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A new cytotoxic polycyclic polyprenylated acylphloroglucinol from Garcinia nujiangensis screened by the LC-PDA and LC-MS
Authors:Zhongyan Tang  Lihua Lu  Xiaoyong Zhou  Weiping Song  Yuedong Tang
Institution:1. Department of Emergency and Critical Care Medicine, Jin Shan Hospital, Fudan University, Shanghai, China;2. Department of Neonatology, Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, China
Abstract:Abstract

A new polycyclic polyprenylated acylphloroglucinol (1), nujiangefolin D, together with five known analogues (2–6), were isolated from the fruits of Garcinia nujiangensis. Compound 1 was screened by the LC-MS and LC-PDA. The structure of 1 was elucidated on the basis of extensive spectroscopic techniques including 1?D and 2?D NMR and MS analyses. The compounds isolated were evaluated for their cytotoxic activities against three cancer cell lines, 1 showed moderate cytotoxic activity against Hela, PANC-1, and MDA-MB-231 cell lines with IC50 values of 5.6?±?0.1, 9.1?±?0.2, and 8.3?±?0.2?μM, respectively. The antitumor mechanism was explained via virtual docking of 1 to the main sites in the human serine/threonine-protein kinase mTOR (mTOR) crystal structure (PDB code: 4DRI). Furthermore, 1 may inhibit Hela cell proliferation through mTOR by the western blotting analysis. Taken together, 1 may be a potential mTOR inhibitor used for the treatment of cervical cancer.
Keywords:Polycyclic polyprenylated acylphloroglucinol  cytotoxic  molecular docking  mTOR  Garcinia nujiangensis
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