Development and synthesis of diffractaic acid analogs as potent inhibitors of colorectal cancer stem cell traits

Scientific Reports, Journal Year: 2025, Volume and Issue: 15(1)

Published: Feb. 25, 2025

In recent years, evidence for the anti-cancer activity of lichen secondary metabolites has been rapidly increasing. this study, we synthesised analogues diffractaic acid, a metabolite, and evaluated their ability to suppress colorectal cancer stem potential. Among 10 compounds after H/CH₃/benzylation acid structure or modifications in an aromatic hydrophobic domain, TU3 more inhibition effect on potential compared other compounds. The compound targets ALDH1 suppresses key signalling pathways such as WNT, STAT3, NF-κB, Hedgehog, AP-1. Inhibition these by contribute attenuate survival mechanisms cell thus inhibit progression.

Language: Английский

Screening of Chemical Profile by LC–MS/MS and Assessment of Biological Properties of Achillea sintenisii Hub. Mor. From Turkey

Chemistry & Biodiversity, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 26, 2025

ABSTRACT The aim of this study was to determine the secondary metabolites n ‐hexane, ethyl acetate, methanol, and water extracts Achillea sintenisii Hub. Mor. ascertain their divergent biological properties. LC–MS/MS analysis performed identify bioactive compounds. anticancer properties samples were tested against human breast (MCF‐7 MDA‐MB‐453) colon (HT‐29) cancer cell lines by XTT assay. anti‐Alzheimer's studies using Ellman's antimicrobial carried out Kirby–Bauer disc diffusion method. antioxidative potential evaluated on basis 2,2‐diphenyl‐1‐picrylhydrazyl scavenging ferric reducing antioxidant power assays, revealed 27 phytochemicals, including high concentrations quinic acid, gentisic chlorogenic luteolin, cynaroside, caffeic acid. Ethyl acetate extract exhibited most potent cytoxicity MDA‐MB‐453 cells, with an IC 50 value 83.05 µg/mL. All showed stronger inhibitory activity acetylcholinesterase butyrylcholinesterase compared tacrine. methanol considerable Enterococcus faecalis , approaching level vancomycin. Methanol possessed highest DPPH power. These findings render A, a promising source for pharmaceutical, cosmetic, food industries.

Language: Английский

5-methyl-N'-(thiophen-2-ylmethylene)-1H-pyrazole-3-carbohydrazide as potent anticancer agent: Synthesis, spectroscopic characterization, anticancer activity and DFT studies

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: unknown, P. 140919 - 140919

Published: Nov. 1, 2024

Language: Английский