Journal articles: 'In vitro gastrointestinal assay'

1

Amano, Yuto, Hiroshi Honda, Yuko Nukada, Naohiro Ikeda, Masayuki Yamane, Koji Nakano, Akiyo Kameyama, and Osamu Morita. "Safety Pharmacological Evaluation of the Coffee Component, Caffeoylquinic Acid, and Its Metabolites, Using Ex Vivo and In Vitro Profiling Assays." Pharmaceuticals 12, no. 3 (July 17, 2019): 110. http://dx.doi.org/10.3390/ph12030110.

Full text

Abstract:

Although coffee components have gained interest for use as pharmaceuticals, little is known about their safety pharmacological effects. Hence, we aimed to evaluate the safety pharmacological effects of a chlorogenic acid (CGA)-related compound contained in coffee, 5-O-caffeoylquinic acid (5-CQA), and its metabolites, 5-O-feruloylquinic acid (5-FQA), caffeic acid (CA), and ferulic acid (FA). Langendorff perfused heart assay, electrophysiological assay of acute rat hippocampal slices, and in vitro Magnus assay of gastrointestinal tracts were conducted at 1–100 µM. Moreover, in vitro profiling assays against 38 major targets were conducted. In the Langendorff assay, no significant adverse effects were observed. In the electrophysiological assay, although epileptiform discharge rates were increased at 10 µM CA with 4-aminopyridine, and area under the curve (AUC) and number of population spike were increased at 10 µM FA with bicuculline, dose dependency was not confirmed, and no significant changes were observed at 1 µM and by CGAs alone. In the Magnus assay, a slight increase in contraction activity was observed at >1 µM FA in the stomach fundi and 100 µM 5-CQA in the ileum, suggesting enterokinesis promotion. No significant interactions were observed in the in vitro profiling assays. Therefore, CGAs could have a fundamental function as safe pharmaceuticals.

APA, Harvard, Vancouver, ISO, and other styles

2

Podsędek, Anna, Małgorzata Redzynia, Elżbieta Klewicka, and Maria Koziołkiewicz. "Matrix Effects on the Stability and Antioxidant Activity of Red Cabbage Anthocyanins under Simulated Gastrointestinal Digestion." BioMed Research International 2014 (2014): 1–11. http://dx.doi.org/10.1155/2014/365738.

Full text

Abstract:

Red cabbage is, among different vegetables, one of the major sources of anthocyanins. In the present study an in vitro digestion method has been used to assay the influence of the physiological conditions in the stomach and small intestine, as well as faecal microflora on anthocyanins stability in red cabbage and anthocyanin-rich extract. The recovery of anthocyanins during in vitro gastrointestinal digestion was strongly influenced by food matrix. The results showed that other constituents present in cabbage enhanced the stability of anthocyanins during the digestion. The amount of anthocyanins (HPLC method) and antioxidant capacity (ABTS and FRAP assays) strongly decreased after pancreatic-bile digestion in both matrices but total phenolics content (Folin-Ciocalteu assay) in these digestions was higher than in initial samples. Incubation with human faecal microflora caused further decline in anthocyanins content. The results obtained suggest that intact anthocyanins in gastric and products of their decomposition in small and large intestine may be mainly responsible for the antioxidant activity and other physiological effects after consumption of red cabbage.

APA, Harvard, Vancouver, ISO, and other styles

3

Jovanović, Miloš, Zorica Drinić, Dubravka Bigović, Ana Alimpić-Aradski, Sonja Duletić-Laušević, and Katarina Šavikin. "In vitro antineurodegenerative activity and in silico predictions of blood-brain barrier penetration of Helichrysum plicatum flower extract." Lekovite sirovine, no. 40 (2020): 45–51. http://dx.doi.org/10.5937/leksir2040045j.

Full text

Abstract:

This study aimed to assess the antineurodegenerative and antioxidant activity of Helichrysum plicatum flower extract, as well as to identify extract ingredients with acceptable pharmacokinetic parameters such as gastrointestinal absorption, blood-brain barrier permeation, and P-glycoprotein-mediated effusion for optimal therapeutic brain exposure. Antioxidant activity was evaluated by ABTS, FRAP, and b-carotene bleaching assays, while antineurodegenerative activity was tested using acetylcholinesterase (AChE) and tyrosinase (TYR) inhibitory activity assays. In the ABTS test, the dry extract at the highest applied concentration (500 µg/mL) showed better or similar antioxidant activity compared to the standards. In the b-carotene assay, all applied concentrations of the extract showed significantly higher activity than vitamin C. No concentration-dependent activity was observed in the AChE assay, while in the TYR assay the lowest extract concentration (100 µg/mL) showed the highest percentage of inhibition (27.92 %). Pharmacokinetic parameters of compounds were predicted by in silico SwissADME online tool in accordance by the rules of drug-likeness. According to the pharmacokinetic properties, we concluded that pentoxymethoxylated flavones may represent CNS drug candidates for further studies.

APA, Harvard, Vancouver, ISO, and other styles

4

Miret, Silvia, Leo Abrahamse, and Els M. de Groene. "Comparison of in Vitro Models for the Prediction of Compound Absorption across the Human Intestinal Mucosa." Journal of Biomolecular Screening 9, no. 7 (October 2004): 598–606. http://dx.doi.org/10.1177/1087057104267162.

Full text

Abstract:

Several in vitro assays have been developed to evaluate the gastrointestinal absorption of compounds. Our aim was to compare 3 of these methods: 1) the bio-mimetic artificial membrane permeability assay (BAMPA) method, which offers a high-throughput, noncellular approach to the measurement of passive transport; 2) the traditional Caco-2 cell assay, the use of which as a high-throughput tool is limited by the long cell differentiation time (21 days); and 3) The BioCoat™ high-throughput screening Caco-2 Assay System, which reduces Caco-2 cell differentiation to 3 days. The transport of known compounds (such as cephalexin, propranolol, or chlorothiazide) was studied at pH 7.4 and 6.5 in BAMPA and both Caco-2 cell models. Permeability data obtained was correlated to known values of human absorption. Best correlations ( r = 0.9) were obtained at pH 6.5 for BAMPA and at pH 7.4 for the Caco-2 cells grown for 21 days. The Caco-2 BioCoat™ HTS Caco-2 Assay System does not seem to be adequate for the prediction of absorption. The overall results indicate that BAMPA and the 21-day Caco-2 system can be complementary for an accurate prediction of human intestinal absorption.

APA, Harvard, Vancouver, ISO, and other styles

5

Nolasco, Emerson, Mike Naldrett, Sophie Alvarez, Philip E. Johnson, and Kaustav Majumder. "Bioactivity of Cooked Standard and Enriched Whole Eggs from White Leghorn and Rhode Island Red in Exhibiting In-Vitro Antioxidant and ACE-Inhibitory Effects." Nutrients 13, no. 12 (November 25, 2021): 4232. http://dx.doi.org/10.3390/nu13124232.

Full text

Abstract:

Hen breed, diet enrichment, cooking methods, and gastrointestinal (GI) digestion modulates the bioaccessibility of the bioactive compounds in eggs, but their synergistic role in modulating bioactivity is still unclear. The present study evaluates the effect of hen breed, diet enrichment, and GI digestion on the cooked whole egg-derived peptides in-vitro antioxidant and antihypertensive activities. Standard and enriched whole eggs from White Leghorn (WLH) and Rhode Island Red (RIR) hens were boiled or fried and subjected to GI digestion. Antioxidant activity was measured through oxygen radical absorbance capacity (ORAC) and gastrointestinal epithelial cell-based assays, and the antihypertensive capacity by in-vitro Angiotensin-I Converting Enzyme (ACE) inhibition assay. WLH fried standard egg hydrolysate showed a high ORAC antioxidant activity but failed to show any significant antioxidant effect in the cell-based assay. No significant differences were observed in the antihypertensive activity, although enriched samples tended to have a higher ACE-inhibitory capacity. The peptide profile explained the antioxidant capacities based on antioxidant structural requirements from different peptide fractions, while previously reported antihypertensive peptides were found in all samples. The study validates the importance of physiologically relevant models and requires future studies to confirm mechanisms that yield bioactive compounds in whole egg hydrolysates.

APA, Harvard, Vancouver, ISO, and other styles

6

Rosa, S. S. Santa, F. O. Santos, H. G. Lima, I. M. A. Reis, D. S. A. Cassiano, I. J. C. Vieira, R. Braz-Filho, et al. "In vitro anthelmintic and cytotoxic activities of extracts of Persea willdenovii Kosterm (Lauraceae)." Journal of Helminthology 92, no. 6 (October 25, 2017): 674–80. http://dx.doi.org/10.1017/s0022149x17000979.

Full text

Abstract:

AbstractThis study describes the effects of extracts and fractions of Persea willdenovii leaves against goat gastrointestinal nematodes and their cytotoxicity on Vero cells. The in vitro ovicidal and larvicidal activities of the crude ethanolic, hexane, ethyl acetate (EAE), butanolic and residual hydroethanolic extracts were assessed through the inhibition of egg hatching and larval motility assays. The most active extract (EAE) was then fractionated by chromatography in an open column containing silica gel, to furnish six fractions (Fr1–Fr6), which were also tested. The cytotoxicity of active extracts and fractions was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and trypan blue exclusion assay. The EAE and two fractions (Fr1 and Fr2) showed inhibitory activity in the egg hatching of gastrointestinal nematodes of goats in a concentration-dependent manner. The effective concentrations for 50% inhibition (EC50) of egg hatching were 2.3, 0.12 and 2.94 mg/ml for EAE, Fr1 and Fr2, respectively. All extracts and fractions were not effective in inhibiting 50% of motility of infective larvae. EAE and Fr2 had IC50 values (50% inhibitory concentration) of 4.95 and 2.66 mg/ml, respectively. Fr1 showed a slight cytotoxic effect (cellular inviability <30%) only after 48 h of treatment (MTT test). Gas chromatography–mass spectrometry (GC–MS) analysis showed the presence of six fatty acid ethyl esters, a fatty acid methyl ester and a long-chain ketone in the most active fraction. These constituents identified in P. willdenovii can be related to the high ovicidal activity and relatively non-toxic effect of the extracts.

APA, Harvard, Vancouver, ISO, and other styles

7

Yu, Shengwu, Anika Singh, Huiying Zhang, and David D. Kitts. "An in vitro Method to Determine Intestinal Bioavailability of Glucosamine Salt Mixture." Journal of Nutritional Health & Food Science 9, no. 1 (February 10, 2021): 1–6. http://dx.doi.org/10.15226/jnhfs.2021.001180.

