Cancer chemopreventive agents (antitumor-promoters) from Ajuga decumbens.
Cancer chemopreventive agents (antitumor-promoters) from Ajuga decumbens.
复制标题
DOI：
10.1021/np990033w
复制
发表时间：
1999-05
影响因子：
5.1
通讯作者：
M. Takasaki;H. Tokuda;H. Nishino;T. Konoshima
中科院分区：
文献类型：
--
作者：
M. Takasaki;H. Tokuda;H. Nishino;T. Konoshima
从筋骨草（Ajuga decumbens）的开花全植物中分离的16个化合物（1-16）已经测试了它们对由肿瘤促进剂12-O-十四烷酰基佛波醇-13-乙酸酯（TPA）诱导的EB病毒早期抗原（EBV-EA）的抑制作用，作为抗肿瘤促进剂（潜在的癌症化学预防剂）的初步筛选测试。5个化合物（6、9和12-14）显示出对EBV-EA诱导的强抑制作用。在这些活性化合物中，该植物的两个主要成分，cyasterone（6）和8-acetylharpagide（13），在小鼠皮肤体内两阶段致癌过程中显示出有效的抗肿瘤促进活性，使用7，12-二甲基苯并[a]蒽作为引发剂和TPA作为促进剂。此外，化合物13在小鼠肺肿瘤模型中也表现出有效的化学预防活性。
Sixteen compounds (1-16) isolated from the flowering whole plant of Ajuga decumbens have been tested for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) induction by the tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA), as a primary screening test for antitumor-promoters (potential cancer chemopreventive agents). Five compounds (6, 9, and 12-14) showed strong inhibitory effects on EBV-EA induction. Of these active compounds, two major constituents of this plant, cyasterone (6) and 8-acetylharpagide (13), showed potent antitumor-promoting activities on a mouse-skin in vivo two-stage carcinogenesis procedure, using 7, 12-dimethylbenz[a]anthracene as initiator and TPA as promoter. Further, compound 13 also exhibited potent chemopreventive activity in a mouse pulmonary tumor model.