (WHcAg) and e antigen (WHeAg) of woodchuck hepatitis virus (WHV) alone or in fusion to the extracellular domain of woodchuck CTLA-4 and CD28 were constructed. Immunizations of mice with plasmids expressing WHcAg or WHeAg led to a specific immunoglobulin G2a (IgG2a)-dominant antibody response. In contrast, fusions of WHcAg to CTLA-4 and CD28 induced a specific antibody response with comparable levels of IgG1 and IgG2a. Furthermore, the specific IgG1 response to WHcAg/WHeAg developed immediately after a single immunization with the CTLA-4-WHcAg fusion. Woodchucks were immunized with plasmids expressing WHeAg or the CTLA-4-WHcAg fusion and subsequently challenged with WHV. CTLA-4-WHcAg showed an improved efficacy in induction of protective immune responses to WHV. In particular, the anti-WHsAg antibody response developed earlier after challenge in woodchucks that received immunizations with CTLA-4-WHcAg, consistent with the hypothesis that anti-WHs response is dependent on a Th cell response to WHcAg. In conclusion, the use of fusion genes represents a generally applicable strategy to improve DNA vaccination.
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Wang, Zhaoguo, Xiaorui Zhai, Jiayuan Fang, Hongyan Wu, Yunyun Cheng, Yuan Gao, Xi Chen, Shuo Zheng, Songcai Liu, and Linlin Hao. "Peptide−Calcium Chelate from Antler (Cervus elaphus) Bone Enhances Calcium Absorption in Intestinal Caco-2 Cells and D-gal-Induced Aging Mouse Model." Nutrients 14, no. 18 (September 10, 2022): 3738. http://dx.doi.org/10.3390/nu14183738.
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Antler bone calcium (AB−Ca) and bioactive peptides (ABPs) were extracted from antler bones (Cervus elaphus) to maximize their value. In this study, 0.14 g calcium was obtained from 1 g antler bone. The peptide−calcium chelate rate was 53.68 ± 1.80%, and the Gly, Pro, and Glu in ABPs were identified to donate most to the increased calcium affinity through the mass spectrometry. Fourier transform infrared spectroscopy showed that calcium predominantly interacted with amino nitrogen atoms and carboxyl oxygen atoms, thereby generating a peptide–calcium chelate. The peptide−calcium chelates were characterized using scanning electron microscopy. A Caco-2 cell monolayer model showed that ABPs significantly increased calcium transport. Furthermore, the D-gal-induced aging mouse model indicated that the ABPs + AB−Ca group showed higher Ca and PINP levels, lower P, ALP, and CTX-1content in serum, and considerably higher tibia index and tibia calcium content. Results showed that ABPs + AB-Ca increased bone formation and inhibited bone resorption, thereby providing calcium supplements for ameliorating senile osteoporosis (SOP).
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Zhang, Wenrui. "Bioactivity Applications of Lycium Barbarum Polysaccharide In Regulating Human Health." Highlights in Science, Engineering and Technology 11 (August 23, 2022): 152–57. http://dx.doi.org/10.54097/hset.v11i.1362.
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For approximately 2,000 years, Lycium barbarum was regarding as a traditional medicine, and was believed that Wolfberry can nourish the liver, eyes, and kidneys. The fruit of Goji berries can also be eaten as food, and these berries have various biological importance, its anti-inflammatory, antioxidant, anti-tumor, hypoglycemic, hypolipidemic and anti-aging effects were discovered. Among those bioactive components, the most important one is Lycium Barbarum polysaccharide (LBP). LBP main structures include β-(1→3)-galp, α-(1→4)-galA, α-(1→6)-glc, β-(1→6)-galp, β-(1→4)-galp, and α-(1→5)-ara. There are various ways in which LBP is extracted. Various studies have demonstrated that LBP possess various biological activities. The main activities of LBP are anti-oxidation, anti-cancer and metabolic regulation. It can also be used in nerve damage repair, liver protection and eye protection. In this article, the structure of LBP and its medicinal value will be summarized as a reference for its further applications.
