Berman J D, Rainey P, Santi D V
J Exp Med. 1983 Jul 1;158(1):252-7. doi: 10.1084/jem.158.1.252.
Formycin B is metabolized by cutaneous Leishmania amastigotes within cultured human macrophages to give formycin B 5'-monophosphate and formycin A 5'-mono-, di-, and triphosphates. Formycin A is also incorporated into RNA. The activity of formycin B against amastigotes was correlated with the levels of formycin A metabolites formed in the parasites. Uninfected macrophages also convert formycin B into the same products, but the levels are markedly lower than those seen in infected macrophages. The results suggest that a sufficient therapeutic index exists to warrant consideration of formycin B as an anti-leishmanial drug in humans.
间型霉素B在培养的人巨噬细胞内被皮肤利什曼原虫无鞭毛体代谢，生成间型霉素B 5'-单磷酸酯以及间型霉素A 5'-单磷酸酯、二磷酸酯和三磷酸酯。间型霉素A也会掺入RNA中。间型霉素B对无鞭毛体的活性与寄生虫中形成的间型霉素A代谢物水平相关。未感染的巨噬细胞也会将间型霉素B转化为相同的产物，但水平明显低于感染巨噬细胞中的水平。结果表明存在足够的治疗指数，值得考虑将间型霉素B作为人类抗利什曼原虫药物。
