Persson K, Whiss P A, Nyhlén K, Jacobsson-Strier M, Glindell M, Andersson R G
Division of Pharmacology, Department of Medicine and Care, Faculty of Health Sciences, Linköping University, SE-581 85, Linköping, Sweden.
Eur J Pharmacol. 2000 Oct 6;406(1):15-23. doi: 10.1016/s0014-2999(00)00647-6.
This study investigates the effects of exogenous and endogenous nitric oxide (NO) on human circulating and endothelial angiotensin-converting enzyme activity and platelet aggregation. The NO donor S-nitroso-N-acetylpenicillamine (10(-8)-10(-6) M) significantly and dose-dependently inhibited serum angiotensin-converting enzyme activity. The concomitant addition of S-nitroso-N-acetylpenicillamine to angiotensin-converting enzyme inhibitor-treated (captopril or enalaprilat) serum, further reduced angiotensin-converting enzyme activity. In cultured endothelial cells from human umbilical veins (HUVECs), both S-nitroso-N-acetylpenicillamine and 3-morpholinosydnonimine (SIN-1) significantly reduced angiotensin-converting enzyme activity. An additative effect was seen with a combined treatment of captopril and S-nitroso-N-acetylpenicillamine. Treatment with the NO synthase inhibitor N(G)-monomethyl-L-arginine (L-NMMA) did not affect angiotensin-converting enzyme activity. Thrombin inhibited endothelial angiotensin-converting enzyme activity, an effect that was abolished when cells were pretreated with L-NMMA. Adenosine 5'-diphosphate (ADP)-induced platelet aggregation was inhibited with S-nitroso-N-acetylpenicillamine, SIN-1 and nitroglycerine. Captopril did not affect aggregation, while a high concentration of enalaprilat (10(-4) M) reduced it. The concomitant addition of 10(-5) M angiotensin-converting enzyme inhibitor to NO donor-treated platelets resulted in a further reduction of platelet aggregation. This effect was most evident with SIN-1 and enalaprilat. In conclusion, both exogenous and endogenous NO inhibit human angiotensin-converting enzyme activity. NO donors and angiotensin-converting enzyme inhibitors act in concert to inhibit angiotensin-converting enzyme and platelet aggregation.
本研究调查外源性和内源性一氧化氮(NO)对人循环及内皮血管紧张素转换酶活性和血小板聚集的影响。NO供体S-亚硝基-N-乙酰青霉胺(10⁻⁸ - 10⁻⁶ M)显著且呈剂量依赖性地抑制血清血管紧张素转换酶活性。将S-亚硝基-N-乙酰青霉胺添加到经血管紧张素转换酶抑制剂(卡托普利或依那普利拉)处理的血清中,可进一步降低血管紧张素转换酶活性。在人脐静脉培养的内皮细胞(HUVECs)中,S-亚硝基-N-乙酰青霉胺和3-吗啉代辛二酮(SIN-1)均显著降低血管紧张素转换酶活性。卡托普利和S-亚硝基-N-乙酰青霉胺联合治疗呈现相加效应。用NO合酶抑制剂N(G)-单甲基-L-精氨酸(L-NMMA)处理不影响血管紧张素转换酶活性。凝血酶抑制内皮血管紧张素转换酶活性,而当细胞用L-NMMA预处理时该效应被消除。腺苷5'-二磷酸(ADP)诱导的血小板聚集被S-亚硝基-N-乙酰青霉胺、SIN-1和硝酸甘油抑制。卡托普利不影响聚集,而高浓度的依那普利拉(10⁻⁴ M)可降低聚集。将10⁻⁵ M血管紧张素转换酶抑制剂添加到经NO供体处理的血小板中,可进一步降低血小板聚集。该效应在SIN-1和依那普利拉中最为明显。总之,外源性和内源性NO均抑制人血管紧张素转换酶活性。NO供体和血管紧张素转换酶抑制剂协同作用以抑制血管紧张素转换酶和血小板聚集。