Department of Pharmacy, General Hospital of Shenyang Military Area Command, Shenyang 110840, China; School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
Int Immunopharmacol. 2014 Mar;19(1):37-44. doi: 10.1016/j.intimp.2013.12.026. Epub 2014 Jan 5.
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.
白线性诱导因子（WLIP）是从马勃菌属真菌Lasiosphaera fenzlii Reich. 中分离得到的一种脂肽，它首次被报道具有抗菌活性。然而，目前尚无关于 WLIP 抗肿瘤作用的报道。在本研究中，我们报道了 WLIP 对 K562 细胞的抗癌作用及其对 PPAR-γ 激活途径的潜在影响。结果表明，WLIP 对 K562 细胞表现出强烈的增殖抑制作用。此外，WLIP 被发现能诱导细胞凋亡和 G0/G1 期阻滞。Surflex-Dock 程序的建模结果表明，PPAR-γ 可能是 WLIP 的潜在抗肿瘤靶点，这一结果在荧光素酶报告基因检测和 Western blot 中 PPAR-γ 表达的实验中得到了证实。此外，WLIP 能够下调 K562 细胞中 Bcl-xL 和 Cyclin-D1 的表达。总之，我们的新发现表明，WLIP 可能在癌症的预防和治疗中具有潜在的应用价值，这也是首次表明 WLIP 的抗肿瘤作用可能是通过调节 PPAR-γ 激活途径介导的。
