Konishi T, Takasaki M, Tokuda H, Kiyosawa S, Konoshima T
Kyoto Pharmaceutical University, Japan.
Biol Pharm Bull. 1998 Sep;21(9):993-6. doi: 10.1248/bpb.21.993.
To search for possible anti-tumor-promoters, we carried out the primary screening of seventeen diterpenes (1-17) isolated from the resinous wood of Excoecaria agallocha (Euphorbiaceae) using an in vitro synergistic assay system. Of these diterpenes, ent-16-hydroxy-3-oxo-13-epi-manoyloxide (5), (13R,14R)-ent-8alpha,13;14,15-diepoxy-13-epi- labda-3beta-ol (8) ent-3beta-hydroxy-15-beyeren-2-one (10) and ent-15-hydroxy-labda-8(17),13E-dien-3-one (14) exhibited significant inhibitory effects on Epstein-Barr virus (EBV) activation induced by the tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA). Furthermore, 10 exhibited remarkable anti-tumor-promoting activity in vivo on a two-stage carcinogenesis test of mouse tumor using 7,12-dimethylbenz[a]-anthracene (DMBA) as an initiator and TPA as a promoter.
为了寻找可能的抗肿瘤促进剂，我们使用体外协同检测系统对从海漆（大戟科）树脂木材中分离出的17种二萜（1-17）进行了初步筛选。在这些二萜中，对映-16-羟基-3-氧代-13-表-马尼氧化物（5）、（13R，14R）-对映-8α，13；14，15-二环氧-13-表-拉布达-3β-醇（8）、对映-3β-羟基-15-贝叶烯-2-酮（10）和对映-15-羟基-拉布达-8（17），13E-二烯-3-酮（14）对肿瘤促进剂12-O-十四烷酰佛波醇-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，在以7,12-二甲基苯并[a]蒽（DMBA）为引发剂、TPA为促进剂的小鼠肿瘤两阶段致癌试验中，10在体内表现出显著的抗肿瘤促进活性。
