目的 基于FGFR1蛋白靶點(diǎn)篩選淫羊藿中抗骨質(zhì)疏松的藥效成分。方法 采用維甲酸灌胃14 d復(fù)制大鼠骨質(zhì)疏松模型，給予淫羊藿提取物進(jìn)行干預(yù)；采用Western blotting法檢測(cè)各組大鼠股骨FGFR1蛋白的表達(dá)，用UPLC-Q-TOF-MS確認(rèn)提取物中化學(xué)成分。基于FGFR1靶點(diǎn)進(jìn)行分子虛擬對(duì)接篩選藥效成分。結(jié)果 淫羊藿能夠改善大鼠骨質(zhì)疏松癥狀，并提高FGFR1蛋白的表達(dá)。淫羊藿提取物中指認(rèn)出23種化合物，其中淫羊藿苷、淫羊藿次苷I、箭藿苷C可與FGFR1可以有效對(duì)接。結(jié)論 淫羊藿中淫羊藿苷、淫羊藿次苷I、箭藿苷C可能通過(guò)上調(diào)FGFR1發(fā)揮抗骨質(zhì)疏松作用。

Objective To Screen the medicinal components of anti-osteoporosis in Epimedii Herba based on FGFR1. Methods The osteoporosis of rats was induced by given retinoic acid intragastrically for 14 d, and were treated with Epimedii Herba extract. The expression of FGFR1 protein in the femur was detected by Western blotting, and the chemical constituents of the extract were confirmed by UPLC-Q-TOF-MS method. The effective components were screened based on the target of FGFR1 by molecular docking. Results Epimedii Herba had a significant function of anti-osteoporosis, and could increase the expression of FGFR1 protein in rats. Icariin, icarisid I and sagittatoside C were picked out among the 23 identified compounds in extract, and could be effectively docked with FGFR1. Conclusion Icariin, icarisid I and sagittatoside C may play an anti-osteoporotic effect by up-regulating FGFR1.

國(guó)家科技支撐計(jì)劃項(xiàng)目（2011BAI07B08）；長(zhǎng)江學(xué)者和創(chuàng)新團(tuán)隊(duì)發(fā)展計(jì)劃資助項(xiàng)目（IRT_14R41）