Abstract:
A new triterpenoid compound 1* (scandine A1) was obtained from 95% ethanol extract of Uncaria laevigata. Meanwhile, eleven described compounds were also isolated for the first time from Uncaria laevigata. Herein, compound 2 exhibited strong diastolic cardio-cerebrovascular activity (EC50BA = 9.22 μM and EC50CA = 14.65 μM), which was not been previously described. Compound 1* also showed certain diastolic cardio-cerebrovasculary activity. Network pharmacology indicated that the diastolic cardio-cerebrovascular activity of compound 2 was most correlated with the Ras signalling pathway. Molecular docking confirmed that it exhibited strong binding activity with target protein (matrix metalloproteinase inhibitor-1). Moreover, compound 2 demonstrated significant potential on cardio-cerebrovascular activity in vitro. Overall, compounds 1* and 2 with good diastolic cardio-cerebrovascular activity were discovered in this work.
摘要:
从钩藤的95%乙醇提取物中获得了新的三萜化合物1*(scandineA1)。同时,还首次从Uncarialaevigata中分离出11个所述化合物。在这里,化合物2表现出强烈的舒张性心脑血管活动(EC50BA=9.22μM和EC50CA=14.65μM),这是以前没有描述过的。化合物1*还显示出一定的舒张心脑血管活性。网络药理学表明,化合物2的舒张性心脑血管活性与Ras信号通路最相关。分子对接证实其表现出与靶蛋白(基质金属蛋白酶抑制剂-1)的强结合活性。此外,化合物2在体外显示了对心脑血管活性的显着潜力。总的来说,在这项工作中发现了具有良好舒张心脑血管活性的化合物1*和2。