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Sabbadini, Fabio, Monica Bertolini, Domenico Mangiameli, Serena Contarelli, Zoë Johnson, Michael M. Lahn, Silvia Pietrobono, and Davide Melisi. "Abstract 1064: Targeting stromal autotaxin synergizes with TGF beta inhibition in pancreatic cancer." Cancer Research 82, no. 12_Supplement (June 15, 2022): 1064. http://dx.doi.org/10.1158/1538-7445.am2022-1064.
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Abstract The TGFβ receptor inhibitor galunisertib (GAL) has been demonstrated as an effective strategy for the treatment of pancreatic cancer (PC) patients, in part through the modulation of stromal microenvironment. However, alternative pathways driving stromal paracrine signals might impair its effect. Autotaxin (ATX) is an enzyme that converts lysophosphatidylcholine into its bioactive lipid, lysophosphatidic acid (LPA), which in turn promotes inflammation and fibrosis, and contributes to treatment resistance. IOA-289 is a novel ATX inhibitor in clinical development for the treatment of tumors burdened with a high degree of stromal involvement. Here, we hypothesized that ATX could sustain an adaptive response upon inhibition of TGFβ receptor signaling, impairing GAL antitumor activity.Among ten different murine PC orthotopic models, mice bearing RC416 tumors had the highest plasma levels of TGFβ1 as well as high infiltration of cancer associated fibroblasts (CAFs) and fibrosis as measured by Masson’s staining. In coculture models of RC416 with murine pancreatic stellate cells (mPSC4), we measured a significant overexpression of ATX upon treatment with galunisertib mainly by mPSC4, which showed a skewing toward an inflammatory iCAF phenotype through the upregulation of CXCL1 and LY6C1 and the down-regulation of myCAF markers including ACTA2 and Taglin. In the RC416-mPSC4 coculture model, anti-tumor activity was achieved with a combination of gemcitabine plus GAL plus IOA-289, whereas these treatments were ineffective in single culture conditions. Mice bearing RC416 tumors reached a statistically significantly longer survival following treatment with gemcitabine plus IOA-289 or gemcitabine plus GAL [median overall survival (mOS)= 35 days, p<0.05] compared with any single treatment or no treatment control. Most importantly, mice treated with the triple combination of gemcitabine plus IOA-289 and galunisertib had a significantly longer survival than any double combination treatments [mOS=47 days, p<0.05]. In mice treated with gemcitabine in combination with IOA-289 and/or GAL we measured a significantly reduced infiltration of CAFs, a reduction in plasma levels of CTGF and a diminished degree of fibrosis compared with any single control treatment.In conclusion, we demonstrate that the overexpression of autotaxin by stromal PSC might be an adaptive mechanism in response to TGFβ receptor inhibition. IOA-289 is a novel agent that warrants further clinical development in combination with gemcitabine plus GAL for the treatment of PC patients. Citation Format: Fabio Sabbadini, Monica Bertolini, Domenico Mangiameli, Serena Contarelli, Zoë Johnson, Michael M. Lahn, Silvia Pietrobono, Davide Melisi. Targeting stromal autotaxin synergizes with TGF beta inhibition in pancreatic cancer [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2022; 2022 Apr 8-13. Philadelphia (PA): AACR; Cancer Res 2022;82(12_Suppl):Abstract nr 1064.
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Truong Thi, Thanh Dung, and Tri Nguyen Minh. "Biochemical compositions, antioxidant activity, and in vitro antibacterial activity of extract from wild bitter melon (Momordica charantia var. abbreviata Ser.)." Heavy metals and arsenic concentrations in water, agricultural soil, and rice in Ngan Son district, Bac Kan province, Vietnam 4, no. 2 (May 25, 2021): 109–14. http://dx.doi.org/10.47866/2615-9252/vjfc.3787.