Full text

Abstract:

Glucosamine is an amino sugar commonly used to improve joint health. It is often available for consumers as specialized supplements, the matrixes of which are formulated with components that facilitate enhancing functionality of the bioactive glucosamine. The primary objective of this study was to determine the in vitro bioaccessibility and bioavailability of a commercial glucosamine sulphate supplement, formulated with a mineral clay mixture. We used a modified a 3-step in vitro digestion procedure that included oral, gastric, and gastrointestinal digestions to assess bioaccessibility. Bioavailability followed using a Caco2 cell permeability test. Glucosamine bioaccessibility was not affected by gastric digestion and only marginally affected by gastrointestinal digestion (e.g., > 90% recovery). Bioavailability was dramatically lower, averaging approximately 15%, but similar for both the glucosamine reference standard and clay mineral mix glucosamine formulated product. Our in vitro bioavailability measurement of glucosamine, corrected for bioaccessibility, agree with values from in vitro rodent models. We conclude that the in vitro 3-step digestion of glucosamine, used to mimic gastrointestinal digestion, followed by the Caco2 permeability assay represents an alternative method to assess digestibility and bioavailability of formulated glucosamine products. Keywords: Glucosamine; Clay Mineral Mix; Bioaccessibility; Bioavailability

APA, Harvard, Vancouver, ISO, and other styles

8

Tariq, K. A., M. Z. Chishti, F. Ahmad, A. S. Shawl, and M. A. Tantray. "Evaluation of anthelmintic activity of Iris hookeriana against gastrointestinal nematodes of sheep." Journal of Helminthology 82, no. 2 (June 2008): 135–41. http://dx.doi.org/10.1017/s0022149x08912360.

Full text

Abstract:

AbstractThe objective of this study was to evaluate the anthelmintic efficacy of Iris hookeriana Linn. rhizome against gastrointestinal nematodes of sheep. A worm motility inhibition assay was used for in vitro study and a faecal egg count reduction assay was used for an in vivo study. The in vitro study revealed anthelmintic effects of crude aqueous extracts and crude ethanolic extracts on live Trichuris ovis worms (P ≤ 0.05) as evident from their paralysis and/or death at 8 h after exposure. The aqueous extracts of I. hookeriana resulted in a mean worm motility inhibition of 54.0%, while ethanolic extracts resulted in a mean worm motility inhibition of 84.6%. The mean mortality index of aqueous extracts was 0.55, while for ethanolic extracts it was 0.85. The lethal concentration 50 for aqueous extracts was 0.45 mg ml− 1 and for ethanolic extracts it was 0.15 mg ml− 1. The in vivo anthelmintic activity of aqueous and ethanolic extracts of I. hookeriana in sheep naturally infected with mixed species of gastrointestinal nematodes demonstrated a maximum (45.62%) egg count reduction in sheep treated with ethanolic extracts at 2 g kg− 1 body weight on day 10 after treatment, closely followed by ethanolic extracts at 1 g kg− 1 body weight on day 10 after treatment (43.54% egg count reduction). The aqueous extracts resulted in a maximum of 31.53% reduction in faecal egg counts on day 10 after treatment with 1 g kg− 1 body weight. Thus ethanolic extracts exhibited greater anthelmintic activity under both in vitro and in vivo conditions; this could be due to the presence of alcohol-soluble active ingredients in I. hookeriana. From the present study it can be suggested that I. hookeriana rhizome exhibited significant anthelmintic activity against gastrointestinal nematodes of sheep and has the potential to contribute to the control of gastrointestinal nematode parasites of small ruminants.

APA, Harvard, Vancouver, ISO, and other styles

9

Tomar, R. S., and S. Preet. "Evaluation of anthelmintic activity of biologically synthesized silver nanoparticles against the gastrointestinal nematode, Haemonchus contortus." Journal of Helminthology 91, no. 4 (July 4, 2016): 454–61. http://dx.doi.org/10.1017/s0022149x16000444.

Full text

Abstract:

AbstractThe present study focuses on the in vitro anthelmintic activity of silver nanoparticles (AgNPs) synthesized using the aqueous extract of Azadirachta indica against Haemonchus contortus. The synthesized AgNPs were characterized by ultraviolet–visible (UV-Vis) spectrophotometry, scanning electron microscopy (SEM), transmission electron microscopy (TEM) and X-ray diffraction (XRD) studies. The UV-Vis spectrum exhibited a sharp peak at 420 nm, which was validated by electron microscopy, indicating the preparation of spherical nanoparticles measuring 15–25 nm in size. The in vitro study was based on an egg hatch assay (EHA) and adult motility inhibition assays. Six concentrations of AgNPs were used for EHA, ranging from 0.00001 to 1.0 μg/ml, and a range of 1–25 μg/ml was used for adult worms. The highest concentration induced 85 ± 2.89% egg hatch inhibition. The IC50 value for EHA was 0.001 μg/ml, whereas in vitro adult H. contortus motility inhibition was produced at 7.89 μg/ml (LC50). The effectiveness of A. indica leaf extract (aqueous) was also evaluated, which showed an IC50 value for EHA of 115.67 μg/ml, while the LC50 against adult H. contortus was 588.54 μg/ml. The overall findings of the present study show that the experimental plant extract contains reducing properties for the synthesis of AgNPs which, in turn, showed potent anthelmintic properties. This is the first report where AgNPs have been tested for their anthelmintic properties in an in vitro model.

APA, Harvard, Vancouver, ISO, and other styles

10

Duque-Soto, Carmen, Alejandra Quintriqueo-Cid, Ascensión Rueda-Robles, Paz Robert, Isabel Borrás-Linares, and Jesús Lozano-Sánchez. "Evaluation of Different Advanced Approaches to Simulation of Dynamic In Vitro Digestion of Polyphenols from Different Food Matrices–A Systematic Review." Antioxidants 12, no. 1 (December 31, 2022): 101. http://dx.doi.org/10.3390/antiox12010101.

Full text

Abstract:

Phenolic compounds have become interesting bioactive antioxidant compounds with implications for obesity, cancer and inflammatory gastrointestinal pathologies. As the influence of digestion and gut microbiota on antioxidant behavior is yet to be completely elucidated, and due to limitations associated to in vivo studies, dynamic in vitro gastrointestinal models have been promoted. A systematic review was conducted of different databases (PubMed, Web of Science and Scopus) following PRISMA guidelines to assess different dynamic digestion models and assay protocols used for phenolic compound research regarding bioaccesibility and interaction with colonic microbiota. Of 284 records identified, those including dynamic multicompartmental digestion models for the study of phenolic compound bioaccesibility, bioactivity and the effects of microbiota were included, with 57 studies meeting the inclusion criteria. Different conditions and experimental configurations as well as administered doses, sample treatments and microbiological assays of dynamic digestion studies on polyphenols were recorded and compared to establish their relevance for the dynamic in vitro digestion of phenolic compounds. While similarities were observed in certain experimental areas, a high variability was found in others, such as administered doses. A description of considerations on the study of the digestion of phenolic compounds is proposed to enhance comparability in research.

APA, Harvard, Vancouver, ISO, and other styles

11

Anna, Torkova, Kononikhin Alexey, Bugrova Anna, Khotchenkov Vyacheslav, Tsentalovich Mikhail, and Medvedeva Ulia. "Effect of in Vitro Gastrointestinal Digestion on Bioactivity of Poultry Protein Hydrolysate." Current Research in Nutrition and Food Science Journal 4, Special-Issue-October (October 6, 2016): 77–86. http://dx.doi.org/10.12944/crnfsj.4.special-issue-october.10.

Full text

Abstract:

In vitro simulated gastrointestinal digestion (GID) was performed to evaluate changes in bioactive properties of Poultry protein hydrolysate HCP Premium P150 (PPH) showing strong antioxidant (448.2±37.0 µM TE/g of protein) and moderate Angiotensin-I converting enzyme inhibitory activity (IC50 0.617±0.022 mg/ml). Antioxidant and ACE-inhibitory activity were measured with use of ORAC assay and FRET-substrate methods, correspondingly. Gastric digestion (GD) increased ACE inhibitory activity 2.23 times and didn’t change antioxidant activity of PPH significantly. The subsequent intestinal digestion increased antioxidant activity 1.29 times and didn’t change ACE-inhibitory activity significantly. New potent ACE-inhibitory peptides: APGAPGPVG (IC50 16.2±3.8 µM), PDLVF (IC50 84.9±6.3 µM) and antioxidant dipeptide WG (2.29±0.04 µM TE/µM) were identified in the digested PPH. The digested PPH proved to be a rich source of antioxidant and ACE inhibiting molecules and could be a potential new food ingredient used for prevention or treatment of socially significant diseases.

APA, Harvard, Vancouver, ISO, and other styles

12

Morais, Helena. "Antioxidant Activity of Fruits toward Iron under Gastrointestinal Conditions." Natural Product Communications 3, no. 3 (March 2008): 1934578X0800300. http://dx.doi.org/10.1177/1934578x0800300308.

Full text

Abstract:

The objectives of this study were to determine the antioxidant activity of fruits containing polyphenolics, namely anthocyanins, and their capacity to reduced Fe (III) to Fe (II) under simulated gastrointestinal conditions. The antioxidant capacity of fruits against prooxidant iron was determined using an in vitro assay. All the fruits exhibited variable antioxidant activity to iron in comparison to the control, both in the presence and absence of digestive enzymes and bile salts. For the fruits containing anthocyanins it was possible to obtain a positive correlation between total ferrous iron and anthocyanins content. There are strong negative correlations between phenolic compounds and dialyzable ferrous iron.

APA, Harvard, Vancouver, ISO, and other styles

13

Helal, Mohamed A., Ahmed M. Abdel-Gawad, Omnia M. Kandil, Marwa M. E. Khalifa, Gareth W. V. Cave, Alison A. Morrison, David J. Bartley, and Hany M. Elsheikha. "Nematocidal Effects of a Coriander Essential Oil and Five Pure Principles on the Infective Larvae of Major Ovine Gastrointestinal Nematodes In Vitro." Pathogens 9, no. 9 (September 9, 2020): 740. http://dx.doi.org/10.3390/pathogens9090740.

