PMID- 7489361 OWN - NLM STAT- MEDLINE DCOM- 19960102 LR - 20221207 IS - 1078-8956 (Print) IS - 1078-8956 (Linking) VI - 1 IP - 10 DP - 1995 Oct TI - Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis. PG - 1046-51 AB - 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. FAU - Pisha, E AU - Pisha E AD - Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago 60612, USA. FAU - Chai, H AU - Chai H FAU - Lee, I S AU - Lee IS FAU - Chagwedera, T E AU - Chagwedera TE FAU - Farnsworth, N R AU - Farnsworth NR FAU - Cordell, G A AU - Cordell GA FAU - Beecher, C W AU - Beecher CW FAU - Fong, H H AU - Fong HH FAU - Kinghorn, A D AU - Kinghorn AD FAU - Brown, D M AU - Brown DM AU - et al. LA - eng GR - U01 CA 52956/CA/NCI NIH HHS/United States PT - Journal Article PT - Research Support, U.S. Gov't, P.H.S. PL - United States TA - Nat Med JT - Nature medicine JID - 9502015 RN - 0 (Antineoplastic Agents, Phytogenic) RN - 0 (Growth Inhibitors) RN - 0 (Guanidines) RN - 0 (Pentacyclic Triterpenes) RN - 0 (Triterpenes) RN - SCQ4EZQ113 (pimagedine) RN - V10TVZ52E4 (Putrescine) RN - 4G6A18707N (Betulinic Acid) SB - IM MH - Animals MH - Antineoplastic Agents, Phytogenic/*pharmacology MH - Apoptosis MH - *DNA Damage MH - Growth Inhibitors/*pharmacology MH - Guanidines/pharmacology MH - Humans MH - Liver Neoplasms/pathology MH - Melanoma/*pathology MH - Melanoma, Experimental/pathology MH - Mice MH - Mice, Nude MH - Pentacyclic Triterpenes MH - Putrescine/pharmacology MH - Skin Neoplasms/pathology MH - Triterpenes/*pharmacology MH - Tumor Cells, Cultured/drug effects MH - Betulinic Acid EDAT- 1995/10/01 00:00 MHDA- 1995/10/01 00:01 CRDT- 1995/10/01 00:00 PHST- 1995/10/01 00:00 [pubmed] PHST- 1995/10/01 00:01 [medline] PHST- 1995/10/01 00:00 [entrez] AID - 10.1038/nm1095-1046 [doi] PST - ppublish SO - Nat Med. 1995 Oct;1(10):1046-51. doi: 10.1038/nm1095-1046.