生物活性NIM811((Melle-4)cyclosporin;SDZNIM811)是一种具有口服活性的线粒体渗透转换(mitochondrialpermeabilitytransition)和亲环蛋白(cyclophilin)双抑制剂，对丙型肝炎病毒(HCV)具有很强的体外活性。靶点Cyclophilin,MitochondrialPermeabilityTransitionInhibitor体外研究NIM811inducesaconcentration-dependentreductionofHCVRNAintherepliconcellswithanIC50of0.66μMat48h.Inaddition,thecombinationofNIM811withalphaIFNsignificantlyenhancesanti-HCVactivitieswithoutcausinganyincreaseofcytotoxicity.NIM811blocksthemitochondrialpermeabilitytransitioninducedbycalciumandinorganicphosphate.体内研究NIM811preventsmitochondrialdepolarizationtherebyattenuatesliverinjury,stimulatesregenerationandimprovesliverfunctionandsurvival.
