Guerard Pascal, Rakotoniaina Zo, Goirand Françoise, Rochette Luc, Dumas Monique, Lirussi Frederic, Bardou Marc
Laboratory of Experimental Cardiovascular Physiopathology and Pharmacology (EA2979), IFR 100 Faculty of Medicine, BP 87900, 21000, Dijon, France.
Naunyn Schmiedebergs Arch Pharmacol. 2006 Sep;373(6):401-14. doi: 10.1007/s00210-006-0082-1. Epub 2006 Aug 1.
HMG-CoA reductase inhibitors improve endothelial function and exert antiproliferative effects on vascular smooth muscle cells of systemic vessels. This study was aimed to assess the protective effects of pravastatin (an HMG-CoA reductase inhibitor) against monocrotaline-induced pulmonary hypertension in rats. Pravastatin (PS, 10 mg/kg/day) or vehicle were given orally for 28 days to Wistar male rats injected or not with monocrotaline (MC, 60 mg/kg intraperitonealy) and treated or not by N(omega)-nitro-L-arginine methyl ester (L-NAME) 15 mg/kg/day. At 4 weeks, monocrotaline-injected rats developed severe pulmonary hypertension, with an increase in right ventricular pressure (RVP) and right ventricle/left ventricle+septum weight ratio (RV/LV+S), associated with a decrease in pulmonary artery dilation induced either by acetylcholine or sodium nitroprusside. Hypertensive pulmonary arteries exhibited an increase in medial thickness, medial wall area, endothelial cell apoptosis, and a decrease of endothelial nitric oxide synthase (eNOS) expression. Monocrotaline-rat lungs showed a significant decrease of eNOS expression (4080+/-27 vs 12189+/-761 arbitrary density units [ADU] for MC and control groups respectively, P<0.01) and a significant increase of cleaved caspase-3 expression by western blotting (Control=11628+/-2395 vs MC=2326+/-2243 ADU, P<0.05). A non-significant trend toward a reduced mortality was observed with pravastatin (relative risk of death = 0.33; 95% confidence interval [0.08-1.30], P= 0.12 for MC+PS vs MC groups). Pravastatine induced a protection against the development of the pulmonary hypertension (RVP in mmHg: 30+/-3 vs 45+/-4 and RV/LV+S: 0.46+/-0.04 vs 0.62+/-0.05 for MC+PS and MC groups respectively, P<0.05) and was associated with a significant reduction of MC-induced thickening (61+/-6 mum vs 81+/-3 mum for MC+PS and MC groups respectively, P= 0.01) of the medial wall of the small intrapulmonary arteries. Pravastatin partially restored acetylcholine-induced pulmonary artery vasodilation in MC rats (Emax=65+/-5% and 46+/-3% for MC+PS and MC group respectively, P<0.05) but had no effect on acetylcholine-induced pulmonary artery vasodilation in MC+L-NAME rats. It also prevented apoptosis and restored eNOS expression of pulmonary artery endothelial cells, as well as in the whole lung. Pravastatin reduces the development of monocrotaline-induced pulmonary hypertension and improves endothelium-dependent pulmonary artery relaxation, probably through a reduced apoptosis and a restored eNOS expression of endothelial cells.
HMG-CoA还原酶抑制剂可改善内皮功能,并对全身血管的血管平滑肌细胞发挥抗增殖作用。本研究旨在评估普伐他汀(一种HMG-CoA还原酶抑制剂)对大鼠野百合碱诱导的肺动脉高压的保护作用。将Wistar雄性大鼠分为注射或未注射野百合碱(60mg/kg腹腔注射),并分别用或不用15mg/kg/天的N(ω)-硝基-L-精氨酸甲酯(L-NAME)处理,给予普伐他汀(PS,10mg/kg/天)或赋形剂口服28天。4周时,注射野百合碱的大鼠出现严重肺动脉高压,右心室压力(RVP)和右心室/左心室+室间隔重量比(RV/LV+S)增加,同时乙酰胆碱或硝普钠诱导的肺动脉扩张减少。高血压肺动脉的中膜厚度、中膜壁面积增加,内皮细胞凋亡,内皮型一氧化氮合酶(eNOS)表达减少。野百合碱处理的大鼠肺组织中eNOS表达显著降低(MC组和对照组分别为4080±27和12189±761任意密度单位[ADU],P<0.01),通过蛋白质印迹法检测发现裂解的半胱天冬酶-3表达显著增加(对照组=11628±2395 vs MC组=2326±2243 ADU,P<0.05)。普伐他汀治疗组观察到死亡率有降低趋势,但无统计学意义(死亡相对风险=0.33;95%置信区间[0.08-1.30],MC+PS组与MC组相比P=0.12)。普伐他汀可预防肺动脉高压的发生(MC+PS组和MC组的RVP分别为30±3 mmHg和45±4 mmHg,RV/LV+S分别为0.46±0.04和0.62±0.05,P<0.05),并与显著降低MC诱导的肺小动脉中膜壁增厚相关(MC+PS组和MC组分别为61±6μm和81±3μm,P=0.01)。普伐他汀可部分恢复MC大鼠乙酰胆碱诱导的肺动脉舒张功能(MC+PS组和MC组的Emax分别为65±5%和46±3%,P<0.05),但对MC+L-NAME大鼠乙酰胆碱诱导的肺动脉舒张功能无影响。它还可预防肺动脉内皮细胞凋亡并恢复eNOS表达,以及在整个肺组织中的表达。普伐他汀可能通过减少内皮细胞凋亡和恢复eNOS表达,降低野百合碱诱导的肺动脉高压的发生,并改善内皮依赖性肺动脉舒张功能。