国产洛伐他汀治疗原发性高脂血症的临床观察

本文对国产"洛伐他汀"的降脂疗效进行了临床观察，通过与进口"美降之"对76例原发性高脂血症患者的疗效对比显示：国产洛伐他汀组血清总胆固醇（TC）和低密度脂蛋白（LDL－C）在第四周明显降低．平均下降值分别为1．7±1．74（mmol／L），1．53±1．16mmol／L）；在第八周平均下降值分别为2．04±1．64（mmol／L），1．67±1．96（mmol／L）。在第四周和第八周血清胆固醇下降的总有效率分别为65．2％和94．5％。第八周的有效率明显高于第四周。与美降之组相比，降脂疗效无显著性差异P＞0．06。服药期间两组均未发生严重不良反应，表明国产洛伐他汀亦是高效、安全的降低血清胆固醇的药物之一。     

维持性血液透析患者C反应蛋白的变化及洛伐他汀的干预研究

目的探讨维持性血液透析患者C反应蛋白变化,以及洛伐他汀对其的影响。方法维持性血液透析患者20例,洛伐他汀剂量20 mg/d口服,观察12周;观察指标包括血总胆固醇、甘油三酯、低密度脂蛋白胆固醇(LDL-C)、高密度脂蛋白胆固醇(HLD-C)、血C反应蛋白、白蛋白。结果维持性血液透析组治疗前C反应蛋白水平升高,使用洛伐他汀12周后血总胆固醇、甘油三酯、LDL-C均明显降低,而HDL-C上升,C反应蛋白从治疗前(10.83±3.0)mg/L降至(7.78±2.16)mg/L(P<0.05)。血白蛋白经洛伐他汀12周治疗后上升,从治疗前(32.47±4.65)g/L上升至(34.47±6.78)g/L(P<0.05),白蛋白上升与血C反应蛋白下降呈负相关(r=-0.305,P<0.05)。结论维持性血液透析患者存在微炎症状态,洛伐他汀对维持性血液透析患者除降脂外,还具有抗炎作用,能明显降低血C反应蛋白水平。     

土曲霉洛伐他汀合成调控基因lovE的克隆与表达

目的 克隆表达土曲霉洛伐他汀合成调控基因lovE,为研究lovE蛋白的生物学功能奠定基础.方法 利用原核表达载体pET21b(+)构建lovE原核表达质粒,并在大肠杆菌中通过IPTG诱导表达;亲和层析法纯化重组蛋白.结果 构建了pET-lovE原核表达质粒,经原核表达和亲和层析获得6×His-lovE融合蛋白,蛋白纯度...     

HPLC法测定洛伐他汀烟酸缓释片中烟酸的含量

目的:建立测定洛伐他汀烟酸缓释片中烟酸含量的方法。方法:采用高效液相色谱法。色谱柱为ZorbaxC8柱,流动相为乙腈-甲醇-0.01mol.L-1己烷磺酸钠-冰醋酸(4:6:89:1),流速为1.0mL.min-1,检测波长为263nm,柱温为25℃,进样量为20μL。结果:烟酸检测浓度在20.12～100.6μg.mL-1范围内与峰面积积分值呈良好的线性关系(r=0.9999);平均加样回收率为99.71%,RSD=0.43%(n=9)。结论:本方法操作简便、结果准确,可用于该制剂中烟酸的定量分析及制剂质量控制。     

辛伐他汀联合阿昔莫司对高脂血症患者颈动脉粥样斑块的影响

【目的】观察辛伐他汀联合阿昔莫司对颈动脉粥样硬化斑块的影响。【方法】117例高脂血症并颈动脉粥样硬化斑块患者并随机分为三组：辛伐他汀组（39例）,在常规治疗基础上加辛伐他汀40mg,每晚1次;阿昔莫司组（39例）,在常规治疗基础上加阿昔莫司,250mg,每天2次;联合治疗组（39例）,在常规治疗基础上加阿昔莫司,每天2次,辛伐他汀40mg,每晚1次。患者均连续服药6个月,并均于服药前和服药后第6个月检查颈动脉粥样硬化斑块大小、血脂水平。【结果】三组患者治疗前后相比较血脂下降、颈动脉斑块消退差异均有显著性（P〈0．05）,其中联合用药组血脂变化、颈动脉斑块消退治疗后最为明显,与其他组比较差异有显著性（P〈0．05）。【结论】辛伐他汀联合阿昔莫司能够更有效地消退颈动脉斑块,其效果优于单独应用辛伐他汀或阿昔莫司。     