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Wild bitter melon (Momordica charantia var. abbreviata Ser.) is a type of vine that grows wildly in the mountains and plains in Vietnam. The main use parts of the tree are fruit, stem, and leaf that can be eaten as vegetables. This study aims to (1) identify several bioactive chemical compounds in the stems and leaves of bitter melon trees in the forests in the district of Mang Yang, Gia Lai province; (2) evaluate the nutrient composition, antioxidant activity, and antimicrobial ability of fresh juice and extract with ethanol 70°. The results indicated that fresh juice and ethanol 70° extract currently inhibited the growth of experimental strains of microorganisms, in which ethanol 70o extract gives the highest antimicrobial effect. The qualitative results determined that the chemical components of wide bitter melon consist of flavonoids, saponins, tannins, free reducing sugar, organic acids, starch, and fatty acids as the basis for the standardization of exploitation of medicinal resources this material.
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Li, Peipei, Junlu Bai, XiaoJun Zhang, Zhongyong Yan, Pengfei He, and Yin Chen. "Structure and Anticoagulant Activity of a Galactofuranose-Containing Sulfated Polysaccharide from the Green Seaweed, Codium isthmocladum." Molecules 27, no. 22 (November 18, 2022): 8012. http://dx.doi.org/10.3390/molecules27228012.
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A water-soluble sulfated polysaccharide, F2-1, was obtained from the marine green alga, Codium isthmocladum, using ion-exchange and size-exclusion chromatography. Structure analysis showed that the F2-1 was a sulfated arabinan comprising Ara, Rha, Man, Gal, and Xyl with an 18% sulfate content and a molecular weight of 100 kDa. Methylation analysis combined with desulfation, GC-MS, IR, and NMR spectroscopy showed that the backbone of F2-1 was →4)-β-L-Arap(1→ residue. Its 2-O and/or 3-O positions showed sulfate modification; additionally, the 2-O or 3-O position showed branch points. The side chains were composed of →5)-β-D-Galf, (1→2,6)-β-D-Galf(1→, (1→2)-β-L-Rhap4S, →4)-α-D-Glcp(1→, and terminal α-D-Galp(1→ and β-D-Xylp(1→. Polysaccharides containing β-D-galactofuranose are rarely found in seaweed. F2-1 exhibited significant anticoagulant activity in vitro. Our findings suggested that the green-tide alga, Codium isthmocladum, can be considered as a useful resource for bioactive polysaccharides.
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Hooijdonk, Ben van, David Woolley, Ian Warrington, and Stuart Tustin. "Rootstocks Modify Scion Architecture, Endogenous Hormones, and Root Growth of Newly Grafted ‘Royal Gala’ Apple Trees." Journal of the American Society for Horticultural Science 136, no. 2 (March 2011): 93–102. http://dx.doi.org/10.21273/jashs.136.2.93.
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‘Royal Gala’ apple scions (Malus ×domestica) were grafted onto 1-year-old rootstock stools of ‘M.9’ (M.9), ‘M.M.106’ (MM.106), ‘Merton 793’ (M.793), and ‘Royal Gala’ [R.G (control)] to elucidate how the dwarfing apple rootstock (M.9) modified scion architecture, the time from grafting when this started, and whether changes in scion architecture were explained by some endogenous hormones present within the scion. At the end of the first season of growth (April), the final length and node number of the primary shoot were similar for scions on M.9 and R.G. However, M.9 appeared to limit the number of secondary shoots formed on the primary shoot during summer. In addition, the proportion of secondary shoots that were actively extending in fall was lower for M.9; consequently, the final mean length of the secondary shoots was slightly shorter for M.9 compared with R.G. Collectively, these subtle effects of M.9 significantly reduced the final total shoot length of the scion compared with R.G. The final dry weight of the scion and root system was also lower for M.9 than MM.106, M.793, and R.G. The mean rate of indole-3-acetic acid diffusing from the apex of the primary shoot progressively declined from February onward irrespective of rootstock, whereas the mean concentration of zeatin riboside (ZR) in the xylem sap increased during the same period, and these events appeared to coincide with cumulative increases in the number of axillary growing points formed on the scion. Despite this general trend, M.9 had a greater concentration of ZR in the xylem sap during February compared with R.G, but the primary shoot on M.9 did not develop more axillary growing points, indicating that other endogenous hormonal signals were also involved in regulating scion branching. By March, M.9 lowered gibberellin A19 (GA19) concentration in the xylem sap of the scion significantly compared with R.G. We conclude that dwarfing apple rootstocks may limit root-produced GA19 supplied to shoot apices of the scion, where GA19 may be a precursor of bioactive gibberellin A1 required for shoot extension growth.
