Journal articles on the topic '2'.3-Dihydroxyflavone'
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1
Labarrière, Luc, Aurélien Moncomble, and Jean-Paul Cornard. "pH dependency of the structural and photophysical properties of the atypical 2′,3-dihydroxyflavone." RSC Advances 10, no. 58 (2020): 35017–30. http://dx.doi.org/10.1039/d0ra06833k.
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Nassira GHEMBAZA, Nabila BELYAGOUBI-BENHAMMOU, Amel ZITOUNI, Fethi TOUL, Serge MICHALET, and Fawzia ATIK- BEKKARA. "Rapid identification analysis of chemical constituents of Sedum villosum L. (Orpin.) by UHPLC-DAD-HRSM." Journal of Natural Product Research and Applications 1, no. 01 (September 17, 2021): 15–23. http://dx.doi.org/10.46325/jnpra.v1i01.2.
Abstract:
In the present paper, we are interested, for the first time, to separate and identify two glycosyl the flavones from Sedum villosum L, family Crassulaceae collected in the flowering phase in Lakhdar Oued, village of Tlemcen (Algeria). The crude methanolic extract of the flowers part was fractionated on column chromatography, and eluted with dichloromethane/methanol each time with increasing polarity of methanol; 24 fractions were separated. One of these fractions named F16 showed more antioxidant activity to scavenge DPPH free radical with percentage inhibition of 94.849 %. F16 was separated by thin-layer chromatography (TLC) to give 10 compounds. We were chosen the sub-fractions F16.8, which has antioxidative activity of 77.02 %, provided two major molecules of glycosyl the flavones, analysed by ultra-highperformance liquid chromatography coupled to mass spectrometry (UHPLC-DAD-HRSM). Compound 1 was identified as 7, 3'-dihydroxyflavone-5-O-dihexosyl-4'-O-deoxyhexose and compound 2 was 7, 3'-dihydroxyflavone-5-O-hexose- 4'-O-deoxyhexose.
3
Datta, Bidyut Kanti, Tahamina Iasmin, and Mohammad A. Rashid. "Further Flavonoids from Polygonum viscosum Buch-Ham. ex D. Don. (Polygonoceae)." Dhaka University Journal of Pharmaceutical Sciences 15, no. 1 (August 8, 2016): 27–30. http://dx.doi.org/10.3329/dujps.v15i1.29189.
Abstract:
Three additional flavonoids such as 5,7,4?-trihydroxy-3,8,3?-trimethoxy flavonol (1), 5,7-dihydroxyflavone (chrysin, 2) and 5,6,7-trihydroxyflavone (baicalein, 3) were obtained from the methanol extract of whole plant of Polygonum viscosum. The structure of the isolated compounds was established exclusively by ultraviolet (UV) spectroscopy, mass spectrometry (MS) and a series of Nuclear Magnetic Resonance (NMR) analysis.Dhaka Univ. J. Pharm. Sci. 15(1): 27-30, 2016 (June)
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Sakalauskas, Andrius, Agne Janoniene, Gediminas Zvinys, Kamile Mikalauskaite, Mantas Ziaunys, and Vytautas Smirnovas. "Exploring the Formation of Polymers with Anti-Amyloid Properties within the 2′3′-Dihydroxyflavone Autoxidation Process." Antioxidants 11, no. 9 (August 30, 2022): 1711. http://dx.doi.org/10.3390/antiox11091711.
Abstract:
Amyloid-β and α-synuclein aggregation into amyloid fibrils is linked to the onset and progression of Alzheimer’s and Parkinson’s diseases. While there are only a few disease-modifying drugs, it is essential to search for new, more effective ways to encounter these neurodegenerative diseases. Multiple research articles have shown that the autoxidation of flavone is a critical factor for activating the inhibitory potential against the protein aggregation. Despite this, the structure of the newly-formed inhibitors is unknown. In this research, we examined the autoxidation products of 2′,3′-dihydroxyflavone that were previously shown to possess one of the most prominent inhibitory effects against amyloid-β aggregation. Their analysis using HPLC suggested the formation of polymeric molecules that were isolated using a 3 kDa cut-off. These polymeric structures were indicated as the most potent inhibitors based on protein aggregation kinetics and AFM studies. This revelation was confirmed using MALDI-TOF and NMR. We also show that active molecules have a tendency to reduce the Amyloid-β and α-synuclein aggregates toxicity to SH-SY5Y cells.
5
Cody, Vivian, Joseph Luft, Mary Mc Court, and Klaus Irmscher. "Conformational analysis of flavonoids: Crystal and molecular structure of 3?,5?-dibromo-3-methyl-6,4?-dihydroxyflavone (1:2) triphenylphosphine oxide complex." Structural Chemistry 2, no. 6 (October 1991): 601–6. http://dx.doi.org/10.1007/bf00673444.
6
Fatoki, Toluwase, Stanley Chukwuejim, Omodele Ibraheem, Christiana Oke, Blessing Ejimadu, Isaiah Olaoye, Oluwabukola Oyegbenro, et al. "Harmine and 7,8-dihydroxyflavone synergistically suitable for amyotrophic lateral sclerosis management: An in silico study." Research Results in Pharmacology 8, no. 3 (August 25, 2022): 49–61. http://dx.doi.org/10.3897/rrpharmacology.8.83332.
Abstract:
Introduction: Amyotrophic lateral sclerosis (ALS) is a fatal neurological disease characterized by progressive degeneration of both upper and lower motor neurons, resulting in paralysis and eventually leads to death from respiratory failure typically within 3 to 5 years of symptom onset. The aim of this work was to predict the pharmacokinetics and identify unique protein targets that are associated with potential anti-ALS phytochemicals and FDA-approved drugs, by in silico approaches. Materials and methods: Standard computational tools (webserver and software) were used, and the methods used are clustering analysis, pharmacokinetics and molecular target predictions, and molecular docking simulation. Results and discussion: The results show that riluzole, β-asarone, cryptotanshinone, harmine and 7,8-dihydroxyflavone have similar pharmacokinetics properties. Riluzole and harmine show 95% probability of target on norepinephrine transporter. Huperzine-A and cryptotanshinone show 100% probability of target on acetylcholinesterase. 7,8-dihydroxyflavone shows 35% probability of target on several carbonic anhydrases, 40% probability of target on CYP19A1, and 100% probability of target on inhibitor of nuclear factor kappa B kinase beta subunit and neurotrophic tyrosine kinase receptor type 2, respectively. Harmine also shows 95% probability of target on dual specificity tyrosine-phosphorylation-regulated kinases, threonine-protein kinases (haspin and PIM3), adrenergic receptors, cyclin-dependent kinases (CDK5 and CDK9), monoamine oxidase A, casein kinase I delta, serotonin receptors, dual specificity protein kinases (CLK1, CLK2, and CLK4), and nischarin, respectively. Also, the results of gene expression network show possible involvement of CDK1, CDK2, CDK4, ERK1, ERK2 and MAPK14 signaling pathways. This study shows that riluzole and harmine have closely similar physicochemical and pharmacokinetics properties as well as molecular targets, such as norepinephrine transporter (SLC6A2). Harmine, huperzine-A and cryptotanshinone could modulate acetylcholinesterase (AChE), which is involved in ALS-pathogenesis. The impact of 7,8-dihydroxyflavone on several carbonic anhydrases (CA) I, II, VII, IX, XII, and XIV, as well as CYP19A1, could help in remediating the respiratory failure associated with ALS. Conclusion: Overall, harmine is found to be superior to riluzole, and the combination of harmine with 7,8-dihydroxyflavone can provide more effective treatment for ALS than the current regime. Further work is needed to validate the predicted therapeutic targets of harmine identified in this study on ALS model or clinical trials, using in silico, in vitro and in vivo techniques. Graphical abstract:
7
Jiang, Meng, Xing Su, Jianling Liu, Chunli Zheng, and Xiaogang Li. "Systems Pharmacology-Dissection of the Molecular Mechanisms of Dragon’s Blood in Improving Ischemic Stroke Prognosis." Evidence-Based Complementary and Alternative Medicine 2020 (May 18, 2020): 1–14. http://dx.doi.org/10.1155/2020/4858201.
