Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis

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

doi:10.1038/nm1095-1046

Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis

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

Gastroenterologic and General Surgery

Research output: Contribution to journal › Article › peer-review

721 Scopus citations

Abstract

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 preciinicai development for the treatment or prevention of malignant melanoma.

Original language	English (US)
Pages (from-to)	1046-1051
Number of pages	6
Journal	Nature Medicine
Volume	1
Issue number	10
DOIs	https://doi.org/10.1038/nm1095-1046
State	Published - Oct 1995

ASJC Scopus subject areas

Biochemistry, Genetics and Molecular Biology(all)

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Pisha, E., Chai, H., Lee, I. S., Chagwedera, T. E., Farnsworth, N. R., Cordell, G. A., Beecher, C. W. W., Fong, H. H. S., Kinghorn, A. D., Brown, D. M., Wani, M. C., Wall, M. E., Hieken, T. J., Gupta, T. K. D., & Pezzuto, J. M. (1995). Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis. Nature Medicine, 1(10), 1046-1051. https://doi.org/10.1038/nm1095-1046

Pisha, E, Chai, H, Lee, IS, Chagwedera, TE, Farnsworth, NR, Cordell, GA, Beecher, CWW, Fong, HHS, Kinghorn, AD, Brown, DM, Wani, MC, Wall, ME, Hieken, TJ, Gupta, TKD & Pezzuto, JM 1995, 'Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis', Nature Medicine, vol. 1, no. 10, pp. 1046-1051. https://doi.org/10.1038/nm1095-1046

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title = "Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis",

abstract = "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 preciinicai development for the treatment or prevention of malignant melanoma.",

author = "Emily Pisha and Heebyung Chai and Lee, {Ik Soo} and Chagwedera, {Tangai E.} and Farnsworth, {Norman R.} and Cordell, {Geoffrey A.} and Beecher, {Christopher W.W.} and Fong, {Harry H.S.} and Kinghorn, {A. Douglas} and Brown, {Daniel M.} and Wani, {Mansukh C.} and Wall, {Monroe E.} and Hieken, {Tina J.} and Gupta, {Tapas K.Das} and Pezzuto, {John M.}",

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AU - Farnsworth, Norman R.

AU - Cordell, Geoffrey A.

AU - Beecher, Christopher W.W.

AU - Fong, Harry H.S.

AU - Kinghorn, A. Douglas

AU - Brown, Daniel M.

AU - Wani, Mansukh C.

AU - Wall, Monroe E.

AU - Hieken, Tina J.

AU - Gupta, Tapas K.Das

AU - Pezzuto, John M.

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Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis

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