Okano M, Fukamiya N, Tagahara K, Tokuda H, Iwashima A, Nishino H, Lee K H
Department of Interdisciplinary Studies on Natural Environment, Faculty of Integrated Arts and Sciences, Hiroshima University, Japan.
Cancer Lett. 1995 Aug 1;94(2):139-46. doi: 10.1016/0304-3835(95)03839-o.
Short-term in vitro assays for tumor promoters and anti-tumor promoters (Epstein-Barr virus activation test) were carried out for 45 quassinoids. As a result, some quassinoids showed potent activity, more than 50% inhibition at a molar ratio of 1:1 (TPA/quassinoids). These results led to the following structure-activity relationships: (1) a methyleneoxy bridge and side chain enhance the activity and (2) a sugar moiety reduces the activity.
对45种苦木素类化合物进行了肿瘤启动子和抗肿瘤启动子的短期体外测定(爱泼斯坦-巴尔病毒激活试验)。结果显示,一些苦木素类化合物表现出较强的活性,在摩尔比为1:1(TPA/苦木素类化合物)时抑制率超过50%。这些结果得出了以下构效关系:(1)亚甲氧基桥和侧链增强活性;(2)糖部分降低活性。