摘要
目的:研究传统中药材全蝎三种热稳定性多肽BmKcug2、BmKcug2-P1 和Martentoxin-P2 的消化酶抗性.方法:结合重组表达、消化酶耐受实验、高效液相色谱技术及结构分析,评价多肽BmKcug2、BmKcug2-P1 和Martentoxin-P2 的肠胃蛋白酶稳定性.结果:多肽BmKcug2 对胃蛋白酶、胰蛋白酶、α-胰凝乳蛋白酶都有很好的稳定性;多肽BmKcug2-P1 对胃蛋白酶稳定性较好,对胰蛋白酶也具有一定的抗性,但对α-胰凝乳蛋白酶稳定较差;多肽Martentoxin-P2 的酶稳定性谱与BmKcug2-P1 类似.结论:本研究发现了全蝎毒腺中存在多肽能够耐受肠胃蛋白酶的消化作用,阐明了全蝎毒腺中多肽的消化酶稳定性,为深入研究全蝎中有效药用成分提供了思路,为系统研究全蝎多肽活性成分和口服给药途径之间的关系奠定了基础.
Abstract
Objective To investigate the digestive enzyme resistance of three thermostable peptides(BmKcug2,BmKcug2-P1,and Martentoxin-P2)from Scorpio,a traditional Chinese medicinal material.Methods The stability of BmKcug2,BmKcug2-P1,and Martentoxin-P2 for gastrointestinal proteases was evaluated using recombinant expression,digestive en-zyme tolerance assay,high-performance liquid chromatography,and structural analysis.Results BmKcug2 showed good stability for gastric protease,pancreatic protease,and α-chymotrypsin.BmKcug2-P1 exhibited good stability for gastric protease and certain resistance to trypsin,but poor stability for α-chymotrypsin.Martentoxin-P2 had similar enzyme stabil-ity profile to that of BmKcug2-P1.Conclusion This paper discovered peptides in the venom glands of Scorpio that with-stand the digestive effects of gastrointestinal proteases.It elucidated the stability of the peptides for digestive enzymes,pro-viding ideas for in-depth research on effective ingredients in Scorpio.Additionally,the paper laid the foundation for system-atic research on the relationship between active ingredients of peptides from Scorpio and oral administration pathways.
基金项目
国家自然科学基金青年基金(82204602)
湖北省自然科学基金青年基金(2022CFB956)
湖北医药学院人才启动金项目(2021QDJZR022)