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Application of tetrahydroberberrubine in preparation of heart protection medicine

A tetrahydroberberine and cardioprotection technology, applied in the field of biomedicine, can solve the problems of limited application, low absolute bioavailability of berberine, low water solubility, etc. Interstitial fibrosis, chemical stabilization effect

Active Publication Date: 2021-12-14
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the absolute bioavailability of berberine is as low as 0.68%, the absolute bioavailability of berberine hydrochloride is 2.29%, and the water solubility is extremely low, which limits its wide application in clinical practice.

Method used

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  • Application of tetrahydroberberrubine in preparation of heart protection medicine
  • Application of tetrahydroberberrubine in preparation of heart protection medicine
  • Application of tetrahydroberberrubine in preparation of heart protection medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 4

[0083] Embodiment 1 Tetrahydroberbererythine (THBru) intragastric administration of LD to mice 50 determination

[0084] 1. Experimental method:

[0085] Determination of LD of tetrahydroberbererythrine (THBru) intragastrically administered to mice by Bilss method 50 . The specific method is as follows: take 30 Kunming mice, half male and half female, weighing 18-22 g, and the mice are fasted for 16 hours before the experiment, and are randomly divided into 6 groups, 5 mice in each group, and raised in separate cages according to the dosage from high to low. , weigh for registration, and mark mice with ear tags. Take the concentrated solution that the No. 8 mouse gavage needle can just pass through as the maximum concentration of administration, that is, 100g·kg -1 , according to the dosage interval of 5, 0.032g·kg -1 , 0.16g·kg -1 , 0.8g·kg -1 , 4g·kg -1 , 20g·kg -1 , 100g·kg -1 Mice were administered intragastrically. Immediately after administration, observe the ...

Embodiment 2 4

[0091] Embodiment 2 Tetrahydroberberine (THBru) improves cardiac function in mice

[0092] 1. Experimental method

[0093] Thirty 8-month-old male Kunming mice were randomly divided into six groups: Sham sham operation group, TAC model group, TAC+THBru low-dose group (TAC+THBru 10 mg·kg -1 ), TAC+THBru high-dose group (TAC+THBru 20mg·kg -1 ), TAC+berberine group (TAC+BBR 20mg·kg -1 ), TAC+Captopril group (TAC+Captopril 10mg·kg -1 ), 5 in each group.

[0094]Aortic coarctation (transverse aortic constriction, TAC) to establish a mouse model of pressure load-induced heart failure. After the mice had anesthesia reactions such as loss of corneal reflex, decreased muscle strength, and flaccid paralysis, the mice were fixed on the operating board in a supine position. Mice were intubated orally and connected to a ventilator. Ventilator parameter setting: respiratory rate 105-110 times / min, tidal volume 2-3 ml / min. Hair removal cream was used to remove the mouse hair at the po...

Embodiment 3 4

[0098] Example 3 Tetrahydroberberine (THBru) inhibits cardiomyocyte hypertrophy

[0099] 1. Experimental method

[0100] Experimental animals and grouping are the same as in Example 2. HE staining was used to evaluate the pathological changes of cardiac tissue.

[0101] The specific method of HE staining of paraffin tissue sections: before staining, the paraffin in the paraffin tissue sections must be removed with xylene, rinsed with distilled water for 1 minute, stained with hematoxylin for 3-5 minutes; rinsed with tap water for 30 minutes; stained with eosin for 1 minute minutes, then placed in 80%, 95% and absolute ethanol in turn, each for 1 minute; finally placed in xylene for 2 minutes, dried in the air, and sealed with neutral gum. The size of the cross-section of the heart and the thickness of the ventricular wall were observed by taking pictures under a microscope.

[0102] 2. Experimental results

[0103] The overall mouse heart size is figure 2 shown. from ...

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Abstract

The invention relates to an application of tetrahydroberberrubine in preparation of a heart protection medicine. Pharmacological experiments of tetrahydroberberrubine show that tetrahydroberberrubine can significantly improve cardiac dysfunction induced by pressure load, and has an obvious heart protection effect; and meanwhile, myocardial cell hypertrophy and interstitial fibrosis can be remarkably inhibited, the heart remodeling process is prevented, and the heart is prevented from entering the heart failure stage. In addition, the tetrahydroberberrubine compound is high in bioavailability, low in toxicity, stable and easy to produce, transport, store and take, and is a heart protection medicine with a wide application prospect.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to the use of tetrahydroberbererythrine in the preparation of a medicine for heart protection, especially for treating heart failure. Background technique [0002] Heart failure (HF) is one of the main causes of death from various heart diseases, and it is a common complex syndrome in clinical practice. Heart failure has a high morbidity rate, and the five-year survival rate after diagnosis is similar to that of patients with malignancy. This high mortality directly reflects the insufficiency of modern treatment, and it is urgent to develop new heart failure drugs for early heart disease to improve the quality of life of patients. This is not only a severe challenge facing the whole society, but also a hot spot in life science research today. [0003] The occurrence of heart failure is related to hemodynamic abnormalities, neuroendocrine hormone disorders, myocardial injury, ventricular r...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K45/06A61P9/00A61P9/04A61P9/10
CPCA61K31/4375A61K45/06A61P9/00A61P9/04A61P9/10A61K2300/00
Inventor 张勇杨宝峰刘鑫韩维娜林园王磊
Owner HARBIN MEDICAL UNIVERSITY
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