Full text

Abstract:

The anthelmintic effects of extracted coriander oil and five pure essential oil constituents (geraniol, geranyl acetate, eugenol, methyl iso-eugenol, and linalool) were tested, using larval motility assay, on the third-stage larvae (L3s) of Haemonchus contortus, Trichostrongylus axei, Teladorsagia circumcincta, Trichostrongylus colubriformis, Trichostrongylus vitrinus and Cooperia oncophora. Coriander oil and linalool, a major component of tested coriander oil, showed a strong inhibitory efficacy against all species, except C. oncophora with a half maximal inhibitory concentration (IC50) that ranged from 0.56 to 1.41% for the coriander oil and 0.51 to 1.76% for linalool. The coriander oil and linalool combinations conferred a synergistic anthelmintic effect (combination index [CI] <1) on larval motility comparable to positive control (20 mg/mL levamisole) within 24 h (p < 0.05), reduced IC50 values to 0.11–0.49% and induced a considerable structural damage to L3s. Results of the combined treatment were validated by quantitative fluorometric microplate-based assays using Sytox green, propidium iodide and C12-resazurin, which successfully discriminated live/dead larvae. Only Sytox green staining achieved IC50 values comparable to that of the larval motility assay. The cytotoxicity of the combined coriander oil and linalool on Madin–Darby Canine Kidney cells was evaluated using sulforhodamine-B (SRB) assay and showed no significant cytotoxic effect at concentrations < 1%. These results indicate that testing essential oils and their main components may help to find new potential anthelmintic compounds, while at the same time reducing the reliance on synthetic anthelmintics.

APA, Harvard, Vancouver, ISO, and other styles

14

Chang, Brian S., Tao Yang, Edmund S. Cibas, and Jonathan A. Fletcher. "An in vitro cytologic assay for evaluation of the KIT signaling pathway in gastrointestinal stromal tumors." Modern Pathology 20, no. 5 (March 30, 2007): 579–83. http://dx.doi.org/10.1038/modpathol.3800779.

Full text

APA, Harvard, Vancouver, ISO, and other styles

15

Bondzio, A., H. Martens, and R. Einspanier. "Introducing an in vitro cell model to assay gastrointestinal responses to recombinant feed compounds like Cry1Ab." Journal für Verbraucherschutz und Lebensmittelsicherheit 1, S1 (November 2006): 111–12. http://dx.doi.org/10.1007/s00003-006-0102-6.

Full text

APA, Harvard, Vancouver, ISO, and other styles

16

Zádor, Ferenc, Amir Mohammadzadeh, Mihály Balogh, Zoltán S. Zádori, Kornél Király, Szilvia Barsi, Anna Rita Galambos, et al. "Comparisons of In Vivo and In Vitro Opioid Effects of Newly Synthesized 14-Methoxycodeine-6-O-sulfate and Codeine-6-O-sulfate." Molecules 25, no. 6 (March 17, 2020): 1370. http://dx.doi.org/10.3390/molecules25061370.

Full text

Abstract:

The present work represents the in vitro (potency, affinity, efficacy) and in vivo (antinociception, constipation) opioid pharmacology of the novel compound 14-methoxycodeine-6-O-sulfate (14-OMeC6SU), compared to the reference compounds codeine-6-O-sulfate (C6SU), codeine and morphine. Based on in vitro tests (mouse and rat vas deferens, receptor binding and [35S]GTPγS activation assays), 14-OMeC6SU has µ-opioid receptor-mediated activity, displaying higher affinity, potency and efficacy than the parent compounds. In rats, 14-OMeC6SU showed stronger antinociceptive effect in the tail-flick assay than codeine and was equipotent to morphine, whereas C6SU was less efficacious after subcutaneous (s.c.) administration. Following intracerebroventricular injection, 14-OMeC6SU was more potent than morphine. In the Complete Freund’s Adjuvant-induced inflammatory hyperalgesia, 14-OMeC6SU and C6SU in s.c. doses up to 6.1 and 13.2 µmol/kg, respectively, showed peripheral antihyperalgesic effect, because co-administered naloxone methiodide, a peripherally acting opioid receptor antagonist antagonized the measured antihyperalgesia. In addition, s.c. C6SU showed less pronounced inhibitory effect on the gastrointestinal transit than 14-OMeC6SU, codeine and morphine. This study provides first evidence that 14-OMeC6SU is more effective than codeine or C6SU in vitro and in vivo. Furthermore, despite C6SU peripheral antihyperalgesic effects with less gastrointestinal side effects the superiority of 14-OMeC6SU was obvious throughout the present study.

APA, Harvard, Vancouver, ISO, and other styles

17

Bin Kabir, Mohammad Hazzaz, Frances Cagayat Recuenco, Nur Khatijah Mohd Zin, Nina Watanabe, Yasuhiro Fukuda, Hironori Bando, Kenichi Watanabe, Hiroki Bochimoto, Xuenan Xuan, and Kentaro Kato. "Identification of potent anti-Cryptosporidium new drug leads by screening traditional Chinese medicines." PLOS Neglected Tropical Diseases 16, no. 11 (November 28, 2022): e0010947. http://dx.doi.org/10.1371/journal.pntd.0010947.

Full text

Abstract:

Cryptosporidium spp. are gastrointestinal opportunistic protozoan parasites that infect humans, domestic animals, and wild animals all over the world. Cryptosporidiosis is the second leading infectious diarrheal disease in infants less than 5 years old. Cryptosporidiosis is a common zoonotic disease associated with diarrhea in infants and immunocompromised individuals. Consequently, cryptosporidiosis is considered a serious economic, veterinary, and medical concern. The treatment options for cryptosporidiosis are limited. To address this problem, we screened a natural product library containing 87 compounds of Traditional Chinese Medicines for anti-Cryptosporidium compounds that could serve as novel drug leads and therapeutic targets against C. parvum. To examine the anti-Cryptosporidium activity and half-maximal inhibitory doses (EC50) of these compounds, we performed in vitro assays (Cryptosporidium growth inhibition assay and host cell viability assay) and in vivo experiments in mice. In these assays, the C. parvum HNJ-1 strain was used. Four of the 87 compounds (alisol-A, alisol-B, atropine sulfate, and bufotalin) showed strong anti-Cryptosporidium activity in vitro (EC50 values = 122.9±6.7, 79.58±13.8, 253.5±30.3, and 63.43±18.7 nM, respectively), and minimum host cell cytotoxicity (cell survival > 95%). Furthermore, atropine sulfate (200 mg/kg) and bufotalin (0.1 mg/kg) also showed in vivo inhibitory effects. Our findings demonstrate that atropine sulfate and bufotalin are effective against C. parvum infection both in vitro and in vivo. These compounds may, therefore, represent promising novel anti-Cryptosporidium drug leads for future medications against cryptosporidiosis.

APA, Harvard, Vancouver, ISO, and other styles

18

Speciale, Antonio, Romina Bashllari, Claudia Muscarà, Maria Sofia Molonia, Antonella Saija, Shikha Saha, Peter J. Wilde, and Francesco Cimino. "Anti-Inflammatory Activity of an In Vitro Digested Anthocyanin-Rich Extract on Intestinal Epithelial Cells Exposed to TNF-α." Molecules 27, no. 17 (August 23, 2022): 5368. http://dx.doi.org/10.3390/molecules27175368.

Full text

Abstract:

Background: The consumption of foods rich in anthocyanins (ACN) have been associated with beneficial properties in chronic inflammatory disorders such as intestinal bowel diseases (IBD). These effects were attributed not only to a direct antioxidant mechanism but also to the modulation of cell redox-dependent signaling. However, ACN bioavailability is low for their poor stability in the digestive tract, so ACN gastrointestinal digestion should be considered. Methods: To have a more realistic knowledge of the effects of ACN, we performed an in vitro simulated gastrointestinal digestion of an ACN-rich purified and standardized bilberry and blackcurrant extract (BBE), followed by an evaluation of ACN composition modification (HPLC-DAD and pH differential method) and antioxidant activity (FRAP assay). Then, we studied the effects of BBE gastrointestinal extract on Caco-2 exposed to TNF-α. Results: The results confirmed the high instability of ACN in the mild alkaline environment of the small intestine (17% recovery index). However, the digested BBE maintained part of its bioactivity. Additionally, BBE gastrointestinal extract inhibited the TNF-α-induced NF-κB pathway in Caco-2 and activated the Nrf2 pathway. Conclusions: Although ACN stability is affected by gastrointestinal digestion, the anti-inflammatory and antioxidant activity of digested extracts were confirmed; thus, the loss of ACN can probably be counterweighed by their metabolites. Then, ACN introduced by diet or food supplements could represent an approach for IBD prevention.

APA, Harvard, Vancouver, ISO, and other styles

19

Seminare, Patrizia, Gennadij Bogdanov, Giovanni Codacci-Pisanelli, Carlo Leonetti, Nina Konovalova, Raya Diatchkovskaya, Letizia Gargano, Teresa Aronne, and Fabrizio Franchi. "Comparative in Vitro and in Vivo Study of a Nitroxyl Derivative of 5-Fluorouracil (Magnizil) on Human Gastrointestinal Tumors." Tumori Journal 81, no. 4 (July 1995): 278–82. http://dx.doi.org/10.1177/030089169508100413.

Full text

Abstract:

Aims and background There is much interest in nitroxyl derivatives of cytotoxic agents. We evaluated the potential activity of magnizil, a derivative of 5-fluorouracil, on human gastrointestinal tumors in 3 different in vitro and in vivo experimental models. Methods The activities of magnizil and 5-fluorouracil were comparatively determined in vitro on the HT29 cell line by a clonogenic assay and on tumor clinical specimens by an antimetabolic assay. The activity of both the drugs against human tumors was also assessed in mice with the subrenal capsule assay. Results A similar cytotoxic activity was found for magnizil and 5-fluorouracil on the HT29 cell line. As regards human tumors, a lower activity was observed for the nitroxyl derivative than for 5-fluorouracil, with response rates of 25% and 50%, respectively, at comparable concentrations. Moreover, among the tumors transplanted in the subrenal capsule of mice, two were sensitive to magnizil and 3 to 5-fluorouracil. Conclusions Even though experimental results on human tumors indicate a somewhat lower activity for magnizil than the parent compound, its low toxicity and the possibility to clinically use high doses suggest the opportunity to further investigate the potential of this new anticancer agent on larger series of colorectal cancers in experimental systems.

APA, Harvard, Vancouver, ISO, and other styles

20

Irum, S., H. Ahmed, B. Mirza, K. Donskow-Łysoniewska, A. Muhammad, M. Qayyum, and S. Simsek. "In vitro and in vivo anthelmintic activity of extracts from Artemisia parviflora and A. sieversiana." Helminthologia 54, no. 3 (September 1, 2017): 218–24. http://dx.doi.org/10.1515/helm-2017-0028.

