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Bioorganic & Medicinal Chemistry Letters
Volume 39, 2021, 127915

Evaluation of the antiproliferative activity of 106 marine microbial metabolites against human lung cancer cells and potential antiproliferative mechanism of purpuride G

Hengju Gea, Muran Shia,c, Xiao-Yuan Lianb, Zhizhen Zhanga

Ocean College, Zhoushan Campus, Zhejiang University, Zhoushan 316021, China.

Abstract

A total of 106 marine microbial metabolites were evaluated for their antiproliferative activity against human lung cancer cells. Results showed that 23 compounds exhibited activity in inhibiting the proliferation of A549 and H157 cells with IC50 values ranging from 1.5 to 48.2 μM. Pyrrospirone F, chrysophanol, physcion, and purpuride G are the four most active compounds with IC50 values of 1.5–7.3 μM. Further investigation of purpuride G (a newly discovered sesquiterpene lactone) demonstrated its potent antiproliferative activity against six different lung cancer cells of A549, H157, H460, H1299, H1703, and PC9 with IC50 values of 2.1–3.3 μM. The antiproliferative activity of purpuride G against cancer cells is related to block cell cycle, induce apoptosis through regulating the apoptotic proteins Bcl-2 and Bax, and inhibit glycolysis by downregulating two key glycolytic enzymes of hexokinase 2 and pyruvate kinase M2.

Keywords: Marine microbial metabolites, Antiproliferative activity, Purpuride G, Cell cycle arrest, Apoptosis and apoptotic proteins, Glycolysis inhibition.

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