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尼日利亚菌素钠盐 |
CAS No.: |
28643-80-3 |
分子式: |
C40H67O11Na |
分子量: |
746.94 |
备注: |
中文名称尼日利亚菌素钠盐中文同义词尼日利亚菌素钠盐;尼日利亚菌素钠盐,来源于吸水链霉菌;尼日利亚菌素钠盐,来源于链霉菌,吸湿性菌;NIGERICIN(钠盐形式);尼日利亚菌素钠;尼日利亚菌素钠NIGERICINSODIUMSALT;尼日利亚菌素,钠盐,吸水链霉菌;尼日利亚霉素(钠盐)英文名称Nigericinsodiumsalt英文同义词Nigericinsodiumsalt;PolyetherinA,AzalomycinM,HelixinC,AntibioticK178,AntibioticX-464;AntibioticK178,AntibioticX464,AzalomycinM,HelexinC,PolyetherinA;Sodium(2R)-2-[(3S,6R)-6-[[(2S,4R,5R,7R,9R,10R)-2-[(5S)-5-[(2R,3S,5R)-5-[(2S,3S,5R,6R)-6-hydroxy-6-(hydroxymethyl)-3,5-dimethyloxan-2-yl]-3-methyloxolan-2-yl]-5-methyloxolan-2-yl]-9-methoxy-2,4,10-trimethyl-1,6-dioxaspiro[4.5]decan-7-yl]methyl]-3-methyloxan-2-yl]propanoate;Nigericin,monosodiumsalt;Nsc292567;Nigericinsodiumsalt,AntibioticK178,AntibioticX464,AzalomycinM,HelexinC,PolyetherinA;NigericinsodiuMsaCAS号28643-80-3分子式C40H69NaO11分子量748.97EINECS号608-231-4相关类别微生物代谢物;抗生素;聚醚类抗生素;抗生素及抗病毒;生化试剂;原料药;试剂盒-细胞分析试剂盒;APIMol文件28643-80-3.mol结构式尼日利亚菌素钠盐性质熔点approximate255℃储存条件2-8°C溶解度溶于氯仿、甲醇或乙醇形态溶液在储存期间颜色可能会变暗颜色白色Merck13,6569BRN3892398稳定性可在-20°下的DMSO或乙醇溶液保存长达2个月。InChIKeyMOYOTUKECQMGHE-NTQCAYBPSA-MLogP4.817(est)尼日利亚菌素钠盐用途与合成方法生物活性Nigericin钠盐是从Streptomyceshygroscopicus衍生的抗生素,通过充当H+,K+和Pb2+的离子载体起作用。Nigericin可以激活NLRP3炎性体以诱导促炎和免疫刺激过程。靶点TargetValuePotassiumchannel()Hydrogenchannel()Pb2+()NLRPChemicalbook3()体外研究Nigericin(0.1µM)decreasesinhibitsproliferationandclonogenicityofH460lungcancercellsinadosedependentmanner.NigericininhibitsmigrationandinvasionofH460lungcancercells.Nigericin(0.1-10nM)hasapparentlyadualeffectoncellvolume,thatisashrinkingeffectatlowerNigericinconcentrationsandaswellingeffectathigherconcentrations.Nigericin(0.1-1nM)significantlydecreasescytosolicpH(pHi),andslightlyincreasesthepHiat5and10nM.NigericinexhibitshighertoxicityonS18cellsthanS26cells,withIC50of2.03±0.55μMand4.77±2.35μM,respectively.NigericincanselectivelykillcancerstemcellsinNPCinvitro.NigericindramaticallyreducesthemigrationabilityofS18andHONE-1cells.NigericinexhibitsgteattoxicityfortheHT29andSW116celllinewithIC50of12.92±0.25μmoland15.86±0.18μmol.Nigericinalsoshowsadecreasedabilitytoformcoloniesunderanchorage-independentconditionsinastandardsoftagarassay.体内研究Ngericin(4mg/kg,i.p.)significantlyreducestumorgrowthandactssynergisticallywiththechemotherapeuticagentDDP,asshownbythetumorvolumes.NigericinmarkedlydecreasesBmi-1invivo.OverexpressionofBmi-1partiallyrestoresCSCcontentandmetastaticabilityofNPCcellsunderNigericintreatment.ThedownregulationofBmi-1maybeinvolvedintheinhibitoryeffectofNigericinonCSCsinNPC. |
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