Compound stybenpropol a and its application in preventing and treating atherosclerosis

A technology of atherosclerosis and compounds, applied in the field of medicine, can solve the problems of few active ingredients research, achieve the effect of protecting from injury and death, increasing the level of nitric oxide, and inhibiting inflammatory damage

Active Publication Date: 2020-01-10
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Benzoin is a resin of the bark of Styraxtonkinensis (Styraxtonkinensis), a benzoin family plant. It is widely distributed in many parts of Southeast Asia. In recent years, studies have shown that benzoin has anti-inflammatory, antipyretic and anti-tumor effects. It is widely used clinically as a traditional Chinese medicine. Enhance cardiovascular function and alleviate the symptoms of atherosclerosis, but there are very few studies on its specific active ingredients, so it is urgent to research and develop natural sources of prevention and treatment of atherosclerosis under the guidance of traditional Chinese medicine theory and modern pharmacodynamics hardening drugs

Method used

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  • Compound stybenpropol a and its application in preventing and treating atherosclerosis
  • Compound stybenpropol a and its application in preventing and treating atherosclerosis
  • Compound stybenpropol a and its application in preventing and treating atherosclerosis

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Effect test

Embodiment 1

[0061] The extraction and identification of embodiment 1 Stybenpropol A

[0062] 1. Extraction method

[0063] The 95% ethanol extract of benzoin resin was extracted with ethyl acetate, separated repeatedly by traditional column chromatography, and finally separated by Pre-HPLC to obtain a monomeric compound, which was designated as Stybenpropol A.

[0064] The method that concrete extracts compound Stybenpropol A from benzoin comprises the following steps:

[0065] S1. Take the dried benzoin resin (5Kg) and add 40L of 95% ethanol to cold-soak and extract 3 times, each time for 24h, and combine the concentrated extracts to obtain the total extract (4.2Kg). The total extract was suspended with an appropriate amount of warm water, extracted three times with petroleum ether (1:1), and then extracted three times with ethyl acetate (1:1) to obtain ethyl acetate extract (3.8Kg).

[0066] S2. Take 2Kg of ethyl acetate extract, dissolve in an appropriate amount of methanol, and carr...

Embodiment 2

[0078] Example 2 Stybenpropol A protects HUVECs cells from TNF-a-induced damage

[0079] The HUVECs injury model induced by TNF-α was established under different concentrations of TNF-α (0, 6.25, 12.5, 25, 50, 100, 200ng / mL). Cell viability was detected at 12, 24 and 48 h after treatment using the CCK-8 assay. Such as figure 2 As shown in panel A, TNF-α treatment resulted in a time- and dose-dependent decrease in cell viability compared to the control group. Specifically, compared with the blank control group, the cell viability decreased to 50% after 12 hours of 12.5 ng / mL TNF-α treatment.

[0080] To determine the optimal conditions under which Stybenpropol A can protect HUVECs from TNF-α-induced injury, it was first determined whether Stybenpropol A had cytotoxic or proliferative effects on HUVECs. From figure 2 In panel B, it can be seen that the cell viability of HUVECs did not change after being treated with Stybenpropol A (0-200 μM) for 24 hours. It can therefore...

Embodiment 3

[0081] Example 3 Effect of Stybenpropol A on the Secretion of Vasoprotective Factor Nitric Oxide by Endothelial Cells Induced by TNF-a

[0082] The effect of Stybenpropol A on the secretion of vascular protective factor nitric oxide from endothelial cells induced by TNF-a was as follows: image 3 shown, from image 3 It can be seen that compared with the normal control group, the nitric oxide content in the model group was significantly reduced (P50μM), the content of nitric oxide secreted by HUVECs induced by TNF-a increased to a certain extent (P<0.01or P<0.05), and it was dose-dependent.

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Abstract

The invention belongs to the technical field of medicine, and particularly discloses compound stybenpropol a and application thereof in improving atherosclerosis (AS). According to the invention, thenovel compound stybenprop a is extracted from benzoin, and research results show that in human umbilical vein endothelial cells HUVECs) injured by tumor necrosis factor (TNF-alpha), the stybenprop a can inhibit endothelial cell inflammatory damage by inhibiting TNF-alpha-induced NF-kappa b activation and nuclear translocation and enhancing expression of anti-apoptotic protein Bcl-2 so as to increase the level of nitric oxide secretion and reduce the levels of vascular adhesion molecules and pro-inflammatory factors, the compound stybenpropol a can significantly inhibit TNF-alpha-induced inflammatory injury and apoptosis of the HUVECs, provides a new choice and approach for the development of anti-atherosclerosis drugs and has a good application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine. More specifically, it relates to a benzoin compound Stybenpropol A and its application in preventing and treating atherosclerosis. Background technique [0002] Atherosclerosis (AS) is the common pathological basis of increasing morbidity, disability and mortality of cardiovascular and cerebrovascular diseases. The global death toll based on AS accounts for 50% of all deaths, far exceeding the second place. The cause of death—tumor, seriously affects people's health and has attracted widespread attention all over the world. Therefore, how to effectively reduce the morbidity and mortality of atherosclerosis has become an important problem faced by clinical and scientific researchers in our country. [0003] Inflammation accompanies all stages of AS from plaque formation to eventual rupture, progressively narrowing the coronary arteries, leading to a series of serious clinical complications. Dys...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/78A61K31/235A61P9/10A61P29/00A61P43/00
CPCA61P9/10A61P29/00A61P43/00C07C69/78
Inventor 王峰张丽张卿鄢琼芳王淑美
Owner GUANGDONG PHARMA UNIV
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