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Novel application of 2,3,5,4-tetrahydroxy-stilbene-2-O-beta-D-Glucoside (TSG) in preventing and/or treating hyperhomocysteinemia (HHcy)

A technology of cysteinemia and stilbene glycosides, which is applied in the field of medicine, can solve problems that have not been reported before, achieve wide application prospects, inhibit the upregulation of B-type endothelin receptors, and inhibit the activation of the effect

Inactive Publication Date: 2019-12-24
陕西含光生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Stilbene glycoside (2,3,5,4-Tetrahydroxy-stilbene-2-O-β-D-Glucoside, TSG) has a wide range of pharmacological effects, including anti-inflammatory, anti-oxidation, inhibition of platelet aggregation, and protection of vascular endothelial cells Function and inhibit phenotype conversion of vascular smooth muscle cells to achieve anti-atherosclerotic and anti-hypertensive effects, but its effect on HHcy has not been reported

Method used

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  • Novel application of 2,3,5,4-tetrahydroxy-stilbene-2-O-beta-D-Glucoside (TSG) in preventing and/or treating hyperhomocysteinemia (HHcy)
  • Novel application of 2,3,5,4-tetrahydroxy-stilbene-2-O-beta-D-Glucoside (TSG) in preventing and/or treating hyperhomocysteinemia (HHcy)
  • Novel application of 2,3,5,4-tetrahydroxy-stilbene-2-O-beta-D-Glucoside (TSG) in preventing and/or treating hyperhomocysteinemia (HHcy)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1. TSG inhibits Hcy-induced vascular smooth muscle contraction response

[0013] Different concentrations of TSG (10 -4 M, 10 -3.5 M, 10 -3 M) respectively co-incubated with Hcy (100 μM) for 24 hours to observe the effect of TSG on Hcy-induced vasoconstriction induced by vasoconstrictor substances (KCl, PE or 5-HT) in rat superior mesenteric artery. The results showed that, compared with the Hcy (100μM) group, TSG (10 -3.5 M, 10 -3 M) It can inhibit the vasoconstriction response of blood vessels induced by Hcy to KCl, PE or 5-HT (Pfigure 1 A, B, C). These results show that TSG can reduce the sensitivity of Hcy-induced blood vessels to vasoconstrictor substances, and inhibit the constriction effect of such substances on blood vessels.

Embodiment 2

[0014] Example 2. TSG inhibits the endothelin receptor-mediated contraction of vascular smooth muscle and the expression of its receptor protein caused by Hcy. Different concentrations of TSG (10 -4 M, 10 -3.5 M, 10 -3 M) Co-incubated with Hcy (100 μM) for 24 hours, and observed the ET of TSG on Hcy A and ET B Receptor-Mediated Contraction Response and ET in Rat Superior Mesenteric Artery A and ET B Effect of receptor protein expression. The results showed that, compared with the Hcy (100μM) group, TSG (10 -3.5 M, 10 -3 M) It can inhibit the vasoconstriction response induced by ET-1 or S6c induced by Hcy (P figure 2 A, B). Moreover, TSG significantly downregulated Hcy-increased superior mesenteric artery ET B Receptor level (P figure 2 C, D, E). These results show that TSG can downregulate Hcy-induced ET B Receptor upregulation and its mediated vasoconstrictor response.

Embodiment 3

[0015] Example 3. Effect of TSG on blood pressure of HHcy mice

[0016] The systolic blood pressure and diastolic blood pressure of the mice in the HHcy group were significantly higher than those in the control group in the first, second, third, and fourth weeks of the experiment (P image 3 A, B). These data suggest that TSG can inhibit the HHcy-induced blood pressure increase.

[0017] In summary, the experimental studies have confirmed that stilbene glycoside has a therapeutic effect on hyperhomocysteinemia in experimental animals, suggesting that it has a significant prospect of being used in the development of prevention and treatment of hyperhomocysteinemia.

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Abstract

The invention relates to a novel application of 2,3,5,4-tetrahydroxy-stilbene-2-O-beta-D-Glucoside (TSG) in preventing and / or treating hyperhomocysteinemia (HHcy). The invention discloses pharmacologic actions of TSG which can remarkably relax superior mesenteric arteries of rats, inhibit homocysteine induced B type endothelin receptor up-regulation and inhibit activation of mitogen-activated protein kinase / nuclear factor kB / B type endothelin receptor signal axes so as to significantly treat the HHcy, and the blank that no drugs for treating the HHcy exist clinically is filled up.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a new application of stilbene glycoside in preventing and / or treating hyperhomocysteinemia. Background technique [0002] It is known clinically that the method to reduce the high homocysteine ​​(Hcy) in the blood of patients with hyperhomocysteinemia (HHcy) is to supplement folic acid, or to take group B vitamins in combination, and there is no specialized medicine for the treatment of HHcy. HHcy is an independent risk factor in the occurrence and development of cardiovascular and cerebrovascular diseases, and the mechanism of damage to target organs such as the heart, kidney, and blood vessels is also very complicated. Therefore, for drugs to treat HHcy, it is required on the one hand to reduce the level of Hcy in the blood, and on the other hand On the one hand, it should also protect myocardium, vascular smooth muscle, endothelial cells and nervous system function...

Claims

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Application Information

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IPC IPC(8): A61K31/7034A61P9/12A61P9/10A61P25/00A61P3/00
CPCA61K31/7034A61P9/12A61P9/10A61P25/00A61P3/00
Inventor 王四旺贾敏周暄宣杨倩谢艳华王静
Owner 陕西含光生物科技有限公司
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