Attenuation of LPS-induced inflammation by ICT, a derivate of icariin, via inhibition of the CD14/TLR4 signaling pathway in human monocytes

作者:Wu, Jinfeng; Zhou, Junmin; Chen, Xianghong; Fortenbery, Nicole; Eksioglu, Erika A.; Wei, Sheng*; Dong, Jingcheng
来源:International Immunopharmacology, 2012, 12(1): 74-79.
DOI:10.1016/j.intimp.2011.10.015

摘要

Objective: To evaluate the anti-inflammatory potential of ICT in LPS stimulated human innate immune cells. Background: 3, 5, 7-Trihydroxy-4'-methoxy-8-(3-hydroxy-3- methylbutyl)-flavone (ICT) is a novel derivative of icariin, the major active ingredient of Herba Epimedii, an herb used in traditional Chinese medicine. We previously demonstrated its anti-inflammatory potential in a murine macrophage cell line as well as in mouse models. Methods: We measured TNF-alpha production by ELISA, TLR4/CD14 expression by flow cytometry, and NF-kappa B and MAPK activation by western blot all in LPS-stimulated PBMC, human monocytes, or THP-1 cells after treatment with ICT. Results: ICT inhibited LPS-induced TNF-a production in THP-1 cells, PBMCs and human monocytes in a dose-dependent manner. ICT treatment resulted in down-regulation of the expression of CD14/TLR4 and attenuated NF-kappa B and MAPK activation induced by LPS. Conclusion: We illustrate the anti-inflammatory property of ICT in human immune cells, especially in monocytes. These effects were mediated, at least partially, via inhibition of the CD14/TLR4 signaling pathway.