Abstract:
Ethnopharmacological Relevance. Dragon’s blood (DB) is a widely used traditional Chinese medicine that has many pharmacological effects, including antiplatelet aggregation, promoting epidermal growth, and anti-inflammatory and antioxidant activities. The main component of Longxuetongluo capsule and Dragon’s blood dropping pills is DB’s standard phenolic extract, which was used for ischemic stroke prognosis in China. Aim of Study. To dissect the molecular mechanisms of Dragon’s blood (DB) in improving ischemic stroke prognosis. Materials and Methods. (1) Based on system-pharmacology platform, the potential active compounds of DB are screened out according to ADME. (2) The ischemic stroke-related targets are predicted by utilizing these active compounds as probes, mapping the targets to the CTD database to establish a molecular-target-disease network. (3) To analyze the mechanism of DB treatment for the prognosis of ischemic stroke, we used the Metascape and DAVID databases to construct “ischemic stroke pathways”. (4) PC12 cells were used to explore the protective effect of loureirin B on oxygen-glucose deprivation/reperfusion (OGD/R) injury, and BV-2 cells were used to determine the anti-inflammation effect of 4′,7-dihydroxyflavone. Results. Finally, we obtained 38 active compounds and 58 stroke-related targets. Network and pathway analysis indicate that DB is effective in the treatment of ischemic stroke by enhancing cell survival and inhibiting inflammatory and antiplatelet activation. In in vitro experiments, the main component loureirin B promoted the expression of HO-1 and Bcl-2 via positive regulation of PI3K/AKT/CREB and Nrf2 signaling pathways in PC12 cells against OGD/R damage. And the anti-inflammatory activity of 4′,7-dihydroxyflavone was related to the inhibition of COX-2, TNF-α, and IL-6 in LPS-induced BV-2 cells. Conclusions. In our study, the results illustrated that DB in improving ischemic stroke prognosis may involve enhancing cell survival and antioxidant, anti-inflammation, and antiplatelet activities.
8
CODY, V., J. LUFT, M. MC COURT, and K. IRMSCHER. "ChemInform Abstract: Conformational Analysis of Flavonoids: Crystal and Molecular Structure of 3′,5′-Dibromo-3-methyl-6,4′-dihydroxyflavone (1:2) Triphenylphosphine Oxide Complex." ChemInform 23, no. 4 (August 22, 2010): no. http://dx.doi.org/10.1002/chin.199204046.
9
Gu, Jian-Qiao, Yuehong Wang, Scott G. Franzblau, Gloria Montenegro, and Barbara N. Timmermann. "Constituents of Quinchamalium majus with Potential Antitubercular Activity." Zeitschrift für Naturforschung C 59, no. 11-12 (December 1, 2004): 797–802. http://dx.doi.org/10.1515/znc-2004-11-1206.
Abstract:
Antitubercular bioassay-guided fractionation of the dichloromethane extracts of the above-ground biomass and roots of Quinchamalium majus led to the identification of six known constituents, betulinic acid (1), daucosterol (2), 5,7-dihydroxyflavone (3), oleanolic acid (4), (D)-2S-pinocembrin (5), and ursolic acid (6), for the first time in this species. Their chemical structures were determined on the basis of spectroscopic evidence and chemical transformation methods. All of these compounds along with additional 11 analogues were evaluated for their antitubercular potential against Mycobacterium tuberculosis in a microplate alamar blue assay, and the primary structure-activity relationships (SARs) for 4 and 6 were discussed. In addition, all the isolates were tested for cytotoxicity against African green monkey Vero cells in order to evaluate for their selectivity potential.
10
Egwuatu, Ifeanyi Anthony, Chiadikobi Lawrence Ozoemena, Emeka Williams Ugwuishi, Christian Chiemeka Ozor, Augustine Oviosun, and Favour Onwene. "Deciphering the Ameliorative Potential of 5, 7-dihydroxyflavone (Chrysin) on Doxorubicin-Induced Cardiotoxicity by Modulating Oxidative Stress in Rats." Scholars International Journal of Anatomy and Physiology 6, no. 11 (November 23, 2023): 181–90. http://dx.doi.org/10.36348/sijap.2023.v06i11.005.
Abstract:
Doxorubicin-induced cardiotoxicity is the leading cause of morbidity and mortality among cancer survivors. The present study aimed to investigate the ameliorative effect of 5, 7-dihydroxyflavone (chrysin) against doxorubicin-induced cardiotoxicity in Wistar rats. Thirty-five adult male Wistar albino rats were randomly allocated into seven groups (n = 5 each) which consisted of normal control (group 1) receiving phosphate buffer saline (0.4 ml), positive control (Group 2) received 2mg\kg of doxorubicin (DOX) through an intraperitoneal route once weekly for 21 days, chrysin low dose and chrysin high dose (Group 3 and 4) received oral administration of chrysin 50&100mg/kg for 21 days, chrysin low dose and DOX, chrysin medium dose and DOX and chrysin high dose and DOX(group 5, 6, and 7) received 2mg/kg of DOX once weekly with 50, 100 and 150mg/kg of chrysin for 21 days. Significant elevations in cardiac troponin I (cTnI) and histological lesions, which corresponded with oxidative stress, inflammation, apoptotic indicators, and cardiotoxicity when compared to controls, were indicative of DOX-induced cardiotoxicity. Malondialdehyde (MDA), a sign of oxidative stress, SOD, CPK (creatinine phosphokinase), TBARS (thiobarbituric acid reactive substance), and CAT (catalase) were also elevated in the DOX group. The DOX group also had increased levels of cardiac inflammatory markers, including as interleukin-1 (IL-1), interleukin-6 (IL-6), and the apoptotic marker caspase-3. 5, 7-dihydroxyflavone (chrysin) significantly mitigated, but did not entirely reverse, the cardiotoxicity caused by DOX by reducing the histopathological scores of cardiomyopathies and lowering cTnI in comparison to the DOX group. Additionally, chrysin reduced MDA to substantially similar levels as the control. Following chrysin administration, significant decreases in IL-1, IL-6, and caspase-3 were also seen in comparison to the DOX-only group. All things considered, these findings point to chrysin's protective action against DOX-induced cardiotoxicity, which may have been rendered possible by oxidative stress, inflammatory, and apoptotic suppression.
