Ito C, Itoigawa M, Furukawa H, Ichiishi E, Mukainaka T, Okuda M, Ogata M, Tokuda H, Nishino H
Faculty of Pharmacy, Meijo University, Tempaku, Nagoya, Japan.
Cancer Lett. 1999 Jul 19;142(1):49-54. doi: 10.1016/s0304-3835(99)00147-0.
In our joint project in the search for anti-tumor promoters from natural plant sources, we carried out a primary screening of 12 phenylpropanoids isolated from Boronia pinnata Sm. (Rutaceae) by examining their possible inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate in Raji cells. All tested compounds in this study showed inhibitory activity against the EBV activation even at 1 x 10 mol ratio without any cytotoxicity. Among 12 phenylpropanoids tested, boropinal-C (1), boropinol-A (5), boropinol-C (9) and 3-(3'-methoxy-4'-prenyloxy)phenyl-1-propene (10), all having a 4'-(3-methylbut-2-enyloxy) group, a so-called prenyloxy group, showed more potent activities. Furthermore, 3-(3'-methoxy-4'-prenyloxy)phenyl-1-propene (10) also exhibited remarkable inhibitory effects on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. This investigation indicated that certain phenylpropanoids might be valuable anti-tumor promoters.
在我们从天然植物来源寻找抗肿瘤促效剂的联合项目中，我们对从羽叶硼属植物（芸香科）中分离出的12种苯丙素类化合物进行了初步筛选，通过检测它们对12 - O - 十四酰佛波醇 - 13 - 乙酸酯在Raji细胞中诱导的爱泼斯坦 - 巴尔病毒早期抗原（EBV - EA）激活的可能抑制作用。本研究中所有测试化合物即使在1×10摩尔比时也显示出对EBV激活的抑制活性，且无任何细胞毒性。在测试的12种苯丙素类化合物中，硼皮纳醇 - C（1）、硼皮诺醇 - A（5）、硼皮诺醇 - C（9）和3 -（3'-甲氧基 - 4'-异戊烯氧基）苯基 - 1 - 丙烯（10），均含有一个4' -（3 - 甲基丁 - 2 - 烯氧基）基团，即所谓的异戊烯氧基，显示出更强的活性。此外，3 -（3'-甲氧基 - 4'-异戊烯氧基）苯基 - 1 - 丙烯（10）在体内两阶段致癌试验中也对小鼠皮肤肿瘤促进表现出显著的抑制作用。这项研究表明某些苯丙素类化合物可能是有价值的抗肿瘤促效剂。