In vivo evidence of duality effects for lovastatin in a nude mouse cancer model

Statins, hydroxy‐methyl‐glutaryl coenzyme A reductase inhibitors, are the most effective medication for lowering cholesterol, cardiovascular morbidity and mortality. On the basis of our previous in vitro experimental results on an anaplastic thyroid cancer cell line, we designed a nude mouse model in which cancer cells were seeded subcutaneously to examine the potential anticancer effects of lovastatin in vivo. As expected, tumor growth was significantly reduced in the mice treated with 5 or 10 mg/kg/day of lovastatin compared with the positive control group. However, the tumor grew much faster in the mice treated with 1 mg/kg/day of lovastatin than in the positive control group. We suspect this result might be related to vascular endothelial growth factor. In this model, we found that lovastatin inhibits tumor growth at a high dosage (5 or 10 mg/kg/day), suggesting it could be used as an effectively adjuvant chemotherapy for cancer. However, it also promotes tumor growth at a low dosage (1 mg/kg/day). This duality effect should be further studied for patients treated with various dosages of statins.     

辛伐他汀与洛伐他汀治疗高脂血症疗效比较

目的 :观察小剂量辛伐他汀与洛伐他汀治疗高脂血症的疗效和安全性。方法 :12 9例原发性高胆固醇血症随机分为 2组 ,辛伐他汀组 64例 (男性 30例 ,女性 34例 ;年龄 51a±s8a)给予辛伐他汀5mg ,po ,qn× 3mo ;洛伐他汀组 65例 (男性 32例 ,女性 33例 ;年龄 57a± 9a)给予洛伐他汀 10mg ,po ,qn× 3mo。结果 :治疗 3mo后 2组均有TC ,TG ,LDL C ,ApoB10 0 显著下降及HDL C升高作用 ;经t检验 ,治疗前后差别均有非常显著意义(P <0 .0 1) ,2组间比较HDL C ,ApoAI升高差别有显著意义 (P <0 .0 5) ,LDL C ,ApoB10 0 降低差别有非常显著意义 (P <0 .0 1)。 2组均未见明显不良反应。结论 :小剂量辛伐他汀和洛伐他汀治疗高脂血症疗效较好且安全     

Percutaneous lovastatin accelerates bone healing but is associated with periosseous soft tissue inflammation in a canine tibial osteotomy model

Experimental studies have shown the ability of statins to stimulate bone formation when delivered locally or in large oral doses, however most have been studied in rodents. This anabolic effect is through the selective activation of BMP‐2. Our purpose was to determine the effects of local treatment with lovastatin on bone healing in mammals as a preclinical animal model. We administered lovastatin (6 mg/kg) by percutaneous injection to a canine tibial osteotomy stabilized with external fixation. We found that lovastatin improved bone healing after a single injection into the fracture site assessed by serial radiography and histology at bone union. However, lovastatin treatment resulted in adverse local soft tissue inflammation. These results suggest that percutaneous lovastatin injection may be a useful adjuvant treatment over the course of bone healing to augment fracture repair, although further investigation into the mechanism of soft tissue adverse effects is warranted. © 2013 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 32:210–216, 2014.     

Influence of lovastatin therapy on metabolism of low density lipoproteins in mixed hyperlipidaemia

Abstract. To determine the mechanisms whereby HMG-CoA reductase inhibitors lower the levels of low density lipoproteins (LDL) in patients with mixed hyperlipidaemia. LDL turnover studies were conducted in 12 such patients during placebo and then during treatment with lovastatin. Drug therapy reduced total cholesterol and triglyceride concentrations by 33% and 32%, respectively. During lovastatin therapy, LDL-cholesterol levels fell by 37%, and LDL-apo B concentrations decreased by an average of 29%. The decrease in LDL-apo B concentrations on lovastatin therapy was largely due to an increase in fractional catabolic rates (FCRs) for LDL apo B. The average increase in FCRs was 34%, whereas transport rates (production rates) for LDL apo B remained unchanged. These results strongly suggest that an increase in LDL-receptor activity is the major mechanism whereby LDL levels are lowered during lovastatin therapy. The data do not indicate that this drug inhibited the input of apo B-containing lipoproteins, which would have been expected to result in a decrease in the rate of production of LDL.