Application of des-O-methyllasiodiplodin in preparation of medicament for treating hypertension

A technology of methyl-maodiposen and hypertension, which is applied in the directions of drug combination, pharmaceutical formula, cardiovascular system diseases, etc., can solve the problem of no research report on the therapeutic effect of hypertension, and achieve good treatment of hypertension and good treatment. effect of effect

Inactive Publication Date: 2013-04-17
NANJING CHILDRENS HOSPITAL AFFILIATED TO NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chinese patent 200810200074.4 discloses benzomacrolide compound (3R)-de-O-methylmadipredrine, its derivatives and their preparation methods and uses; 201110079284.4 discloses 3R-de-O-methyl The use of mateprenol in the preparation of drugs for the prevention or treatment of depression; but there is no research report on its therapeutic effect on hypertension

Method used

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  • Application of des-O-methyllasiodiplodin in preparation of medicament for treating hypertension
  • Application of des-O-methyllasiodiplodin in preparation of medicament for treating hypertension
  • Application of des-O-methyllasiodiplodin in preparation of medicament for treating hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Pharmacological effects of des-O-methylmadipredrine (DML) on hypertension

[0018] 1. Animal model preparation and experimental grouping

[0019] Establishment and grouping of animal models: 13-week-old SD rats (220-250g), anesthetized by intraperitoneal injection of pentobarbital (40mg / Kg BW), made a midline abdominal incision, separated and ligated the left renal artery, renal vein and retroureter , Left nephrectomy was performed, and the abdominal cavity was closed layer by layer, and the postoperative recovery was 1 week. In the experiment, 38 rats surviving after left nephrectomy were randomly divided into 4 groups, the control group (n=8): drinking tap water; the model group (n=10) and the low Dosage and high-dose treatment group (10 rats in each group): Place a rubber medium made of 200mg / Kg deoxycorticosterone acetate (DOCA) and silica gel under the skin between the shoulder blades on both sides of the rat, and give 1% NaCl drinking water ; The rats...

Embodiment 2

[0044] Example 2 The antihypertensive effect of de-O-methylmadiprene on spontaneously hypertensive rats

[0045] 1. Materials and methods

[0046] 1. Grouping of experimental animals: 30 male spontaneously hypertensive rats (SHR) (16 weeks old, body weight 280-320g), were randomly divided into 3 groups, 10 in each group, respectively SHR control group, de-O- Low-dose and high-dose treatment groups of methylmadiprene. Ten healthy male Wistar-Kyoto (WKY) rats of the same age and weight were used as the normotensive control group. The des-O-methylmadiprene low-dose treatment group and the high-dose treatment group were given 20 and 40 mg·Kg respectively -1 d -1 , gavage, 1 time / day, the SHR control group and the WKY normotensive control group were given the same amount of distilled water by gavage for 8 consecutive weeks.

[0047] 2. Measurement of systolic blood pressure in rats: The systolic blood pressure (SBP) was measured once a week by tail artery manometry, and each ra...

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Abstract

The invention discloses an application of des-O-methyllasiodiplodin in preparation of a medicament for treating hypertension. Experimental studies show that the des-O-methyllasiodiplodin can well reduce caudal arterial blood pressure, central aortic systolic blood pressure, central aortic diastolic blood pressure, central aortic mean blood pressure and pulse wave velocity of spontaneously hypertensive rats (SHR), improve the artery elastic function, reduce the aortic media thickness and vascular wall collagen fibers and increase the inside diameters of blood vessels, and has a good effect of preventing and treating the hypertension. Obvious adverse response is avoided in the experimental process, and the des-O-methyllasiodiplodin is expected to be developed into a new-generation safe and effective medicament for preventing and treating the hypertension.

Description

technical field [0001] The present invention relates to des-O-methylmaidepredrine compounds, in particular to the application of des-O-methylmaudepredrine in the preparation of medicines for treating hypertension. Background technique [0002] Hypertension is the most common chronic disease and has become a major public health problem worldwide. According to the research conducted by WHO in 2004, the number of deaths caused by hypertension is 7.5 million cases in the world every year, and the loss of disability-adjusted life years caused by it ranks fifth. In the past few decades, the prevalence of hypertension in my country has been increasing rapidly, especially since the reform and opening up, with the changes in people's lifestyles and the acceleration of the aging process, the increase in the prevalence of hypertension has accelerated. The estimated number of hypertensive adults in my country has increased from 30 million in 1960 to 59 million in 1980, and then increas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P9/12
Inventor 张爱华黄松明
Owner NANJING CHILDRENS HOSPITAL AFFILIATED TO NANJING MEDICAL UNIV
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