摘要
目的 :研究硝基精氨酸赖氨酸三肽对组成型一氧化氮合酶 (c NOS)和诱导型一氧化氮合酶 (i NOS)的抑制程度。方法 :1用大鼠腹腔巨噬细胞作培养 ,检测硝基精氨酸赖氨酸三肽对 i NOS的抑制程度。 2用大鼠离体主动脉条孵育 ,检测硝基精氨酸赖氨酸三肽对 c NOS的抑制程度。结果 :1硝基精氨酸赖氨酸三肽(1× 10 - 4 mol/ L)可显著抑制大鼠腹腔巨噬细胞产生一氧化氮 (NO,P<0 .0 1) ,较 NG硝基 L 精氨酸(L NNA)作用增强 (P<0 .0 1)。 2硝基精氨酸赖氨酸三肽 (1× 10 - 4 mol/ L)可显著减少大鼠腹腔巨噬细胞内环磷酸鸟苷 (c GMP)水平 (P<0 .0 1) ,较 L NNA作用增强 (P<0 .0 5 )。 3与 L NNA相比 ,硝基精氨酸赖氨酸三肽 (1.5× 10 - 4 mol/ L )对大鼠主动脉壁 c NOS的抑制程度减小 (P<0 .0 5 )。结论 :1硝基精氨酸赖氨酸三肽抑制大鼠腹腔巨噬细胞内 i NOS活性显著强于 L NNA,而抑制大鼠血管壁 c NOS活性显著弱于 L NNA。
Objective:To investigate the inhibitory effect of a new highly selective inducible nitric oxide synthase (iNOS) inhibitorN Gnitroargininelysine tripeptide on cNOS and iNOS induction.Methods:Rat peritoneal macrophages were cultured to test the inhibitory effect of the tripeptide on iNOS.Also,rat isolated aortic slices were incubated to test the inhibitory effect of the tripeptide on cNOS.Results:The new synthetic tripeptide (1×10 -4 mol/L) could significantly inhibit nitric oxide production in peritoneal macrophages ( P <0 01),and it had strong inhibitory effect compared to LNNA ( P <0 01).Meanwhile,the tripeptide (1×10 -4 mol/L) could significantly reduce the cGMP level in peritoneal macrophages ( P <0 01),and the effect was more potent than LNNA( P <0 05).Compared with LNNA,however,the new synthetic tripeptide (1 5×10 -4 mol/L) had less inhibitory effect on cNOS of rat aorta ( P <0 05).Conclusions:The synthetic tripeptide showed strong inhibitory effect on iNOS in peritoneal macrophages,and only a weak influence on cNOS of rat aorta compared with LNNA.
出处
《中国危重病急救医学》
CAS
CSCD
2000年第12期742-744,共3页
Chinese Critical Care Medicine
基金
国家新药研究与开发基金资助项目(No.96-901-05-44)