Full text

Abstract:

SummaryIn the northern areas of Pakistan, the use of Artemisia based therapeutics is a common practice. Plants of genus Artemisia are known to possess anthelmintic and therapeutic effect. Infections caused by gastrointestinal nematodes are major threat to livestock industry across the world resulting in loss of production and indirect economic losses due to high cost of anthelmintic drugs. Present study was carried out to evaluate in vitro and in vivo effect of Artemisia sieversiana and Artemisia parviflora on Haemonchus contortus, a parasitic nematode of small ruminants. Methanolic plant extract was tested against three different developmental stages using an egg hatch assay, infective larvae and adult worm motility assay. Different concentrations were used for the bioassays and post exposure mortality was recorded after 8 hr for adult worms and infective larvae, while egg inhibition percentage was observed after 27 hr. A highly significant ability to inhibit the egg hatching (100 %) was recorded for both plant extracts while, the highest activity for adult worm assay and larvicidal assay was 90 % for A. sieversiana. The highest activity for adult motility and larvicidal assay for A. parviflora was 89 % and 86.6 % respectively. For in vivo trials maximum parentage reduction was 77.0 % for A. sieversiana and 73.6 % for A. parviflora. It is concluded that selected plant extracts were effective in reducing worm burden in animals.

APA, Harvard, Vancouver, ISO, and other styles

21

Ivanov, Marija, Uroš Gašić, Dejan Stojković, Marina Kostić, Danijela Mišić, and Marina Soković. "New Evidence for Artemisia absinthium L. Application in Gastrointestinal Ailments: Ethnopharmacology, Antimicrobial Capacity, Cytotoxicity, and Phenolic Profile." Evidence-Based Complementary and Alternative Medicine 2021 (July 22, 2021): 1–14. http://dx.doi.org/10.1155/2021/9961089.

Full text

Abstract:

Artemisia absinthium L. (Asteraceae) is traditionally used for gastrointestinal ailments and disorders linked to numerous risk factors including microbial infections. We aimed to provide contemporary evidence for its ethnopharmacological use and determine its antimicrobial capacity and mode of action, cytotoxicity, and phenolic constituents. Ethnopharmacological survey was conducted using semistructured interviews. Antimicrobial and antibiofilm capacities were determined by microdilution/crystal violet assay, respectively. Modes of action tested include estimation of exopolysaccharide production (congo red binding assay) and interference with membrane integrity (crystal violet uptake and nucleotide leakage assay). Cytotoxicity was determined using crystal violet assay. Polyphenolic profiling was done by advanced liquid chromatography/mass spectrometry (UHPLC-LTQ OrbiTrap MS). Artemisia absinthium in Serbia is traditionally used for gastrointestinal disorders, among others. Further study revealed high antifungal capacity of herb ethanolic extract towards range of Candida species (MIC 0.5–1 mg/mL) along with promising antibacterial activities (MIC 0.25–4 mg/mL). Interference with membrane integrity could be observed as a possible antimicrobial mechanism. Antibiofilm potential can be considered as high (towards C. krusei) to limited (towards P. aeruginosa) and moderate based on reduction in exopolysaccharide content. In concentrations up to 400 µg/mL, no cytotoxicity was observed towards HaCaT and HGF-1 cell lines. Polyphenolic analysis revealed twenty-one different constituents. A. absinthium usage as a gastrointestinal ailment remedy has been confirmed in vitro by its antimicrobial capacity towards microorganisms whose presence is linked to the diseases and associated complications and noncytotoxic nature of the natural product. The observed activities could be attributed to the present phenolic compounds.

APA, Harvard, Vancouver, ISO, and other styles

22

Firus Khan, Al’aina Yuhainis, Faizah Abdullah Asuhaimi, Tara K. Jalal, Fatimah Opeyemi Roheem, Hatim Abdullah Natto, Muhammad Farid Johan, Qamar Uddin Ahmed, and Ridhwan Abdul Wahab. "Hystrix brachyura Bezoar Characterization, Antioxidant Activity Screening, and Anticancer Activity on Melanoma Cells (A375): A Preliminary Study." Antioxidants 8, no. 2 (February 12, 2019): 39. http://dx.doi.org/10.3390/antiox8020039.

Full text

Abstract:

Porcupine bezoars (PBs) are masses of undigested calcareous concretions formed within the gastrointestinal tract. There are undocumented claims that PBs have antioxidant activity and can treat cancers. However, limited scientific study has been carried out to verify these traditional claims. Hence, this study was conducted to characterize the chemical profile and validate the antioxidant and anticancer activity against melanoma cells (A375). PB extract was initially subjected to Fourier-transform infrared spectroscopy (FTIR), gas chromatography–mass spectrometry (GCMS), total phenolic content (TPC), and total flavonoid content (TFC) analyses. The bioautography of antioxidant assays, namely 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazy (DPPH), and β-carotene was performed. An in vitro A375 cell viability assay, apoptosis assay, cell cycle arrest assay, and gene expression assay were carried out as well. The experimental finding revealed 5,10-diethoxy-2,3,7,8-tetrahydro-1H,6H-dipyrrolo[1,2-a:1’,2’-d]pyrazine, ursodeoxycholic acid, and cholest-5-en-3-ol (3 beta)-, carbonochloridate are major compounds detected in PB extract. PB extract has low phenolic content, viz. 698.7 ± 0.93 (µg GAE/5 mg dry weight). The bioautography antioxidant assays revealed a potent antioxidant effect (ABTS > DPPH > β-carotene), with free radical scavenging activity. Furthermore, PB extract exhibited dose- and time-dependent inhibition of cancer activity on A375 cells due to the exhibition of apoptosis via an intrinsic pathway.

APA, Harvard, Vancouver, ISO, and other styles

23

Orengo, Kenneth Otieno, James Mucunu Mbaria, Maingi Ndichu, Kitaa Jafred, and Mitchel Otieno Okumu. "Preliminary Phytochemical Composition and In Vitro Anthelmintic Activity of Aqueous and Ethanol Extracts of Olea africana against Mixed Gastrointestinal Worms in Dogs." Evidence-Based Complementary and Alternative Medicine 2022 (August 16, 2022): 1–8. http://dx.doi.org/10.1155/2022/5224527.

Full text

Abstract:

Olea africana is used by some indigenous communities in Kenya to control gastrointestinal worms in animals. Plant-based anthelmintics are gaining popularity globally in the control of gastrointestinal worms in animals. The egg hatch inhibition assay was used to assess the in vitro anthelmintic efficacy of aqueous and ethanol leaf extracts of O. africana against the eggs of mixed gastrointestinal helminths in dogs. Probit regression was used to calculate the concentration of extracts that inhibited egg hatching by 50% (IC50). Albendazole was used as a control. Standard techniques were used to quantify the phytochemicals in the extracts. The aqueous extract had an IC50 of 1.85 mg/mL (1.64–2.10), and the ethanol extract had an IC50 of 0.25 mg/mL (0.23–0.26). Quantitative phytochemical analysis revealed that aqueous and ethanol extracts of O. africana contained alkaloids (19.40 and 61.60%), saponins (24.00 and 6.00%), phenols (0.95 and 1.28 mg/g gallic acid equivalents (GAE)), flavonoids (8.71 and 12.26 mg/g catechin equivalents (CE)), and tannins (67.30 and 76.30 mg/g of tannic acid equivalent (TAE)), respectively. O. africana has dose-dependent anthelmintic effects against mixed gastrointestinal worms in dogs. These findings support the traditional use of Olea africana as a treatment option for gastrointestinal worms in dogs.

APA, Harvard, Vancouver, ISO, and other styles

24

Beak, Douglas G., Nicholas T. Basta, Kirk G. Scheckel, and Samuel J. Traina. "Bioaccessibility of Arsenic Bound to Corundum Using a Simulated Gastrointestinal System." Environmental Chemistry 3, no. 3 (2006): 208. http://dx.doi.org/10.1071/en05067.

Full text

Abstract:

Environmental Context. Ingestion of soil contaminated with arsenic is an important pathway for human exposure to arsenic. The risk posed by ingestion of arsenic-contaminated soil depends on how much arsenic is dissolved in the gastrointestinal tract. Aluminum oxides are common components in the soil and act as a sink for arsenic. Knowledge of the behavior of arsenic associated with aluminum oxide surfaces in a simulated gastrointestinal tract will provide an understanding of the ingestion risk of arsenic-contaminated soil to humans. Abstract. Arsenate adsorbed to oxide surfaces may influence the risk posed by incidental ingestion of arsenic-contaminated soil. Arsenate sorbed to corundum (α-Al2O3), a model Al oxide, was used to simulate ingested soil that has AsV sorbed to Al oxides. An in vitro assay was used to simulate the gastrointestinal tract and ascertain the bioaccessibility of arsenate bound to corundum. The surface speciation of arsenate was determined using extended X-ray absorption fine structure and X-ray absorption near edge structure spectroscopy. The arsenate sorption maximum was found to be 470 mg kg–1 and the surface speciation of the sorbed arsenate was inner-sphere binuclear bidenate. The AsV was found to only be bioaccessible during the gastric phase of the in vitro assay. When the sorbed AsV was <470 mg kg–1 (i.e., the sorption maxima) the bioaccessible As was below detection levels, but when sorbed AsV was ≥470 mg kg–1 the bioaccessible As ranged from 9 to 16%. These results demonstrate that the bioaccessibility of arsenate is related to the concentration and the arsenate binding capacity of the binding soil.

APA, Harvard, Vancouver, ISO, and other styles

25

Abidi, A., E. Sebai, M. Dhibi, MA Darghouth, and H. Akkari. "Chemical analyses and evaluation of the anthelmintic effects of Origanum majorana essential oil, in vitro and in vivo studies." Veterinární Medicína 65, No. 11 (November 26, 2020): 495–505. http://dx.doi.org/10.17221/115/2019-vetmed.

Full text

Abstract:

Because of the development of resistance in helminths against major anthelmintic drugs, the search for alternatives is necessary. Medicinal plants are being studied as an alternative source of anthelmintics against gastrointestinal nematodes. The objective of this study is to analyse the chemical composition and evaluate the anthelmintic efficacy of Origanum majorana essential oil. The determination of the chemical composition by gas chromatography/mass chromatography (GC/MS) revealed that the essential oil was dominated by terpenoids, particularly carvacrol (35.65%) and terpenic hydrocarbons p-cymene (15.82%). The in vitro anthelmintic effects against Haemonchus contortus were assessed by an egg hatch assay (EHA) and an adult worm motility assay (AWMA) compared with the reference drug albendazole. The essential oil showed ovicidal activity at all the tested concentrations (1, 2, 4 and 8 mg/ml) and more than 80% egg hatching inhibition was observed at the highest dose (8 mg/ml). Exposure to 0.5 mg/ml of the essential oil for eight hours induced a 50% inhibition in the worm motility. The in vivo study was performed on H. polygyrus by measuring the egg count reduction (ECR) and adult worm count reduction (AWCR) following the treatment of the animals with different doses (2 000, 4 000 and 5 000 mg/kg) of the plant essential oil, and 22 mg/kg of albendazole as the positive control. The results showed that 5 000 mg/kg of the essential oil inhibited the egg count and adult worm count by 76.3 and 74.0%, respectively, seven days post treatment. These findings support the possible use of O. majorana essential oil to control gastrointestinal nematodes.

