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N-取代肌肽酰胺类衍生物的合成及生物活性

臧皓 孙佳明 黄晓光 纪扬 代婷婷 高晓晨 李晓东 张辉

高等学校化学学报Issue(12):2567-2579,13.
高等学校化学学报Issue(12):2567-2579,13.DOI:10.7503/cjcu20140395

N-取代肌肽酰胺类衍生物的合成及生物活性

Synthesis and Biological Activity of N-substituted Carnosine Amide Derivatives

臧皓 1孙佳明 1黄晓光 2纪扬 2代婷婷 1高晓晨 1李晓东 2张辉1

作者信息

  • 1. 长春中医药大学中医药与生物工程研发中心,长春130117
  • 2. 吉林省博大伟业制药有限公司,长春130117
  • 折叠

摘要

Abstract

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.

关键词

肌肽衍生物/丙烯醛清除/脾细胞增殖/过氧化氢损伤预保护/血浆稳定性

Key words

Carnosine derivative/Acrolein scavenging/Spleen cell proliferation/Hydrogen peroxide injury protection/Plasma stability

分类

化学化工

引用本文复制引用

臧皓,孙佳明,黄晓光,纪扬,代婷婷,高晓晨,李晓东,张辉..N-取代肌肽酰胺类衍生物的合成及生物活性[J].高等学校化学学报,2014,(12):2567-2579,13.

基金项目

国家自然科学基金(批准号:81373936)、吉林省科技发展计划项目(批准号:20140203015YY)和吉林省教育厅“双十”培育项目(批准号:吉教科合字[2014]第71号)资助.覮 Supported by the National Natural Science Foundation of China(No.81373936), the Science and Technology Development Funds of Jilin Province, China(No.20140203015YY) and the “Double Ten” Development Project of Jilin Province Department of Education, China(No. Ji-JiaoKeHeZi[2014]No.71) (批准号:81373936)

高等学校化学学报

OA北大核心CSCDCSTPCD

0251-0790

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