Bioassay-guided isolation of cytotoxic constituents from the flowers of Aquilaria sinensis
作者机构：Key Laboratory of Economic Plants and Biotechnology and Yunnan Key Laboratory for Wild Plant ResourcesKunming Institute of BotanyChinese Academy of SciencesKunming 650201People’s Republic of China School of Chemical Biology and EnvironmentYuxi Normal UniversityYuxi 653100People’s Republic of China College of ScienceYunnan Agricultural UniversityKunming 650201People’s Republic of China
出 版 物：《Natural Products and Bioprospecting》 (应用天然产物（英文）)
年 卷 期：2022年第12卷第1期
页 面：128-136页
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：Funding was provided by Beijing Sino-Science Aquilaria Technology Co. Ltd. Beijing China (Grant No.KET202101)
主 题：Thymelaeaceae Aquilaria sinensis Paclitaxel-resistant lung cancer cells Cucurbitane-type triterpenoids
摘 要：Bioassay-guided fractionation of the EtOH extract from the flowers of Aquilaria sinensis(Lour.)Spreng.(Thyme-laeaceae)led to the isolation of a new cucurbitane-type triterpenoid,aquilarolide A(1),along with five known compounds(2-6).The structure of 1 was elucidated by extensive 1D and 2D nuclear magnetic resonance(NMR)experiments and mass spectrometry(MS)data and theoretical calculations of its electronic circular dichroism(ECD)*** A,cucurbitacin E(3),cucurbitacin B(4),and 7-hydroxy-6-methoxy-2-[2-(4-methoxyphenyl)ethyl]-4H-1-benzopyran-4-one(6)showed significant cytotoxicity against human lung adenocarcinoma SPC-A-1,human lung squamous cell carcinoma NCI-H520,human lung adenocarcinoma A549,and paclitaxel-resistant A549(A549/Taxol)cell *** four active compounds,with IC_(50) values ranging from 0.002 to 0.91μM,had better inhibitory activities against A549/Taxol cells than paclitaxel(IC_(50)=1.80μM).Among them,cucurbitacin E(IC_(50)=0.002μM)is the most *** studies are needed to evaluate their in vivo antitumor activities and to clarify their mechanisms.
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