APA, Harvard, Vancouver, ISO, and other styles

26

Vincze, Anna, Gergő Dargó, and György Tibor Balogh. "Cornea-PAMPA as an Orthogonal in Vitro Physicochemical Model of Corneal Permeability." Periodica Polytechnica Chemical Engineering 64, no. 3 (May 25, 2020): 384–90. http://dx.doi.org/10.3311/ppch.15601.

Full text

Abstract:

The present study was aimed to investigate the relationships between permeability and membrane retention values (logPe and MR) of the in vitro non-cellular permeability assay, corneal-PAMPA in comparison with experimental Caco-2 permeability data and calculated physicochemical properties (MW, clogP, clogD7.4 , TPSA). For the investigation, 50 structurally and physicochemically diverse drugs were selected and measured in PAMPA model optimized for corneal permeability. The results showed corneal-PAMPA model's orthogonality in terms of passive diffusion to the FDA approved Caco-2 as a gastrointestinal absorption model, while the comparison with physicochemical properties revealed trends between logPe , MR and the lipophilicity descriptors and TPSA.

APA, Harvard, Vancouver, ISO, and other styles

27

Keating, Christopher, Vicente Martinez, Jean Pierre Valentin, and David Grundy. "The evaluation of an in vitro motility assay for its potential to predict gastrointestinal adverse drug reactions." Journal of Pharmacological and Toxicological Methods 60, no. 2 (September 2009): 230. http://dx.doi.org/10.1016/j.vascn.2009.04.091.

Full text

APA, Harvard, Vancouver, ISO, and other styles

28

Keating, Christopher, Vicente Martinez, Lorna Ewart, Stephen Gibbons, Luke Grundy, Jean-Pierre Valentin, and David Grundy. "The validation of an in vitro colonic motility assay as a biomarker for gastrointestinal adverse drug reactions." Toxicology and Applied Pharmacology 245, no. 3 (June 15, 2010): 299–309. http://dx.doi.org/10.1016/j.taap.2010.03.014.

Full text

APA, Harvard, Vancouver, ISO, and other styles

29

Mason, Emily, Lamia L’Hocine, Allaoua Achouri, Mélanie Pitre, and Salwa Karboune. "Health Promoting Bioactive Properties of Novel Hairless Canary Seed Flour after In Vitro Gastrointestinal Digestion." Foods 9, no. 7 (July 14, 2020): 932. http://dx.doi.org/10.3390/foods9070932.

Full text

Abstract:

The bioactive properties and health-promoting effects of two novel yellow (C09052, C05041) and two brown (Calvi, Bastia) hairless canary seed (Phalaris canariensis L.) cultivars were investigated in comparison to two common cereal grains (wheat and oat). The cereal flours were digested using the standardized INFOGEST in vitro human gastrointestinal digestion model. The three-kilo dalton molecular weight cutoff (3 kDa MWCO) permeate of the generated digestates was assessed in vitro for their antioxidant, chelating, antihypertensive and antidiabetic activities. The results showed no significant differences in studied bioactivities between yellow and brown canary seed cultivars, except for antioxidant activity by the DPPH and chelating Fe2+ assays, where brown cultivars had higher activities. Canary seeds had superior or equivalent antioxidant activity than those from oat and wheat. The anti-hypertensive activity (Angiotensin-converting enzyme (ACE) inhibition) in yellow canary seed cultivars was significantly higher than that of oat and wheat, particularly for C09052 and Calvi varieties. Peptides exhibiting the highest antihypertensive activity from the permeate of the C09052 canary seed variety were further fractionated and identified by mass spectrometry. Forty-six peptides were identified belonging to 18 proteins from the Pooideae subfamily. Fourteen of the parent proteins were homologous to barley proteins. Peptides were analyzed in silico to determine potential bioactivity based on their amino acid composition. All 46 peptides had potential anti-hypertensive and anti-diabetic activities and 20 had potential antioxidant activity, thereby validating the in vitro assay data. Canary seed peptides also exhibited potential antiamnestic, antithrombotic, immunostimulating, opioid and neuro-activity, demonstrating important potential for health promoting effects, particularly against cardiovascular disease.

APA, Harvard, Vancouver, ISO, and other styles

30

Ali-Shtayeh, Mohammed Saleem, Rana Majed Jamous, Salam Yousef Abu Zaitoun, and Iman Basem Qasem. "In-vitro screening of acetylcholinesterase inhibitory activity of extracts from Palestinian indigenous flora in relation to the treatment of Alzheimer’s disease." Functional Foods in Health and Disease 4, no. 9 (September 1, 2014): 381. http://dx.doi.org/10.31989/ffhd.v4i9.149.

Full text

Abstract:

Background: Cholinesterase inhibitory therapy serves as a strategy for the treatment of Alzheimer’s disease (AD). Several acetylcholinesterase inhibitors (AChEIs) are used for the symptomatic treatment of AD. These compounds have been reported to have adverse effects, including gastrointestinal disturbances. This study was therefore partly aimed at investigating in vitro possible AChEIs in herbal medicines traditionally used in Palestine to treat cognitive disorders, and to point out the role of these plants as potential sources for development of newly potent and safe natural therapeutic agents of AD. Assay of AChE activity plays an important role in vitro characterization of drugs including potential treatments for AD. The most widely used method, is based on Ellman’s method. The reactant used in this method shows chemical reactivity with oxime antidots and thiol leading to false positive reactions. A new alternative assay could be of high interest.Methods: The effect on AChE activity of 92 extracts of 47 medicinal plants were evaluated using a new micro-well plate AChE activity (NA-FB) and Ellman’s assays. In addition, antioxidant activity using DPPH was determined.Results: The main advantages of the new method (NA-FB) is that the colorimetric change is better observable visually allowing spectrophotometric as well as colorimetric assay, and does not show any chemical reactivity with thiol. 67.4% and 37% of extracts inhibited AChE by >50% using the NA-FB and Ellman’s assays, respectively. Using NA-FB assay, 84 extracts interacted reversibly with the enzyme, of which Mentha spicata (94.8%), Foeniculum vulgare (89.81), and Oxalis pes-caprae (89.21) were most potent, and 8 showed irreversible inhibition of which leaves of Lupinus pilosus (92.02%) were most active. Antioxidant activity was demonstrated by 73 extracts Majorana syriaca (IC50 0.21mg/ml), and Rosmarinus officinalis (0.38) were the most active.Conclusions: NA-FB assay has shown to be simple, accurate, sensitive, spectrophotometric and colorimetric, and superior to Ellman’s, and therefore can be used efficiently for qualitative and quantitative studies of AChEI activities of extracts. Palestinian flora have shown to be a rich source for, new and promising agents (AChEIs) for the treatment of AD Further studies are needed to isolate and identify the active compounds responsible for AChEI activities.Keywords: Alzheimer's disease, ACh, medicinal plants, β-naphthyl acetate, micro-well plate AChE activity Assay (NA-FB)

APA, Harvard, Vancouver, ISO, and other styles

31

Lakshmi Ragavan, Mangala, and Nilanjana Das. "MOLECULAR IDENTIFICATION OF PROBIOTIC YEAST STRAINS AND THEIR CHARACTERIZATION." Asian Journal of Pharmaceutical and Clinical Research 10, no. 10 (September 1, 2017): 339. http://dx.doi.org/10.22159/ajpcr.2017.v10i10.20052.

Full text

Abstract:

Objective The objective of the present study was to identify the potential yeast isolates at themolecular level and evaluate their probiotic characteristics.MethodsMolecular characterization was done for 5 potential probiotic yeast strains. In vitro assays have been conducted to evaluate the probiotic properties such as NaCl tolerance, autoaggregation and co-aggregation. Haemolyticactivity, urease activity and cytotoxicity tests were carried out for safety assay during the characterization of yeast strains.ResultsIn this study, the yeast strains viz. LM,MR,GOI,GII2and WI were identified at molecular level and named as Yarrowialipolytica VIT-MN01, Kluyveromyces lactis VIT-MN02, Lipomyces starkeyi VIT-MN03, Saccharomycopsis fibuligera VIT-MN04, Brettanomyces custersianus VIT-MN05 respectively. Maximum autoaggregation and coaggregationwere noted in case of Lipomyces starkeyi VIT-MN03, Saccharomycopsis fibuligeraVIT-MN04, and Brettanomyces custersianus VIT-MN05. In vitro toxicity assay was performed and all the yeast strains showednon-toxic nature.ConclusionFive yeast strains have been studied for their probiotic characteristics and identified at molecular level. Out offive yeast strains, three strains showed maximum adhesion ability,which is a prerequisite for colonization and protection of gastrointestinal tract. All the yeast strains are validated as a safe bioresources because of their non - hemolytic activities and non-production of urease. It can be concluded that the identified yeast strainscan serve as promising probiotics in various fields offood industry.

APA, Harvard, Vancouver, ISO, and other styles

32

Carrasco, Nicolás, Maritza Garrido, Iván Montenegro, Alejandro Madrid, Ricardo Hartley, Iván González, Mariaignacia Rubilar, Joan Villena, and Manuel Valenzuela-Valderrama. "Antitumoral Activity of Leptocarpha rivularis Flower Extracts against Gastric Cancer Cells." International Journal of Molecular Sciences 24, no. 2 (January 11, 2023): 1439. http://dx.doi.org/10.3390/ijms24021439.

