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雷公藤内酯酮 |
| CAS No.: |
38647-11-9 |
| 分子式： |
C20H22O6 |
| 分子量： |
358.39 |
| 备注： |
中文名称雷公藤内酯酮中文同义词雷公藤内酯酮(雷藤酮,雷公藤羰内酯);雷公藤内酯酮,来源于前胡;雷公藤内酯酮(雷藤酮;雷公藤内酯酮(标准品);雷藤酮,雷公藤羰内酯;雷藤酮;雷公藤内酯酮;雷公藤羰内酯英文名称Triptonide英文同义词TRIPTONIDE;TRIPTONIDE(PRIMARYSTANDARD);NSC165677;PG492;(3bS,4aS,5aS,6aS,7aS,7bS,8aS,8bS)-6a-Isopropyl-8b-methyl-3b,4,4a,7a,7b,8b,9,10-octahydrotrisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1,6(3H,6aH)-dione;14-Deoxy-14-oxotriptolide;Triptolide,14-deoxy-14-oxo;Triptonide,98%,fromPeucedanumpraeruptorumDunnCAS号38647-11-9分子式C20H22O6分子量358.39EINECS号相关类别天然产物;植提标准品;中药对照品;标准品;植物提取物;对照品;中草药成分;标准品-中药标准品;新品;标准品-中药标准品;标准品，对照品;Heterocycles;chemicalreagent;pharmaceuticalintermediate;phytochemical;referencestandardsfromChinesemedicinalherbs(TCM).;standardizedherbalextractMol文件38647-11-9.mol结构式雷公藤内酯酮性质熔点251～252℃沸点581.1±50.0°C(Predicted)密度1.48±0.1g/cm3(Predicted)储存条件Inertatmosphere,Storeinfreezer,under-20°C溶解度二氯甲烷（微溶）、甲醇（微溶）形态固体颜色灰白色至浅米色雷公藤内酯酮用途与合成方法概述雷公藤内酯酮是从雷公藤中分离得到的一个二萜类化合物，是雷公藤的有效成份之一，它与雷公藤内酯醇结构相似，活性也相当，其结构式如下。雷公藤内酯酮具有抗雄性生育作用和对免疫功能具有一定的影响。生物活性Triptonide(NSC165677;PG492)是从雷公藤中鉴定出的一种天然产物。Triptonide是一种Wnt信号抑制剂，其IC50约为0.3nM。Triptonide具有免疫抑制、抗炎、抗生育、神经保护和抗淋巴瘤作用。靶点TargetValueWnt/β-catenin()体外研究TriptonideblocksWnt/β-cateninsignalingviaC-terminaltransactivationdomainofβ-catenin,andpromotsapoptosisinWnt-dependentcancercells.TriptonidepotentlyinhibitstheproliferationofhumanB-lymphomaRajiandT-lymphomaJurkatcellswithIC50of5.7nMand4.8nM,respectively.Triptonide(2.5-10nM;6days)significantlysuppressesB-lymphomacellcolony-formingcapability.TriptonChemicalbookide(20nM;3days)promotesapoptosisthroughactivationofPARPandcaspase3,butreductionofBCL2proteinlevelsinthelymphomacells.Triptonide(5-10nM;72hours)markedlyreducesbothtotalandphosphorylatedLynproteins,anddiminishesLyndownstreamERKandATKsignalpathways.CellProliferationAssayCellLine:B-lymphomaRajicells,T-lymphomaJurkatcellsConcentration:0-80nMIncubationTime:3days,6daysResult:Inhibitedlymphomacelltumorigeniccapabilityinadose-dependentmanner.ApoptosisAnalysisCellLine:RajicellsConcentration:5nM,10nM,20nMIncubationTime:3daysResult:Didnotsignificantlyinduceapoptosisattheeffectivetumorgrowth-inhibitory(2.5-10nM);moderatelyinducedlymphomacellapoptosis(20nM).WesternBlotAnalysisCellLine:RajicellsConcentration:5nM,10nM,20nMIncubationTime:3daysResult:Didnotvigorouslyactivatedpro-apoptoticproteinsPARPandcaspase3inlymphomacells(5-10nM);significantlyactivatedPARPandcaspase3(20nM);significantlyreducedanti-apoptoticBCL2levels.RT-PCRCellLine:RajicellsConcentration:5nM,10nMIncubationTime:72hoursResult:SignificantlydiminishedLynmRNAlevelsinthelymphomacells.体内研究Triptonide(5mg/kg;i.p.;daily;for34days)exertsastronganti-lymphomaeffectinmice.AnimalModel:Eight-week-oldfemaleNOD/SCIDmice(18-22g),with3x107RajicellsxenograftDosage:5mg/kgAdministration:Intraperitonealinjection,daily,for34daysResult:Potentlyinhibitedlymphomacellgrowthandtumorigeniccapability.化学性质黄色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于雷公藤。用途雷公藤内酯酮具有抗肿瘤免疫调节抗炎的作用。用途用于含量测定/鉴定/药理实验等。药理药效:治疗麻风反应,治疗类风湿性关节炎,治疗肺结核及其他慢性肺部疾病。 |
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