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狼毒大戟中的瑞香烷型二萜类化合物及其细胞毒性活性。

Daphnane-type diterpenoids from Euphorbia fischeriana Steud and their cytotoxic activities.

作者信息

Xie Rihan, Xia Guiyang, Zhu Jianxun, Lin Pengcheng, Fan Xiaona, Zi Jiachen

机构信息

College of Pharmacy, Jinan University, Guangzhou 510632, People's Republic of China.

Key Laboratory of Chinese Internal Medicine of Ministry of Education and Beijing, Dongzhimen Hospital, Beijing University of Chinese Medicine, Beijing 100700, People's Republic of China.

出版信息

Fitoterapia. 2021 Mar;149:104810. doi: 10.1016/j.fitote.2020.104810. Epub 2020 Dec 23.

Abstract

Two new daphnane-type diterpenoids fischerianin A (1) and fischerianin B (2), as well as two known ones langduin A (3) and langduin A (4), were isolated from the extracts of Euphorbia fischeriana Steud dry roots. Their structures including the absolute stereochemistry were determined by various spectroscopic methods and comparing their experimental and calculated CD spectra. 1 and 2 harbor a ketal group and a 9,13-oxide bridge in their C ring which is rare in daphnane-type diterpenoids. In cytotoxic assays, moderately inhibitory activities of 1-4 against human cancer cell lines (human malignant melanoma cell line, A375; human liver carcinoma cell line, HepG2; human promyelocytic leukemia cell line, HL-60; human Caucasian chronic myelogenous leukemia cell line, K562; human cervix epithelioid carcinoma cell line, HeLa) were observed, with IC values ranging from 5.31 to 21.46 μM.

摘要

从狼毒大戟干燥根的提取物中分离出两种新的瑞香烷型二萜化合物狼毒大戟素A(1)和狼毒大戟素B(2),以及两种已知化合物狼毒亭A(3)和狼毒亭A(4)。通过各种光谱方法并比较其实验和计算的圆二色光谱确定了它们的结构,包括绝对立体化学。1和2在其C环中含有一个缩酮基团和一个9,13-氧化物桥,这在瑞香烷型二萜化合物中很少见。在细胞毒性试验中,观察到1-4对人癌细胞系(人恶性黑色素瘤细胞系A375、人肝癌细胞系HepG2、人早幼粒细胞白血病细胞系HL-60、人高加索慢性粒细胞白血病细胞系K562、人宫颈上皮样癌细胞系HeLa)具有中等抑制活性,IC值范围为5.31至21.46μM。

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