Abstract |
Bioassay-guided separation of extracts from the culture broth and mycelium of the fungus Trichothecium roseum, aiming at the discovery for cancer preventive agents, resulted in the isolation of three new trichothecene sesquiterpenes, trichothecinols A-C (1-3) together with three known analogues, trichothecin (4), trichodermol (5) and trichothecolone (6). Compounds 1-6 exhibited remarkably potent inhibition against Epstein-Barr virus early antigen ( EBV-EA) activation induced by the tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA). Further compound 1 strongly inhibited TPA-induced tumor promotion on mouse skin initiated with 7,12-dimethylbenz[a] anthracene (DMBA) in two-stage carcinogenesis tests. These results suggest that compound 1 might be a valuable lead for further evaluation as a cancer preventive agent. In addition to their cancer preventive activity, compound 2 was found to show modest antifungal activity against Crypotcoccus albidus and Saccharomyces cerevisiae.
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Authors | Kazuhide Konishi, Akira Iida, Masafumi Kaneko, Kiyoshi Tomioka, Harukuni Tokuda, Hoyoku Nishino, Yuko Kumeda |
Journal | Bioorganic & medicinal chemistry
(Bioorg Med Chem)
Vol. 11
Issue 12
Pg. 2511-8
(Jun 12 2003)
ISSN: 0968-0896 [Print] England |
PMID | 12757719
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Anti-Infective Agents
- Anticarcinogenic Agents
- Antigens, Viral
- Epstein-Barr virus early antigen
- Trichothecenes
- Tetradecanoylphorbol Acetate
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Topics |
- Animals
- Anti-Infective Agents
(pharmacology)
- Anticarcinogenic Agents
(chemistry, isolation & purification, pharmacology)
- Antigens, Viral
(drug effects)
- Carcinogenicity Tests
- Cell Survival
(drug effects)
- Humans
- Mice
- Mitosporic Fungi
(chemistry)
- Molecular Structure
- Nuclear Magnetic Resonance, Biomolecular
- Papilloma
(chemically induced, pathology, prevention & control)
- Skin Neoplasms
(chemically induced, pathology, prevention & control)
- Tetradecanoylphorbol Acetate
(toxicity)
- Trichothecenes
(chemistry, isolation & purification, pharmacology)
- Tumor Cells, Cultured
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