ChelerythrineinteractswiththecatalyticdomainofPKC,isacompetitiveinhibitorwithrespecttothephosphateacceptor(histoneIIIS)withKivalueof0.7μMandanon-competitiveinhibitorwithrespecttoATP.ChelerythrineshowspotentcytotoxiceffectsagainstL-1210cellswithIC50of0.53μM.ChelerythrinedoesnotalteranyactivityofPKA,TPKandCa/CM-PK,andtheChelerythrineinhibitoryeffectonPKCactivitydoesnotvaryamongthevarioussubstratesincludingGS,MLC,MBPandFibrinogen.^[1]ChelerythrineinhibitsPKCactivityincrudecellextractsfromSQ-20Bcellsinadosedependentmanner.ChelerythrinedecreasescellviABIlityasdeterminedbytheMTTassayinadose-dependentmannerinSCC35,JSQ3,SQ20BandSCC61cells.^[2]Chelerythrinechloride(5μM)suppressesVEGF-inducedexpressionofICAM-1,VCAM-1,andE-selectininHUVECs.Chelerythrinechloride(5μM)suppressesVEGF-inducedNF-κBactivityinHUVECs.Chelerythrinechloride(5μM)allsuppressesbasalandVEGF-inducedleukocyteadhesivenessinHUVECs.^[3]Chelerythrine(6mM-30mM)rapidlyinducespyknosis,shrinkageandsubsequentcelldeathincardiacmyocytes.Chelerythrine(30μM)-inducedmyocytedeathisaccompaniedbynuclearfragmentationandactivationofcaspase-3and-9inprimarycultureofneonatalratventricularmyocytes.Chelerythrine(10μM)causescytochromecreleasefrommitochondria,suggestingthatROSmediateschelerythrine-inducedcytochromecreleaseincardiacmyocytes.^[4]ChelerythrinedisplacesthefluorescentlylabeledBH3domainpeptidefromarecombinantGST-BcLXLfusionproteinwithIC50of1.5μM.Chelerythrineat2.5μMand5μMfor16hoursinducesasubstantialdecreaseinmitochondrialpotentialasindicatedbyanincreaseinJC-1greenfluorescenceinhumanneuroblastomaSH-SY5Ycells.Chelerythrine(5μM)alsoinducestheappearanceofsub-G1DNAthatisindicativeofapoptosisinSH-SY5Ycells.Chelerythrine(10μM)inducesmitochondrialpotentialchange,CytCreleasefromthemitochondriainSH-SY5Ycells.^[5]

Chelerythrine(5mg/kgi.p.)resultsintumorgrowthdelayinmicebearingSQ-20Bxenografts.^[2]Chelerythrine(5mg/kg)treatmentsignificantlyincreasesTUNEL-positivenucleiinthemyocardiumaswellascleavedformsofcaspase-3and-9inadultrat.^[4]