Article ID Journal Published Year Pages File Type
2540804 International Immunopharmacology 2014 8 Pages PDF
Abstract

•The anti-tumor effect of WLIP was found for the first time.•The molecular docking result showed that PPAR-γ might be the potential anti-tumor target of WLIP.•The anti-tumor effect of WLIP might be mediated through modulation of PPAR-γ activation pathway.•WLIP was able to down-regulate the expression of Bcl-xL, Cyclin-D1 in K562 cells.

White-line-inducing principle (WLIP), a lipodepsipeptide isolated from Lasiosphaera fenzlii Reich., which is one of the puffballs, for the first time, has been reported to exhibit anti-microbial activity. However, there are no reports regarding the anti-tumor effects of WLIP. In this study, we reported the anti-cancer effects of WLIP on K562 cells, and its potential effect on the PPAR-γ activation pathway. The obtained results showed that WLIP exerted strong anti-proliferative effect on K562 cells. Moreover, WLIP was found to increase apoptosis and induce G0/Gl arrest. Modeling results from the Surflex-Dock program suggested that PPAR-γ might be the potential anti-tumor target of WLIP, which was confirmed by the experiments that WLIP increased the activity in luciferase reporter assay and the expression of PPAR-γ in Western blot. Besides, WLIP was able to down-regulate the expression of Bcl-xL, Cyclin-D1 in K562 cells. In summary, our novel observations suggested that WLIP might have a potential implication in cancer prevention and treatment, and also showed for the first time that the anti-tumor effect of WLIP might be mediated through modulation of the PPAR-γ activation pathway.

Graphical abstractWhite-line-inducing principle (WLIP), a lipodepsipeptide isolated from Lasiosphaera fenzlii Reich., might have a potential implication in cancer prevention and treatment. And it also showed for the first time that the anti-tumor effect of WLIP might be mediated through modulation of the PPAR-γ activation pathway.Figure optionsDownload full-size imageDownload as PowerPoint slide

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