三叶鱼藤中鱼藤酮类化合物的癌症化学预防活性。

Cancer chemopreventive activity of rotenoids from Derris trifoliata.

作者信息

Ito Chihiro, Itoigawa Masataka, Kojima Naoki, Tan Hugh T-W, Takayasu Junko, Tokuda Harukuni, Nishino Hoyoku, Furukawa Hiroshi

机构信息

Faculty of Pharmacy, Meijo University, Nagoya, Japan.

出版信息

Planta Med. 2004 Jan;70(1):8-11. doi: 10.1055/s-2004-815447.

DOI:10.1055/s-2004-815447

PMID:14765285

Abstract

A study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) led to the isolation and identification of one new rotenoid, 6aalpha,12aalpha-12a-hydroxyelliptone ( 3), together with five other known rotenoids. In a search for novel cancer chemopreventive agents (anti-tumor promoters), we carried out a primary screening of five of the rotenoids isolated from the plant for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12- O-tetradecanoylphorbol 13-acetate (TPA) in Raji cells. The inhibitory activity of 3 was found to be equivalent to that of beta-carotene without any cytotoxicity. Deguelin ( 4) and alpha-toxicarol ( 5) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. This investigation indicated that rotenoids might be valuable anti-tumor promoters.

摘要

对鱼藤（豆科）茎的化学成分进行研究，分离并鉴定出一种新的鱼藤酮类化合物，6aα,12aα - 12a - 羟基椭圆玫瑰树酮（3），以及其他五种已知的鱼藤酮类化合物。为了寻找新型癌症化学预防剂（抗肿瘤促进剂），我们对从该植物中分离出的五种鱼藤酮类化合物进行了初步筛选，以研究它们对12 - O - 十四烷酰佛波醇13 - 乙酸酯（TPA）诱导的Raji细胞中EB病毒早期抗原（EBV - EA）激活的抑制作用。发现化合物3的抑制活性与β - 胡萝卜素相当，且无任何细胞毒性。在体内两阶段致癌试验中，鱼藤素（4）和α - 毒卡罗酚（5）对小鼠皮肤肿瘤促进表现出显著的抑制作用。该研究表明，鱼藤酮类化合物可能是有价值的抗肿瘤促进剂。