11
Stompor, Monika, Marta Świtalska, and Joanna Wietrzyk. "Synthesis and biological evaluation of acyl derivatives of hydroxyflavones as potent antiproliferative agents against drug resistance cell lines." Zeitschrift für Naturforschung C 73, no. 1-2 (January 26, 2018): 87–93. http://dx.doi.org/10.1515/znc-2017-0093.
Abstract:
AbstractThe synthesis of hydroxyflavone derivatives is described. The acyl derivatives of 3-, 6-, 7-hydroxyflavones (compounds2,4,6, respectively) and chrysin (5,7-dihydroxyflavone,7) were obtained in high yields and evaluated in vitro for their cytotoxic activity against several cancer cell lines of different origin: MCF-7 (breast cancer), A549 (nonsmall cell lung cancer), MES-SA (uterine sarcoma), LoVo (colon cancer), drug-resistant human cancer cells (MES-SA/DX5, LoVo/DX) and also towards non-cancer cell line MCF-10A (normal breast epithelial cells). The flavones modified with acyl group showed higher antiproliferative activity than free hydroxyflavones. The highest activity was noted for 3-acetoxyflavone (2), which proved active against LoVo, LoVo/DX, and MES-SA cell lines (IC50from 4.7 μM to 7.8 μM, respectively). The highest ability to overcome the barrier of resistance (resistance index=0.82) against the drug-resistant MES-SA/DX5 cells compared to the parental drug-sensitive MES-SA cell line was found for 7-acetoxyflavone (6).
12
Gabriela, Nuño, Alberto María Rosa, Zampini Iris Catiana, Cuello Soledad, Ordoñez Roxana Mabel, Sayago Jorge Esteban, Baroni Veronica, Wunderlin Daniel, and Isla María Ines. "The Effect of Zuccagnia punctata, an Argentine Medicinal Plant, on Virulence Factors from Candida Species." Natural Product Communications 9, no. 7 (July 2014): 1934578X1400900. http://dx.doi.org/10.1177/1934578x1400900712.
Abstract:
Zuccagnia punctata Cav. has been used as a traditional medicine in Argentina for the treatment of bacterial and fungal infections. In this study, we evaluated the ability of Z. punctata extract (ZpE) and compounds isolated from it to inhibit the growth and virulence factors of Candida species. ZpE showed inhibitory activity against planktonic cells of all assayed Candida species with MIC values of 400 μg/mL and with MFC values between 400 and 1,200 μg/mL. The principal identified compounds by HPLC-MS/MS and UV-VIS were chalcones (2′,4′-dihydroxy-3′-methoxychalcone, 2′,4′- dihydroxychalcone), flavones (galangin, 3,7-dihydroxyflavone and chrysin) and flavanones (naringenin, 7-hydroxyflavanone and pinocembrine). These compounds were more effective as inhibitors than the extracts upon biofilm formation as well as on preformed Candida biofilm and yeast germ tube formation. Furthermore, ZpE and chalcones are able to inhibit exoenzymes, which are responsible for the invasion mechanisms of the pathogens. All these effects could moderate colonization, thereby suppressing the pathogen invasive potential. Our results indicate that ZpE and chalcones could be used in antifungal therapy.
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Chagas, Maria do Socorro S., Maria D. Behrens, Carla J. Moragas-Tellis, Gabriela X. M. Penedo, Adriana R. Silva, and Cassiano F. Gonçalves-de-Albuquerque. "Flavonols and Flavones as Potential anti-Inflammatory, Antioxidant, and Antibacterial Compounds." Oxidative Medicine and Cellular Longevity 2022 (September 6, 2022): 1–21. http://dx.doi.org/10.1155/2022/9966750.
Abstract:
Plant preparations have been used to treat various diseases and discussed for centuries. Research has advanced to discover and identify the plant components with beneficial effects and reveal their underlying mechanisms. Flavonoids are phytoconstituents with anti-inflammatory, antimutagenic, anticarcinogenic, and antimicrobial properties. Herein, we listed and contextualized various aspects of the protective effects of the flavonols quercetin, isoquercetin, kaempferol, and myricetin and the flavones luteolin, apigenin, 3 ′ ,4 ′ -dihydroxyflavone, baicalein, scutellarein, lucenin-2, vicenin-2, diosmetin, nobiletin, tangeretin, and 5-O-methyl-scutellarein. We presented their structural characteristics and subclasses, importance, occurrence, and food sources. The bioactive compounds present in our diet, such as fruits and vegetables, may affect the health and disease state. Therefore, we discussed the role of these compounds in inflammation, oxidative mechanisms, and bacterial metabolism; moreover, we discussed their synergism with antibiotics for better disease outcomes. Indiscriminate use of antibiotics allows the emergence of multidrug-resistant bacterial strains; thus, bioactive compounds may be used for adjuvant treatment of infectious diseases caused by resistant and opportunistic bacteria via direct and indirect mechanisms. We also focused on the reported mechanisms and intracellular targets of flavonols and flavones, which support their therapeutic role in inflammatory and infectious diseases.
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Egwuatu, Ifeanyi Anthony, Emeka Godson Anyanwu, Augustine Oviosun, Abraham John Chukwuebuka, Chiadikobi Lawrence Ozoemena, Ekene Valentine Ugbor, and Maduadichie Arinze Godswill. "Ameliorative Effects of 5-7, Dihydroxy Flavone (Chrysin) on Hippocampus of Wistar Rats with Doxorubicin-induced Cognitive Impairment." Journal of Complementary and Alternative Medical Research 22, no. 2 (June 5, 2023): 49–61. http://dx.doi.org/10.9734/jocamr/2023/v22i2456.
Abstract:
Concern is increasing regarding the effect of chemotherapy induced cognitive impairment on oncology patients. This sought to investigate the effect of 5-7, dihydroxyflavone on the hippocampus of wistar rats with Doxorubicin induced cognitive impairment. 30 male Wistar rats were procured and acclimatized for 14 days with feed and water, they were divided into six (6) experimental groups of five (5) animals each. Group 1 served as normal control. Group 2 was induced with 2mg/kg of DOX and was untreated. Group 3 received 150mg/kg of Chrysin. Groups 4, 5 and 6 were induced with 2mg/kg of doxorubicin and treated with Chrysin at doses of 50mg/kg, 100mg/kg, and 150mg/kg respectively. The study lasted for 21 days. The body weight of the animals were recorded three (3) times before and after induction and then recorded again at the end of the 21 days treatment. At the end of the experiment, there were significantly increase in body weight. The increase was more pronounce in group 1 and group 2. In the oxidative stress analysis and ELISA analysis on the levels of inflammatory cytokines (IL-1 & IL-6), there was a significant increase in the levels compared to the control group 1. In the neurobehavioural test, group 6 had a high spontaneous alternation percentage compared to other groups. The treatment with Chrysin significantly had an ameliorative effect on the treated animal groups and in group 3. The result from this work suggest that Chrysin extract had an ameliorative effect on cognitive impairment of the hippocampus.
