Konoshima T, Takasaki M, Tokuda H, Nishino H
Kyoto Pharmaceutical University, Yamashina-ku, Japan.
Cancer Lett. 2000 Aug 31;157(1):87-92. doi: 10.1016/s0304-3835(00)00479-1.
In the course of our continuing search for novel cancer chemopreventive agents from natural sources, several kinds of Labiatae plants were screened. Consequently, the iridoid glycoside derivative, 8-acetylharpagide (8-AcHarp), was obtained from the flowering whole plant of Ajuga decumbens as an active constituent. This glycoside exhibited the remarkable inhibitory effect on two-stage carcinogenesis test of mouse skin tumors induced by nitric oxide (NO) donor, (+/-)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexen eamide (NOR 1) as an initiator and 12-O-tetradecanoylphorbol-13-acetate (TPA) as a promoter. Further, 8-AcHarp exhibited potent anti-tumor-promoting activity on two-stage carcinogenesis test of mouse hepatic tumor using N-nitrosodiethylamine (DEN) as an initiator and phenobarbital (PB) as a promoter.
在我们持续从天然来源寻找新型癌症化学预防剂的过程中，对几种唇形科植物进行了筛选。结果，从平卧筋骨草的开花全株中获得了环烯醚萜苷衍生物8-乙酰哈帕苷（8-AcHarp）作为活性成分。该苷对一氧化氮（NO）供体（±）-（E）-甲基-2-[(E)-羟基亚氨基]-5-硝基-6-甲氧基-3-己烯酰胺（NOR 1）作为引发剂、12-O-十四酰佛波醇-13-乙酸酯（TPA）作为促癌剂诱导的小鼠皮肤肿瘤的两阶段致癌试验表现出显著的抑制作用。此外，8-AcHarp对以N-亚硝基二乙胺（DEN）作为引发剂、苯巴比妥（PB）作为促癌剂的小鼠肝癌两阶段致癌试验表现出强大的抗肿瘤促进活性。
