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Application of bufalin in preparation of medicine for treating atherosclerosis

A technology of atherosclerosis and bufalin, applied in the field of medicine, can solve problems such as limited effects, achieve the effects of reducing adhesion, expanding the scope of application, and reducing transendothelial migration

Pending Publication Date: 2022-01-21
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above-mentioned treatment methods have limited effects, and it is urgent to discover new therapeutic target drugs

Method used

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  • Application of bufalin in preparation of medicine for treating atherosclerosis
  • Application of bufalin in preparation of medicine for treating atherosclerosis
  • Application of bufalin in preparation of medicine for treating atherosclerosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Example 1 In Vivo Atherosclerosis Pharmacological Activity Test

[0064] 1. Animal experiments: the present invention uses ApoE with a C57 / BL6 background - / - Mice were used as the research objects, and the model of atherosclerosis was established by feeding high-fat food, and the prevention model and treatment model of bufalin were established to evaluate the therapeutic effect of bufalin on atherosclerosis.

[0065] Prevention Model: ApoE - / - Mice were fed high-fat diet for 13 weeks, and at the same time, 1 mg / kg bufalin was injected intraperitoneally, once a day, 6 times a week, for 13 consecutive weeks. At the end of the experiment, the mice were sacrificed, the aortas were taken for Oil Red O staining, and blood was collected to detect blood lipids and inflammatory factors. ApoE of the control group and bufolin-treated - / - The representative pictures of oil red O staining of mouse aorta and the statistical results of aortic plaque are as follows: figure...

Embodiment 2

[0074] Example 2 In Vitro Cytology Experiment

[0075] Taking primary endothelial cell HUVEC as the research object, firstly treat HUVEC cells with bufalin for 24 hours, then treat HUVEC cells with TNFα or IL-1β, collect samples 6 hours later, and detect SRC-3, ICAM-1, p-p65 and p65 expression. In addition, THP-1 cells were used to detect the effects of bufalin on monocyte adhesion and transendothelial migration.

[0076] Treat HUVEC cells with bufalin for 24 hours, then treat HUVEC cells with TNFα or IL-1β, collect samples 6 hours later, and detect the protein expressions of SRC-3, ICAM-1, p-p65 and p65. The result is as Figure 5 shown.

[0077] Treated with bufalin for 24 hours, added calcein-labeled THP1 monocytes, and then treated with TNFα or IL-1β for 6 hours, took pictures with a fluorescence microscope, and calculated the ratio of the number of THP1 adhered to HUVECs to the number of total HUVECs. The result is as Image 6 shown.

[0078] HUVEC cells were spread...

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Abstract

The invention discloses application of bufalin in preparation of a medicine for treating atherosclerosis. According to the invention, in-vivo and in-vitro experiments prove that bufalin can be used for treating atherosclerosis induced by high-fat food, and possibly, the bufalin reduces the expression of ICAM-1 at a transcriptional level through an NF-kappa B pathway, so that the adhesion of mononuclear cells to HUVEC endothelial cells and the transendothelial migration are reduced. The bufalin can treat atherosclerosis, has a protection effect on aorta, is safe and effective, and can provide a new target for treatment of atherosclerosis.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to the new medical application of bufalin, in particular to the application of bufalin in the preparation of drugs for treating atherosclerosis. Background technique [0002] Bufalin belongs to the steroidal compound and is the effective active ingredient of toad venom, which is a traditional oriental Chinese medicine obtained from the dried secretion of the skin glands and post-auricular glands of toads. Its molecular formula is C 24 h 34 o 4 , its chemical structural formula (abcam) is as follows: [0003] [0004] Bufalin is a potential inhibitor of SRC-3, by inhibiting Na + , K + -ATPase increases intracellular Na + Concentration, and by adjusting the Na + / Ca 2+ Pump activity leads to intracellular Ca 2+ Accumulation, resulting in increased contractility of cardiomyocytes and vasoconstriction. Bufalin has cardiotonic, anti-inflammatory and anti-tumor effects. [00...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61P9/10
CPCA61K31/585A61P9/10
Inventor 黄峥嵘陈文博刘诗晓丁康熙李卫华
Owner XIAMEN UNIV
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