Novel diterpenoids with potent inhibitory activity against endothelium cell HMEC and cytotoxic activities from a well-known TCM plant Daphne genkwa
Novel diterpenoids with potent inhibitory activity against endothelium cell HMEC and cytotoxic activities from a well-known TCM plant Daphne genkwa
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DOI：
10.1016/j.bmc.2004.10.054
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发表时间：
2005-02-01
影响因子：
3.5
通讯作者：
Yue, HM
中科院分区：
文献类型：
--
作者：
Zhan, ZJ;Fan, CQ;Yue, HM
12个新的高氧瑞香烷型二萜类化合物Genkwanines A-L(1-12)，以及4个已知的二萜类化合物(13-16)。从著名中药材玄参的花蕾中分离得到3株。通过波谱方法，特别是二维核磁共振波谱(HMQC、HMBC、NOESY)对新结构进行了确证。对所有化合物1-16的抑制内皮细胞HMEC增殖活性和对两种肿瘤细胞株的细胞毒活性进行了评价，发现化合物1-16具有显著的结构相关性。化合物4、8、10、13和14中有5个化合物在2.90-15.0微米的IC50水平上对血管内皮细胞HMEC表现出较强的抑制活性。(C)2004爱思唯尔有限公司。保留所有权利。
Twelve highly oxygenated novel daphnane-type diterpenoids genkwanines A-L (1-12), together with four known diterpenes (13-16). were isolated from the bud of Daphne genkwa, a well-known traditional Chinese medicine (TCM). The new structures were elucidated on the basis of spectral methods, especially 2D NMR spectra (HMQC, HMBC, NOESY). Inhibitory activity against endothelium cell HMEC proliferation and cytotoxic activities against two tumor cell lines were assessed for all the compounds 1-16, and found to be significant and structure related. A number of compounds showed very potent cytotoxic activities against two tumor cell lines at the IC50 levels of 0.15-8.40 muM, and most interestingly five of the compounds 4, 8, 10, 13, and 14 exhibited strong activity to inhibit the endothelium cell HMEC at the IC50 levels of 2.90-15.0 muM. (C) 2004 Elsevier Ltd. All rights reserved.