生物活性NIM811((Melle-4)cyclosporin;SDZNIM811)是一種具有口服活性的線粒體滲透轉(zhuǎn)換(mitochondrialpermeabilitytransition)和親環(huán)蛋白(cyclophilin)雙抑制劑,對(duì)丙型肝炎病毒(HCV)具有很強(qiáng)的體外活性。靶點(diǎn)Cyclophilin,MitochondrialPermeabilityTransitionInhibitor體外研究NIM811inducesaconcentration-dependentreductionofHCVRNAintherepliconcellswithanIC50of0.66μMat48h.Inaddition,thecombinationofNIM811withalphaIFNsignificantlyenhancesanti-HCVactivitieswithoutcausinganyincreaseofcytotoxicity.NIM811blocksthemitochondrialpermeabilitytransitioninducedbycalciumandinorganicphosphate.體內(nèi)研究NIM811preventsmitochondrialdepolarizationtherebyattenuatesliverinjury,stimulatesregenerationandimprovesliverfunctionandsurvival.
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