Itoigawa Masataka, Ito Chihiro, Tokuda Harukuni, Enjo Fumio, Nishino Hoyoku, Furukawa Hiroshi
Faculty of Pharmacy, Meijo University, Tempaku-ku, Nagoya 468-8503, Japan.
Cancer Lett. 2004 Oct 28;214(2):165-9. doi: 10.1016/j.canlet.2004.05.005.
In our joint project involving search of anti-tumor promoters from natural plant sources, six phenylpropanoids and seven phytoquinoids isolated from three Illicium plants (Illiciaceae) were tested for their inhibitory activities against Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate in Raji cells. All tested compounds showed inhibitory activity against the EBV-EA activation even at 1 x 10mol ratio, and the inhibitory activity of their compounds was found to be more than that of beta-carotene. Two phenylpropanoids having prenyl group, 4-allyl-2-methoxy-6-(3-methyl-2-butenyl)phenol (3) and 4-allyl-2,6-dimethoxy-3-(3-methyl-2-butenyl)phenol (4), showed more potent activities as anti-tumor promoters (IC50 224 and 217 mol ratio/TPA, respectively). The presence of a prenyl moiety in the phenylpropanoids plays an important role in anti-tumor promoting activity as xanthone, coumarin and flavonoid previously reported. This investigation indicated that prenylated phenylpropanoids might be valuable as potential cancer chemopreventive agents.
在我们从天然植物来源寻找抗肿瘤促进剂的联合项目中,对从三种八角属植物(八角科)中分离出的六种苯丙素类化合物和七种植物醌类化合物进行了测试,考察它们对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)激活的抑制活性。所有测试化合物即使在1×10⁻⁶mol比例下也显示出对EBV-EA激活的抑制活性,并且发现它们的抑制活性高于β-胡萝卜素。两种具有异戊烯基的苯丙素类化合物,4-烯丙基-2-甲氧基-6-(3-甲基-2-丁烯基)苯酚(3)和4-烯丙基-2,6-二甲氧基-3-(3-甲基-2-丁烯基)苯酚(4),作为抗肿瘤促进剂表现出更强的活性(IC50分别为224和217μmol比例/TPA)。如先前报道的呫吨酮、香豆素和黄酮类化合物一样,苯丙素类化合物中异戊烯基部分的存在在抗肿瘤促进活性中起重要作用。这项研究表明,异戊烯基化苯丙素类化合物作为潜在的癌症化学预防剂可能具有价值。