Application of fructus chaenomelis betulinic acid in preparing medicine for resisting hypertensive myocardial fibrosis

A technology of betulinic acid and anti-hypertension, applied in the direction of anhydride/acid/halide active ingredients, application, drug combination, etc., can solve the problems of large side effects, single antihypertensive way of western medicine, etc., to reduce secretion and improve heart structure and functional impairment, to solve the effect of a single pathway of action

Inactive Publication Date: 2018-06-15
SOUTHERN MEDICAL UNIVERSITY
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Problems solved by technology

[0004] The purpose of the present invention is to provide the application of papaya betulinic acid in antihypertensive myocardial fibrosis, the main active ingredient betulinic acid extracted from papaya can be used to prepare antihypertensive myocardial fibrosis medicine, and solve the single antihypertensive approach and side effects of western medicine Major issues, providing a basis for extracting active ingredients of traditional Chinese medicine to lower blood pressure and improve myocardial fibrosis

Method used

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  • Application of fructus chaenomelis betulinic acid in preparing medicine for resisting hypertensive myocardial fibrosis
  • Application of fructus chaenomelis betulinic acid in preparing medicine for resisting hypertensive myocardial fibrosis
  • Application of fructus chaenomelis betulinic acid in preparing medicine for resisting hypertensive myocardial fibrosis

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Embodiment 1

[0038] 1. Specific experimental steps

[0039] (1) Network pharmacology prediction:

[0040] ① Find out the main active ingredients of papaya according to the TCMSP Chinese medicine database;

[0041] ②Find out the target genes related to hypertensive myocardial fibrosis from the GeneCards database;

[0042] ③ Combining the two groups of target genes to take the intersection, and according to oral bioavailability (Oral bioavailability) ≥ 30%, drug-like properties (Drug-like Properties) ≥ 0.18, drug half-life (Drughalf-life) ≥ 4, human colon adenocarcinoma Cell absorption model score (Caco-2) ≥ -0.4 and other relevant pharmacokinetic indicators screened out the main components of papaya that act on myocardial fibrosis in hypertension.

[0043] (2) Serum medicinal chemistry verification:

[0044]① Ten 12-week-old male spontaneously hypertensive rats were randomly divided into 5 groups, including spontaneous hypertensive rat model group (spontaneous hypertensive rat, SHR) and ...

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Abstract

The invention discloses application of fructus chaenomelis betulinic acid in preparing a medicine for resisting hypertensive myocardial fibrosis, and belongs to the technical field of biological medicines. The fructus chaenomelis betulinic acid is applied to treat treating spontaneously hypertensive rats (SHR), and the result shows that after drug administration treatment for 12 weeks, blood pressure of each group of SHR is reduced, and serum endothelin (ET) contents of each dosage group of fructus chaenomelis betulinic acid and a captopril CAP group are remarkably reduced; the nitric oxide (NO) content is remarkably improved; according to each dosage group of fructus chaenomelis betulinic acid, the contents of MCP-1, TNF-alpha, IL-1, IL-6, CRP and MDA can be reduced, so that the result shows that the fructus chaenomelis betulinic acid can be beneficial to reducing of the content of cardiac muscle tissue inflammatory factors, reducing of damage of oxidative stress on tissues, improvingof tissue oxidation resistance, and improving of myocardial fibrosis through multiple target points.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to the application of betulinic acid of papaya in the preparation of antihypertensive myocardial fibrosis drugs. Background technique [0002] Hypertension is a common disease that endangers the health of our people, and myocardial fibrosis (Myocardial Fibrosis, MF) is the main cardiac pathological change caused by hypertension, and it is also one of the important causes of various cardiovascular events. Therefore, it is of great significance to study the inhibition and reversal of myocardial fibrosis. Researches at home and abroad in recent years believe that the mechanism of myocardial fibrosis is the result of excessive accumulation of collagen fibers in the normal tissue structure of the myocardium, a significant increase in the concentration of collagen in the heart tissue, or a change in the composition of collagen. At present, most anti-myocardial fibrosis res...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P9/12A61P9/00A23L33/105A61K36/732
CPCA23V2002/00A61K31/56A61K36/732A23L33/105A23V2200/326A23V2200/30A23V2250/21A61K31/19A61K31/401A61K36/185A61P9/10
Inventor 张国华陈凯黄裕刘馨庄宇鑫管怡晴党文振马韵词
Owner SOUTHERN MEDICAL UNIVERSITY
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