CAJ | 학술논문

目的评价特异性cGMP依赖性蛋白激酶G(PKG)抑制剂(D)-DT-2对内毒素(LPS)孵育大鼠胸主动脉血管环收缩功能的影响.方法实验Ⅰ 取SD大鼠胸主动脉血管环,采用随机数字表法分为3组(n=5):KH液组、DT2组和DDT2组,用50 μmol/L 8-Br-cGMP孵育25 min后加入上述各药,比较各组血管环的张力变化.实验Ⅱ 将SD大鼠胸主动脉血管环,采用随机数字表法分为4组(n=5):对照组、LPS组、LPS-DT2组和LPS-DDT2组,在体外测定LPS孵育3h后各组血管环在苯肾上腺素(PE)作用下最大收缩力(Emax)以及产生最大收缩力的半数有效浓度(EC50).结果实验ⅠPKG抑制剂DT-2和(D)-DT-2能够使8-Br-cGMP舒张的血管环收缩,DDT2组血管环的Emax明显高于DT2组(P＜0.05).实验ⅡDT-2和(D)-DT-2均可以显著提高LPS孵育血管环的收缩功能；与LPS组比较,LPS-DT2组和LPS-DDT2组Emax升高,EC50降低(P＜0.01).LPS-DDT2组与LPS-DT2组相比Emax升高,EC50降低(P＜0.05).结论 PKG抑制剂可提高内毒素孵育血管环的收缩功能,(D)-DT-2恢复血管反应性的作用强于DT-2.
목적 평개특이성cGMP의뢰성단백격매G(PKG)억제제(D)-DT-2대내독소(LPS)부육대서흉주동맥혈관배수축공능적영향.방법 실험Ⅰ 취SD대서흉주동맥혈관배,채용수궤수자표법분위3조(n=5):KH액조、DT2조화DDT2조,용50 μmol/L 8-Br-cGMP부육25 min후가입상술각약,비교각조혈관배적장력변화.실험Ⅱ 장SD대서흉주동맥혈관배,채용수궤수자표법분위4조(n=5):대조조、LPS조、LPS-DT2조화LPS-DDT2조,재체외측정LPS부육3h후각조혈관배재분신상선소(PE)작용하최대수축력(Emax)이급산생최대수축력적반수유효농도(EC50).결과 실험ⅠPKG억제제DT-2화(D)-DT-2능구사8-Br-cGMP서장적혈관배수축,DDT2조혈관배적Emax명현고우DT2조(P＜0.05).실험ⅡDT-2화(D)-DT-2균가이현저제고LPS부육혈관배적수축공능；여LPS조비교,LPS-DT2조화LPS-DDT2조Emax승고,EC50강저(P＜0.01).LPS-DDT2조여LPS-DT2조상비Emax승고,EC50강저(P＜0.05).결론 PKG억제제가제고내독소부육혈관배적수축공능,(D)-DT-2회복혈관반응성적작용강우DT-2.
Objective To investigate the effect of specific cGMP-dependent protein kinase G (PKG) inhibitor (D)-DT-2 on the contractile function of rat vascular rings after being exposed to lipopolysaccharide (LPS).Methods The experiment was performed in 2 parts.Part Ⅰ:The Sprague-Dawley rat thoracic aortic rings were randomly divided into 3 groups (n =5 each):KH group,DT-2 group and (D)-DT-2 group.KH,DT-2 and (D)-DT-2 were added to the aortic ring after being dilated with 8-Br-cGMP 50 μmol/L for 25 min and the changes in tension of vascular rings were measured.Part Ⅱ:The rat thoracic aortic rings were randomly divided into 4 groups (n =5 each):control group,LPS group,LPS-DT2 group and LPS-(D)-DT2 group.After being incubated with LPS for 3 h in vitro.The Emax and EC50 were compared among the 4 groups.Results Part Ⅰ:Both DT-2 and (D)-DT-2 could contract the vascular rings dilated with 8-Br-cGMP and the Emax was significantly higher in (D)-DT-2 group than DT-2 group (P ＜0.05).Part Ⅱ]:Both DT-2 and (D)-DT-2 significantly improved the contractile function of vascular ring after being exposed to LPS.Emax was significantly higher,while EC50 was lower in groups DT-2 and (D)-DT-2 than in LPS group (P ＜0.01).Emax was significantly increased,while EC50 was decreased in LPS-(D)-DT-2 group as compared with LPS-DT-2 group (P ＜ 0.05).Conclusion PKG inhibitor can improve the contractile function of the vascular rings incubated with LPS and the efficacy of (D)-DT-2 is better than DT-2 in recovering the vascular reactivity.