SMA SMA-copolymer conjugates of AHPP: a polymeric inhibitor of xanthine oxidase with therapeutic potentials against hypertension

摘要

4-amino-6-hydroxypyrazolo[3,4-d]pyrimidine (AHPP) is a potent inhibitor of xanthine oxidase (XO) and showed remarkable antihypertensive effect. However, its poor water-solubility hampers its therapeutic application. In this study we prepared a water soluble polymeric conjugates of AHPP, by using a styrene maleic acid copolymer (SMA, SMA-AHPP), which showed similar inhibitory activity against XO comparable to parental AHPP. Upon intravenously injection or oral administration of SMA-AHPP blood pressures of SHR rats significantly reduced, which continued for at least 24 h. These findings strongly suggest the potential value of SMA-AHPP as an antihypertensive agent.