Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90

<i>Ginkgo biloba</i> L. has been used in traditional Chinese medicine (TCM) for thousands of years. However, the anti-cancer properties of ginkgolic acids (GAS) isolated from <i>G. biloba</i> have not been investigated in human nasopharyngeal carcinoma cells. In this study, G...

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Autores principales:	Hong-Mei Li, Hui Ma, Xiaolong Sun, Bohan Li, Chengjiang Cao, Yiqun Dai, Meilin Zhu, Cheng-Zhu Wu
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	ginkgolic acids Hsp90 nasopharyngeal carcinoma migration invasion apoptosis Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/1df063679ebf4c5bab5e7df5f2421cd2
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id	oai:doaj.org-article:1df063679ebf4c5bab5e7df5f2421cd2
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spelling	oai:doaj.org-article:1df063679ebf4c5bab5e7df5f2421cd22021-11-11T18:33:45ZAnti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 9010.3390/molecules262165751420-3049https://doaj.org/article/1df063679ebf4c5bab5e7df5f2421cd22021-10-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6575https://doaj.org/toc/1420-3049<i>Ginkgo biloba</i> L. has been used in traditional Chinese medicine (TCM) for thousands of years. However, the anti-cancer properties of ginkgolic acids (GAS) isolated from <i>G. biloba</i> have not been investigated in human nasopharyngeal carcinoma cells. In this study, GAS exhibited an inhibitory effect on the ATPase activity of heat shock protein 90 (Hsp90) and anti-proliferative activities against four human cancer cell lines, with IC<sub>50</sub> values ranging from 14.91 to 23.81 μg·mL<sup>−1</sup>. In vivo experiments confirmed that GAS inhibited tumor growth in CNE-2Z cell-xenografted nude mice with low hepatotoxicity. We further demonstrated that GAS suppressed migration and invasion and induced the apoptosis of CNE-2Z cells by inducing the degradation of Hsp90 client proteins (MMP-2, MMP-9, Her-2, c-Raf, Akt, and Bcl-2). Together, GAS are new Hsp90 inhibitors by binding to Hsp90 (hydrogen bond and hydrophobic interaction). Thus, GAS from <i>G. biloba</i> might represent promising Hsp90 inhibitors for the development of anti-nasopharyngeal carcinoma agents.Hong-Mei LiHui MaXiaolong SunBohan LiChengjiang CaoYiqun DaiMeilin ZhuCheng-Zhu WuMDPI AGarticleginkgolic acidsHsp90nasopharyngeal carcinomamigrationinvasionapoptosisOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6575, p 6575 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	ginkgolic acids Hsp90 nasopharyngeal carcinoma migration invasion apoptosis Organic chemistry QD241-441
spellingShingle	ginkgolic acids Hsp90 nasopharyngeal carcinoma migration invasion apoptosis Organic chemistry QD241-441 Hong-Mei Li Hui Ma Xiaolong Sun Bohan Li Chengjiang Cao Yiqun Dai Meilin Zhu Cheng-Zhu Wu Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90
description	<i>Ginkgo biloba</i> L. has been used in traditional Chinese medicine (TCM) for thousands of years. However, the anti-cancer properties of ginkgolic acids (GAS) isolated from <i>G. biloba</i> have not been investigated in human nasopharyngeal carcinoma cells. In this study, GAS exhibited an inhibitory effect on the ATPase activity of heat shock protein 90 (Hsp90) and anti-proliferative activities against four human cancer cell lines, with IC<sub>50</sub> values ranging from 14.91 to 23.81 μg·mL<sup>−1</sup>. In vivo experiments confirmed that GAS inhibited tumor growth in CNE-2Z cell-xenografted nude mice with low hepatotoxicity. We further demonstrated that GAS suppressed migration and invasion and induced the apoptosis of CNE-2Z cells by inducing the degradation of Hsp90 client proteins (MMP-2, MMP-9, Her-2, c-Raf, Akt, and Bcl-2). Together, GAS are new Hsp90 inhibitors by binding to Hsp90 (hydrogen bond and hydrophobic interaction). Thus, GAS from <i>G. biloba</i> might represent promising Hsp90 inhibitors for the development of anti-nasopharyngeal carcinoma agents.
format	article
author	Hong-Mei Li Hui Ma Xiaolong Sun Bohan Li Chengjiang Cao Yiqun Dai Meilin Zhu Cheng-Zhu Wu
author_facet	Hong-Mei Li Hui Ma Xiaolong Sun Bohan Li Chengjiang Cao Yiqun Dai Meilin Zhu Cheng-Zhu Wu
author_sort	Hong-Mei Li
title	Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90
title_short	Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90
title_full	Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90
title_fullStr	Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90
title_full_unstemmed	Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90
title_sort	anti-cancer properties of ginkgolic acids in human nasopharyngeal carcinoma cne-2z cells via inhibition of heat shock protein 90
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/1df063679ebf4c5bab5e7df5f2421cd2
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Anti-Cancer Properties of Ginkgolic Acids in Human Nasopharyngeal Carcinoma CNE-2Z Cells via Inhibition of Heat Shock Protein 90

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