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Phytother Res. 2011 Nov;25(11):1732-5. doi: 10.1002/ptr.3514. Epub 2011 Apr 28.

Icariin induces the expression of toll-like receptor 9 in ana-1 murine macrophages.

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Guangxi Botanic Garden of Medicinal Plants, No. 189, Changgang Road, Nanning 530023, PR China.


Icariin is the major pharmacologically active compound of Herba epimedii which has been used as a tonic, aphrodisiac and an antirheumatic in traditional Chinese medicine. This study analysed the effect of icariin on the expression of Toll-like receptor 9 (TLR9) which plays an important role in regulation of the innate immune response. Stimulation of Ana-1 murine macrophages with icariin induced a significant dose-dependent expression of TLR9, and its mRNA expression which increased from 3 h post-treatment was approximately five-fold that of DMSO-treated cells. Several molecules, such as myeloid differentiation factor 88, tumor necrosis factor-α and interleukin 6, which are involved in the TLR9 downstream signaling pathway, were also significantly up-regulated in response to icariin stimulation. Our findings demonstrated that icariin is able to induce the expression of TLR9.

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