Takasaki M, Konoshima T, Kozuka M, Tokuda H
Kyoto Pharmaceutical University, Japan.
Biol Pharm Bull. 1995 Mar;18(3):435-8. doi: 10.1248/bpb.18.435.
To search for possible anti-tumor-promoters (chemopreventive agents), we carried out a primary screening of 21 euglobals (acylphloroglucinol-monoterpene or -sesquiterpene structures) isolated from the juvenile leaves of five species of Eucalyptus plants using an in vitro synergistic assay system. Of these compounds, euglobal-G1--G5 (1-5), -Am-2 (15) and -III (16) exhibited significant inhibitory effects on Epstein-Barr virus (EBV) activation induced by the tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA). Furthermore, the effects of compounds 1 and 16 on the cell cycle of Raji cells were also examined by a flow cytometer, and both compounds 1 and 16 exhibited strong inhibition on the effect of the cell cycle induced by TPA. These two euglobals (1 and 16) exhibited remarkable anti-tumor-promoting effects on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test.
为了寻找可能的抗肿瘤促进剂（化学预防剂），我们使用体外协同测定系统对从五种桉树植物的幼叶中分离出的21种真球蛋白（酰基间苯三酚 - 单萜或 - 倍半萜结构）进行了初步筛选。在这些化合物中，真球蛋白 -G1--G5（1 - 5）、-Am-2（15）和 -III（16）对肿瘤促进剂12 - O - 十四酰佛波醇 - 13 - 乙酸酯（TPA）诱导的爱泼斯坦 - 巴尔病毒（EBV）激活表现出显著的抑制作用。此外，还通过流式细胞仪检测了化合物1和16对Raji细胞周期的影响，化合物1和16均对TPA诱导的细胞周期效应表现出强烈抑制作用。在体内两阶段致癌试验中，这两种真球蛋白（1和16）对小鼠皮肤肿瘤促进表现出显著的抗肿瘤促进作用。
