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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 are highly bioactive and have high selectivity for drug targets. They have good development prospects in the treatment of diseases such as neuropathic pain. Natural conotoxins, however, are susceptible to proteolysis in the body. Cyclization can increase their stability in the human body and thus have oral activity. In this paper, the stability and activity changes of α-conotoxin Vc1.1 and MII after cyclization, cyclization synthesis method as an example, the progress of conotoxin cyclization research are summarized, indicating that the cyclized conotoxin will It may play an important role in the treatment of diseases such as neuropathic pain.