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
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Acceso en línea:https://doaj.org/article/1df063679ebf4c5bab5e7df5f2421cd2
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Sumario:<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.