Precise discovery of a STAT3 inhibitor from Eupatorium lindleyanum and evaluation of its activity of anti-triple-negative breast cancer.

Natural Product Research
Bo YangHua Jun Zhao

Abstract

Michael reaction acceptors (MRAs) are a class of active compounds. There is a great prospect to screen STAT3 inhibitors from Eupatorium lindleyanum, furthermore, to discover lead compounds for anti-triple-negative breast cancer (TNBC). In this study, glutathione (GSH) was employed, and a UPLC-MS screening method was developed to discover MRAs. We screened MRAs which can inhibit STAT3 using a STAT3-dependent reporter system. Six sesquiterpene lactones, including a new compound Eupalinolide O (1), together with five known compounds, Eupalinolide I (2), Eupalinolide K (3), Eupalinolide H (4), Eupalinolide J (5) and Eupalinolide G (6) were isolated. Eupalinolide J was identified as MRA that decreased luciferase activity of STAT3. Preliminary activity assessment showed that Eupalinolide J could inhibit the viability of TNBC cell lines. We demonstrated that Eupalinolide J, which is a natural typical MRA, has a notable inhibition of STAT3 activity and a potential cytotoxic activity against TNBC cell lines.

References

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Citations

Jul 20, 2018·Chemistry, an Asian Journal·Abdul SadeerPak-Hing Leung
Mar 1, 2020·Cell Communication and Signaling : CCS·Jia-Hui MaXia Li
May 16, 2019·Journal of Experimental & Clinical Cancer Research : CR·Jiang-Jiang QinWei-Dong Zhang
Apr 2, 2019·Natural Product Research·Yong HouJunxing Dong
Nov 21, 2020·Neoplasia : an International Journal for Oncology Research·Zhihui ZhuHuajun Zhao
May 18, 2021·Chemistry & Biodiversity·Han ChenXiaoling Lu

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Methods Mentioned

BETA
NMR

Software Mentioned

GraphPad Prism

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