CAJ | 학술논문

以肌肽为原料,对伯氨基进行了结构修饰,合成了11种肌肽衍生物.化合物的结构经核磁共振、紫外-可见光谱及高分辨质谱分析确证.丙烯醛清除活性测试结果表明,在实验浓度下大部分化合物表现出一定的清除丙烯醛活性,尤其是化合物4k对丙烯醛的清除活性高于肌肽.脾细胞增殖活性测试结果表明,在实验浓度下大部分化合物表现出一定的脾细胞增殖活性,特别是化合物4b,4d和4k对脾细胞的增殖活性高于阳性对照伴刀豆球蛋白A.过氧化氢诱导血管内皮细胞损伤的预保护实验结果表明,在实验浓度下大部分化合物表现出一定的预保护作用,其中化合物4a,4j和4k对过氧化氢诱导血管内皮细胞损伤的预保护作用大于肌肽.血浆稳定性实验结果表明,与肌肽相比,11种化合物均具有很好的血浆稳定性.
이기태위원료,대백안기진행료결구수식,합성료11충기태연생물.화합물적결구경핵자공진、자외-가견광보급고분변질보분석학증.병희철청제활성측시결과표명,재실험농도하대부분화합물표현출일정적청제병희철활성,우기시화합물4k대병희철적청제활성고우기태.비세포증식활성측시결과표명,재실험농도하대부분화합물표현출일정적비세포증식활성,특별시화합물4b,4d화4k대비세포적증식활성고우양성대조반도두구단백A.과양화경유도혈관내피세포손상적예보호실험결과표명,재실험농도하대부분화합물표현출일정적예보호작용,기중화합물4a,4j화4k대과양화경유도혈관내피세포손상적예보호작용대우기태.혈장은정성실험결과표명,여기태상비,11충화합물균구유흔호적혈장은정성.
A series of carnosine derivatives were synthesized by modification of primary amino groups of carnosine, eleven target compounds were obtained and characterized by NMR, UV-Vis and HR-MS. Acrolein scavenging activity test results showed that most compounds exhibited some acrolein scavenging activities, es-pecially compound 4k showed the highest acrolein scavenging activity which was stronger than carnosine. Spleen cell proliferation test results showed that most compounds exhibited some spleen cell proliferation activi-ties, compounds 4b, 4d and 4k showed stronger spleen cell proliferation activities than the positive control conA. Hydrogen peroxide injury pre-protection results showed that most compounds exhibited some pre-protec-tion effects, especially compounds 4a, 4j and 4k showed stronger ECV-304 cell pre-protection effects than carnosine. Plasma stability assay results showed that compared with carnosine, eleven compounds had good plasma stability.