Full text

Abstract:

Leptocarpha rivularis is a native South American plant used ancestrally by Mapuche people to treat gastrointestinal ailments. L. rivularis flower extracts are rich in molecules with therapeutic potential, including the sesquiterpene lactone leptocarpin, which displays cytotoxic effects against various cancer types in vitro. However, the combination of active molecules in these extracts could offer a hitherto unexplored potential for targeting cancer. In this study, we investigated the effect of L. rivularis flower extracts on the proliferation, survival, and spread parameters of gastric cancer cells in vitro. Gastric cancer (AGS and MKN-45) and normal immortalized (GES-1) cell lines were treated with different concentrations of L. rivularis flower extracts (DCM, Hex, EtOAc, and EtOH) and we determined the changes in proliferation (MTS assay, cell cycle analysis), cell viability/cytotoxicity (trypan blue exclusion assay, DEVDase activity, mitochondrial membrane potential MMP, and clonogenic ability), senescence (β-galactosidase activity) and spread potential (invasion and migration assays using the Boyden chamber approach) in all these cells. The results showed that the DCM, EtOAc, and Hex extracts display a selective antitumoral effect in gastric cancer cells by affecting all the cancer parameters tested. These findings reveal an attractive antitumoral potential of L. rivularis flower extracts by targeting several acquired capabilities of cancer cells.

APA, Harvard, Vancouver, ISO, and other styles

33

Chen, Zheng, Jinfeng Chen, Xiaodong Wei, Huiying Hua, Ruiming Hu, Nengshui Ding, Jinhua Zhang, et al. "Antiviral Activities of Carbazole Derivatives against Porcine Epidemic Diarrhea Virus In Vitro." Viruses 13, no. 12 (December 16, 2021): 2527. http://dx.doi.org/10.3390/v13122527.

Full text

Abstract:

Porcine epidemic diarrhea virus (PEDV), an enteric coronavirus, causes neonatal pig acute gastrointestinal infection with a characterization of severe diarrhea, vomiting, high morbidity, and high mortality, resulting in tremendous damages to the swine industry. Neither specific antiviral drugs nor effective vaccines are available, posing a high priority to screen antiviral drugs. The aim of this study is to investigate anti-PEDV effects of carbazole alkaloid derivatives. Eighteen carbazole derivatives (No.1 to No.18) were synthesized, and No.5, No.7, and No.18 were identified to markedly reduce the replication of enhanced green fluorescent protein (EGFP) inserted-PEDV, and the mRNA level of PEDV N. Flow cytometry assay, coupled with CCK8 assay, confirmed No.7 and No.18 carbazole derivatives displayed high inhibition effects with low cell toxicity. Furthermore, time course analysis indicated No.7 and No.18 carbazole derivatives exerted inhibition at the early stage of the viral life cycle. Collectively, the analysis underlines the benefit of carbazole derivatives as potential inhibitors of PEDV, and provides candidates for the development of novel therapeutic agents.

APA, Harvard, Vancouver, ISO, and other styles

34

Chao, Po-Kuan, Shau-Hua Ueng, Li-Chin Ou, Teng-Kuang Yeh, Wan-Ting Chang, Hsiao-Fu Chang, Shu-Chun Chen, et al. "1-(2,4-Dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one." Anesthesiology 126, no. 5 (May 1, 2017): 952–66. http://dx.doi.org/10.1097/aln.0000000000001568.

Full text

Abstract:

Abstract Background The authors investigated the pharmacology and signaling pathways of the opioid receptors modulated by compound 1, 1-(2,4-dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one. Methods In vitro studies of compound 1 were assessed by using a radioligand-binding assay (n = 3), a cyclic adenosine monophosphate assay (n = 3), a β-arrestin assay (n = 3), an internalization assay (n = 3), and an immunohistochemistry (n = 8). In vivo studies of compound 1 were characterized using a tail-flick test (n = 5 to 6), tail-clip test (n = 7), von Frey hair test (n = 5), and charcoal meal test (n = 5). Results Compound 1 elicited robust effects in μ-opioid (mean ± SD; binding affinity: 15 ± 2 nM; cyclic adenosine monophosphate assay: 24 ± 6 nM), δ-opioid (82 ± 7 nM; 1.9 ± 0.1 μM), and κ-opioid (76 ± 9 nM; 1.4 ± 0.5 μM) receptor–expressing cells. Compound 1 acts as a full agonist of β-arrestin-2 recruitment in μ-opioid (1.1 ± 0.3 μM) and δ-opioid (9.7 ± 1.9 μM) receptor–expressing cells. Compound 1 caused less gastrointestinal dysfunction (charcoal meal test: morphine: 82 ± 5%; compound 1: 42 ± 5%) as well as better antinociception in mechanical pain hypersensitivity (tail-clip test: morphine: 10 ± 3 s; compound 1: 19 ± 1 s) and in cancer-induced pain (von Frey hair test: morphine: 0.1 ± 0.1 g; compound 1: 0.3 ± 0.1 g) than morphine at equi-antinociceptive doses. Conclusions Compound 1 produced antinociception with less gastrointestinal dysfunction than morphine.

APA, Harvard, Vancouver, ISO, and other styles

35

Shahed-Al-Mahmud, Md, and Hasib Al Hasan. "In-vitro Anthelmintic Activity of Aqueous Extract of Leaves of Cleome Rutidosperma DC. (Capparidaceae) Against Haemonchus Contortus." Research in Pharmacy and Health Sciences 4, no. 1 (February 15, 2018): 415–18. http://dx.doi.org/10.32463/rphs.2018.v04i01.03.

Full text

Abstract:

Background: Cleome rutidosperma is annual herb found in different places in Bangladesh. Its leaves used as the treatment for Helminthiasis associated with Haemonchus contortus. This parasite is one of the most pathogenic nematodes and responsible for anemia, edema, and death of cattle’s, mainly during summer in warm, humid climates as like Bangladesh. The aim of the study to investigate the in-vitro anthelmintic activity of aqueous extract C. rutidosperma (AECR) leaves against H. contortus. Methods: We performed phytochemical analysis and in-vitro anthelmintic assay to determine the possible phytochemicals, caused by anthelmintic activity against H. contortus. Results: In-vitro anthelmintic assay, the AECR at the doses of 25; 50 and 100mg/mL significantly (p< 0.01) and (p< 0.001) paralyzed and caused the death of H. contortus in a dose-dependent manner. Reference standard drug Albendazole (15 mg/mL) exerts almost same effect as AECR. No paralyzed and death observed at the control group when treated with 0.9% normal saline. Conclusion: This data confirmed that the aqueous extract C. rutidosperma has the in-vitro anthelmintic activity of against H. contortus. C. rutidosperma may offer an alternative source for the control of gastrointestinal nematodes of cattle’s.

APA, Harvard, Vancouver, ISO, and other styles

36

Vega-Rojas, Lineth Juliana, Ivan Luzardo-Ocampo, Juan Mosqueda, Dulce María Palmerín-Carreño, Antonio Escobedo-Reyes, Alejandro Blanco-Labra, Konisgmar Escobar-García, and Teresa García-Gasca. "Bioaccessibility and In Vitro Intestinal Permeability of a Recombinant Lectin from Tepary Bean (Phaseolus acutifolius) Using the Everted Intestine Assay." International Journal of Molecular Sciences 22, no. 3 (January 21, 2021): 1049. http://dx.doi.org/10.3390/ijms22031049.

Full text

Abstract:

Tepary bean (Phaseolus acutifolius) lectins exhibit differential in vitro and in vivo biological effects, but their gastrointestinal interactions and digestion have not yet been assessed. This work aimed to evaluate the changes of a recombinant Tepary bean lectin (rTBL-1) through an in vitro and ex vivo gastrointestinal process. A polyclonal antibody was developed to selectively detect rTBL-1 by Western blot (WB) and immunohistochemical analysis. Everted gut sac viability was confirmed until 60 min, where protein bioaccessibility, apparent permeability coefficient, and efflux ratio showed rTBL-1 partial digestion and absorption. Immunoblot assays suggested rTBL-1 internalization, since the lectin was detected in the digestible fraction. The immunohistochemical assay detected rTBL-1 presence at the apical side of the small intestine, potentially due to the interaction with the intestinal cell membrane. The in silico interactions between rTBL-1 and some saccharides or derivatives showed high binding affinity to sialic acid (−6.70 kcal/mol) and N-acetylglucosamine (−6.10 kcal/mol). The ultra-high-performance liquid chromatography–electron spray ionization–quantitative time-of-flight coupled to mass spectrometry (UHPLC–ESI–QTOF/MS) analysis showed rTBL-1 presence in the gastric content and the non-digestible fraction after intestinal simulation conditions. The results indicated that rTBL-1 partially resisted the digestive conditions and interacted with the intestinal membrane, whereas its digestion allowed the absorption or internalization of the protein or the derivative peptides. Further purification of digestion samples should be conducted to identify intact rTBL-1 protein and digested peptides to assess their physiological effects.

APA, Harvard, Vancouver, ISO, and other styles

37

Venardou, Brigkita, John V. O’Doherty, Marco Garcia-Vaquero, Claire Kiely, Gaurav Rajauria, Mary J. McDonnell, Marion T. Ryan, and Torres Sweeney. "Evaluation of the Antibacterial and Prebiotic Potential of Ascophyllum nodosum and Its Extracts Using Selected Bacterial Members of the Pig Gastrointestinal Microbiota." Marine Drugs 20, no. 1 (December 30, 2021): 41. http://dx.doi.org/10.3390/md20010041.

Full text

Abstract:

Ascophyllum nodosum and its extracts are promising antibacterial and prebiotic dietary supplements for pigs. The objectives of this study were to evaluate the effects of the increasing concentrations of: (1) two whole biomass samples of A. nodosum with different harvest seasons, February (ANWB-F) and November (ANWB-N), in a weaned pig faecal batch fermentation assay, and (2) A. nodosum extracts produced using four different extraction conditions of a hydrothermal-assisted extraction methodology (ANE1–4) and conventional extraction methods with water (ANWE) and ethanol (ANEE) as solvent in individual pure culture growth assays using a panel of beneficial and pathogenic bacterial strains. In the batch fermentation assay, ANWB-F reduced Bifidobacterium spp. counts (p < 0.05) while ANWB-N increased total bacterial counts and reduced Bifidobacterium spp. and Enterobacteriaceae counts (p < 0.05). Of the ANE1–4, produced from ANWB-F, ANWE and ANEE that were evaluated in the pure culture growth assays, the most interesting extracts were the ANE1 that reduced Salmonella Typhimurium, enterotoxigenic Escherichia coli and B. thermophilum counts and the ANE4 that stimulated B. thermophilum growth (p < 0.05). In conclusion, the extraction method and conditions influenced the bioactivities of the A. nodosum extracts with ANE1 and ANE4 exhibiting distinct antibacterial and prebiotic properties in vitro, respectively, that merit further exploration.

