Fukuda Yuko, Sakai Kuniyoshi, Matsunaga Shunyo, Tokuda Harukuni, Tanaka Reiko
Department of Medicinal Chemistry, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
Chem Biodivers. 2005 Mar;2(3):421-8. doi: 10.1002/cbdv.200590021.
In a search for cancer chemopreventive agents from natural sources, four lupane-type and seven oleanane-type triterpenoids, and ten synthetic analogs were screened as potential anti-tumor promoters by using the in vitro short-term 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced Epstein-Barr virus early antigen (EBV-EA) activation assay. Among them, 25-acetoxy-3alpha-hydroxyolean-12-en-28-oic acid (1) and 3beta,25-epoxy-3alpha-hydroxylup-20(29)-en-28-oic acid (2) were examined for anti-tumor promoting activity in a two-stage carcinogenesis assay on mouse skin with 7,12-dimethylbenz[a]anthracene (DMBA) and TPA as promoter. 25-Acetoxy-3alpha-hydroxyolean-12-en-28-oic acid (1) and 3beta,25-epoxy-3alpha-hydroxylup-20(29)-en-28-oic acid (2) showed moderate inhibitory activities.
为了从天然来源寻找癌症化学预防剂，通过体外短期12-O-十四烷酰佛波醇-13-乙酸酯（TPA）诱导的爱泼斯坦-巴尔病毒早期抗原（EBV-EA）激活试验，筛选了四种羽扇豆烷型和七种齐墩果烷型三萜类化合物以及十种合成类似物作为潜在的抗肿瘤促进剂。其中，25-乙酰氧基-3α-羟基齐墩果-12-烯-28-酸（1）和3β,25-环氧-3α-羟基羽扇-20(29)-烯-28-酸（2）在以7,12-二甲基苯并[a]蒽（DMBA）为起始剂、TPA为促进剂的小鼠皮肤两阶段致癌试验中检测了抗肿瘤促进活性。25-乙酰氧基-3α-羟基齐墩果-12-烯-28-酸（1）和3β,25-环氧-3α-羟基羽扇-20(29)-烯-28-酸（2）表现出中等抑制活性。
