Semisynthesis and Non-Small-Cell Lung Cancer Cytotoxicity Evaluation of Germacrane-Type Sesquiterpene Lactones from Elephantopus scaber

Ren, Hui Zhang, Yang-Yang Li, Ya-Ling Bai, Ming Yan, Qiu-Lin Huang, Xiao-Xiao Cui, Wei Zhao, Hongwei Gu, Liwei Liu, Qingbo Yao, Guo-Dong Song, Shao-Jiang

Journal of natural products2022，Vol.85Issue(2) ：13.DOI:10.1021/acs.jnatprod.1c00936

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NSTL
Amer Chemical Soc

Semisynthesis and Non-Small-Cell Lung Cancer Cytotoxicity Evaluation of Germacrane-Type Sesquiterpene Lactones from Elephantopus scaber

Ren, Hui ¹Zhang, Yang-Yang ¹Li, Ya-Ling ¹Bai, Ming ¹Yan, Qiu-Lin ¹Huang, Xiao-Xiao ¹Cui, Wei ¹Zhao, Hongwei ²Gu, Liwei ³Liu, Qingbo ¹Yao, Guo-Dong ¹Song, Shao-Jiang¹

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作者信息

1. Shenyang Pharmaceut Univ
2. Jilin Yizheng Pharmaceut Grp Co Ltd
3. China Acad Chinese Med Sci
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Abstract

Two series of germacrane-type sesquiterpene lactones were produced by semisynthetic modulation of scaberol C, which was prepared by a standard chemical transformation from an Elephantopus scaber extract. Their inhibition activities against non-small-cell lung cancer cells were screened, and preliminary structure-activity relationships were also established. Among them, monomeric analog 1u and dimeric analog 3d exhibited superior anti-non-small-cell lung cancer cytotoxic potencies with IC50 values of 4.3 and 0.7 mu M against A549 cells, respectively, and were more active than cisplatin and the standard sesquiterpene lactones, parthenolide and scabertopin. Further studies revealed that compounds 1u and 3d cause G2/M phase arrest and induce apoptosis through the activation of mitochondrial pathways in A549 cells. Collectively, the results obtained suggest that compounds 1u and 3d are promising anti-non-small-cell lung cancer lead compounds.

Key words

APOPTOSIS/THERAPY/PATHWAY/DEATH/HL-60

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出版年

2022

Journal of natural products

CCR

ISSN：0163-3864

被引量4

参考文献量40

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