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Mehdi, Syed Hassan, Md Zafaryab, Sana Nafees, Asad Khan, Irfan Ahmad, Zubair Bin Hafeez, and Moshahid Alam Rizvi. "Chrysin Sensitizes Human Lung Cancer Cells to Tumour Necrosis Factor Related Apoptosis-Inducing Ligand (TRAIL) Mediated Apoptosis." Asian Pacific Journal of Cancer Biology 4, no. 2 (August 3, 2019): 27–33. http://dx.doi.org/10.31557/apjcb.2019.4.2.27-33.
Abstract:
Background: Lung cancer is the primary cause of cancer deaths worldwide. Thus, the requisite for more coherent methods to lung cancer therapy is needed. Purpose: Chrysin (5, 7-dihydroxyflavone) is a naturally occurring flavonoid having a wide range of pharmacological properties and is commonly found in fruits, vegetables, honey and propolis. In our study, we have hypothesized that chrysin would have anticancer activity on L132 lung cancer cell line.Methods: The cytotoxic effects were assessed by MTT and NRU assay. DAPI was used to evaluate the cell death. The pro- or anti-apoptotic proteins were detected by Western Blot assay, and, besides, mRNA expression was analysed with RT-PCR. In silico study of chrysin was performed to identify suitable inhibitors against the protein function. Results: Results indicated that chrysin enhanced the inhibitory effects of TRAIL (Tumour Necrosis Factor Related Apoptosis-Inducing Ligand) in comparison to TNF-α (tumour necrosis factor) on cell viability in L132 lung cancer cells and altered nuclear morphology of cells was observed in DAPI (4’,6-diamidino-2-phenylindole) staining after 48 hrs treatment. Treatment with chrysin enhances TRAIL-induced apoptosis by increasing the expression of apoptosis-related proteins including caspase-3, 8, 9 and Bax, whereas the expression of Bcl-2 was decreased. Chrysin was docked with caspase-3, 8, 9, Bax, and Bcl-2 proteins to identify suitable inhibitors against the protein function.Conclusion: We concluded that chrysin sensitizes lung cancer cells to TRAIL-induced apoptosis and may be considered for future studies as a promising therapeutic candidate for human lung cancer.
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Ademuwagun, Ibitayo Abigail, Gbolahan Oladipupo Oduselu, Solomon Oladapo Rotimi, and Ezekiel Adebiyi. "Pharmacophore-Aided Virtual Screening and Molecular Dynamics Simulation Identifies TrkB Agonists for Treatment of CDKL5-Deficiency Disorders." Bioinformatics and Biology Insights 17 (January 2023): 117793222311582. http://dx.doi.org/10.1177/11779322231158254.
Abstract:
Therapeutic intervention in cyclin-dependent kinase-like 5 (CDKL5) deficiency disorders (CDDs) has remained a concern over the years. Recent advances into the mechanistic interplay of signalling pathways has revealed the role of deficient tropomyosin receptor kinase B (TrkB)/phospholipase C γ1 signalling cascade in CDD. Novel findings showed that in vivo administration of a TrkB agonist, 7,8-dihydroxyflavone (7,8-DHF), resulted in a remarkable reversal in the molecular pathologic mechanisms underlying CDD. Owing to this discovery, this study aimed to identify more potent TrkB agonists than 7,8-DHF that could serve as alternatives or combinatorial drugs towards effective management of CDD. Using pharmacophore modelling and multiple database screening, we identified 691 compounds with identical pharmacophore features with 7,8-DHF. Virtual screening of these ligands resulted in identification of at least 6 compounds with better binding affinities than 7,8-DHF. The in silico pharmacokinetic and ADMET studies of the compounds also indicated better drug-like qualities than those of 7,8-DHF. Postdocking analyses and molecular dynamics simulations of the best hits, 6-hydroxy-10-(2-oxo-1-azatricyclo[7.3.1.05,13]trideca-3,5(13),6,8-tetraen-3-yl)-8-oxa-13,14,16-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1,3,6,9,11,15-hexaen-5-one (PubChem: 91637738) and 6-hydroxy-10-(8-methyl-2-oxo-1H-quinolin-3-yl)-8-oxa-13,14,16-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1,3,6,9,11,15-hexaen-5-one (PubChem ID: 91641310), revealed unique ligand interactions, validating the docking findings. We hereby recommend experimental validation of the best hits in CDKL5 knock out models before consideration as drugs in CDD management.
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Mohos, Violetta, Eszter Fliszár-Nyúl, Gabriella Schilli, Csaba Hetényi, Beáta Lemli, Sándor Kunsági-Máté, Balázs Bognár, and Miklós Poór. "Interaction of Chrysin and Its Main Conjugated Metabolites Chrysin-7-Sulfate and Chrysin-7-Glucuronide with Serum Albumin." International Journal of Molecular Sciences 19, no. 12 (December 17, 2018): 4073. http://dx.doi.org/10.3390/ijms19124073.
Abstract:
Chrysin (5,7-dihydroxyflavone) is a flavonoid aglycone, which is found in nature and in several dietary supplements. During the biotransformation of chrysin, its conjugated metabolites chrysin-7-sulfate (C7S) and chrysin-7-glucuronide (C7G) are formed. Despite the fact that these conjugates appear in the circulation at much higher concentrations than chrysin, their interactions with serum albumin have not been reported. In this study, the complex formation of chrysin, C7S, and C7G with human (HSA) and bovine (BSA) serum albumins was investigated employing fluorescence spectroscopic, ultrafiltration, and modeling studies. Our major observations/conclusions are as follows: (1) Compared to chrysin, C7S binds with a threefold higher affinity to HSA, while C7G binds with a threefold lower affinity; (2) the albumin-binding of chrysin, C7S, and C7G did not show any large species differences regarding HSA and BSA; (3) tested flavonoids likely occupy Sudlow’s Site I in HSA; (4) C7S causes significant displacement of Sudlow’s Site I ligands, exerting an even stronger displacing ability than the parent compound chrysin. Considering the above-listed observations, the high intake of chrysin (e.g., through the consumption of dietary supplements with high chrysin contents) may interfere with the albumin-binding of several drugs, mainly due to the strong interaction of C7S with HSA.
18
Balta, Cornel, Alina Ciceu, Hildegard Herman, Marcel Rosu, Oana Maria Boldura, and Anca Hermenean. "Dose-Dependent Antifibrotic Effect of Chrysin on Regression of Liver Fibrosis: The Role in Extracellular Matrix Remodeling." Dose-Response 16, no. 3 (July 1, 2018): 155932581878983. http://dx.doi.org/10.1177/1559325818789835.
