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雷公藤內(nèi)酯酮 |
CAS No.: |
38647-11-9 |
分子式: |
C20H22O6 |
分子量: |
358.39 |
備注: |
中文名稱雷公藤內(nèi)酯酮中文同義詞雷公藤內(nèi)酯酮(雷藤酮,雷公藤羰內(nèi)酯);雷公藤內(nèi)酯酮,來源于前胡;雷公藤內(nèi)酯酮(雷藤酮;雷公藤內(nèi)酯酮(標(biāo)準(zhǔn)品);雷藤酮,雷公藤羰內(nèi)酯;雷藤酮;雷公藤內(nèi)酯酮;雷公藤羰內(nèi)酯英文名稱Triptonide英文同義詞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號38647-11-9分子式C20H22O6分子量358.39EINECS號相關(guān)類別天然產(chǎn)物;植提標(biāo)準(zhǔn)品;中藥對照品;標(biāo)準(zhǔn)品;植物提取物;對照品;中草藥成分;標(biāo)準(zhǔn)品-中藥標(biāo)準(zhǔn)品;新品;標(biāo)準(zhǔn)品-中藥標(biāo)準(zhǔn)品;標(biāo)準(zhǔn)品,對照品;Heterocycles;chemicalreagent;pharmaceuticalintermediate;phytochemical;referencestandardsfromChinesemedicinalherbs(TCM).;standardizedherbalextractMol文件38647-11-9.mol結(jié)構(gòu)式雷公藤內(nèi)酯酮性質(zhì)熔點251~252℃沸點581.1±50.0°C(Predicted)密度1.48±0.1g/cm3(Predicted)儲存條件Inertatmosphere,Storeinfreezer,under-20°C溶解度二氯甲烷(微溶)、甲醇(微溶)形態(tài)固體顏色灰白色至淺米色雷公藤內(nèi)酯酮用途與合成方法概述雷公藤內(nèi)酯酮是從雷公藤中分離得到的一個二萜類化合物,是雷公藤的有效成份之一,它與雷公藤內(nèi)酯醇結(jié)構(gòu)相似,活性也相當(dāng),其結(jié)構(gòu)式如下。雷公藤內(nèi)酯酮具有抗雄性生育作用和對免疫功能具有一定的影響。生物活性Triptonide(NSC165677;PG492)是從雷公藤中鑒定出的一種天然產(chǎn)物。Triptonide是一種Wnt信號抑制劑,其IC50約為0.3nM。Triptonide具有免疫抑制、抗炎、抗生育、神經(jīng)保護和抗淋巴瘤作用。靶點TargetValueWnt/β-catenin()體外研究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.體內(nèi)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.化學(xué)性質(zhì)黃色結(jié)晶粉末,可溶于甲醇、乙醇、DMSO等有機溶劑,來源于雷公藤。用途雷公藤內(nèi)酯酮具有抗腫瘤免疫調(diào)節(jié)抗炎的作用。用途用于含量測定/鑒定/藥理實驗等。藥理藥效:治療麻風(fēng)反應(yīng),治療類風(fēng)濕性關(guān)節(jié)炎,治療肺結(jié)核及其他慢性肺部疾病。 |
結(jié)構(gòu)式: |
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聯(lián)系人: |
金經(jīng)理 |
地 址: |
湖北省武漢市東湖新技術(shù)開發(fā)區(qū)光谷大道03號 |
郵 編: |
430000 |
電 話: |
18995560451 |
手 機: |
15102708508 |
傳 真: |
18995560451 |
Q Q: |
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網(wǎng) 址: |
www.hbdhchem.com |
電子郵件: |
709783996@qq.com |
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