Function of resveratrol in atherosclerosis

2018-08-18

Introduction 

Resveratrol is also known as stilbene III. Its chemical name is (E)-3,5,4-trihydroxystilbene. It is a non-flavonoid polyphenol compound containing a stilbene structure. It is mainly from grape (red wine), Polygonum cuspidate, peanuts, mulberry and other plants, and is often combined with glucose in the form of glycosides. So far, resveratrol has proved that it can inhibit the growth and spread of tumors, improve microcirculation and cardiac function, remove or inhibit the formation of free radicals, such as antiseptic and anti-inflammatory effects, and inhibit the release of inflammatory mediators, immunoregulation, and liver protection. Health products, food, cosmetics and other fields are widely used.

Fig 1. The route of synthesis of resveratrol.

 Fig 1. The route of synthesis of resveratrol.

Fig 1. The route of synthesis of resveratrol.

Pharmacologic action

Resveratrol can effectively inhibit platelet aggregation in blood circulation and reduce the extent of atherosclerosis and myocardial infarction. Platelets contain epoxidase-1 (COX-1), which synthesizes thromboxane A2. Thromboxane A2 is an efficient vasoconstrictor, which promotes platelet aggregation, and the epoxidase-2 (COX-2) exists in vascular endothelial cells, which can promote the synthesis of prostaglandins (including precursors). Prostaglandins can promote vasodilation and inhibit platelet aggregation. Resveratrol has a strong inhibitory effect on epoxide COX-1, but has little inhibitory effect on cyclooxygenase COX-2. It can inhibit the synthesis of thromboxane A2, prevent thrombosis, ensure stable blood flow and prevent myocardial ischemia.

Function

Resveratrol can prevent atherosclerosis through a variety of mechanisms. It reduces blood lipid levels, increases the content of high-density lipoprotein (HDL), inhibits oxidation of low-density lipoprotein LDL, adjusts LDL cholesterol ratio and reduces arteriosclerosis index. Resveratrol is a natural antioxidant that lowers blood viscosity and inhibits platelet clotting and vasodilation. It can also keep the blood flowing smoothly, prevent the formation of coronary heart disease and protect the cardiovascular system.

Pharmacokinetics and metabolism

After resveratrol enters the digestive tract, it is absorbed into the blood circulation with the conjugate or free form of a grape glycoside in the small intestine. Studies have shown showed that resveratrol enters the blood circulation after the liver metabolism; combined with glucoside, the half-life in vivo is about 3.5 hours, and the blood circulates into the tissues and organs after liver metabolism, thus exerting biological effects. Five resveratrol monosulfate, resveratrol and monosulfate resveratrol metabolites have been found in urine. The resveratrol metabolites are also active, and the half-life of resveratrol is about 9.2 hours, much higher than that of resveratrol monomer.

References:

Guido A. Gualdoni, Dietmar Fuchs, Gerhard J. Zlabinger. Resveratrol intake enhances indoleamine-2,3-dioxygenase activity in humans. Pharmacological Reports. 2016, 68(5), 1065-1068.

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