Abstract:
Liver fibrosis represents an overaccumulation of extracellular matrix (ECM). This study was designed to investigate the effect of chrysin on established ECM overproduction in carbon tetrachloride (CCl4) mouse liver fibrosis. Experimental fibrosis was induced by intraperitoneal injection of 2 mL/kg CCl4 twice a week, for 7 weeks. Mice were orally treated with 3 doses of chrysin (5,7-dihydroxyflavone). For the assessment of the spontaneous reversion of fibrosis, CCl4-treated mice were investigated after 2 weeks of recovery time. Silymarin was used as a standard of liver protection. In fibrotic livers, the results showed the upregulation of collagen I (Col I) and tissue inhibitors of metalloproteinase 1 (TIMP-1) and modulation of matrix metalloproteinases (MMPs), which led to an altered ECM enriched in Col, confirmed as well by electron microscopy investigations. Treatment with chrysin significantly reduced ultrastructural changes, downregulated Col I, and restored TIMP-1/MMP balance, whereas in the group observed for the spontaneous regression of fibrosis, they remained in the same pattern with fibrotic livers. In this study, we have shown chrysin efficacy to attenuate dose-dependent CCl4-stimulated liver ECM accumulation by regulation of MMP/TIMP imbalance and inhibition of Col production. We have shown the dose-dependent chrysin efficiency in attenuation of CCl4-induced liver ECM accumulation by regulation of MMP/TIMP imbalance and inhibition of Col production. Our findings suggest that chrysin oral administration may introduce a new strategy for treating liver fibrosis in humans.
19
Klebe, Damon, Mahima Tibrewal, Deep R. Sharma, Rachna Vanaparthy, Sunil Krishna, Merina Varghese, Bokun Cheng, et al. "Reduced Hippocampal Dendrite Branching, Spine Density and Neurocognitive Function in Premature Rabbits, and Reversal with Estrogen or TrkB Agonist Treatment." Cerebral Cortex 29, no. 12 (March 16, 2019): 4932–47. http://dx.doi.org/10.1093/cercor/bhz033.
Abstract:
Abstract Preterm-born children suffer from neurological and behavioral disorders. Herein, we hypothesized that premature birth and non-maternal care of preterm newborns might disrupt neurobehavioral function, hippocampal dendritic arborization, and dendritic spine density. Additionally, we assessed whether 17β-estradiol (E2) replacement or the TrkB receptor agonist, 7,8-dihydroxyflavone (DHF), would reverse compromised dendritic development and cognitive function in preterm newborns. These hypotheses were tested by comparing preterm (E28.5) rabbit kits cared and gavage-fed by laboratory personnel and term-kits reared and breast-fed by their mother doe at an equivalent postconceptional age. Neurobehavioral tests showed that both premature-birth and formula-feeding with non-maternal care led to increased anxiety behavior, poor social interaction, and lack of novelty preference compared with term-kits. Dendritic branching and number of total or mushroom dendritic spines were reduced in the CA1 field of preterm-kits compared with term controls. While CDC42 and Rac1/2/3 expression levels were lower, RhoA-activity was higher in preterm-kits compared with term controls. Both E2 and DHF treatment reversed prematurity-induced reduction in spine density, reduced total RhoA-GTPase levels, and enhanced cognitive function. Hence, prematurity and non-maternal care result in cognitive deficits, and reduced dendritic arbors and spines in CA1. E2 replacement or DHF treatment might reverse changes in dendritic spines and improve neurodevelopment in premature infants.
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Zhang, Tianlu, Dong Zhou, Miaofen Chen, Hui Zou, Qi Tang, Ying Lu, and Yajie Zheng. "Effects of the Fibrous Root of Polygonatum cyrtonema Hua on Growth Performance, Meat Quality, Immunity, Antioxidant Capacity, and Intestinal Morphology of White-Feathered Broilers." Antibiotics 12, no. 11 (November 15, 2023): 1627. http://dx.doi.org/10.3390/antibiotics12111627.
Abstract:
This study was designed to evaluate the effects of different doses of the fibrous roots of Polygonatum cyrtonema Hua on the growth performance, slaughter parameters, meat quality, immune function, cytokines, antioxidant capacity, and intestinal morphology of white-feathered broilers. Also, the mechanism to improve immune functions of broilers was explored through network pharmacology and molecular docking technology. A total of 360 AA-white-feathered broilers were randomly divided into six groups (not separated by sex), with six repetitions per group (n = 10). The groups were as follows: basal diet (CON group), basal diet supplemented with 300 mg/kg aureomycin (ANT group), basal diet supplemented with 2%, 3%, and 4% fibrous root raw powder (LD, MD, and HD group), or basal diet supplemented with 3% fibrous root processed powder (PR group), in a 42-day experiment. The dietary inclusion of P. cyrtonema fibrous roots increased slaughter performance (p < 0.05), reduced the fat rate (p < 0.05), improved intestinal morphology (p < 0.05), and improved the immune organ index to varying degrees. It also significantly improved pH reduction, drip loss, and pressure loss of breast muscle and leg muscle (p < 0.05). Furthermore, it significantly improved immune and antioxidant functions including decreased MDA content of serum (p < 0.01), increased GSH-Px content (p < 0.01), IgG, IgA, and C4 contents (p < 0.05), and increased expression of IL-2 and IFN-γ (p < 0.01). Additionally, the mechanism by which fibrous roots improve immune function in broilers was explored using network pharmacology and molecular docking technology. Network pharmacology and molecular docking revealed that flavonoids such as baicalein, 4′,5-Dihydroxyflavone, 5,7-dihydroxy-6,8-dimethyl-3-(4′-hydroxybenzyl)-chroman-4-one, and 5,7-dihydroxy-3-(2′-hydroxy-4′-methoxybenzyl)-6,8-dimethyl-chroman-4-one were key components that enhanced immune function through the MAPK1 and other key targets involved in regulating the MAPK signaling pathway. From the findings, it can be concluded that incorporating P. cyrtonema Hua fibrous root as a natural feed supplement and growth promoter in broiler diets had a positive impact on bird health and performance.
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Li, Chunhou, Xican Li, Jingyuan Zeng, Rongxin Cai, Shaoman Chen, Ban Chen, and Xiaojun Zhao. "Detection of Adulterated Naodesheng Tablet (Naodesheng Pian) via In-Depth Chemical Analysis and Subsequent Reconstruction of Its Pharmacopoeia Q-Markers." Molecules 29, no. 6 (March 20, 2024): 1392. http://dx.doi.org/10.3390/molecules29061392.
Abstract:
Naodesheng Tablet (Naodesheng Pian), a traditional Chinese medicine formula for stroke treatment, is made up of five herbal medicines, i.e., Sanqi, Gegen, Honghua, Shanzha, and Chuanxiong. However, the current Pharmacopoeia quality-marker (Q-marker) system cannot detect possible adulteration. Our study tried to use a new strategy, i.e., standards-library-dependent ultra-high-performance liquid chromatography-quadrupole-Orbitrap mass spectrometry (UHPLC-Q-Orbitrap MS/MS) putative identification, to reconstruct the Q-marker system. Through the strategy, 30 isomers were successfully differentiated (such as 2′-hydroxygenistein, luteolin, and kaempferol; ginsenoside Rg2 and ginsenoside Rg3; ginsenoside Rf and ginsenoside Rg1). In particular, 11 compounds were unexpectedly found in Naodesheng, including 2′-hydroxygenistein, 7,4′-dihydroxyflavone, pectolinarigenin, 7-methoxy-4′-hydroxyisoflavone, scoparone, matrine, 3,3′,4′,5,6,7,8-heptamethoxyflavone, 5-hydroxyflavone, diosgenin, chloesteryl acetate, and (+)-4-cholesten-3-one. In total, 68 compounds were putatively identified and fully elucidated for their MS spectra. Subsequently, relevant compounds were further investigated using UV-vis scanning experiments, semi-quantitative analysis, and quantum chemical calculation. Finally, five adulterated Naodesheng Tablets were used for validation experiments. The experiment successfully detected five adulterated ones via a lower-version LC-MS analysis. On this basis, three new candidates (hydroxy safflor yellow A (HSYA), citric acid, and levistilide A), along with puerarin and notoginsenoside R1, are re-nominated as the Q-markers for LC-MS analysis. The LC-MS analysis of puerarin, notoginsenoside R1, HSYA, citric acid, and levistilide A can clearly detect adulteration regarding all five herbal medicines mentioned above. Therefore, the reconstructed Q-markers are described as a “perfect” quality control system to detect adulteration in Naodesheng and will offer a valuable recommendation for the Pharmacopoeia Commission.
