川芎嗪和灯盏乙素是从云贵地区特有的植物川芎和灯盏细辛中提取分离得到。川芎嗪具有防治脑缺血和溶栓活性，灯盏乙素苷元在临床上广泛用于治疗心脑血管疾病，具有自由基清除活性。二者在临床应用中的共同缺点为生物利用度低。本项目拟在前期研究基础上，进一步优化孪药。具体是将川芎嗪和灯盏乙素苷元通过L-氨基酸拼合在同一化学实体中，合成具有溶栓和自由基清除双重活性的抗缺血性脑卒中孪药，发挥二者协同作用的同时克服各自的缺陷。项目拟通过研究目标化合物对损伤神经细胞的保护作用，抗血小板聚集活性，以及脑缺血再灌注损伤的保护作用，发现效果最优的孪药，为创制自主知识产权的新型缺血性脑卒中治疗药物奠定理论和实践基础，推进贵州特色药材川芎和灯盏细辛的中药现代化进程。

The low bioavailability is the main factors affecting the clinical curative effect of Tertramethylpyrazine, which has strong thrombolytic activity, and Scutellarein with potent free radical scavenging activity. There are not twin drug design reports about Tertramethylpyrazine and Scutellarin before the project. This project intends to design and synthesis twin drug by combining Tertramethylpyrazine and Scutellarin into a chemical entity through L-amino acid, base upon twin drug mechanism. The model of H2O2-induced cortical neuronal cell.injury, ADP-induced platelet aggregation and a rat Middle Cerebral Artery Occlusion (MCAO) stroke will be used to evaluate free radical scavenging and thrombolytic activity respectively. This project intend to discover prodrugs which have significant thrombolytic activity and free radical scavenging activity, so as to lay the bases for the theory and practice for creating novel antiischemic stroke twin drug, promote modernization process of Ligusticum chuanxiong Hort. and Erigerm breviscapus.