Bestatin hydrochloride, also known as Ubenimex, is an inhibitor of aminopeptidase B and N (APN)/CD13 [1].

Bestatin, an antibiotic of microbial origin, is a potent inhibitor of some aminopeptidases which can be administered to cultured cells, intact animals and humans with low toxicity. It has been used as an useful tool to assess the physiological role of certain mammalian exopeptidases in the regulation of the immune system, the growth of tumors and their invasion of surrounding tissues, and the degradation of cellular proteins [2].

In vivo: In a mouse dorsal air sac assay, oral administration of bestatin (100-200 mg/kg/day) showed a significant inhibitory activity against the melanoma cell-induced angiogenesis. Bestatin also inhibited the tube-like formation of human umbilical vein endothelial cells (HUVECs). Furthermore, after the orthotopic implantation of B16-BL6 melanoma cells into mice, bestatin administration (50-100 mg/kg/day, i.p) reduced the number of vessels oriented towards the established primary tumor mass on the dorsal side of mice [1].

References:

[1]. Aozuka Y1, Koizumi K, Saitoh Y, Ueda Y, Sakurai H, Saiki I. Anti-tumor angiogenesis effect of aminopeptidase inhibitor bestatin against B16-BL6 melanoma cells orthotopically implanted into syngeneic mice. Cancer Lett. 2004 Dec 8;216(1):35-42.

[2]. Scornik OA1,Botbol V.Bestatin as an experimental tool in mammals. Curr Drug Metab.2001 Mar;2(1):67-85.

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