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Cancer Preventive Agents. Part 1: Chemopreventive Potential of Cimigenol, cimigenol-3,15-dione, and Related Compounds

Nobuko Sakurai, Mutsuo Kozuka, Harukuni Tokuda, Teruo Mukainaka, Fumio Enjo, Hoyoku Nishino, Masahiro Nagai, Yojiro Sakurai, Kuo-Hsiung Lee

Bioorg Med Chem. 2005 Feb 15;13(4):1403-8.

PMID: 15670948

Abstract:

In continuation of our previous report, cimigenol (1) and 15 related compounds were screened as potential antitumor promoters by using the in vitro short-term 12-O-tetradecanoylphorbol-13-acetate (TPA)--induced Epstein-Barr virus early antigen (EBV-EA) activation assay. Cimigenol-3,15-dione (2) displayed the greatest potency (100% inhibition at 1000 mol ratio/TPA) and consequently was further examined for antitumor-promoting activity in a two-stage carcinogenesis assay of mouse skin tumors (DMBA/TPA). In this assay, compound 2 showed significant activity, reducing the number of papillomas per mouse to 48% of the control group at 20 weeks. In addition, compounds 1 and 2 were examined for antitumor-initiating activity in a two-stage carcinogenesis assay of mouse skin tumors induced by peroxynitrite as an initiator and TPA as a promoter. Results showed that these two triterpenoids were almost equipotent with epigallocatechin gallate (EGCG) and slightly more potent than tocinol (group V), the positive controls. Thus, compounds 1 and 2 exhibited not only strong antitumor-promoting activity but also significant antitumor-initiating effect on mouse skin. These data suggest that both compounds might be valuable chemopreventors.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP27994112 Cimigenol 3-β-D-xyloside Cimigenol 3-β-D-xyloside 27994-11-2 Price
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