A new cytotoxic polycyclic polyprenylated acylphloroglucinol from Garcinia nujiangensis screened by the LC-PDA and LC-MS.
Autor: Tang, Zhongyan; Lu, Lihua; Zhou, Xiaoyong; Shen, Jie; Song, Weiping; Tang, Yuedong; Xia, Zhengxiang
Publication year: 2020
Natural product research
issn:1478-6427 1478-6419
doi: 10.1080/14786419.2018.1539983
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 IC(50) 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.
Language: eng
Rights:
Pmid: 30623680
Tags: Humans; Female; Cell Line, Tumor; Cell Proliferation/drug effects; Drug Screening Assays, Antitumor; Fruit/chemistry; Molecular Structure; Mass Spectrometry; Chromatography, Liquid; Antineoplastic Agents, Phytogenic/*isolation & purification/pharmacology; Molecular Docking Simulation; molecular docking; cytotoxic; Garcinia nujiangensis; Garcinia/*chemistry; mTOR; Phloroglucinol/analogs & derivatives/*isolation & purification/toxicity; Polycyclic polyprenylated acylphloroglucinol; TOR Serine-Threonine Kinases/antagonists & inhibitors; Uterine Cervical Neoplasms/drug therapy
Link: https://pubmed.ncbi.nlm.nih.gov/30623680/
