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Isolation and characterization of cytotoxic withanolides from the calyx of Physalis alkekengi L. var franchetii.
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2020-01-25 , DOI: 10.1016/j.bioorg.2020.103614
Yi Sun 1 , Tao Guo 2 , Fang-Bo Zhang 1 , Ya-Nan Wang 3 , Zhiguo Liu 1 , Shanshan Guo 1 , Li Li 3
Affiliation  

Phytochemical investigation into the calyx of Physalis alkekengi L. var franchetii (Mast) Makino resulted in the isolation of ten cytotoxic withanolides, including five new withanolides, 1-5. Compounds 2-4 were obtained as epimeric withaphysalins. The new structures were elucidated by extensive spectroscopic analyses and electronic circular dichroism (ECD) calculations. The withanolides were evaluated for their cytotoxic activities against the A549 and K562 cell lines. Compounds 1 and 8 exhibited potent cytotoxic activity against both cell lines with IC50 values of 1.9-4.3 μM and induced typical apoptosis as evaluated by flow cytometric analysis. Further studies indicated that 1 and 8 displayed antitumour effects by suppressing the PI3K-Akt-mTOR signalling pathway.

中文翻译:

酸浆无性系花萼花萼中细胞毒性withanolides的分离和表征。

对酸浆酸浆(Malisino alkekengi L. var franchetii)的花萼的植物化学研究导致分离出十种具有细胞毒性的醇化物,其中包括五种新的1-5。获得化合物2-4,其为具有连接异构的卟啉类。通过广泛的光谱分析和电子圆二色性(ECD)计算来阐明新结构。评估了withanolides对A549和K562细胞株的细胞毒活性。通过流式细胞术分析评估,化合物1和8对两种细胞系均表现出强大的细胞毒活性,IC50值为1.9-4.3μM,并诱导了典型的细胞凋亡。进一步的研究表明1和8通过抑制PI3K-Akt-mTOR信号通路显示出抗肿瘤作用。
更新日期:2020-01-26
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