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McKhann, Heather I., Nancy L. Paiva, Richard A. Dixon, and Ann M. Hirsch. "Chalcone Synthase Transcripts Are Detected in Alfalfa Root Hairs Following Inoculation with Wild-Type Rhizobium meliloti." Molecular Plant-Microbe Interactions® 10, no. 1 (January 1997): 50–58. http://dx.doi.org/10.1094/mpmi.1997.10.1.50.
Abstract:
Flavonoids are involved in a number of critical events in the interaction between nitrogen-fixing bacteria and legumes. To get a better understanding of the importance of flavonoids in the earliest stages of the alfalfa-Rhizobium meliloti symbiosis, we followed the expression of two chal-cone synthase (CHS) gene family members as well as of chalcone isomerase (CHI) and isoflavone reductase (IFR) genes. CHS transcripts increased 2 to 4 dpi (days post-inoculation) with wild-type rhizobia, but not after inoculation with the heterologous R. leguminosarum bv. trifolii or with an exopolysaccharide (exo) mutant of R. meliloti. CHS transcripts were detected in the root hairs and epidermal cells of the root hair zone, and infrequently in nodule pri-mordia. Insignificant CHI and IFR mRNA accumulation over control levels was observed in response to rhizobial inoculation. The slight increase in CHS transcript accumulation following wild-type R. meliloti inoculation was correlated with an observed increase in root flavonoid content as well as a change in the nod gene-inducing activity of the root exudate. The nod gene-inducing flavonoids exuded from wild-type rhizobia-inoculated roots were identified as 4′, 7-dihydroxyflavone and 4, 4′ dihydroxy-2′-methoxychalcone. Although there was a slight increase over the uninoculated controls in the level of medicarpin-3-O-glucoside 6″-O-malonate (MGM) in extracts of roots inoculated with rhizobia, IFR transcript accumulation was not significantly elevated over that of the controls. Moreover, no medicarpin aglycone was detected in the inoculated roots. Thus, although inoculation with wild-type rhizobia triggers some of the genes induced during an interaction between a host and a pathogen, the expression of these genes in the Rhizobium-legume interaction is at a very low level, suggesting that rhizobia have evolved a mechanism(s) to avoid triggering the host's defense responses.
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Kamat, Siya, Madhuree Kumari, Kuttuvan Valappil Sajna, Sandeep Kumar Singh, Kaushalendra, Ajay Kumar, and C. Jayabaskaran. "Improved Chrysin Production by a Combination of Fermentation Factors and Elicitation from Chaetomium globosum." Microorganisms 11, no. 4 (April 12, 2023): 999. http://dx.doi.org/10.3390/microorganisms11040999.
Abstract:
Flavonoids encompass a heterogeneous group of secondary metabolites with exceptional health benefits. Chrysin, a natural dihydroxyflavone, possesses numerous bioactive properties, such as anticancer, antioxidative, antidiabetic, anti-inflammatory, etc. However, using traditional sources of chrysin involves extracting honey from plants, which is non-scalable, unsustainable, and depends on several factors, including geography, climatic conditions, and the season, which limits its production at a larger scale. Recently, microbial production of desirable metabolites has garnered attention due to the cost-effectiveness, easy scale-up, sustainability, and low emission of waste. We previously reported for the first time the chrysin-producing marine endophytic fungus Chaetomium globosum, associated with a marine green alga. To extend our understanding of chrysin biosynthesis in C. globosum, in the present study, we have assessed the presence of flavonoid pathway intermediates in C. globosum extracts using LC-MS/MS. The presence of several key metabolites, such as dihydrokaempferol, chalcone, galangin, baicalein, chrysin, p-Coumaroyl-CoA, and p-Cinnamoyl-CoA, indicates the role of flavonoid biosynthesis machinery in the marine fungus. Further, we have aimed to enhance the production of chrysin with three different strategies: (1) optimizing the fermentation parameters, namely, growth medium, incubation time, pH, and temperature; (2) feeding key flavonoid pathway intermediates, i.e., phenylalanine and cinnamic acid; (3) elicitation with biotic elicitors, such as polysaccharide, yeast extract, and abiotic elicitors that include UV radiation, salinity, and metal stress. The combined effect of the optimized parameters resulted in a 97-fold increase in the chrysin yield, resulting in a fungal cell factory. This work reports the first approach for enhanced production of chrysin and can serve as a template for flavonoid production enhancement using marine endophytic fungi.
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Bhosale, Pritam Bhagwan, Abuyaseer Abusaliya, Hun Hwan Kim, Sang Eun Ha, Min Yeong Park, Se Hyo Jeong, Preethi Vetrivel, et al. "Apigetrin Promotes TNFα-Induced Apoptosis, Necroptosis, G2/M Phase Cell Cycle Arrest, and ROS Generation through Inhibition of NF-κB Pathway in Hep3B Liver Cancer Cells." Cells 11, no. 17 (September 1, 2022): 2734. http://dx.doi.org/10.3390/cells11172734.
Abstract:
Apigetrin (7-(β-D-glucopyranosyloxy)-4′,5-dihydroxyflavone), a glycoside bioactive dietary flavonoid derived from Taraxacum officinale and Teucrium gnaphalodes, is known to possess anticancer, antioxidant, and anti-inflammatory effects on numerous cancers. In the present study, we examined the effect of apigetrin in Hep3B hepatocellular cancer cell line (HCC). Apigetrin inhibited cell growth and proliferation of Hep3B cells, as confirmed by MTT and colony formation assay. We used apigetrin at concentrations of 0, 50, and 100 µM for later experiments. Of these concentrations, 100 µM of apigetrin showed a significant effect on cell inhibition. In apigetrin-treated Hep3B cells, cell cycle arrest occurred at the G2/M phase. Apoptosis and necroptosis of Hep3B cells treated with apigetrin were confirmed by Annexin V/propidium iodide (PI) staining and flow cytometry results. Morphological observation through 4′,6-diamidino-2-phenylindole (DAPI) staining showed intense blue fluorescence representing chromatin condensation. Hematoxylin staining showed necroptotic features such as formation of vacuoles and swelling of organelles. Apigetrin increased reactive oxygen species (ROS) levels in cells, based on fluorescence imaging. Furthermore, the underlying mechanism involved in the apoptosis and necroptosis was elucidated through western blotting. Apigetrin up-regulated TNFα, but down-regulated phosphorylation of p-p65, and IκB. Apigetrin inhibited the expression of Bcl-xl but increased Bax levels. Up-regulation of cleaved PARP and cleaved caspase 3 confirmed the induction of apoptosis in apigetrin-treated Hep3B cells. Additionally, necroptosis markers RIP3, p-RIP3, and p-MLKL were significantly elevated by apigetrin dose-dependently, suggesting necroptotic cell death. Taken together, our findings strongly imply that apigetrin can induce apoptosis and necroptosis of Hep3B hepatocellular cancer cells. Thus, apigetrin as a natural compound might have potential for treating liver cancer.
