他汀化合物即羟甲戊二酰辅酶A还原酶抑制剂,是最有效的降脂药物,具有重要经济价值,其研究开发是天然产物和应用微生物领域的研究热点。体外检测方法是他汀药物开发的基础,他汀化合物体外检测可以分为生物与化学检测法两大类。生物检测法以他汀化合物具有的生物活性为基础,包括以其具有HMG-CoA还原酶的抑制活性、抑制细胞生长、抗菌活性而分别建立的HMG-CoA还原酶活性测定法、细胞生长测定法和抗菌活性测定法。化学检测是以他汀化合物所具有的化学性质为基础,应用分析仪器检测建立的方法,包括紫外分光光度法、薄层层析法、高效液相色谱法、超临界流体色谱技术、毛细管电泳法等。
The statins (or HMG-CoA reductase inhibitors) are the most potent and cost effective cholesterol-lowering agents. The research and development of statins has become one of the important research projects in both natural product and applied microbiology fields. This paper mainly addresses the research advances in the in vitro identification of statins. The methods used are bioassays and chemical assays. The former, based on statins' biological activities, mainly includes assay of HMG-CoA reductase activity, determination of cell growth and analysis of antifungal activity, and later, based on their chemical characteristics, are UV-spectrophotometric method, thin layer chromatography analysis (TLC), high performance liquid chromatography analysis (HPLC), supercritical fluid chromatography analysis (SFC), and capillary electrophoresis analysis (CE).