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7,4'-di(mono succinate)o-ethoxy-daidzein and novel medical uses thereof

A technology of succinic acid monoester and daidzein, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of restricting widespread use, low bioavailability, and poor water solubility of isoflavones

Inactive Publication Date: 2008-09-03
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility and low bioavailability of isoflavones, its widespread use is limited.

Method used

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  • 7,4'-di(mono succinate)o-ethoxy-daidzein and novel medical uses thereof
  • 7,4'-di(mono succinate)o-ethoxy-daidzein and novel medical uses thereof
  • 7,4'-di(mono succinate)o-ethoxy-daidzein and novel medical uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Effect of DZ5 on normal pressure and hypoxia resistance of mice

[0021] 90 mice, weighing 20±2g, half male and half male, were randomly divided into 9 groups. Normal saline group, DZ540mg / kg, 80mg / kg, 160mg / kg group and nimodipine injection 40μg / kg group. After 10 minutes of tail vein injection, the mice were respectively moved into 150ml jars filled with 10g of fresh soda lime at the bottom, and sealed with a cap. The survival time was observed, and respiratory arrest was regarded as the death sign. Take another 4 groups of mice as above, and give normal saline and DZ540mg / kg, 80mg / kg, 160mg / kg respectively. After 10 minutes of administration, 2 mg / kg of isoproterenol hydrochloride was injected intraperitoneally, and immediately put into jars and sealed. The observation method is the same as before. And calculate the survival time extension rate (%) according to the following formula:

[0022]

[0023] The experimental results show that DZ580mg / kg a...

Embodiment 2

[0027] Example 2: Effect of DZ5 on Acute Cerebral Ischemia in Mice

[0028]50 mice (20±2g) were randomly divided into 5 groups, 10 in each group, half male and half male, respectively i v. physiological saline, DZ540mg / kg, 80mg / kg, 160mg / kg and nimodipine injection 40μg / kg. After 10 minutes, the mouse was quickly decapitated from the neck behind both ears, and the gasping time of the mouse was observed in a double-blind method.

[0029] And calculate the survival time extension rate (%) according to the following formula:

[0030]

[0031] The experimental results show that DZ580mg / kg and 160mg / kg can significantly prolong the panting time of decapitated mice, which is significantly different from that of the normal saline control group (P<0.05 and P<0.01 respectively), and nimodipine can also significantly The panting time of decapitated mice was prolonged (P<0.01). See Tab 2 for the results.

[0032] Tab 2 Effects of DZ5 on persistent time of gasping of isolated head...

Embodiment 3

[0035] Example 3: Mouse bilateral common carotid artery and vagus nerve ligation

[0036] According to the method of Example 2, the drugs were divided into groups, and the bilateral common carotid arteries and vagus nerves were ligated with No. 0 silk thread 10 minutes after the drug administration. The survival time of the mice was observed, and respiratory arrest was used as the death index.

[0037] The experimental results show that DZ580mg / kg and 160mg / kg can significantly prolong the survival time of mice with bilateral common carotid artery and vagus nerve ligation, which is significantly different from that of the normal saline control group (P<0.05 and P<0.01, respectively). Nimodipine can also significantly prolong the survival time of mice with bilateral common carotid artery and vagus nerve ligation (P<0.01). See Tab 3 for the results.

[0038] Tab 3 Effects of DZ5 on survival time of mice subjected to bilateral carotid artery ligation. (Mean±SD, n=10)

[0039] ...

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Abstract

The invention discloses new pharmaceutical uses of 7, 4'- di(mono succinate) oxyethoxypropyl daidzein. Pharmacological activity research is carried out to DZ5 by an experimental model for mice under atmospheric hypoxia tolerance, an experimental model for mice acute cerebral ischemia, an experimental model for bilateral common carotid arteries and vagus nerve ligation, an experimental model for mice KCN poisoning, an experimental model for mice NaNO2 poisoning and experimental model for learning and remembering, an action model for rat cortical neuron damage caused by anoxia of DZ5, an effect model for rat myocardial ischemia caused by hypophysin, an experimental model for vitro anti platelet aggregation, an experimental model for vivo anti platelet aggregation, and an effect model for arterial thrombosis in rabbits. Proved by the result, DZ5 has the functions of anti-cerebral ischemia and anoxia, anti-myocardial ischemia and anoxia, antagonistic memory disorders, anti-platelet aggregation and thrombosis, and protection of rat cortical neuron damage caused by anoxia. DZ5 can be mixed with a pharmacologically acceptable carrier or excipient to prepare medicine compositions.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to 7,4'-bis(succinic acid monoester)oxyethoxy-pueraria daidzein (DZ5) and its new application in medicine, in particular to 7,4'-bis(succinic acid monoester) Ester) oxyethoxy-didzein in the preparation of anti-cerebral ischemia, hypoxia, anti-myocardial ischemia, hypoxia, antagonism memory impairment, anti-platelet aggregation and anti-thrombosis, protection of rat cortical nerves caused by hypoxia Application of meta-damaging drugs. Background technique [0002] Cardiovascular and cerebrovascular diseases are major diseases that endanger human health and life. According to the World Health Report of the World Health Organization in 2000, the number of deaths from cardiovascular and cerebrovascular diseases in the world is 16.97 million, accounting for 30.3% of the total death population. In my country, the morbidity and mortality of cardiovascular and cerebrovascular diseases rank ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/36A61K31/352A61P9/10A61P25/28A61P7/02
Inventor 王淑君姚崇顺
Owner SHENYANG PHARMA UNIVERSITY
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