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Bicyclic polyprenylated acylphloroglucinol-related meroterpenoids as potent DRAK2 inhibitors from Hypericum patulum

文献类型：期刊论文

作者Huang, Jin-Chang6; Jia, Xin-Yu5; Lv, Yi-Fan6; Xu, Hong-Hong4; Han, Ming4; Yu, Qiang-Qiang6; Lu, Yu-Ting4; Yang, Hong-Xun3; Yang, Yang1,2,4; Li, Jing-Ya1,2,4
刊名PHYTOCHEMISTRY
出版日期2025-04-01
卷号232页码:10
关键词Hypericum patulum Hypericaceae Meroterpenoids Hyperpatins A-H Death-associated protein kinase-related apoptosis-inducing kinase 2 Glucose-stimulated insulin secretion
ISSN号0031-9422
DOI10.1016/j.phytochem.2024.114375
英文摘要As a both edible and medicinal plant, Hypericum patulum (Hypericaceae) is used as a natural herbal tea, scented tea, and folk medicine. In this study, eight undescribed bicyclic polyprenylated acylphloroglucinol-related meroterpenoids named hyperpatins A-H, along with eight known ones, were isolated from this plant. Their structures were elucidated on the basis of spectroscopic techniques, chemical method, X-ray crystallographic experiments, and electronic circular dichroism analyses. Hyperpatins A-H possess a characteristic pyran ring system diversely fused with the bicyclo[3.3.1]nonane-2,4,9-trione core, and hyperpatins C and D incorporate a unique alpha,beta-unsaturated aldehyde moiety. Some of the isolates exhibited potent inhibitory effects on death-associated protein kinase-related apoptosis-inducing kinase 2 with IC50 values ranging from 2.60 +/- 0.29 to 17.93 +/- 3.08 mu M. This is the first report of DRAK2 inhibitory activity for acylphloroglucinol-related meroterpenoids. The most active molecule hyperpatins C showed binding affinity with DRAK2 by hydrogen-bond and hydrophobic interactions in molecular docking and promoted the glucose-stimulated insulin secretion ability of primary islets.
WOS关键词ABSOLUTE-CONFIGURATION ; DERIVATIVES ; HYPERFORIN ; DISCOVERY ; APOPTOSIS ; 1,2-DIOLS ; ANALOGS
资助项目National Natural Science Foundation of China, China[82425058] ; National Natural Science Foundation of China, China[82200885] ; National Natural Science Foundation of China, China[82470835] ; Shanghai Frontiers Science Center of Drug Target Identification and Delivery, China ; Shanghai Jiao Tong University ; Shanghai Rising-Star Program[24QA2701700] ; [22277074]
WOS研究方向Biochemistry & Molecular Biology ; Plant Sciences
语种英语
WOS记录号WOS:001404577800001
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/315932]  
专题新药研究国家重点实验室
通讯作者Li, Jing-Ya; Hou, Ai-Jun
作者单位1.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Sinopharm Chem Reagent Co Ltd, Shanghai 200002, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China
5.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China
6.Shanghai Jiao Tong Univ, Shanghai Frontiers Sci Ctr Drug Target Identificat, Sch Pharmaceut Sci, Shanghai 200240, Peoples R China
推荐引用方式
GB/T 7714		 Huang, Jin-Chang,Jia, Xin-Yu,Lv, Yi-Fan,et al. Bicyclic polyprenylated acylphloroglucinol-related meroterpenoids as potent DRAK2 inhibitors from Hypericum patulum[J]. PHYTOCHEMISTRY,2025,232:10.
APA Huang, Jin-Chang.,Jia, Xin-Yu.,Lv, Yi-Fan.,Xu, Hong-Hong.,Han, Ming.,...&Hou, Ai-Jun.(2025).Bicyclic polyprenylated acylphloroglucinol-related meroterpenoids as potent DRAK2 inhibitors from Hypericum patulum.PHYTOCHEMISTRY,232,10.
MLA Huang, Jin-Chang,et al."Bicyclic polyprenylated acylphloroglucinol-related meroterpenoids as potent DRAK2 inhibitors from Hypericum patulum".PHYTOCHEMISTRY 232(2025):10.

入库方式： OAI收割

来源：上海药物研究所

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