What is Polydatin？
Polydatin(PD) is an extract of the plant Polygonum cuspidatum. It has a variety of biological activities and has antioxidant, anti-inflammatory, neuroprotective, cardioprotective and immunomodulatory effects. Polydatin is a glycosylated derivative of resveratrol. It has higher water solubility, stability and antioxidant capacity than resveratrol.
The Function of Polydatin
1. Effect on cardiovascular system
1) Effect on cardiomyocytes
Studies on rat cardiomyocytes through PD have shown that its cardiotonic effect may directly increase myocardial contractility by increasing the concentration of free calcium ions in individual cells; it may also have the function of enhancing calcium pumps or Na + -Ca2 + exchange proteins. This allows the Ca2+ in the cytoplasm during diastole to be taken back into the sarcoplasmic reticulum or discharged out of the cell faster and more effectively. This effect of PD makes it theoretically superior to digitalis cardiotonic glycosides in cardiac function. It not only makes myocardial contraction more powerful, but also makes myocardial relaxation more complete, thus greatly improving myocardial work efficiency.
2) Effect on vascular smooth muscle cells (VSMC)
Studies on the effects of PD on rat blood smooth muscle cells and human umbilical cord artery smooth muscle cells show that PD has a bidirectional regulatory effect on intracellular calcium and pH. Under normal circumstances, PD not only promotes the entry of extracellular calcium ions into the cells of VSMC, but also induces the release of intracellular calcium, increasing intracellular calcium levels; at the same time, it increases pH to increase vascular tone. During shock, it reduces intracellular calcium concentration and intracellular pH to reduce vascular tension and dilate blood vessels; it can regulate blood vessels by promoting the influx of extracellular sodium ions and using cell depolarization. Its effect may be related to the opening of sodium and potassium channels. And it is reversely regulated by β-adrenergic receptors, H2 receptor system and guanylyl cyclase system.
3) Anti-platelet aggregation effect
Studies have found that PD inhibits platelet aggregation induced by arachidonic acid (AA) and adenosine diphosphate (ADP) both in vivo and in vitro; the effect of PD on platelet aggregation and thromboxane B2 in rabbits was measured using turbidimetric method and radioimmunoassay. (TXB2), it was confirmed that PD6.7 ~ 107.2μmol/L can significantly inhibit AA and ADP-induced rabbit platelet aggregation and TXB2 production. The inhibition rates were 48% ~ 90% and 43% ~ 69% respectively. The inhibition of TXB2 production The rates were 50% ~ 78% and 43% ~ 68% respectively. There was a significant positive correlation between the two inhibition rates; the study also confirmed that PD can also inhibit the aggregation of human platelets. Its main route is through the prostate system. Inhibiting platelet aggregation induced by AA and ADP mainly inhibits cyclooxygenase and reduces thromboxane A2 (TXA2); inhibiting platelet aggregation induced by thrombin may also inhibit platelet aggregation induced by thrombin, in addition to inhibiting cyclooxygenase, and may also increase prostacyclin (PGI2). related to the release.
4) Impact on microcirculation
Injection of PD can restore the cardiac output of burned rats to 91% of that before burns, the ventricular function reaches 100%, the systemic peripheral resistance returns to close to normal, and the survival rate of rats is significantly improved; intravenous injection of PD can promote the emergence of microcirculation in the microcirculation. Arterial blood flow, reducing micro-thrombosis after burns.
5) Effect on vascular endothelial injury-induced thrombus.
PD can significantly reduce the wet weight of thrombus caused by trypsin-induced carotid endothelial damage. The wet weight of thrombus in the PD 5mg/kg and 11mg/kg groups was 6.6 ± 1.8 mg and 4.8 ± 1.6 mg respectively, which was 10.9 ± 10.9 ± in the normal saline group. 1.9mg, there were significant differences in all comparisons.
2. Protective effect against tissue and organ damage caused by various factors.
In the rat ischemia-reperfusion model, Liang Rongneng et al. observed that PD can reduce the peroxide lipid content of brain tissue to varying degrees and increase superoxide dismutase (SOD), catalase, and glutathione levels. Oxidase (GSHPX) activity, reduce brain water content, reduce the damage to brain tissue caused by free radical reactions, and have a protective effect on ischemic brain tissue; and show a dose-effect relationship. PD has a protective effect on extraintestinal organ lung, liver and kidney damage during intestinal ischemia-reperfusion in rabbits, and also reduces tumor necrosis factor (TNF) and lysosomal enzyme (N-acetyl-β-D-glucosaminidase). ) release. Luo Sufang et al. used cultured cardiomyocyte hypoxia-hypoxic injury and chlorpromazine injury models and found that PD could significantly reduce the release of lactate dehydrogenase during cardiomyocyte injury.
3. Hepatoprotective effect
Resveratrol glycosides can protect the liver and inhibit the accumulation of lipid peroxides in the liver. Research on the protective effect of PD on primary cultured rat hepatocytes damaged by CCL4 shows that it can effectively protect damaged hepatocytes and significantly increase cell survival rate in the concentration range of 1×10-7 to 1×10-4mmol/L. , using 1 × 10 -5mmol/L, the survival rate of liver cells reached 88.7%, which is close to the level of normal cultured liver cells. Studies have shown that PD has a significant antioxidant effect on oxidative damage to mouse liver cells caused by hydrogen peroxide within a certain concentration range, and can increase the superoxide dismutase (SOD) and glutathione levels of liver cells. oxidase (GSH-px) activity, reduce GSH consumption, reduce malondialdehyde (MDA) content, inhibit nitric oxide synthase (NOS) activity, reduce the generation and oxidation of nitric oxide (NO), thereby alleviating oxidation The damage caused by substances to hepatocytes significantly reduces the ALT level in the hepatocyte suspension, and its effect is significantly dose-dependent in the range of 0.05-2mmol/L.
4. Lower blood lipids and resist lipid peroxidation
Studies have found that sublingual resveratrol glycoside 2.2 mg·kg/d for 3 days can restore elevated serum cholesterol, low-density lipoprotein/high-density lipoprotein (LDL/HDL) ratio and hematocrit. to normal, and has a tendency to reduce the high shear rate and low shear rate of whole blood. By measuring the degree of lipid peroxidation under the influence of exogenous free radicals, it was found that PD can improve the stability of lipid membranes and has significant anti-lipid peroxidation effects.
Polydatin has significant effects on cardiomyocytes, vascular smooth muscle cells, and improving microcirculation. In addition, resveratrol glycosides can reduce tissue and organ damage caused by various factors, protect the liver, inhibit platelet aggregation, relieve cough and asthma, have antibacterial, antiviral, lower blood lipids and anti-lipid peroxidation effects. Polydatin is a functional ingredient that exists in natural plants and has a variety of pharmacological effects. Due to its low cost and abundant resources, it is an ideal raw material for the production of health food.
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