Miltefosine

CCT抑制剂；10-50µM浓度下可抑制MDCK细胞匀浆中脂质体诱导的CCT活性，并诱导MDCK细胞中CCT从细胞膜易位到细胞质；50µM浓度下可抑制PMA诱导的MDCK和HeLa细胞中磷脂酰胆碱的生物合成；抑制磷脂酰丝氨酸激活的PKC（IC50=62µM）以及PMA诱导的MDCK细胞形态变化和增殖；对L.infantum临床分离株前鞭毛体有效（EC50s=5-25µM）；0.5%浓度下局部应用可完全根除L.amazonensis，并诱导小鼠皮肤利什曼病模型中病变的上皮化。An inhibitor of CCT; inhibits liposome-induced CCT activity in MDCK cell homogenates from 10-50 µM, as well as induces translocation of CCT from the cell membrane to the cytosol in MDCK cells; inhibits PMA-induced phosphatidylcholine biosynthesis in MDCK and HeLa cells at 50 µM; inhibits phosphatidylserine-activated PKC (IC50 = 62 µM), as well as PMA-induced morphological changes and proliferation of MDCK cells; active against clinical isolate promastigotes of L. infantum (EC50s = 5-25 µM); topical application completely eradicates L. amazonensis and induces re-epithelialization of lesions in a mouse model of cutaneous leishmaniasis at 0.5%.分子式C21H46NO4P分子量407.6CCCCCCCCCCCCCCCCOP(OCC[N+](C)(C)C)([O-])=O