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Discovery of 1,3-disubstituted prop-2-en-1-one derivatives as inhibitors of neutrophilic inflammation via modulation of MAPK and Akt pathways.
J Enzyme Inhib Med Chem
December 2024
Graduate Institute of Natural Products, College of Medicine, Chang Gung University, Taoyuan, Taiwan.
Targeting neutrophil function has gained attention as a propitious therapeutic strategy for diverse inflammatory diseases. Accordingly, a series of enone-based derivatives were developed to inhibit neutrophil-mediated inflammation, showing promise for treating inflammatory diseases. These compounds fall into two clusters with distinct effects: one inhibits neutrophilic superoxide (SO) anion production and elastase release triggered by N-formyl-Met-Leu-Phe (fMLF), with compound being most effective (IC values of 1.
View Article and Find Full Text PDFHericium VN, an undescribed compound isolated from and its cytotoxic activity on human brain astrocytoma.
J Asian Nat Prod Res
July 2024
Institute of Marine Biochemistry, VAST, Cau Giay, Hanoi, Vietnam.
is a species of mushroom with high nutritional value that is used mainly as food in tropical countries. Phytochemical study of led to the isolation of an undescribed compound, named as hericium VN (), together with nine known compounds, 1-(2-formyl-1-pyrrolyl)butanoic acid (), herierin III (), 5'-(methylthio)adenosine (), adenosine (), nicotinic acid (), (22,24)-5,8-epidioxyergosta-6,9(11),22-trien-3-ol (), 5,8-peroxycerevisterol (), (22,24)-5,8-epidioxy-egosta-6,22-diene 3---D-glucopyranoside (), and cerevisterol () based on extensive analyses of HR-ESI-MS, 1D and 2D NMR spectra. The absolute configuration of compound was determined by experimental combined with calculated electronic circular dichroism spectra.
View Article and Find Full Text PDF[A new benzopyran glycoside from Gentiana macrophylla].
Zhongguo Zhong Yao Za Zhi
January 2024
School of Biotechnology and Health Sciences, Wuyi University Jiangmen 529020, China Institute of Modern Chinese Medicine, College of Pharmaceutical Sciences, Zhejiang University Hangzhou 310058, China.
Thirteen compounds were isolated and identified from 70% ethanol extract of the roots of Gentiana macrophylla by multi-chromatographic methods, including microporous resin, silica gel, and C_(18) reversed-phase column chromatography, as well as HPLC as follows: macrophylloside G(1), macrophylloside D(2), 5-formyl-2,3-dihydroisocoumarin(3),(+)-medicarpin(4),(+)-syringaresinol(5), liquiritigenin(6),(3R)-sativanone(7),(3R)-3'-O-methylviolanone(8), 4,2',4'-trihydroxychalcone(9), latifolin(10), gentioxepine(11), 6α-hydroxycyclonerolidol(12), and ethyl linoleate(13). Compound 1 was a new benzopyran glycoside. Compounds 4, 6-10, 12, and 13 were isolated for the first time from Gentiana plants.
View Article and Find Full Text PDFOxygen-18 Labeling Reveals a Mixed Fe-O Mechanism in the Last Step of Cytochrome P450 51 Sterol 14α-Demethylation.
Angew Chem Int Ed Engl
February 2024
Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232-0146, USA.
The 14α-demethylation step is critical in eukaryotic sterol biosynthesis, catalyzed by cytochrome P450 (P450) Family 51 enzymes, for example, with lanosterol in mammals. This conserved three-step reaction terminates in a C-C cleavage step that generates formic acid, the nature of which has been controversial. Proposed mechanisms involve roles of P450 Compound 0 (ferric peroxide anion, FeO ) or Compound I (perferryl oxygen, FeO ) reacting with either the aldehyde or its hydrate, respectively.
View Article and Find Full Text PDFAnti-Trypanosomal Bufadienolides from the Oocytes of the Toad (Anura, Bufonidae).
Molecules
December 2023
Centro de Biodiversidad y Descubrimiento de Drogas, Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (INDICASAT-AIP), Panamá 0843-01103, Panama.
Amphibians are widely known as a prolific source of bioactive metabolites. In this work, we isolated and characterized compounds with antiparasitic activity from the oocytes of the toad collected in Panama. Bio-guided isolation and structural elucidation were carried out using chromatographic and spectroscopic techniques, respectively.
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