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New Application of Total Alkaloids of Guanbaifu and Guanfu Nonin

A technology of total alkaloids and Guanbaifu, which is applied in the field of preparation of slow sodium ion channel blockers and antiarrhythmic drugs, can solve the problem of prolonged action potential plateau, easily induced ventricular arrhythmia, syncope and sudden death And other issues

Active Publication Date: 2016-04-06
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In recent years, new targets for long QT syndrome (L-QT, a series of syndromes prone to induce ventricular arrhythmia, syncope and sudden death) and other arrhythmia have been studied. Experiments have shown that the cardiac sodium ion channel gene SCN5A Mutation, resulting in the repeated development of slow sodium current, delaying the current decay, prolonging the plateau period of action potential, and causing L-QT

Method used

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  • New Application of Total Alkaloids of Guanbaifu and Guanfu Nonin
  • New Application of Total Alkaloids of Guanbaifu and Guanfu Nonin
  • New Application of Total Alkaloids of Guanbaifu and Guanfu Nonin

Examples

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Effect test

experiment example 1

[0064] Experimental Example 1: Pharmacological Study on Antiarrhythmic Effects of Total Alkaloid Salts of Guanbaifu

[0065] 1. Experimental materials: Guanbaifu total alkaloid salts, prepared according to Example 3 of the present invention; lidocaine hydrochloride injection, Shandong Yushui Xierkang Pharmaceutical Co., Ltd.; experimental rats are provided by Shanghai Slack Animal Center and Rabbits were provided by the Animal Laboratory of China Pharmaceutical University.

[0066] 2. The protective effect of Guanbaifu total alkali salt on arrhythmia induced by electrical stimulation of rabbit heart

[0067] 2.1 Experimental method

[0068] Twelve rabbits, weighing 2.4±0.6kg, were divided into two groups, 6 in each group, half male and half male, one group was the total alkaloid group of Guanbaifu, and the other group was the lidocaine group. Urethane 1.2g / kg was used for iv anesthesia at the edge of the ear, and the heart was exposed by opening the chest under artificial re...

experiment example 2

[0084] Experimental Example 2 Study on the blocking effect of Guanfu total alkaloids and Guanfu A hydrochloride on myocardial slow sodium ion channel

[0085] 1 Experimental method

[0086] 1.1 Cardiomyocyte isolation

[0087] Normal guinea pigs (male or female, 250±20g) were stunned, and the heart was quickly removed by chest opening, placed in calcium-free Tyrode solution at 4°C, trimmed and hung on the Langendorff apparatus through the aorta, and placed in a 37°C free Calcium Tyrode's solution was perfused at constant temperature at a flow rate of 6-8 mL / min. Perfuse for about 5 minutes, wash away the congestion, and then replace with enzyme-containing calcium-free Tyrode's solution for about 10-15 minutes. When the myocardium becomes loose and translucent, cut off the left ventricle and gently blow it in KB solution with a glass dropper. After filtration, the rod-shaped single ventricular myocytes with clear stripes and smooth surface can be obtained, which are stored in...

experiment example 3

[0099] Experimental Example 3 Study on the Preparation Technology of Total Alkaloids of Guanbaifu

[0100] 1 Comparison of ethanol cold extraction and ethanol heating and reflux extraction of Guanbaifu

[0101] 1.1 Experimental method

[0102] Cold soaking method: crush 500 grams of Guanbaifu granules into 10-20 meshes, soak them in 1000ml 95% ethanol at 25°C for 24 hours, leaching, add 1000ml 95% ethanol for the second time, soaking at 25°C for 12 hours, leaching, add Soak 1000ml of 95% ethanol at 25°C for 4 hours, extract, combine the extracts, filter, and recover ethanol from the filtrate under reduced pressure to obtain a thick alcohol extract, add a small amount of distilled water, place in the refrigerator, cool and filter, remove impurities such as pigments, extract several times with petroleum ether, and Remove the fat-soluble components therein, then extract with chloroform, dehydrate and filter the chloroform extract with anhydrous sodium carbonate, recover chlorofo...

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Abstract

The invention provides a preparation method of total alkaloids of radix aconiti coreani as well as an application of the total alkaloids of radix aconiti coreani in preparing a slow sodium ion channel blocker and an antiarrhythmic medicine. Researches show that both the total alkaloids of radix aconiti coreani and Guanfu A hydrochlorate have an inhibiting effect on a slow sodium current of the ventricular muscle of a guinea pig. The invention particularly relates to an application of the Guanfu base I in preparing enzyme inhibitors for drug metabolism. The invention further provides an application of the Guanfu base A in preparing the slow sodium ion channel blocker.

Description

[0001] The application of the present invention is a divisional application, the original application number is 201210203325.0, the original application date is June 19, 2012, and the original invention name is: new uses of total alkaloids of Guanbaifu and Guanfu nonyl. technical field [0002] The invention relates to the new application of total alkaloids of Guanbaifu and Guanfu nonin. It specifically relates to the application of total alkaloids of Guanbaifu in the preparation of slow sodium ion channel blockers and antiarrhythmic drugs. Background technique [0003] Guanbaifu is the root tuber of Aconitumcoreanum (Levl,) Rapaics, a traditional Chinese medicine. It is one of the common Chinese medicines. It is mainly used for heartache and blood stagnation. Its chemical composition is mainly related to Guanfubase G, GFG, Guanfubase A, GFA, Guanfubase I, GFI, etc. All three are diterpene alkaloids. Modern pharmacological studies have shown that Guanfu A, Guanfuheptan, and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/407A61K36/714A61P9/06A61K125/00
Inventor 王广基柳祥汤依群孙建国刘静涵于鹏曾艳朱天全刘建平杨春华孙申国程志国汪旻晖
Owner CHINA PHARM UNIV
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