来自巴豆和钩腺巴豆的细胞毒性3,4-裂环乌苏烷二萜类化合物。

Cytotoxic 3,4-seco-Atisane Diterpenoids from Croton barorum and Croton goudotii.

作者信息

Rakotonandrasana Olga L, Raharinjato Fanja H, Rajaonarivelo Mialy, Dumontet Vincent, Martin Marie-Thérèse, Bignon Jérôme, Rasoanaivo Philippe

机构信息

Laboratoire de Biothérapeutique, Institut Malgache des Recherches Appliquées, BP 3833, 101 Antananarivo, Madagascar.

出版信息

J Nat Prod. 2010 Oct 22;73(10):1730-3. doi: 10.1021/np1005086. Epub 2010 Sep 17.

DOI:10.1021/np1005086

PMID:20849074

Abstract

In a screening program directed to the discovery of new anticancer agents from Madagascan plants, ethyl acetate extracts of Croton barorum and C. goudotii showed strong cytotoxic activity, with 100% inhibition at 10 μg/mL in a primary screen using the murine lymphocytic leukemia P388 cell line. Bioassay-guided fractionation led to the isolation of two new 3,4-seco-atisane diterpenoids, crotobarin (1) and crotogoudin (2). Their structures were elucidated by spectroscopic data interpretation. Compounds 1 and 2 produced a net progression in the number of cells arrested at the G2/M growth stage in the cell cycle of the K562 human leukemia cell line at 4 μM.

摘要

在一项旨在从马达加斯加植物中发现新型抗癌药物的筛选计划中，巴鲁巴豆（Croton barorum）和古氏巴豆（C. goudotii）的乙酸乙酯提取物表现出很强的细胞毒性活性，在使用小鼠淋巴细胞白血病P388细胞系进行的初步筛选中，在10μg/mL时抑制率达100%。生物测定导向的分级分离导致分离出两种新的3,4-裂贝壳杉烷二萜，巴豆巴林（1）和古氏巴豆素（2）。通过光谱数据解释阐明了它们的结构。化合物1和2在4μM时使K562人白血病细胞系细胞周期中停滞在G2/M生长阶段的细胞数量出现净增加。