Pinostrobin attenuates azoxymethane-induced colorectal cytotoxicity in rats through augmentation of apoptotic Bax/Bcl-2 proteins and antioxidants

SAGE Open Medicine, Journal Year: 2023, Volume and Issue: 11

Published: Jan. 1, 2023

Pinostrobin (5-hydroxy-7-methoxyflavanone; PN) is a natural active ingredient with numerous biological activities extensively utilized in tumour chemotherapy. The present study investigates the chemo-preventive potentials of PN on azoxymethane-mediated colonic aberrant crypt foci rats.Sprague Dawley rats clustered into five groups, normal control (A) and cancer controls were subcutaneously injected saline 15 mg/kg azoxymethane, respectively, nourished 10% tween 20 fed 20; reference (C), azoxymethane (intraperitoneal) 35 5-fluorouracil (5-FU); D E rat groups received subcutaneous injection 30 60 PN, respectively.The acute toxicity trial showed lack any abnormal signs or mortality ingested 250 500 PN. gross morphology colon tissues revealed significantly lower total incidence PN-treated than that controls. Histological examination increased availability bizarrely elongated nuclei, stratified cells higher depletion submucosal glands treatment caused positive modulation apoptotic (Bax Bcl-2) proteins inflammatory cytokines (TNF-α, IL-6 IL-10). Moreover, had antioxidants (superoxide dismutase) malondialdehyde concentrations their tissue homogenates.The chemoprotective efficiency against azoxymethane-induced shown by values inhibition percentage, possibly through augmentation genes responsible for cascade inflammations originating from oxidative stress insults.

Language: Английский

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Mechanistic insight into the mode of inhibition of dietary flavonoids; targeting macrophage migration inhibitory factor

Frontiers in Molecular Biosciences, Journal Year: 2024, Volume and Issue: 11

Published: June 10, 2024

Introduction: The Macrophage Migration Inhibitory Factor (MIF), a key pro-inflammatory mediator, is responsible for modulating immune responses. An array of inflammatory and autoimmune diseases has been linked to the dysregulated activity MIF. significance in physiological as well pathophysiological phenomena underscores potential MIF an attractive target with pharmacological relevance. Extensive research past uncovered number inhibitors, while ISO-1, or (S, R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole acetic acid methyl ester being recognized benchmark standard so far. Recent work by Yang coworkers identified five promising dietary flavonoids, superior compared ISO-1. Nevertheless, exact atomic-level inhibitory mechanism still elusive. Methods: To improve dynamic research, rigorously characterize, compare molecular signatures complexes ISO-1 principal component analysis (PCA) was dynamics (MD) simulations binding free energy calculations. Results: results suggest that blocking tautomerase site these small molecule inhibitors could modify disrupting intrinsic particular functional areas. stability matrices revealed average deviation values ranging from 0.27–0.32 nm residue level fluctuations indicated selected flavonoids confer enhanced relative Furthermore, gyration extracted simulated trajectories were found range 1.80–1.83 nm. Discussion: Although all tested demonstrated remarkable results, one obtained potent particularly Morin Amentoflavone exhibited good correlation biological activity. PCA featured relatively less variance constricted conformational landscape than others. stable ensembles reduced variation turns might be possible reasons their outstanding performance documented previously. present exploration provide comprehensive understanding formed MIF, shedding light on roles impacts. Future studies may benefit knowledge gathered this investigation.

Language: Английский

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Cytotoxic Evaluation, Molecular Docking, Molecular Dynamics, and ADMET Prediction of Isolupalbigenin Isolated from Erythrina subumbrans (Hassk). Merr. (Fabaceae) Stem Bark: Unveiling Its Anticancer Efficacy

OncoTargets and Therapy, Journal Year: 2024, Volume and Issue: Volume 17, P. 829 - 840

Published: Oct. 1, 2024

, a medical plant found in sub-Saharan Africa and the Western Ghats of India, shows promise as potential source bioactive compounds to treat cancer. In our ongoing research on folk plants, we report isolation flavonoid compound from stem bark

Language: Английский

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Flavonoids and other constituents of plants from the genus Knema (Myristicaceae) and their pharmacological studies: An updated review

Vietnam Journal of Chemistry, Journal Year: 2023, Volume and Issue: 61(4), P. 397 - 411

Published: June 13, 2023

Abstract Flavonoids are a diverse group of natural compounds extensively studied in various research articles. They widely distributed the plant kingdom and exhibit biological activities, including antioxidant, anti‐inflammatory, anticancer, antiviral, antimicrobial effects. The genus Knema Lour., which contains many species Southeast Asia, has been traditionally used to treat ailments. current review aims provide comprehensive update on isolation flavonoids other secondary metabolites from Lour. between 1978 2022. It also discusses pharmacological studies these phytochemicals, their effects nematodes, bacteria, cytotoxicity, inflammation, acetylcholinesterase. Through years, 50 have reported demonstrating promising activities. information presented this can scientific foundation for future possible therapeutic applications species. links plants’ observed traditional uses chemical characterization. data was retrieved digital databases, ScienceDirect, Web Science, Scopus, Wiley, Taylor Francis, PubMed, Springer, Google Scholar.

Language: Английский

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New Phenolic Glycosides from Coelogyne fuscescens Lindl. var. brunnea and Their Cytotoxicity against Human Breast Cancer Cells

ACS Omega, Journal Year: 2024, Volume and Issue: unknown

Published: Feb. 9, 2024

The phytochemical investigation of the whole plants Coelogyne fuscescens Lindl. var. brunnea led to discovery three new phenolic glycosides, i.e., coelofusides A–C (1–3) and 12 known compounds (4–15). For first time, we reported nuclear magnetic resonance (NMR) data 4-O-(6′-O-glucosyl-4″-hydroxybenzoyl)-4-hydroxybenzyl alcohol (4) in this study. identification structures newly discovered was done through analysis their spectroscopic [NMR, mass spectrometry, ultraviolet, Fourier transform infrared, optical rotation, circular dichroism (CD)]. In comparison anticancer drugs (i.e., etoposide carboplatin), evaluated potential isolated on two different breast cancer cell lines, namely, T47D MDA-MB-231. Human fibroblast HaCaT cells were used as control cells. After a 48 h incubation, flavidin (8), coelonin (10), 3,4-dihydroxybenzaldehyde (11), oxoflavidin (12) showed significant cytotoxic effects against Among them, exhibited most potent cytotoxicity MDA-MB-231 with an IC50 value 26.26 ± 4.33 μM. staining assay, induced apoptosis after both dose-dependent manner. Furthermore, upregulated expression apoptotic genes, such p53, Bax, poly(ADP-ribose) polymerase, caspase-3, caspase-9 genes while significantly decreasing antiapoptotic protein (Bcl-2) levels.

Language: Английский

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