Hypermonones A-I,New Polyprenylated Acylphloroglucinols from Hypericum monogynum with Multidrug Resistance Reversal Activity
作者机构:State Key Laboratory of Functions and Applications of Medicinal PlantsGuizhou Medical UniversityGuiyangGuizhou 550014China The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of SciencesGuiyangGuizhou 550014China State Key Laboratory of Phytochemistry and Plant Resources in West ChinaKunming Institute of BotanyChinese Academy of SciencesKunmingYunnan 650201China
出 版 物:《Chinese Journal of Chemistry》 (中国化学(英文版))
年 卷 期:2021年第39卷第9期
页 面:2422-2432页
核心收录:
学科分类:081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学]
基 金:supported by the National Natural Science Foundation of China(Nos.U1812403,81872772,and 81960546) the Scie nee and Tech no logy Departme nt of Guizhou Province(Nos.QKH 2020-1Z076,QKHZC4Y203z QKHJC1409,QKHZC2762,and QKHPTRC5008) the High-level Innovative Talents in Guizhou Provinee(Thousand Levels of Talent for Chunmao Yuan in 2018) the"Light of the West"Talent Cultivation Program of Chinese Academy of Sciences for Chunmao Yuan(No.RZ82) the 100 Leading Talents of Guizhou Provinee(fund for Y.M.L) the Guizhou Provincial Engineering Research Center for Natural Drugs
主 题:Hypericum monogynum Phytochemistry Structure elucidation Biological activity Multidrug resistance reversal activity
摘 要:Eleven biogenetically related polyprenylated acylphloroglucinols(PPAPs),including four novel skeletons(1-4)and five new com-pounds(5-9),were isolated from the flowers of Hypericum *** A-D(1-4)represented the first example of a unique dilactone structure containing carbonyl bonded single 5-lactone and tricyclic γ-lactone *** structures were elucidated by NMR analysis,X-ray crystallography,and ECD ***,we revised the structure of hyperibrin B to hy perm on one I(9)via NMR an alysis,a qua ntum computational chemistry method,and hypothetic bios yn thetic con *** compounds(5,6,and 9)with significant MDR reversal activity(RF ranging from 61 to 223)were superior to the positive control verapamil(MCF-7/ADR,RF:53;HepG2/ADRz RF:124).Mechanism study for compound 5 indicated that this compound could inhibit the function of P-gp tran sport rather tha n its expressi on,and the possible recog nition mechanism betwee n compo und 5 and P-gp was predicted by molecular docking.