Puerarin And Its Derivatives Synthesis And Preliminary Activity

Puerarin is one of the main active substances of Radix puerariae, its chemical name is 7, 4'-dihydroxy-8-C-β-D-glucopyranosy1- isoflavone,which has comprehensive pharmacological activities and has been mainly used to treat cardiovascular and cerebrovascular diseases. Puerarin is obtained from natural resources.In this thesis, three total synthetic routes of puerarin was explored and twelve intermediates were synthesized. The synthetic method of A3 had been improved and its yield had been increased. Simultaneously,the synthetic method of B4 had been studied and optimized. Therefore, the practical basis were provided for the further studies of the synthesis of puerarin.A series of new compounds were designed to improve the water-solubility of Puerarin, whose 4'-hydroxy were substituted by alkyl-amino-alkyl groups. Twelve of derivatives were synthesized from puerarin which first reacted with 1,3-dibromopropane and then with amines in two steps.The structures of these compounds were identified by 1HNMR and MS(FAB). Anti-hypoxic effects were evaluated in mice, the results indicated that all compounds expect P12 had certain anti-hypoxic effects under the same dosages. Furthermore, the effects of P1, P3, P4, P7 and P10 were stronger than that of puerarin, and among them P4 was the best.The vasodilator effects of 5 compounds (P1-P6) were evaluated in the trial on rat isolated aortic rings, the results indicated that all compounds expect P3 had significant vasodilator effects. Under the concentration of 10μg/ml, the vasodilator effects of P1, P2 and P5 were stronger than that of puerarin, while the concentration rose to 20μg/ml, only P1 and P2 were stronger and P1 was the best.In conclusion, P1, P2, P3, P4, P5, P7 and P10 were worth to be studied...