Fattah Tanzeela A, Saeed Aamer, Shehzadi Syeda A
Department of Chemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan.
Sulaiman Bin Abdullah Aba Al-Khail-Centre for Interdisciplinary Research in Basic Sciences (SA-CIRBS), International Islamic University, Islamabad 44000, Pakistan.
Curr Org Synth. 2019;16(5):652-670. doi: 10.2174/1570179416666190725095951.
Cardiovascular diseases are among the most threatening problems being faced by twenty-first century humans. The core cause of these diseases is high cholesterol level. Simvastatin (1: Synvinolin) is a well-known cholesterol-lowering drug marketed under the trade name Zocor®, which significantly reduces the risk of cardiovascular diseases related to hypercholesterolemia and is effective in lowering the total plasma cholesterol, low-density and very low-density lipoprotein cholesterol. It also enhances the high-density lipoprotein cholesterol. This review article aims to provide an overview of several chemical and biological methods utilized for the production of simvastatin in high yields and purity. Many robust and scalable methods have been described using lovastatin (2: Mevinolin) as a starting material, produced by the fungal strain of Aspergelius terreus. Enzymatic synthesis of simvastatin is also highlighted in this review. In addition, detailed experimental conditions, as well as the compatibility for industrial-scale preparations of simvastatin are also discussed.
心血管疾病是21世纪人类面临的最具威胁性的问题之一。这些疾病的核心原因是高胆固醇水平。辛伐他汀（1：舒降之）是一种知名的降胆固醇药物，商品名为舒降之®，它能显著降低与高胆固醇血症相关的心血管疾病风险，有效降低血浆总胆固醇、低密度和极低密度脂蛋白胆固醇水平。它还能提高高密度脂蛋白胆固醇水平。这篇综述文章旨在概述几种用于高产率和高纯度生产辛伐他汀的化学和生物学方法。已经描述了许多以洛伐他汀（2：美伐他汀）为起始原料的可靠且可扩展的方法，洛伐他汀由土曲霉真菌菌株产生。本文还重点介绍了辛伐他汀的酶促合成。此外，还讨论了详细的实验条件以及辛伐他汀工业规模制备的兼容性。
