芋螺毒素的环化研究  

Studies on cyclization of conotoxins

作　　者：林波[1] 高炳淼[1] 孟海玲[1] 邴晖[1] 吴勇[1] 长孙东亭[1] 罗素兰[1] 

机构地区：[1]海南大学热带生物资源教育部重点实验室海口市海洋药物重点实验室,海南海口570228

出　　处：《中国海洋药物》2014年第1期70-74,共5页Chinese Journal of Marine Drugs

基　　金：国家高技术研究发展计划(2012AA021706);国家国际科技合作专项(2011DFR31210);长江学者和创新团队发展计划(IRT1123);海南省社会发展科技专项(SF201328);海南省自然科学基金(313047)资助

摘　　要：芋螺毒素生物活性强,对药物作用靶点的选择性高,在治疗神经性疼痛等疾病方面具有很好的开发前景。然而天然芋螺毒素容易受到体内蛋白酶的水解。将其进行环化,可增加它们在人体内的稳定性,从而具有口服活性。本文以α-芋螺毒素Vc1.1和MII环化后的稳定性与活性变化、环化的合成方法为例,对芋螺毒素的环化研究进展进行综述,说明环化的芋螺毒素将有可能在治疗神经性疼痛等疾病中扮演一个重要的角色。Conotoxins have high activity and selectivity at their targets, which has potential for the treatment of neuropathic pain and other diseases. However their potential as therapeutics is limited by their susceptibility to degradation. The stability of conopeptides could be increased by cyclizing, and cyclized conotoxins showed oral therapeutic activity. This review focuses on the development of conotoxin cyclization through cyclization of alpha-conotoxins Vcl. 1 and MII, indicates that cyclization of eonotoxins may play an important role in the treatment of neuropathic pain and other diseases.

关 键 词：芋螺毒素 环化 稳定性 口服活性 

分 类 号：R965[医药卫生—药理学]