Tanaka Reiko, Ishikawa Yohei, Minami Toshifumi, Minoura Katsuhiko, Tokuda Harukuni, Matsunaga Shunyo
Department of Medicinal Chemistry, Osaka University of Pharmaceutical Sciences, Osaka, Japan.
Planta Med. 2003 Nov;69(11):1041-7. doi: 10.1055/s-2003-45153.
Two new serratane-type triterpenoids, 1 and 2, were isolated from the stem bark of Picea jezoensis Carr. var. jezoensis (Pinaceae). Their structures were determined to be 3beta-methoxyserrat-13-en-21beta-ol (1) and 13beta, l4beta-epoxy-3beta-methoxyserratan-21beta-ol (2) on the basis of spectroscopic methods and partial syntheses. Compounds 1 and 2 and their acetates 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. IC50 value evaluation showed that compound 1 was more effective than others. In addition, compounds 1 and 2 were examined for anti-tumor promoting activities in a two-stage carcinogenesis assay of mouse skin tumors induced by 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter. Compounds 1 and 2 exhibited significant anti-tumor promoting effects on mouse skin carcinogenesis.
从鱼鳞云杉（松科）的茎皮中分离出两种新的锯齿烷型三萜化合物1和2。通过光谱方法和部分合成确定它们的结构分别为3β-甲氧基锯齿-13-烯-21β-醇（1）和13β，14β-环氧-3β-甲氧基锯齿烷-21β-醇（2）。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，对化合物1和2及其乙酸酯作为潜在的抗肿瘤促进剂进行了筛选。IC50值评估表明化合物1比其他化合物更有效。此外，在以7,12-二甲基苯并[a]蒽（DMBA）为引发剂、TPA为促进剂诱导的小鼠皮肤肿瘤两阶段致癌试验中，对化合物1和2的抗肿瘤促进活性进行了检测。化合物1和2对小鼠皮肤致癌作用表现出显著的抗肿瘤促进作用。
