Hai-Hui Guo , Chun-Xu Li , Min Yang , Feng-Feng Li , Hui-Yun Yang , Ming Yin , Jia-Peng Wang , Fu-Sheng Wang
{"title":"Gentidelasides A−G: Loganin derivatives from Gentiana delavayi with reducing Aβ secretion via suppressing BACE1 expression","authors":"Hai-Hui Guo , Chun-Xu Li , Min Yang , Feng-Feng Li , Hui-Yun Yang , Ming Yin , Jia-Peng Wang , Fu-Sheng Wang","doi":"10.1016/j.phytochem.2024.114333","DOIUrl":null,"url":null,"abstract":"<div><div>Gentidelasides A−G (<strong>1</strong>−<strong>7</strong>) seven unreported loganin derivatives and fourteen known compounds (<strong>8</strong>−<strong>21</strong>) were isolated from the flowers of <em>Gentiana delavayi</em> Franch. Their structures including absolute configurations were unambiguously elucidated by analysis of extensive NMR spectroscopy, ECD, and HRESIMS, as well as enzymatic hydrolysis. <em>In vitro</em> bioassay, compound <strong>7</strong> showed obvious inhibitory effects on the production of A<em>β</em>40 and A<em>β</em>42, with IC<sub>50</sub> 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 <em>β</em>-site amyloid precursor protein cleaving enzyme 1. The molecular docking simulation revealed that compound <strong>7</strong> inhibited BACE1 through hydrophilic and hydrophobic interactions in the active site cavities.</div></div>","PeriodicalId":20170,"journal":{"name":"Phytochemistry","volume":"230 ","pages":"Article 114333"},"PeriodicalIF":3.2000,"publicationDate":"2024-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Phytochemistry","FirstCategoryId":"99","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0031942224003704","RegionNum":2,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
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 IC50 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.
期刊介绍：
Phytochemistry is a leading international journal publishing studies of plant chemistry, biochemistry, molecular biology and genetics, structure and bioactivities of phytochemicals, including ''-omics'' and bioinformatics/computational biology approaches. Phytochemistry is a primary source for papers dealing with phytochemicals, especially reports concerning their biosynthesis, regulation, and biological properties both in planta and as bioactive principles. Articles are published online as soon as possible as Articles-in-Press and in 12 volumes per year. Occasional topic-focussed special issues are published composed of papers from invited authors.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
