Pisha E, Chai H, Lee I S, Chagwedera T E, Farnsworth N R, Cordell G A, Beecher C W, Fong H H, Kinghorn A D, Brown D M
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago 60612, USA.
Nat Med. 1995 Oct;1(10):1046-51. doi: 10.1038/nm1095-1046.
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.
通过生物测定引导的分级分离，五环三萜类化合物桦木酸被鉴定为一种黑色素瘤特异性细胞毒性剂。在用携带人黑色素瘤的无胸腺小鼠进行的后续研究中，肿瘤生长被完全抑制且无毒性。从多种细胞反应判断，抗肿瘤活性是由细胞凋亡的诱导介导的。桦木酸价格低廉，可从常见天然来源大量获取，特别是白桦树的树皮。该化合物目前正在进行用于治疗或预防恶性黑色素瘤的临床前开发。
