Alkane-6,8-diol: Inhibitor of Tumor Promotion in Two-Stage Carcinogenesis in Mouse Skin

Journal of Medicinal Chemistry
1995.0

Abstract

Cancer prevention is now most urgently required for public health, particularly targeting the promotion stage of carcinogenesis as it can be applied post-exposure to unavoidable tumor-initiating agents. Earlier studies demonstrated extracts from edible plants and crude drugs inhibited 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced inflammatory ear edema, and alkane-6,8-diols isolated from Carthamus tinctorius (safflower) inhibited TPA-induced ear edema and tumor promotion in mouse skin. This study prepared homologs 4a-c of the alkane-6,8-diol series. In mouse assays, C27- and C29-alkane-6,8-diols (4b,c) inhibited TPA-induced inflammatory ear edema with ID50 values of 0.5 and 0.4 mg/ear, respectively, comparable to indomethacin, more effective than quercetin (a known tumor promotion inhibitor) but less than hydrocortisone. C29-alkane-6,8-diol (4c) inhibited tumor promotion by TPA following 7,12-dimethylbenz[a]anthracene (DMBA) initiation: at week 20, the percentage of tumor-bearing mice decreased from 93% to 20%, and the average number of tumors per mouse from 11.1 to 0.9. Since safflower is nontoxic and used in foods, these alkane-6,8-diols are promising chemopreventive agents for cancer.

Knowledge Graph

Similar Paper