Highly Oxygenated Dimeric Grayanane Diterpenoids as Analgesics:TRPV1 and TRPA1 Dual Antagonists from Rhododendron molle
作者机构：Hubei Key Laboratory of Natural Medicinal Chemistry and Resource EvaluationSchool of PharmacyTongji Medical CollegeHuazhong University of Science and TechnologyWuhanHubei430030 China State Key Laboratory of Phytochemistry and Plant Resources in West ChinaKunming Institute of BotanyChinese Academy of SciencesKunmingYunnan650201 China Laboratory of Xinjiang Native Medicinal and Edible Plant Resource ChemistryCollege of Chemistry and Environmental ScienceKashi UniversityKashgarXinjiang844007 China
出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)
年 卷 期：2022年第40卷第19期
页 面：2285-2295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：This work was supported by the Fund of State Key Laboratory of Phytochemistry and Plant Resources in West China(P2022-KF08) the Fund of Laboratory of Xinjiang Native Medicinal and Edible Plant Resource Chemistry(KSUZDSYS202101) the National Natural Science Foundation of China(22107033 and U1703109) the Traditional Chinese Medicine of Hubei Provincial Health Commission(ZY2021M056) the China Postdoctoral Science Foundation(2021M691152)
主 题：Biological activity Dimeric grayanane diterpenoids Natural products Rhododendron molle(Ericaceae) Structure elucidation
摘 要：Six highly oxygenated dimeric grayanane diterpenoids(1—6)including three new ones,bismollethers A—C(1—3),were isolated from the flowers of Rhododendron molle collected at Qichun,Hubei,*** structures and relative configurations of 1—6 were determined by comprehensive spectroscopic data analysis and 13C NMR calculation with DP4+*** absolute configurations of bismollethers A—C(1—3)and birhodomollein B(5)were indubitably assigned by single-crystal X-ray diffraction analysis,revealing the head-to-tail linking manner of diterpenoid *** A(1)is a caged dimeric grayanane diterpenoid linked through two oxygen-bridges of C-2−O−C-14′and C-14−O−C-2′,featuring a unique 1,8-dioxacyclotetradecane *** plausible biosynthesis pathways of 1—6 are *** the isolates displayed significant analgesic activities and their structure-activity relationships were *** diterpenoid dimers were found to be TRPV1 and TRPA1 dual antagonists,and docking studies provide a structural basis to design potent analgesics.
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