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Kistechok, Andrii, Dariusz Wrona, and Tomasz Krupa. "Quality and Nutritional Value of ‘Chopin’ and Clone ‘JB’ in Relation to Popular Apples Growing in Poland." Agriculture 12, no. 11 (November 9, 2022): 1876. http://dx.doi.org/10.3390/agriculture12111876.
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The aim of the study was to describe the physicochemical properties, with particular emphasis on nutritional value, of apples ‘Chopin’ and clone ‘JB’. The new cultivars were compared with the cultivars commonly cultivated in Polish orchards, namely ‘Gala Brookfield’, ‘Šampion’, ‘Ligol’ and ‘Idared’. The study focuses on the evaluation of physicochemical characteristic (firmness, soluble solids content and titratable acidity) and the content of monosaccharides, sucrose and organic acids based on HPLC with an RI detector. In addition, the nutritional value of apples were described separately for the flesh and peel of the fruit, focusing on the assessment of the antioxidant activity and the content of total polyphenols, phenolic acids, flavonols using the HPLC technique. ‘Chopin’ and ‘JB’ clone apples are characterized by very high acidity, over 1%, which is related to the high content of malic acid. The red flesh ‘JB’ clone is characterized by a high content of bioactive compounds in both the peel and flesh of apples. High temperatures and a lack of precipitation contribute to a higher polyphenol content in apples, which proves that apart from the genetic features of the cultivars, the climatic conditions also determine the nutritional value of the fruit.
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Tran, Thien Hien, Le Ke Ha, Duy Chinh Nguyen, Tan Phat Dao, Le Thi Hong Nhan, Dai Hai Nguyen, Trinh Duy Nguyen, Dai-Viet N. Vo, Quoc Toan Tran, and Long Giang Bach. "The Study on Extraction Process and Analysis of Components in Essential Oils of Black Pepper (Piper nigrum L.) Seeds Harvested in Gia Lai Province, Vietnam." Processes 7, no. 2 (January 22, 2019): 56. http://dx.doi.org/10.3390/pr7020056.
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Black pepper (Piper nigrum L.) is a tropical crop with extensive medicinal potential in ethnomedicine and nutraceutical applications. The essential oil of black pepper finds wide applications in inhabitation of respiratory infections and soothing of muscular pains due to its warming and energizing property. The pungent bioactive piperine is responsible for this function, and therefore, efficient technology is required for an optimal extraction process of this compound. In the present article, we have developed a procedure for extracting black pepper essential oil from Vietnam, optimizing conditions that affect the extraction process. The effect of process parameters, namely material size, preservation method, the concentration of sodium chloride, the concentration of soak time, the ratio of material to water, temperature extraction, time extraction on the extraction yield, and relative efficiency were investigated. Results demonstrated that 20 g of black pepper milled with a mesh size of 160 obtained 0.48 g of essential oil (2.4%) at a raw material to water ratio of 1/21 (g/mL) at 150 °C in a time of 5.2 h. GC-MS (Gas chromatography–mass spectrometry) spectra showed that 3-carene (29.21%), D-limonene (20.94%), caryophyllene (15.05%), and β-pinene (9.77%) were present as major components. These results suggested that the essential oil extracted from Vietnamese black pepper is applicable in the manufacturing processes of insecticides and air deodorizers.