APA, Harvard, Vancouver, ISO, and other styles

38

Murineddu, Gabriele, Battistina Asproni, Paola Corona, Sandra Piras, Paolo Lazzari, Stefania Ruiu, Laura Legnani, Lucio Toma, and Gérard A. Pinna. "Development of Oxygen-Bridged Pyrazole-Based Structures as Cannabinoid Receptor 1 Ligands." Molecules 24, no. 9 (April 27, 2019): 1656. http://dx.doi.org/10.3390/molecules24091656.

Full text

Abstract:

In this work, the synthesis of the cannabinoid receptor 1 neutral antagonists 8-chloro-1-(2,4-dichlorophenyl)-N-piperidin-1-yl-4,5-dihydrobenzo-1H-6-oxa-cyclohepta[1,2-c]pyrazole-3-carboxamide 1a and its deaza N-cyclohexyl analogue 1b has led to a deepening of the structure-activity studies of this class of compounds. A series of novel 4,5-dihydrobenzo-oxa-cycloheptapyrazoles analogues of 1a,b, derivatives 1c–j, was synthesized, and their affinity towards cannabinoid receptors was determined. Representative terms were evaluated using in vitro tests and isolated organ assays. Among the derivatives, 1d and 1e resulted in the most potent CB1 receptor ligands (KiCB1 = 35 nM and 21.70 nM, respectively). Interestingly, both in vitro tests and isolated organ assays evidenced CB1 antagonist activity for the majority of the new compounds, excluding compound 1e, which showed a CB1 partial agonist behaviour. CB1 antagonist activity of 1b was further confirmed by a mouse gastrointestinal transit assay. Significant activity of the new CB1 antagonists towards food intake was showed by preliminary acute assays, evidencing the potentiality of these new derivatives in the treatment of obesity.

APA, Harvard, Vancouver, ISO, and other styles

39

Stajcic, Sladjana, Jasna Canadanovic-Brunet, Gordana Cetkovic, Vesna Tumbas-Saponjac, Jelena Vulic, and Vanja Seregelj. "Simulated gastrointestinal digestion and storage stability of tomato waste encapsulates." Acta Periodica Technologica, no. 52 (2021): 239–52. http://dx.doi.org/10.2298/apt2152239s.

Full text

Abstract:

The application of bioactive antioxidant compounds is limited because of their instability. To overcome this drawback, different protection systems including encapsulation have been developed. In this study, for the stabilisation of bioactive compounds (carotenoids and phenolics) extracted from tomato waste, encapsulation with carbohydrate (inulin and gum arabica) and protein (soy protein and pea protein) wall materials by freeze drying method was applied. Content of bioactive compounds and antioxidant properties (determined by DPPH, reducing power and ?-carotene bleaching assay) of encapsulates before and after in vitro digestion was investigated. Also, in obtained encapsulates carotenoid stability during storage at ambient (25 ? 5 ?C) light and dark conditions for four weeks was assessed. The results indicated that release behavior of bioactive compounds and antioxidant activity after digestion of encapsulates varied according to the type of wall material. Protein carriers showed better ability to preserve phenolic compounds through in vitro gastrointestinal digestion in comparison to carbohydrate wall materials. Pea protein showed best carrier properties for delivery of carotenoids, while differently to other used carriers, gum arabica showed minor ability to release carotenoids after in vitro gastrointestinal digestion. During storage higher content of carotenoids was preserved in encapsulates prepared with carbohydrate carriers. All encapsulates retained higher amount of carotenoids under dark conditions. The results of this study showed that assessment of the behavior of encapsulates during digestion and storage is necessary in order of selection appropriate delivery system of bioactive compounds in powder form which can be used as ingredient in functional food products.

APA, Harvard, Vancouver, ISO, and other styles

40

Gajek, Gabriela, Beata Marciniak, Jarosław Lewkowski, and Renata Kontek. "Antagonistic Effects of CAPE (a Component of Propolis) on the Cytotoxicity and Genotoxicity of Irinotecan and SN38 in Human Gastrointestinal Cancer Cells In Vitro." Molecules 25, no. 3 (February 4, 2020): 658. http://dx.doi.org/10.3390/molecules25030658.

Full text

Abstract:

The incidence of gastrointestinal cancers is increasing every year. Irinotecan (CPT-11), a drug used in the treatment of colorectal cancer and gastric cancer, is metabolized by carboxylesterases to an active metabolite, SN-38, which is more cytotoxic. CAPE (caffeic acid phenethyl ester) is an active component of propolis, which has a high antibacterial, antiviral, and antineoplastic potential. This study analyses the impact of CAPE on the cytotoxic (MTT assay), genotoxic (comet assay) and proapoptotic (caspase-3/7 activity) potential of irinotecan and its metabolite SN-38 in cultures of gastrointestinal neoplastic cells (HCT116, HT29, AGS). Cytotoxicity and genotoxicity activities of these compounds were carried out in comparison with human peripheral blood lymphocytes (PBLs) in vitro. The antioxidant potential of CAPE was investigated in relation H2O2-induced oxidative stress in the both neoplastic cells and PBLs. CAPE expressed cytotoxic, genotoxic, and pro-apoptotic activity against AGS, HCT116, and HT29 tumor cells. CAPE, in the presence of different concentrations of irinotecan or SN38, decreased the cytotoxicity, genotoxicity, and pro-apoptotic activity in these cell lines, but it has no such action on normal human peripheral blood lymphocytes.

APA, Harvard, Vancouver, ISO, and other styles

41

Igual, Marta, Ângela Fernandes, Maria Inês Dias, José Pinela, Purificación García-Segovia, Javier Martínez-Monzó, and Lillian Barros. "The In Vitro Simulated Gastrointestinal Digestion Affects the Bioaccessibility and Bioactivity of Beta vulgaris Constituents." Foods 12, no. 2 (January 11, 2023): 338. http://dx.doi.org/10.3390/foods12020338.

Full text

Abstract:

Beetroot (Beta vulgaris L.) is an important root vegetable crop and a valuable food source of micronutrients and bioactive constituents. In this study, the bioaccessibility of minerals, organic acids, and betacyanins in beetroot powder during simulated gastrointestinal digestion was investigated, as well as the antioxidant activity of the final fractions of each phase of the process. Mineral elements were analyzed by inductively coupled plasma optical emission spectroscopy (ICP-OES), organic acids by ultra-fast liquid chromatography with photodiode array detection (UFLC-PDA), and betacyanins by liquid chromatography with diode-array detection and mass spectrometry (HPLC-DAD-ESI/MSn). The oxidative hemolysis inhibition assay was used to assess the ex vivo antioxidant activity. The bioaccessibility of minerals at the end of gastrointestinal digestion ranged from 43 to 65%, depending on the mineral element. Among these, Mg was the most bioaccessible, while Ca and Fe had the lowest bioaccessibility. For organic acids, a major release during digestion was observed for quinic acid. It was also found that betanin (the major betalain in beetroot) was highly unstable during the digestion process, probably due to its hydrophilic nature, which agreed with the significant (p < 0.05) decrease in antioxidant/antihemolytic activity. These results suggest that beetroot antioxidant compounds are unstable under gastrointestinal conditions, and could be useful for future development of novel and more stable beetroot food formulations.

APA, Harvard, Vancouver, ISO, and other styles

42

Batista, Daniela, Pedro L. Falé, Maria L. Serralheiro, Maria-Eduarda Araújo, Catarina Dias, Isabel Branco, Clara Grosso, et al. "Phytochemical Characterization and Biological Evaluation of the Aqueous and Supercritical Fluid Extracts from Salvia sclareoides Brot." Open Chemistry 15, no. 1 (April 29, 2017): 82–91. http://dx.doi.org/10.1515/chem-2017-0011.

Full text

Abstract:

AbstractPlants belonging to the genus Salvia (Lamiaceae) are known to have a wide range of biological properties. In this work, extracts obtained from the aerial parts of Salvia sclareoides Brot. were evaluated to investigate their chemical composition, toxicity, bioactivity, and stability under in vitro gastrointestinal conditions. The composition of the supercritical fluid extract was determined by GC and GC-MS, while the identification of the infusion constituents was performed by HPLC-DAD and LC-MS. The in vitro cytotoxicity of both extracts (0-2 mg/mL) was evaluated in Caco-2 cell lines by the MTT assay. The anti-inflammatory and anticholinesterase activities were determined through the inhibition of cyclooxygenase-1 and acetylcholinesterase enzymes, while β-carotene/linoleic acid bleaching test and the DPPH assays were used to evaluate the antioxidant activity. The infusion inhibited cyclooxygenase-1 (IC50 = 271.0 μg/mL), and acetylcholinesterase (IC50 = 487.7 μg/ mL) enzymes, also demonstrated significant antioxidant properties, as evaluated by the DPPH (IC50 = 10.4 μg/mL) and β-carotene/linoleic acid (IC50 = 30.0 μg/mL) assays. No remarkable alterations in the composition or in the bioactivities of the infusion were observed after in vitro digestion, which supports the potential of S. sclareoides as a source of bioactive ingredients with neuroprotective, anti-inflammatory and antioxidant properties.

APA, Harvard, Vancouver, ISO, and other styles

43

Lorenzo-Rebenaque, Laura, Danish J. Malik, Pablo Catalá-Gregori, Clara Marin, and Sandra Sevilla-Navarro. "In Vitro and In Vivo Gastrointestinal Survival of Non-Encapsulated and Microencapsulated Salmonella Bacteriophages: Implications for Bacteriophage Therapy in Poultry." Pharmaceuticals 14, no. 5 (May 6, 2021): 434. http://dx.doi.org/10.3390/ph14050434.

Full text

Abstract:

The therapeutic use of bacteriophages is recognized as a viable method to control Salmonella. Microencapsulation of phages in oral dosage forms may protect phages from inherent challenges of the gastrointestinal tract in chickens. Therefore, the main objective of this study was to assess the survival of Salmonella BP FGS011 (non-encapsulated and microencapsulated) through the gastrointestinal tract under in vitro as well as in vivo conditions after oral administration to 1-day-old chicks. To this end, the phage FGS011 was encapsulated in two different pH-responsive formulations with polymers Eudragit® L100, and Eudragit® S100 using the process of spray drying. Phages encapsulated in either of the two formulations were able to survive exposure to the proventriculus-gizzard in vitro conditions whereas free phages did not. Moreover, phages formulated in polymer Eudragit® S100 would be better suited to deliver phage to the caeca in chickens. In the in vivo assay, no statistically significant differences were observed in the phage concentrations across the gastrointestinal tract for either the free phage or the encapsulated phage given to chicks. This suggested that the pH of the proventriculus/gizzard in young chicks is not sufficiently acidic to cause differential phage titre reductions, thereby allowing free phage survival in vivo.

