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| 硝基精氨酸—赖氨酸三肽合成及其对一氧化氮合酶的抑制作用 | |
| 引用本文： | 杨军珂,吴赛珠,周可祥,彭师奇,孟素荣,吴宗贵,阮云军,董凤英. 硝基精氨酸—赖氨酸三肽合成及其对一氧化氮合酶的抑制作用[J]. 中国药物化学杂志, 2001, 11(1): 13-16 |
| 作者姓名： | 杨军珂 吴赛珠 周可祥 彭师奇 孟素荣 吴宗贵 阮云军 董凤英 |
| 作者单位： | 1. 第一军医大学南方医院心内科，广东 广州 510515 2. 北京医科大学药学院中德联合实验室，北京 100853 3. 第二军医大学长征医院心内科，上海 200003 |
| 基金项目： | 国家新药研究与开发基金“抗败血性休克的NOS拮抗剂设计与筛选”项目的资助（96-901-05-44） |
| 摘 要： | 液相合成法合成了由左旋精氨酸、左旋赖氨酸组成的硝基精氨酸-赖氨酸三肽HCl．Arg(NO |
| 关 键 词： | 一氧化氮 一氧化氮合酶 一氧化氮合酶抑制剂 硝基精氨酸－赖氨酸三肽 |
| 文章编号： | 1005-0108(2001)01-0013-04 |
Synthesis ofNG-nitro-Arginine-Lysine Tripeptide and Its Inhibition on NOS |
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| YANG Jun ke ,WU Sai zhu ,ZHOU Ke xiang ,PENG Shi qi ,MENG Su rong ,WU Zong gui ,RUAN Yun jun ,DONG Feng ying. Synthesis ofNG-nitro-Arginine-Lysine Tripeptide and Its Inhibition on NOS[J]. Chinese Journal of Medicinal Chemistry, 2001, 11(1): 13-16 | |
| Authors: | YANG Jun ke WU Sai zhu ZHOU Ke xiang PENG Shi qi MENG Su rong WU Zong gui RUAN Yun jun DONG Feng ying |
| Affiliation: | YANG Jun ke 1,WU Sai zhu 1,ZHOU Ke xiang 1,PENG Shi qi 2,MENG Su rong 1,WU Zong gui 3,RUAN Yun jun 1,DONG Feng ying 1 |
| Abstract: | A new tripeptide HCl．Arg(NO2)-Lys(OCH3)-Arg(NO2)·HCl containingL-Arginine and L-Lysine was synthesized by the solusion phase synthesis,the inhibition of the target compound on cNOS and iNOS were studied too.Results of rat peritoneal macrophage culture were:The target compound(10-4 mol/L)could significantly inhibit macrophages to produce NO(P＜0.01),and had more potency than L-NNA(P＜0.01);it could also significantly reduce the level of cGMP in macrophages(P＜0.01),and had more potency than L-NNA(P＜0.05).Results of rat isolated aortic ring incubation was:The target compound(1.5×10-4 mol/L)played less inhibitory role in cNOS of rat aorta,compared with L-NNA(P＜0.05).It is clear by the activity experiment,that the target compound inhibits iNOS in rat peritoneal macrophages more potently than L-NNA and inhibits cNOS less potently than L-NNA. |
| Keywords: | nitric oxide nitric oxide synthase nitric oxide synthase inhibitor N G nitro arginine lysine tripeptide |
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