辛伐他汀对高脂血症患者颈动脉内膜-中层厚度及凝血系统的影响

目的 :观察辛伐他汀对高脂血症患者颈动脉内膜 中层厚度 (IMT)及凝血系统的变化及其非调脂作用 .方法 :高脂血症患者 4 6例口服辛伐他汀 2 0mg ,Qd ,12wk ,分别于治疗前后观察IMT、血脂总胆固醇 (TC)、三酰甘油 (TG)、低密度脂蛋白胆固醇 (LDL C)、高密度脂蛋白胆固醇 (HDL C)、纤维蛋白原 (FIB)、凝血酶原时间 (TT)、活化部分凝血酶时间(APTT)、凝血酶原时间 (PT)改变 .结果 :血脂紊乱组治疗 12wk后的颈动脉IMT变薄 (P <0 .0 0 1) ;TC ,TG ,LDL C ,FIB均有显著降低 (P <0 .0 0 1) ,HDL C升高 (P <0 .0 0 1) ,TT ,APTT均有显著延长 (P <0 .0 0 1) .PT升高 (P <0 .0 0 1) .结论 :调脂作用的辛伐他汀有效调脂同时可发挥其非调脂作用 ,干预、延迟颈动脉IMT的进程 ,改善凝血系统 ,减低血液黏稠度 .     

Effects of Simvastatin on adiponectin and endothelial function in apolipoprotein E-deficient mice

Objective:To investigate the effects of simvastatin,a 3-hydroxy-3-methylglutaryl coenzyme A(HMG-CoA) reductase inhibitor,on adiponectin and markers of endothelial function in apolipoprotein E-deficient mice at an early stage of atherosclerosis. Methods:Twenty-four 6-week old male apoE-deficient mice were randomly divided into two groups: control group(normal saline) and treatment group simvastatin(5 mg/(kg·d). Simvastatin was administered to treatment group mice by gavage and the same volume of normal salin...     

辛伐它汀对血管钙化组织中骨形成蛋白-2表达的影响

目的探讨辛伐它汀对血管钙化组织中骨形成蛋白-2（BMP-2）表达的影响。方法28只清洁级雄性SD大鼠,分为正常对照组、Vit D3组、辛伐他汀组,9周后处死大鼠,观察分析其动脉钙化和BMP-2表达情况。结果正常组血管壁没有BMP-2表达,Vit D3组BMP-2表达明显,辛伐他汀组BMP-2表达较Vit D3组显著减少（P〈0．01）。结论辛伐他汀能降低血管钙化组织中BMP-2表达,这可能是辛伐他汀对血管钙化具有保护作用的因素之一。     

Targeting RhoA/ROCK pathway in pulmonary arterial hypertension

Introduction: Pulmonary arterial hypertension (PAH) is a rare disease with a complex pathogenesis. It is often associated with an increased vascular resistance, whilst in the more advanced stages there is a remodelling of the vascular walls. PAH has an intricate involvement of various signaling pathways, including the ras homolog family member A (RhoA)–Rho kinase (ROCK) axis. Currently, available therapies are not always able to significantly slow PAH progression. Therefore, newer approaches are needed.

Areas covered: In this review, areas covered include the role of the RhoA/ROCK in PAH pathogenesis and the plausibility of its therapeutic targeting. Furthermore, various inhibitory compounds are discussed, including Fasudil and SB-772077-B.

Expert opinion: Currently, specific RhoA/ROCK inhibition is the most promising therapeutic approach for PAH. Research has shown that it suppresses both the components of this axis and the upstream upregulating mediators. An inhaled RhoA/ROCK inhibitor may be a successful future therapy; however, further clinical trials are needed to support this approach.     

Primary and secondary prevention of heart failure with statins

Statins are effective in the prevention of coronary heart disease (CHD), a leading cause of heart failure (HF). Secondary analyses from 11 randomized clinical trials of patients with high-risk acute or stable coronary heart disease, but without HF, suggest that statins may prevent new-onset HF or HF-related hospitalization. In persons with established HF, several cohort studies found an approximate 35% relative risk reduction in all-cause mortality. While ongoing randomized clinical trials will help to determine the efficacy of statins in persons with established HF, it is reasonable to consider this class of medications in patients with a history of cardiovascular disease, dyslipidemia or diabetes mellitus, and who have either developed, or who remain at risk of, HF.     

Simultaneous separation of antihyperlipidemic drugs by green ultrahigh-performance liquid chromatography–diode array detector method: Improving the health of liquid chromatography

Statins in combination with fibrates show beneficial effects on the lipoprotein profile of patients because they have positive complimentary effects on lipid profile. A new green ultrahigh-performance liquid chromatography–diode array detector method for simultaneous analysis of simvastatin (SMV) and fenofibrate (FNF) in standard form, marketed formulations, and self-emulsifying drug delivery system formulations was developed and validated in the present investigation. The method utilized C₁₈ as stationary phase and a combination of methanol:water (8:2) as an eluent. It was found that selected eluent provided short run time (2.5 minutes), better peak symmetry and satisfactory values of other chromatographic parameters such as resolution (Rs = 2.325), capacity factor (k, 3.0 and 4.2 for SMV and FNF, respectively), selectivity (α =1.4), and number of theoretical plates (N, 4265 and 5285 for SMV and FNF, respectively). An excellent linear relationship (r² 0.998 and 0.997 for SMV and FNF, respectively) was observed for linear regression data for the calibration plots. The developed system was validated for accuracy, precision, robustness (˃ 2% for both drugs) and recovery (98–102% for both drugs). Results obtained from the statistical treatment of the values obtained for different parameters proved that the method is suitable, reproducible, and selective for the simultaneous analysis of SMV and FNF in bulk, marketed, and self-emulsifying drug delivery system formulations. The replacement of commonly applied toxic solvents with innocuous and environmentally benign solvents provides a better option than the more toxic processes in drug analysis.     

Beagle犬血浆中辛伐他汀的LC-MS测定

建立了LC-MS法测定Beagle犬血浆中的辛伐他汀。采用C_(18)柱,流动相为乙腈-0.1%甲酸溶液(60:40),以洛伐他汀为内标,采用电喷雾离子化法(ESI)采集正离子,单离子方式检测m/z 419(辛伐他汀)和m/z 405(洛伐他汀)。辛伐他汀在0.5～160ng/ml浓度范围内线性良好,检测限为0.25ng/ml。血浆样品的日内、日间RSD均小于7.7%,方法回收率为92.2%～99.2%,提取回收率为92.8%～100.9%。     

高效液相色谱法测定生长抑素含量及有关物质

目的建立高效液相色谱测定生长抑素含量的方法。方法采用Ominispher C18柱(250 mm×4.6 mm,5μm),流动相A:0.1%TFA水溶液,流动相B:0.1%TFA乙腈溶液,采用梯度洗脱,检测波长:215 nm,流速1.0 mL.min-1。结果方法的线性范围为40~140μg.mL-1。r=0.999 9,平均回收率100.3%,最低检测限为1 ng。结论采用HPLC梯度洗脱法测定生长抑素的含量,分离度好,方法简便,适用于生长抑素的含量测定。