生物活性 | |||
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描述 | Atorvastatin inhibits pre-proET-1 mRNA expression in a concentration- and time-dependent fashion (60-70% maximum inhibition) and reduces immunoreactive ET-1 levels (25-50%), this inhibitory effect is maintained in the presence of oxidized LDL (1-50 mg/mL). Atorvastatin significantly reduces angiotensin II-induced and epidermal growth factor-induced ROS production in VSMCs. Atorvastatin downregulates mRNA expression of the NAD(P)H oxidase subunit nox1 in VSMCs, whereas p22phox mRNA expression is not significantly altered. Atorvastatin inhibits membrane translocation of rac1 GTPase, which is required for the activation of NAD(P)H oxidase. Atorvastatin (0.1 μM) significantly diminishes NF-κB activation induced by Ang II and TNF-α in mononuclear cells and VSMC. Atorvastatin (1 μM) diminishes MCP-1 expression induced by Ang II, TNF-α and is reversed by Mevalonate only in Ang II-stimulated cells. Atorvastatin (1 μM) diminishes IP-10 expression induced by Ang II and by TNF-α in VSMC, and this reduction is partially reversed by Mevalonate. Atorvastatin and Gemfibrozil metabolites, but not the parent drugs, are potent antioxidants against lipoprotein oxidation.[1-2] |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00768638 | Chronic Kidney Disease | Phase 4 | Completed | - | Canada ... 展开 >> Hôtel-Dieu de Québec Hospital Quebec, Canada, G1R2J6 收起 << |
NCT02497638 | Prostate Cancer | Phase 2 | Not yet recruiting | December 2022 | Canada, Ontario ... 展开 >> Princess Margaret Cancer Centre Recruiting Toronto, Ontario, Canada, M5G 2M9 Principal Investigator: Robert Hamilton, MD, MPH, FRCSC Principal Investigator: Neil Fleshner, MD, MPH, FRCSC 收起 << |
NCT00974740 | Type 1 Diabetes | Phase 1 | Terminated(for lack of recruit... 展开 >>ment) 收起 << | - | Germany ... 展开 >> Diabetes-Zentrum Mergentheim Bad Mergentheim, Germany, 97980 Gemeinschaftskrankenhaus Havelhöhe Berlin, Germany, 14089 Helios Klinikum Emil von Behring Berlin, Germany, 14165 Praxis Dr. Friedhelm Schmitten Bestwig-Ramsbeck, Germany, 59909 DDZ Deutsches Diabetes Zentrum Düsseldorf, Germany, 40221 St. Josefs Krankenhaus Heidelberg, Germany, 69115 St. Antonius Krankenhaus, Med. Klinik Köln, Germany, 50968 Praxisklinik Leipzig Leipzig, Germany, 04103 Praxis Dr. Gerhard Willms Leverkusen, Germany, 51373 Praxis Dr. Heinz-Georg Ley Marl, Germany, 45770 Diabetologische Schwerpunktpraxis, Angiologie Münster, Germany, 48145 Praxis Dr. Werner Stürmer Würzburg, Germany, 97070 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.79mL 0.36mL 0.18mL |
8.95mL 1.79mL 0.90mL |
17.90mL 3.58mL 1.79mL |
参考文献 |
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