APA, Harvard, Vancouver, ISO, and other styles

44

Navarro del Hierro, Joaquin, Vieri Piazzini, Guillermo Reglero, Diana Martin, and Maria Camilla Bergonzi. "In Vitro Permeability of Saponins and Sapogenins from Seed Extracts by the Parallel Artificial Membrane Permeability Assay: Effect of in Vitro Gastrointestinal Digestion." Journal of Agricultural and Food Chemistry 68, no. 5 (January 14, 2020): 1297–305. http://dx.doi.org/10.1021/acs.jafc.9b07182.

Full text

APA, Harvard, Vancouver, ISO, and other styles

45

Rao, Priyanka Singh, Emerson Nolasco, Akihiro Handa, Michael J. Naldrett, Sophie Alvarez, and Kaustav Majumder. "Effect of pH and Heat Treatment on the Antioxidant Activity of Egg White Protein-Derived Peptides after Simulated In-Vitro Gastrointestinal Digestion." Antioxidants 9, no. 11 (November 11, 2020): 1114. http://dx.doi.org/10.3390/antiox9111114.

Full text

Abstract:

The study aimed to analyze pH and heat treatment’s effect in modulating the release of peptides with antioxidant activity after simulated gastrointestinal (GI) digestion of Egg white powder (EWP). EWP samples with neutral (EWPN) and alkaline (EWPA) pH were heat-treated at 20, 60, and 90 °C and analyzed for protein aggregation, solubility, and GI digestibility. Heat treatment decreased solubility and induced protein aggregation, which was higher for EWPN as compared to EWPA. The unfolding of EWPA proteins at 60 °C exhibited a higher GI digestibility and antioxidant activity via Oxygen Radical Absorbance Capacity (ORAC) assay as compared to EWPN. Interestingly, a reverse trend was observed in the cellular antioxidant assay, and the GI-digest of EWPN exhibited a higher antioxidant activity. The LC-MS/MS analysis are in concordance with cellular antioxidant activity assay and showed a higher intensity for peptides with potential antioxidant activity in the GI-digest of EWPN. The results indicate that heat treatment but not the pH is a critical factor in improving the protein digestibility and releasing peptides with antioxidant activity after GI digestion.

APA, Harvard, Vancouver, ISO, and other styles

46

Zhao, Jianchun, Wenmin Yuan, Shixiao Wang, Hongwei Zhang, Dan Chen, Xiaochen Niu, Xiaochun Liu, Li Liu, and Jiangming Gao. "Comparative Pharmacokinetics and Tissue Distribution of M10 and Its Metabolite Myricetin in Normal and Dextran-Sodium-Sulfate-Induced Colitis Mice." Molecules 27, no. 23 (November 23, 2022): 8140. http://dx.doi.org/10.3390/molecules27238140.

Full text

Abstract:

M10, a novel myricetin derivative, is an anti-inflammatory agent designed for treatment of colitis. Here, we aim to investigate its pharmacokinetic behavior and tissue distribution in a mouse model with colitis. Pharmacokinetics and tissue distribution of M10 and its metabolite myricetin were compared in normal mice and in dextran-sodium-sulfate (DSS)-induced colitis mice. The role of fecal microbiota was also analyzed during metabolism of M10 in vitro. After oral administration, M10 was very low in the plasma of both normal and diseased mice. However, both M10 and myricetin were mainly distributed in the gastrointestinal tract, including the stomach, colon and small intestine, in physiological and pathological conditions. Significantly, M10 and myricetin were found in higher levels in gastrointestinal tracts with inflamed tissues than in normal tissues of mice. An in vitro assay revealed that 80% of M10 was metabolized to myricetin via fecal microbiota. After oral administration, M10 was not absorbed into circulation but mainly distributed in the inflamed submucosal tissues of colitic mice, where it was metabolized into myricetin to prevent colitis development.

APA, Harvard, Vancouver, ISO, and other styles

47

Straub, T. M., J. R. Hutchison, R. A. Bartholomew, C. O. Valdez, N. B. Valentine, A. Dohnalkova, R. M. Ozanich, and C. J. Bruckner-Lea. "Defining cell culture conditions to improve human norovirus infectivity assays." Water Science and Technology 67, no. 4 (February 1, 2013): 863–68. http://dx.doi.org/10.2166/wst.2012.636.

Full text

Abstract:

Significant difficulties remain for determining whether human noroviruses (hNoV) recovered from water, food, and environmental samples are infectious. Three-dimensional (3-D) tissue culture of human intestinal cells has shown promise in developing an infectivity assay, but reproducibility, even within a single laboratory, remains problematic. From the literature and our observations, we hypothesized that the common factors that lead to more reproducible hNoV infectivity in vitro requires that the cell line be (1) of human gastrointestinal origin, (2) expresses apical microvilli, and (3) be a positive secretor cell line. The C2BBe1 cell line, which is a brush-border producing clone of Caco-2, meets these three criteria. When challenged with Genogroup II viruses, we observed a 2 Log10 increase in viral RNA titer. A passage experiment with GII viruses showed evidence of the ability to propagate hNoV by both quantitative reverse transcription polymerase chain reaction (qRT-PCR) and microscopy. In our hands, using 3-D C2BBe1 cells improves reproducibility of the infectivity assay for hNoV, but the assay can still be variable. Two sources of variability include the cells themselves (mixed phenotypes of small and large intestine) and initial titer measurements using qRT-PCR that measures all RNA vs. plaque assays that measure infectious virus.

APA, Harvard, Vancouver, ISO, and other styles

48

Ou, Kepeng, Youjian Li, Yiling Long, Yafei Luo, Dianyong Tang, and Zhongzhu Chen. "Inhibition of MORC2 Mediates HDAC4 to Promote Cellular Senescence through p53/p21 Signaling Axis." Molecules 27, no. 19 (September 22, 2022): 6247. http://dx.doi.org/10.3390/molecules27196247.

Full text

Abstract:

(1) Background: Colorectal cancer (CRC) is a common gastrointestinal malignancy, accounting for the second largest gastrointestinal tumor. MORC2, a newly discovered chromatin remodeling protein, plays an important role in the biological processes of various cancers. However, the potential mechanistic role of MORC2 in promoting proliferation of CRC carcinoma remains unclear. (2) Methods: The Cancer Genome Atlas database was analyzed using bioinformatics to obtain gene expression and clinical prognosis data. The cell proliferation was assessed by CCK8 and EdU assays, as well as xenograft. SA-beta-gal staining, Western blot, and ELISA assay were using to assess the cell senescence and potential mechanism. (3) Results: Our data showed that MORC2 expression was elevated in CRC patients. Depletion of MORC2 inhibited cellular proliferation both in vivo and in vitro. Further studies showed that the depletion of MORC2 enhanced p21 and p53 expression through decreasing HDAC4 and increasing pro-inflammatory factors IL-6 and IL-8, thus, promoting cellular senescence. (4) Conclusions: We concluded that increased MORC2 expression in CRC might play a critical role in tumorigenesis by regulating the cellular senescence, in addition, MORC2 could be a novel biomarker for clinical outcomes and prognosis and a treatment target for CRC.

APA, Harvard, Vancouver, ISO, and other styles

49

Fichi, Gianluca, Matteo Mattellini, Elisa Meloni, Guido Flamini, and Stefania Perrucci. "In vitro Anthelmintic Activity of Two Aloe-derived Active Principles against Sheep Gastrointestinal Nematodes." Natural Product Communications 12, no. 12 (December 2017): 1934578X1701201. http://dx.doi.org/10.1177/1934578x1701201221.

Full text

Abstract:

The in vitro anthelmintic activity on sheep gastrointestinal strongyle (GIS) eggs and larvae of 0.5% aloin and 0.1% aloe-emodin was investigated. From fresh faecal samples collected by ewes naturally infected by Haemonchus, Trichostrongylus and Teladorsagia nematodes, GIS eggs were isolated and cultivated in Petri dishes (100 eggs/dish). For the in vitro evaluation of the anthelmintic activity of tested compounds, the Egg hatch test (EHT), the Larval development test (LDT) and the Larval mortality/paralysis test (LMT) were used. In each assay, the activity of tested compounds was compared to untreated and treated (0.1% thiabendazole, TBZ) controls. Six repetitions were made through the experiment. Obtained data were statistically elaborated using the X2 test. In EHT, 0.5% aloin gave highly significantly different (P<0.01) results from the untreated controls. In LDT, both 0.1% aloe-emodin and 0.5% aloin almost completely prevented the larval development from L1 to L3, showing no significant differences (P<0.01) when compared to TBZ. In LMT, larval mortality observed in 0.5% aloin treated plates was significantly higher (P<0.01) than that observed in TBZ treated controls. These results show the in vitro anthelmintic properties on sheep GIS of the examined plant secondary metabolites. In LDT and/or LMT, the activity of 0.5% aloin and 0.1% aloe-emodin was comparable to or higher than that of the reference drug.

APA, Harvard, Vancouver, ISO, and other styles

50

Zaffaroni, Nadia, Rosella Silvestrini, Ornella Sanfilippo, Maria Grazia Daidone, Giorgio Bolis, and Patrizia Seminara. "Drug Sensitivity of Different Tumor Lesions from the Same Patient Evaluated by a Short-Term Assay." Tumori Journal 74, no. 2 (April 1988): 137–44. http://dx.doi.org/10.1177/030089168807400203.

Full text

Abstract:

A short-term antimetabolic assay, which considers the interference with [3H]thymidine incorporation as an indicator of drug effect, has been used to comparatively assess the chemosensitivity of different tumor lesions from the same patient. The analysis was performed on primary tumors and their synchronous metastases from 67 patients with breast, ovarian, gastrointestinal and germ cell testicular tumors. A remarkable difference in sensitivity to cytostatic drugs was observed between the two lesions. In contrast, a strong association in chemosensitivity (81.7% agreement rate; p < 0.01) was observed between two synchronous metastases from 17 patients with breast, ovarian, germ cell testicular tumors or malignant melanoma. In addition, the predictive relevance of the antimetabolic assay on clinical response to chemotherapy was analyzed in relation to the type of tumor lesion tested in vitro in a retrospective correlative study on 57 patients with advanced ovarian and germ cell testicular tumors. The objective clinical response was significantly correlated to the in vitro sensitivity of metastases (83.7% agreement rate; p < 0.01), but not to that of the primary tumor.

APA, Harvard, Vancouver, ISO, and other styles

Journal articles on the topic 'In vitro gastrointestinal assay'

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles