Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis
| Autor: | Emily Pisha, Heebyung Chai, Ik-Soo Lee, Tangai E. Chagwedera, Norman R. Farnsworth, Geoffrey A. Cordell, Christopher W.W. Beecher, Harry H.S. Fong, A. Douglas Kinghorn, Daniel M. Brown, Mansukh C. Wani, Monroe E. Wall, Tina J. Hieken, Tapas K. Das Gupta, John M. Pezzuto |
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| Rok vydání: | 1995 |
| Předmět: |
Skin Neoplasms
DNA damage Melanoma Experimental Mice Nude Apoptosis Biology Guanidines General Biochemistry Genetics and Molecular Biology Mice chemistry.chemical_compound Triterpene Betulinic acid Putrescine Tumor Cells Cultured medicine Animals Humans Betulinic Acid Cytotoxicity Melanoma chemistry.chemical_classification Liver Neoplasms General Medicine medicine.disease Antineoplastic Agents Phytogenic Growth Inhibitors Triterpenes chemistry Biochemistry Toxicity Cancer research Experimental pathology Pentacyclic Triterpenes DNA Damage |
| Zdroj: | Nature Medicine. 1:1046-1051 |
| ISSN: | 1546-170X 1078-8956 |
| DOI: | 10.1038/nm1095-1046 |
| Popis: | As a result of bioassay-guided fractionation, betulinic acid, a pentacyclic triterpene, was identified as a melanoma-specific cytotoxic agent. In follow-up studies conducted with athymic mice carrying human melanomas, tumour growth was completely inhibited without toxicity. As judged by a variety of cellular responses, antitumour activity was mediated by the induction of apoptosis. Betulinic acid is inexpensive and available in abundant supply from common natural sources, notably the bark of white birch trees. The compound is currently undergoing preclinical development for the treatment or prevention of malignant melanoma. |
| Databáze: | OpenAIRE |
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