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来自石榴 Cedronia granatensis 的细胞毒性苦木素类化合物。

Cytotoxic quassinoids from Cedronia granatensis.

作者信息

Tischler M, Cardellina J H, Boyd M R, Cragg G M

机构信息

Laboratory of Drug Discovery Research and Development, National Cancer Institute, Frederick, Maryland 21702-1201.

出版信息

J Nat Prod. 1992 May;55(5):667-71. doi: 10.1021/np50083a018.

Abstract

The NCI in vitro primary disease-oriented antitumor screen has been used to select and guide the fractionation of the organic and aqueous extracts of Cedronia granatensis. Two quassinoids, sergiolide [1] and isobrucein B [2], to which the screening panel cell lines exhibited up to a 1000-fold range of differential sensitivity, were isolated. At concentrations of 10(-5)-10(-8) M, the compounds typically produced LC50-level responses against a majority of the melanoma lines and several of the colon, lung, and other solid tumor lines. These and related quassinoids may, therefore, be of interest for in vivo evaluation in appropriate xenograft tumor models.

摘要

美国国立癌症研究所(NCI)的体外原发性疾病导向性抗肿瘤筛选已被用于选择和指导石榴(Cedronia granatensis)有机提取物和水提取物的分级分离。分离出了两种苦木素类化合物,即蛇床子素[1]和异布鲁斯因B[2],筛选小组的细胞系对这两种化合物表现出高达1000倍的差异敏感性。在10^(-5)-10^(-8) M的浓度下,这些化合物通常对大多数黑色素瘤细胞系以及一些结肠、肺癌和其他实体瘤细胞系产生半数致死浓度(LC50)水平的反应。因此,这些以及相关的苦木素类化合物可能在合适的异种移植肿瘤模型中进行体内评估时具有研究价值。

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