岭南中药江南卷柏Selaginella moellendorffii具有“清热凉血”功能，临床适用于血小板减少症，疗效确切，药效物质基础尚不明确。血小板生成素(TPO) 受体是血小板减少症治疗的关键靶点，TPO受体激动剂可特异性结合于骨髓巨核细胞，促进血小板生成。前期研究发现江南卷柏中C3’-C8连接方式的双黄酮类化合物具有显著促进人巨核细胞Dami增殖分化、激动TPO受体等生物活性，为首次发现的天然药物来源非肽类TPO受体激动剂，优选化合物amentoflavone口服给药，可显著减轻和缩短注射卡铂导致小鼠血小板减少程度和时间。本课题拟进一步对卷柏属药用植物双黄酮类化合物进行高效分离及结构鉴定，并对该类化合物进行结构修饰及构效关系研究，探讨C3’-C8双黄酮类衍生物的TPO受体激动作用及治疗化疗导致血小板减少症作用机制，为新型基于TPO受体激动的血小板减少症治疗药物发现奠定研究基础。

Selaginella moellendorffii, a traditional Chinese Medicine in Lingnan area of China, can effectively promote blood circulation and alleviate edema dredge, and cool blood to stop bleeding. However, the active chemical components have not been clarified. Thrombopoietin receptor (TPOR) is the key target in treating thrombocytopenia, and its agonists can specifically bind to TPOR to promote the platelet (PLT) generation. In this study, the bioflavonoids with C3’-C8 linkage isolated in S. moellendorffii were firstly discovered as the natural occurring TPOR agonist of non-peptide, and to have the abilities of promoting the proliferation and differentiation of Dami cells, and activating TPOR. Among these bioflavonoids, the major bioflavonoid component, amentoflavone (AMF), exhibited the best effect. Oral administration of AMF can significantly improve thrombocytopenia induced by carboplatin, which may through activating TPOR. Therefore, in order to lay the foundation for the discovery of novel TPOR agonists for treating chemotherapy-induced thrombocytopenia (CIT), sufficient bioflavonoids in Selaginella genus will be continuing isolated and identified. Also, structure modification of bioflavonoids will be conducted to discuss the structure activity relationships on TPOR, and the bonding form of candidate compounds towards to TPOR will be studied.