生薬脂質調節薬ロバスタチン75330-75-5

Purpose:

Lovastatin is a kind of HMG CoA reductase inhibitor which is used to reduce the cell permeability of cholesterol.
effect:
1. Lipid regulating effect
Lovastatin can block the synthesis of endogenous cholesterol by inhibiting HMG CoA reductase, which is the rate limiting enzyme of cholesterol synthesis. Lovastatin can reduce the content of cholesterol in cells, increase the number of LDL receptors on cell surface, accelerate the uptake and degradation of LDL particles in blood circulation, and reduce the total cholesterol, very low density lipoprotein (VLDL), LDL and triglyceride in plasma. Since the conversion of HMG CoA to mevalonate is an early step in cholesterol biosynthesis pathway, lovastatin does not lead to accumulation of potentially toxic cholesterol substances. HMG CoA can also be quickly reversed into acetyl coenzyme A and participate in other biosynthetic pathways in vivo. This inhibition is incomplete and reversible, and there is a dose-response relationship, Therefore, lovastatin has a significant effect on reducing blood lipid and has less side effects.
Generally speaking, lovastatin mainly plays a role in the following aspects: ① competitive inhibition of HMG CoA reductase activity and reduction of endogenous cholesterol synthesis; ② increase of LDL receptor expression in hepatocytes and increase receptor mediated plasma LDL clearance rate; ③ inhibit migration and proliferation of smooth muscle cells; ④ reduce assembly and secretion of liver lipoprotein.
2. Non lipid regulating effect
Lovastatin can not only significantly reduce blood lipid, but also significantly improve the function of endothelial cells, promote the production of nitric oxide synthase (eNOS), thus increasing the synthesis and release of no, which plays a key role in maintaining normal pulmonary vascular tension and reversing hypoxia induced pulmonary vasoconstriction and vascular remodeling. In addition, lovastatin has anti-inflammatory and antiproliferative effects, which can inhibit the proliferation of mesangial cells and the secretion of extracellular matrix, so as to reduce glomerulosclerosis.
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