皮肤肿瘤促进抑制剂的研究，十二。紫穗槐中的鱼藤酮类化合物。

Studies on inhibitors of skin tumor promotion, XII. Rotenoids from Amorpha fruticosa.

作者信息

Konoshima T, Terada H, Kokumai M, Kozuka M, Tokuda H, Estes J R, Li L, Wang H K, Lee K H

机构信息

Kyoto Pharmaceutical University, Japan.

出版信息

J Nat Prod. 1993 Jun;56(6):843-8. doi: 10.1021/np50096a006.

DOI:10.1021/np50096a006

PMID:8350086

Abstract

As a part of screening studies for chemopreventive agents (anti-tumor-promoters), six North American plants belonging to the Amorpha genus were tested using an in vitro assay system. Of these plants, Amorpha fruticosa exhibited strong inhibitory effects on Epstein-Barr virus early antigen (EBA-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA). Also six rotenoids, amorphispironone [1], tephrosin [2], amorphigenin [3], 12a-hydroxyamorphigenin [4], 12a-hydroxydalpanol [5], and 6'-O-D-glucopyranosyldalpanol [6], were isolated from the leaves of A. fruticosa. Among these retenoids, 1 and 2 exhibited remarkable inhibitory effects of EBV-EA activation induced by TPA. Further, 1 and 2 exhibited significant anti-tumor-promotion effects on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. These investigations suggested that these rotenoids might be valuable anti-tumor-promoters.

摘要

作为化学预防剂（抗肿瘤促进剂）筛选研究的一部分，使用体外检测系统对六种属于紫穗槐属的北美植物进行了测试。在这些植物中，紫穗槐对肿瘤促进剂十四酰佛波醇乙酸酯（TPA）诱导的爱泼斯坦-巴尔病毒早期抗原（EBA-EA）激活具有强烈的抑制作用。此外，还从紫穗槐的叶子中分离出了六种鱼藤酮类化合物，即紫穗槐螺酮[1]、灰叶素[2]、紫穗槐苷元[3]、12α-羟基紫穗槐苷元[4]、12α-羟基达普诺醇[5]和6'-O-D-吡喃葡萄糖基达普诺醇[6]。在这些鱼藤酮类化合物中，1和2对TPA诱导的EBV-EA激活表现出显著的抑制作用。此外，在体内两阶段致癌试验中，1和2对小鼠皮肤肿瘤促进表现出显著的抗肿瘤促进作用。这些研究表明，这些鱼藤酮类化合物可能是有价值的抗肿瘤促进剂。