一个新的过氧化物酶模拟物的合成及抗白内障活性研究

白内障是当今世界上主要的致盲眼病之一，其患病人数每年呈上升趋势．由于白内障的氧化损伤机理已越来越为人们所认识，各种抗氧化剂类物质已被用于白内障的预防和治疗．然而，目前所有这些药物均未达到令人满意的效果．最近几年酶学活性的抗氧化剂的开发越来越受到重视．由细胞色素C水解得到的微酶MP-8，MP-9和MP-11是较好的过氧化物酶模拟物，在眼晶状体白内障模型中验证了其抗白内障作用．但该化合物不易制备，体内易降解，需要更好的模拟酶用于抗白内障药物开发和形成机理研究．

Synthesis and Anti-cataract Activity of a Novel Peroxidase Mimetics

Cataracts are one of the most important causes of blindness. As the mechanism of oxidative damage to cataracts was understood, anti-oxidants, especially peroxidase mimetics, were used to develop the agents to protect the eye and cure cataracts. We have designed and synthesized a nonapeptide (DhHP-6) containing deuterohaemin and histidine, which showed a peroxidase activity by degrading H2O2 and tert-butyl hydroxyl radical in ascorbate-specific peroxidase test. The specific activity is 4.0×103 U/μmol with H2O2 and ascorbate as the substrate. DhHP-6 is capable of protecting cultured rat lenses from cataracts induced by galactose. In the absence of the DhHP-6 big change on lenses was observed.