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Application of benzimidazole derivatives in preparation of medicines for treating congestive heart failure

A technology of benzimidazole and dihydrobenzimidazole is used in 2-aryl-1,3-dihydrobenzimidazole derivatives, and benzimidazole derivatives are used in the field of preparing medicines for treating heart failure

Active Publication Date: 2019-02-15
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still no effective drugs to delay the progression of heart failure clinically.

Method used

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  • Application of benzimidazole derivatives in preparation of medicines for treating congestive heart failure
  • Application of benzimidazole derivatives in preparation of medicines for treating congestive heart failure
  • Application of benzimidazole derivatives in preparation of medicines for treating congestive heart failure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Inhibition of LB2G on cardiac hypertrophy and fibrosis in TAC mice

[0026] 1. Experimental animals: C57 mice, male, weighing 25-30g, SPF grade. The animals were first weighed and numbered, and 18 healthy mice were selected and randomly divided into 3 groups, 6 in each group. Including sham operation group, model control group and medication group (1mg / kg / d).

[0027] 2. Treatment of each group

[0028] 1) Sham operation group: room temperature, 3% pentobarbital sodium anesthetized mice with 1ml / kg body weight, fixed the mice, connected to a ventilator after tracheal intubation, respiratory rate 100 times / min, tidal volume 1ml. The depilatory ointment was applied to the chest area of ​​the mice. After depilation, the chest area was disinfected with 75% alcohol to prepare the skin. Under the halogen lamp, the skin of the second intercostal space was cut with micro scissors, and the pectoralis major, pectoralis minor, and intercostal muscles were cut in sequ...

Embodiment 2

[0052] Example 2: LB2G inhibits the activation of rat heart cells and the signal transduction of Wnt / β-catenin

[0053] 1. Experimental treatment:

[0054] The primary cardiac cells of SD rat suckling mice were extracted, and the cultured rat cardiomyocytes and cardiac fibroblasts were divided into 1.5×10 6 Planted in 6-well cell culture plate, cultured for 1 day, starved for 24 hours, given different doses of LB2G 1 hour in advance, and then given AII (10 -7 M) Stimulate, collect protein after 24h, and carry out Western blot experiment.

[0055] 2. Experimental results

[0056] (I) Experimental results such as Image 6 As shown, LB2G can effectively inhibit the expression of cardiac hypertrophy indexes β-myosin and α-actin mediated by AII. Inhibits Wnt / β-catenin signaling pathway activated by AII.

[0057] (II) If Figure 7 As shown, LB2G inhibited rat heart hypertrophy indicators (cardiac natriuretic peptide, brain natriuretic peptide, β-myosin, α-actin); and Wnt / β-cat...

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Abstract

The invention relates to LB2G serving as a novel and effective drug for blocking an in-vivo key signaling pathway for promoting cardiac hypertrophy and fibrosis so as to inhibit cardiac hypertrophy and cardiac fibrosis in the heart failure progression process and delay and / or reverse the disease course of the heart failure. The invention provides application of the LB2G in treatment of heart failure. The LB2G has obvious curative effects, and does not have any obvious toxic or side effect. Therefore, the LB2G disclosed by the invention can be prepared into a pharmaceutical preparation for treating the heart failure.

Description

technical field [0001] The present invention relates to the use of a benzimidazole derivative in the preparation of a drug for treating heart failure, in particular to the use of a 2-aryl-1,3-dihydrobenzimidazole derivative (LB2G) in the preparation of a drug for treating heart failure use. Background technique [0002] As the global population ages, heart failure has become a significant medical burden worldwide. Heart failure is a syndrome of various heart diseases progressing to an advanced stage. Cardiac hypertrophy is an independent risk factor for heart failure, and it is an inevitable pathophysiological process for the development of various heart diseases to heart failure. Left ventricular hypertrophy often indicates a poor prognosis of heart disease. Clinical trials have further confirmed that improvement of left ventricular hypertrophy often indicates good outcomes for patients with heart disease. prognosis. Therefore, inhibiting cardiac hypertrophy can not only...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4184A61P9/04
CPCA61K31/4184A61P9/04
Inventor 洪雪彭艳
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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