ent-Kauranoids isolated from Isodon eriocalyx var. laxiflora and their structure activity relationship analyses

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• 作者：Wei-Guang Wang^a ; ^&dagger ; ; Jin Yang^a ; ^b ; ^&dagger ; ; Hai-Yan Wu^a ; Ling-Mei Kong^a ; Jia Su^a ; Xiao-Nian Li^a ; Xue Du^a ; Rui Zhan^a ; Min Zhou^a ; Yan Li^a ; Jian-Xin Pu^a ; ^{pujianxin@mail.kib.ac.cn" class="auth_mail" title="E-mail the corresponding author} ; Han-Dong Sun^a
• 关键词：ent-Kaurane ; Diterpenoids ; Isodon
• 刊名：Tetrahedron
• 出版年：2015
• 出版时间：2 December 2015
• 年：2015
• 卷：71
• 期：48
• 页码：9161-9171
• 全文大小：1109 K

文摘

In this report, a new cytotoxic group, a 15-oxo-16伪-H-17-methoxy (or ethoxy)- unit, was suggested from the structure-activity relationship analyses of 39 ent-kaurane diterpenoids, including 17 new compounds (neolaxiflorins I–Y, 1–17) isolated from the leaves of Isodon eriocalyx var. laxiflora using an in vitro cytotoxicity assay against HL-60, SMMC-7721, A-549, MCF-7, and SW-480 human cancer cell lines. This discovery is counter to the rule that the 伪,尾-unsaturated ketone (C-15-C-16-C-17) unit is indispensable for cytotoxicity of the ent-kauranoids. Furthermore, portions of the isolates exhibited inhibitory activity against nitric oxide (NO) production in LPS-activated RAW264.7 macrophages. The NF-魏B inhibitory activity assay suggests a potential novel cytotoxic mechanism for compounds 9 and 22.