摘要
目的建立从中药中高效精准鉴定靶向核受体RXRα的天然活性成分的方法。方法通过受体-配体识别结合的原理,将中药淫羊藿抗炎活性馏分与核受体RXRα蛋白共同孵育,捕获配体小分子,利用高效液相色谱仪、核磁和质谱识别并鉴定配体化合物,生物学技术手段进行化合物活性验证。结果从淫羊藿抗炎馏分中快速筛选出核受体蛋白RXRα的小分子配体宝藿苷Ⅰ,生物学活性测试显示该配体化合物能够有效抑制细胞炎症反应,且具有RXRα依赖性。结论受体-配体识别法能够有效鉴定淫羊藿抗炎馏分中靶向核受体RXRα的活性小分子,该法为天然产物和中药活性成分的精准鉴定提供新的思路,为新型RXRα天然小分子调节剂的快速筛选起到促进作用。
Objective To establish a method that can accurately and efficiently screen potential pharmaceutical agents targeting Nuclear Receptor Retinoid X receptor-a （RXRa） from Traditional Chinese Medicine. Methods Based on the principle of Receptor- Ligand Recognition,the fusion protein of His-RXRaLBD and the active fractions were mixed to incubate for capturing and identif-ying potential ligand of RXRa？and then the identified ligand was evaluated for RXRa-dependent anti- inflammation effect. Results Baohuoside I from Epimedium brevicornum Maxim, was identified as a RXRa binder,and could induce RXRa-dependent anti- in-flammation effect. Conclusion The method was an efficient strategy to accurately identify active compounds from natural products, to expedite the discovery of natural RXRa regulator,and also to share the thought with other receptors in identifying ligand.
出处
《国际检验医学杂志》
CAS
2017年第23期3245-3248,共4页
International Journal of Laboratory Medicine
关键词
RXRα
受体-配体识别
淫羊藿
宝藿苷Ⅰ
抗炎
RXRa
receptor-Ligand Recognition
epimedium brevicornum maxim
baohuoside I
anti-inflammation