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Wollenweber, Eckhard, Karin Mann, Munekazu Iinuma, Toshiyuki Tanaka, and Mizuo Mizuno. "2′,5′-Dihydroxyflavone and its 5′-Acetate — Novel Compounds from the Farinose Exudate of Primula." Zeitschrift für Naturforschung C 43, no. 3-4 (April 1, 1988): 305–7. http://dx.doi.org/10.1515/znc-1988-3-424.
Abstract:
2′,5′-Dihydroxyflavone and its 5′-acetate were isolated from the farinose exudate of Primula japonica and P. pulverulenta. Their structures were elucidated by spectroscopic methods and confirmed by synthesis. Both flavones are novel natural products.
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Kuo, Chen-Miao, Tania N. Hill, and Barend C. B. Bezuidenhoudt. "Crystal structure of 7-benzyloxy-5,6-dihydroxyflavone, C22H16O5." Zeitschrift für Kristallographie - New Crystal Structures 230, no. 3 (September 1, 2015): 193–94. http://dx.doi.org/10.1515/ncrs-2014-0144.
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Silva, David, and Cecilia Nunez. "FLAVONOIDES E ÁCIDOS FENÓLICOS ISOLADOS DOS EXTRATOS METANÓLICOS DAS FOLHAS E GALHOS DE Macrolobium acaciifolium (FABACEAE)." Química Nova, 2024. http://dx.doi.org/10.21577/0100-4042.20240040.
Abstract:
FLAVONOIDS AND PHENOLIC ACIDS ISOLATED FROM Macrolobium acaciifolium (FABACEAE) LEAVES AND BRANCHES METHANOLIC EXTRACTS. The phytochemical study of Macrolobium acaciifolium extracts allowed the isolation and identification of 18 substances, 15 of which are reported for the first time in this species. From the methanolic extract of the leaves, the flavonoids luteolin-3’-O-α-L-rhamnoside (1), neoastilbin (2), astilbin (3), neoisoastilbin (4), isoastilbin (5), quercetin-3-O-α-L-rhamnoside (6), quercetin-3-O-rutinoside (7), kaempferol-3-O-rutinoside (8), quercetin-3-O-glicoside (9) and kaempferol-7-O-rutinoside (10) were isolated. From the methanolic extract of branches, the flavonoids chrysoeriol (13), apigenin (14), 7,4’-dihydroxyflavone (16), eriodictyol (17) and luteolin (18), in addition to the phenolic acids 3,4-dihydroxybenzoic acid (11), 3-methoxy,4-hydroxybenzoate (12) and methyl 3,4-dihydroxybenzoate (15) were isolated. The structural identification of the compounds was established by proton nuclear magnetic resonance (1H NMR), carbon-13 nuclear magnetic resonance (13C NMR), heteronuclear single quantum coherence (HSQC), heteronuclear multiple bond correlation (HMBC) and correlated spectroscopy (COSY) analyses. In this paper, we also discuss about the anisotropic effects on H-1’’, H-2’’, H-5’’ and H-6’’ rhamnose of isomers dihydroflavonoids.
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Aboul Naser, Asmaa F., Yomna R. Ahmed, Mona A. Mohammed, Mohamed Aboelmagd, Mona E. Aboutabl, Entesar E. S. Hassan, Wagdy K. B. Khalil, and Manal A. Hamed. "Inflammatory mediators, oxidative stress and genetic disturbance in rheumatoid arthritis rats supported by alfalfa seeds metabolomic constituents via blocking interleukin‐1receptor." Chemistry & Biodiversity, December 29, 2023. http://dx.doi.org/10.1002/cbdv.202301653.
Abstract:
Rheumatoid arthritis (RA) is an autoimmune disease characterized by aggressive cartilage and bone erosion. This work aimed to evaluate the metabolomic profile of Medicago sativa L. (MS) seeds and explore its therapeutic impact against RA in rats. Arthritis was induced by complete Freund’s adjuvant (CFA) and its severity was assessed by the arthritis index. Treatment with MS seeds butanol fraction and interlukin‐1 receptor antagonist (IL‐1RA) were evaluated through measuring interlukin‐1 receptor (IL‐1R) type 1 gene expression, interlukin‐1 beta (IL‐1β), oxidative stress markers, C‐reactive protein (CRP), tumor necrosis factor‐alpha (TNF‐α), prostaglandin E2 (PGE2), caspase‐3 (Cas‐3), intracellular adhesion molecule‐1 (ICAM‐1), DNA fragmentation, and chromosomal damage. Total phenolics/ flavonoids content in the ethyl acetate, butanol fraction and crude extract of MS seeds were estimated. The major identified compounds were Quercetin, Trans‐taxifolin, gallic acid, 7,4'‐Dihydroxyflavone, Cinnamic acid, Kudzusaponin SA4, Isorhamnetin 3‐O‐beta‐D‐2'',3'',4''‐triacetylglucopyranoside, Apigenin, 5,7,4'‐Trihydroxy‐3'‐methoxyflavone, Desmethylxanthohumol, Pantothenic acid, Soyasapogenol E, Malvidin, Helilandin B, Stigmasterol, and Wairol. Treatment with MS seeds butanol fraction and IL‐1RA enhanced all the biochemical parameters and the histopathological features of the ankle joint. In conclusion, Trans‐taxifolin was isolated for the first time from the genus Medicago. MS butanol fraction seeds extract and IL‐1 RA were considered as anti‐rheumatic agents.
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Johnson, Stephen Mark, Jyoti Watters, and Karanbir Randhawa. "Intermittent Hypoxia during Gestation Disrupts Respiratory Rhythm and Neuroplasticity in Newborn Rat Brainstem‐spinal cord Preparations In Vitro." FASEB Journal 31, S1 (April 2017). http://dx.doi.org/10.1096/fasebj.31.1_supplement.727.2.
