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钩果草中的多聚异戊烯酰基间苯三酚类化合物作为去泛素化蛋白酶 USP7 的抑制剂。

Polyprenylated acylphloroglucinols as deubiquitinating protease USP7 inhibitors from Hypericum hookerianum.

机构信息

Department of Natural Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; School of Pharmacy, University of Chinese Academy of Sciences, Beijing 100049, China.

Institute of Hospital Management, West China Hospital, Sichuan University, Chengdu 610041, China.

出版信息

Fitoterapia. 2020 Oct;146:104678. doi: 10.1016/j.fitote.2020.104678. Epub 2020 Jun 25.

DOI:10.1016/j.fitote.2020.104678
PMID:32593692
Abstract

Hookerianones A - E (1-5), five new polyprenylated acylphloroglucinols (PPAPs), along with six known ones, were isolated from the aerial parts of Hypericum hookerianum. Their structures were elucidated by analyses of MS, NMR, chiroptical properties, biogenetic pathway, and/or single crystal X-ray diffraction. A ubiquitin-rhodamine 110 assay showed that furohyperforin and hypercalin C, two representative PPAPs in this plant, inhibited more than 90% USP7 at the concentration of 10 μM.

摘要

钩藤酮 A-E(1-5),五种新的多聚异戊烯基酰基间苯三酚(PPAPs),以及六种已知的 PPAPs,从贯叶连翘的地上部分分离得到。通过分析 MS、NMR、手性光学性质、生物合成途径和/或单晶 X 射线衍射,确定了它们的结构。泛素-罗丹明 110 测定表明,在 10 μM 的浓度下,该植物中两种代表性的 PPAPs,呋喃贯叶连翘素和高钙素 C,可抑制超过 90%的 USP7。

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