Gentidelasides A-G: Loganin derivatives from Gentiana delavayi with reducing Aβ secretion via suppressing BACE1 expression.

Autor: Guo HH; College of Pharmacy, Dali University, Dali, 671000, Yunnan Province, China., Li CX; College of Pharmacy, Dali University, Dali, 671000, Yunnan Province, China., Yang M; College of Pharmacy, Dali University, Dali, 671000, Yunnan Province, China., Li FF; College of Pharmacy, Dali University, Dali, 671000, Yunnan Province, China., Yang HY; College of Pharmacy, Dali University, Dali, 671000, Yunnan Province, China., Yin M; School of Pharmacy, Shanghai Jiao Tong University, Shanghai, 200240, China., Wang JP; Yunnan Provincial Key Laboratory of Entomological Biopharmaceutical R&D, College of Pharmacy, Dali University, Dali, 671000, Yunnan Province, China. Electronic address: jpwang@dali.edu.cn., Wang FS; College of Pharmacy, Dali University, Dali, 671000, Yunnan Province, China. Electronic address: wfsyn@163.com.
Jazyk: angličtina
Zdroj: Phytochemistry [Phytochemistry] 2025 Feb; Vol. 230, pp. 114333. Date of Electronic Publication: 2024 Nov 14.
DOI: 10.1016/j.phytochem.2024.114333
Abstrakt: Gentidelasides A-G (1-7) seven unreported loganin derivatives and fourteen known compounds (8-21) were isolated from the flowers of Gentiana delavayi Franch. Their structures including absolute configurations were unambiguously elucidated by analysis of extensive NMR spectroscopy, ECD, and HRESIMS, as well as enzymatic hydrolysis. In vitro bioassay, compound 7 showed obvious inhibitory effects on the production of Aβ40 and Aβ42, with IC 50 values of 0.052 ± 0.0023 nM and 1.52 ± 0.95 nM, respectively, which probably exert their prevention of Alzheimer's disease by inhibiting the expression of β-site amyloid precursor protein cleaving enzyme 1. The molecular docking simulation revealed that compound 7 inhibited BACE1 through hydrophilic and hydrophobic interactions in the active site cavities.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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