Cancer preventive agents. Part 1: Chemopreventive potential of cimigenol, cimigenol-3,15-dione, and related compounds

[Display omitted] 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...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2005-02, Vol.13 (4), p.1403-1408
Main Authors: Sakurai, Nobuko, Kozuka, Mutsuo, Tokuda, Harukuni, Mukainaka, Teruo, Enjo, Fumio, Nishino, Hoyoku, Nagai, Masahiro, Sakurai, Yojiro, Lee, Kuo-Hsiung
Format: Article
Language:English
Subjects:
9,19-Cyclolanosterol
Animals
Anticarcinogenic Agents - chemistry
Anticarcinogenic Agents - pharmacology
Antineoplastic agents
Antitumor-initiating effect
Antitumor-promoting effect
Biological and medical sciences
Carcinogenesis, carcinogens and anticarcinogens
Chemical agents
Cimigenol
Cimigenol-3,15-dione
Epstein-Barr virus
Female
General aspects
Lanosterol - analogs & derivatives
Lanosterol - chemistry
Lanosterol - pharmacology
Medical sciences
Mice
Mice, Inbred ICR
Papilloma - prevention & control
Pharmacology. Drug treatments
Skin Neoplasms - prevention & control
Tumors
Two-stage carcinogenesis
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2004.10.062