Hayrettin Ozan Gulcan*, Serkan Yigitkan and Ilkay Erdogan Orhan Pages 1130 - 1137 ( 8 )
High cholesterol and triglyceride levels are mainly related to further generation of lifethreating metabolism disorders including cardiovascular system diseases. Therefore, hypercholesterolemia (i.e., also referred to as hyperlipoproteinemia) is a serious disease state, which must be controlled. Currently, the treatment of hypercholesterolemia is mainly achieved through the employment of statins in the clinic, although there are alternative drugs (e.g., ezetimibe, cholestyramine). In fact, the original statins are natural products directly obtained from fungi-like molds and mushrooms and they are potent inhibitors of hydroxymethylglutaryl-CoA reductase, the key enzyme in the biosynthesis of cholesterol. This review focuses on the first identification of natural statins, their synthetic and semi-synthetic analogues, and the validation of hydroxymethylglutaryl-CoA reductase as a target in the treatment of hypercholesterolemia. Furthermore, other natural products that have been shown to possess the potential to inhibit hydroxymethylglutaryl-CoA reductase are also reviewed with respect to their chemical structures.
HMG-CoA reductase, enzyme inhibition, hypercholesterolemia, natural products, statins, cholesterol.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Eastern Mediterranean University, Famagusta, TRNC, via Mersin 10, Department of Pharmaceutical Botany, Faculty of Pharmacy, Dicle University, 06330 Diyarbakir, Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, 06330 Ankara