首页> 美国卫生研究院文献>Acta Pharmaceutica Sinica. B >Helioscopianoids A–Q bioactive jatrophane diterpenoid esters from Euphorbia helioscopia
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Helioscopianoids A–Q bioactive jatrophane diterpenoid esters from Euphorbia helioscopia

机译:Helioscopianoids A–Q来自大戟属Helioscopia的生物活性麻疯树二萜类酯

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摘要

The EtOH extracts of the whole plants of Euphorbia helioscopia afforded 17 new jatrophane diterpenoid esters, helioscopianoids A–Q (>1—>17), along with eight known compounds (>18–>25). Their structures were elucidated by extensive spectroscopic methods and Mo2(OAc)4-induced ECD analysis, and the structures of compounds >1, >2, and >7 were confirmed by X-ray crystallography. Compounds >1–>17 were evaluated for inhibitory effects on P-glycoprotein (P-gp) in an adriamycin (ADM)-resistant human breast adenocarcinoma cell line (MCF-7/ADR) and neuroprotective effects against serum deprivation-induced and rotenone-induced PC12 cell damage. Compounds >8 and >16 increased the accumulation of ADM in MCF-7/ADR cells by approximately 3-fold at a concentration of 20 μmol/L. Compound >8 could attenuate rotenone-induced PC12 cell damage, and compounds >2, >8, and >12 showed neuroprotective activities against serum deprivation-induced PC12 cell damage.
机译:大戟天芥菜的整个植物的EtOH提取物提供了17种新的麻风树二萜类酯,类天芥菜A-Q(> 1 -> 17 ),以及八种已知化合物(> 18 – > 25 )。通过广泛的光谱方法和Mo2(OAc)4诱导的ECD分析阐明了它们的结构,以及化合物> 1 ,> 2 和> 7 的结构通过X射线晶体学证实。评价了化合物> 1 – > 17 对耐阿霉素(ADM)的人乳腺癌细胞(MCF-7 /)中P-糖蛋白(P-gp)的抑制作用ADR)和抗血清剥夺诱导和鱼藤酮诱导的PC12细胞损伤的神经保护作用。化合物> 8 和> 16 使MCF-7 / ADR细胞中ADM的浓度在20μmol/ L时增加了约3倍。化合物> 8 可以减轻鱼藤酮诱导的PC12细胞损伤,化合物> 2 ,> 8 和> 12 具有神经保护活性抗血清剥夺诱导的PC12细胞损伤。

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