Abstract:
Pregnant women with sleep‐disordered breathing experience intermittent hypoxia, especially during late pregnancy. To test whether intermittent hypoxia exposures during pregnancy (G‐IH; gestational intermittent hypoxia) alter breathing in newborn rats, pregnant rats were exposed to intermittent hypoxia (2 min 10.5% oxygen / 2 min normoxia for 8 h) from gestational day 10 to 21 (exposures completed prior to birth). Newborn rats (P0–P3) were anesthetized and their brainstem‐spinal cords isolated under in vitro conditions. Spontaneous respiratory motor bursts were recorded on cervical spinal roots (C4–C5). G‐IH preparations from P0–P1 rats had a lower baseline burst frequency (8.2 +/− 0.6 bursts/min; n=10) compared to normoxic controls (11.0 +/− 0.3 bursts/min; n=21). After 90 min, burst frequency decreased with time nearly 2× times greater in G‐IH preparations compared to controls. In most G‐IH preparations, there were frequent “pauses” in the rhythm, which resembled spontaneous apneas. With respect to respiratory neuroplasticity, dihydroxyflavone (DHF) application (5 micromolar, 9 min; TrkB receptor agonist) induced long‐lasting 19% increase in respiratory motor burst amplitude in control preparations (n=5) after 90 min. However, only 2/4 G‐IH preparations expressed a DHF‐dependent increase in motor burst amplitude. Also, episodic substance‐P application (100 nanomolar, 3 min on / 7 min wash ×3) induced a long‐lasting (60‐min) increase in respiratory burst frequency in control preparations. However, there was no substance‐P induced frequency plasticity in any G‐IH preparations (n=4). These data suggest that gestational intermittent hypoxia disrupts respiratory rhythm generation and reduces the capacity for expressing respiratory neuroplasticity in newborn rats.Support or Funding InformationNIH Grant: NS085226
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Egwuatu, Ifeanyi Anthony, Chiadikobi Lawrence Ozoemena, and Fortune Kasiemobi Onuorah. "Unveiling the neuroprotective potential of chrysin on the pre-frontal cortex of adult male Wistar rats." South Asian Journal of Health Sciences, March 22, 2024, 1–7. http://dx.doi.org/10.25259/sajhs_15_2023.
Abstract:
Objectives Excessive free radicals in the human body predispose cells within the various systems to an imbalance and accumulation of oxygen-reactive species, known as oxidative stress. The central nervous system is not spared when it comes to these cell and tissue damages. Oxidative stress on the central nervous system may be responsible for anxiety, spatial memory impairment, neuronal cell depletion, and vacuole-tissue degeneration resulting from neurotoxicity. The use of chemotherapeutic agents such as doxorubicin has been implicated in the build-up of this imbalance between oxygen-reactive species and antioxidants. Therefore, it has become an area of research interest to seek antioxidant supplements that may offer neuroprotective effects. This study is aimed to evaluate the protective potential of chrysin on the pre-frontal cortex of male Wistar rats with doxorubicin-induced cognitive impairment. Material and Methods Thirty-five adult Wistar rats (180–200 g) were grouped into seven (1–7; n = 5). Group 1, the normal control, received normal saline treatment only throughout the study. Group 2 was administered with doxorubicin only for 21 days by intraperitoneal injection. Groups 3 and 4 were administered with chrysin in low and high doses for 21 days orally. Groups 5, 6 and 7 were exposed to doxorubicin and chrysin for 21 days intra-peritoneally and orally with low, medium and high doses, respectively. Results Anti-oxidative biomarkers analysed in Group 2 (doxorubicin-only) demonstrated a significant difference when compared to other groups. This corresponded to significant elevations in apoptotic indicators, inflammatory markers and histological lesions, which were indicative of cognitive impairment. 5, 7-dihydroxyflavone (chrysin) significantly mitigated and also reversed cognitive impairment caused by doxorubicin. Conclusion The data showed that chrysin protected against doxorubicin-induced cognitive impairment. This effect is probably made possible by suppressing oxidative stress, inflammation and apoptosis.
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Vidal‐Sanz, Manuel. "Idiosyncratic responses of RGCs to injury and protection." Acta Ophthalmologica 102, S279 (January 2024). http://dx.doi.org/10.1111/aos.16260.
Abstract:
Objectives: The objectives of the study were to investigate the responses of different retinal ganglion cell (RGC) populations to diverse injuries [transient ischemia induced by acute ocular hypertension (AOH), excitotoxicity induced by intravitreal injection of 100 mM N‐methyl D‐aspartate (NMDA) or intra‐orbital optic nerve transection (IONT)] and protection with selective agonists of the tropomyosin related kinase B (TrkB) receptor, brain‐derived neurotrophic factor (BDNF) or 7,8‐Dihydroxyflavone (DHF) or with a voltage‐dependent calcium channel blocker (ITH12657).Methods: Adult Sprague–Dawley rats were used. In the first group, the left eye received a single intravitreal injection of 5 μL vehicle or 5 μg BDNF and was connected to a saline reservoir elevated above the eye to induce an acute ocular hypertension (AOH) and transient ischemia for 75 min. These rats were analysed at different survival intervals from 3 to 45 days.A second group were treated daily subcutaneously with vehicle or ITH5263 (10 mg/kg), or intraperitoneally with vehicle or DHF (5 mg/kg), starting 12 h prior to an intraocular injection of 100 mM N‐methyl‐D‐aspartate (NMDA) to induce retinal excitotoxicity. These rats were analysed at different survival intervals from 3 to 21 days.A third group received a left intra‐orbital optic nerve transection (IONT) to induce axotomy of the RGC population and were treated daily with an intraperitoneal injection of vehicle (0.9% NaCl containing 1% DMSO) or DHF (5 mg/kg diluted in vehicle). These rats were analysed at survival intervals from 3 to 60 days.The retinas were prepared as wholemounts and immunolabelled for Brn3a, melanopsin (m), Osteopontin (OPN) and the T‐box transcription factor T‐brain‐2 (Tbr2) to identify the following retinal ganglion cell populations: Brn3a+, melanopsin+, α‐like (OPN+), α‐ON sustained RGCs (OPN+Tbr2+), α‐ON transient RGCs (OPN+ Brn3a− Tbr2−) and α‐OFF like (OPN+Brn3a+). The labelled RGCs were quantified automatically (Brn3a) or dotted manually and quantified with a graphic software, and distribution of the different populations were represented on topographical maps.Results: Our studies document that:(i) AOH induces progressive loss of Brn3a+RGCs and a significant but not progressive loss of m+RGCs. Treatment with BDNF afforded significant long‐lasting protection for both RGC populations.(ii) Intravitreal injection of NMDA resulted at 7 days in the abrupt significant loss of Brn3a+RGCs, αRGC and αONs‐RGCs without further progression, whereas αOFF‐RGCs died massively. Both m+RGCs and αONtRGCs appear fully resistant to NMDA‐induced excitotoxicity. Both ITH12657 or DHF protect Brn3a+RGC, αRGCs and αONs‐RGCs, but not αOFF‐RGCs.(iii) IONT and vehicle treatment result in a characteristic rapid loss of Brn3a, melanopsin RGCs, αRGCs, αONs‐RGCs and αOFF‐RGCs. DHFs protect Brn3a + RGC, m + RGCs, αRGCs and αONs‐RGCs, but not αOFF‐RGCs.Conclusions: Thus, three different RGC populations (Brn3a+, m+ and α‐like) respond distinctly to different injuries and neuroprotective agents, further adding to the idea that each type of RGC has a unique response to injury and protection. Deciphering the molecular mechanisms of each RGC type will help understand neuronal responses to injury and its possible prevention.