RESUMO
Eleven cyclic diarylheptanoids were screened as potential antitumor promoters by examining the ability of the compounds to inhibit Epstein-Barr virus early antigen activation (induced by 12-O-tetradecanoylphorbol-13-acetate) in Raji cells. 13-Oxomyricanol and myricanone showed the highest activity and also exhibited remarkable inhibitory effects on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. These data suggest that certain diarylheptanoids might be valuable antitumor promoters and/or chemopreventors.
Assuntos
Antineoplásicos/farmacologia , Diarileptanoides , Herpesvirus Humano 4/efeitos dos fármacos , Neoplasias Cutâneas/prevenção & controle , 9,10-Dimetil-1,2-benzantraceno/toxicidade , Animais , Antineoplásicos/química , Carcinógenos/toxicidade , Relação Dose-Resposta a Droga , Feminino , Humanos , Hidrocarbonetos Cíclicos/química , Hidrocarbonetos Cíclicos/farmacologia , Camundongos , Camundongos Endogâmicos ICR , Papiloma/induzido quimicamente , Papiloma/prevenção & controle , Neoplasias Cutâneas/induzido quimicamente , Organismos Livres de Patógenos Específicos , Terpenos/farmacologia , Acetato de Tetradecanoilforbol/farmacologia , Fatores de Tempo , Células Tumorais Cultivadas , Ativação Viral/efeitos dos fármacosRESUMO
As a part of screening studies for anti-tumor promoters, fifteen isoflavonoids isolated from plants of the genus Millettia (Leguminosae) were evaluated by examining their possible inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate in Raji cells. All of the compounds tested in this study showed inhibitory activity against EBV, without showing any cytotoxicity. Auriculasin (11) and millepurone (13), which is an oxidized isoflavone analogue, both having one or more prenyl side-chains and a 3',4'-dihydroxyphenyl group in the molecule, showed more potent activity than any of the other compounds tested. Furthermore, millepurone (13) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. The results of the present investigation indicate that some of these isoflavonoids might be valuable anti-tumor promoters.
