Nishizawa Manabu, Ohtsu Hironori, Tanaka Reiko, Tokuda Harukuni, Katoh Takahiro, Takeo Masatoshi, Node Manabu
Department of Medicinal Chemistry, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
Chem Biodivers. 2007 May;4(5):1003-7. doi: 10.1002/cbdv.200790068.
(11E)-13-Oxo-15,16-dinorlabda-8(20),11-dien-19-oic Acid (1), obtained either from the stem bark of Thuja standishii or readily prepared in larger quantities from the related constituent 2, was found to significantly reduce the formation of papilloma in an in vivo two-stage mouse-skin-carcinogenesis model. Carcinogenesis was initiated by skin exposure to UV-B irradiation and promoted by topical application of 12-O-tetradecanoylphorbol-13-acetate (TPA). Oral administration of 1, starting one week before and ending one week after irradiation, exhibited remarkable effects. First, papilloma formation started two weeks later than in the control group (lacking 1). Second, the average number of skin papilloma after 20 weeks was reduced by ca. 50% in the test group relative to the control.
(11E)-13-氧代-15,16-二降-labda-8(20),11-二烯-19-酸（1），可从柳杉的茎皮中获得，也可从相关成分2大量制备，在体内两阶段小鼠皮肤致癌模型中发现其能显著减少乳头状瘤的形成。致癌过程通过皮肤暴露于UV-B辐射启动，并通过局部应用12-O-十四酰佛波醇-13-乙酸酯（TPA）促进。在辐射前一周开始并在辐射后一周结束口服1，显示出显著效果。首先，乳头状瘤形成比对照组（不含1）晚两周开始。其次，20周后试验组皮肤乳头状瘤的平均数量相对于对照组减少了约50%。
