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Application of a kind of benzimidazole derivative in the preparation of medicine for treating heart failure

A technology of dihydrobenzimidazole and derivatives, applied in the field of preparation of benzimidazole derivatives for treating heart failure, 2-aryl-1,3-dihydrobenzimidazole derivatives

Active Publication Date: 2021-06-04
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 a kind of benzimidazole derivative in the preparation of medicine for treating heart failure
  • Application of a kind of benzimidazole derivative in the preparation of medicine for treating heart failure
  • Application of a kind of benzimidazole derivative in the preparation of medicine for treating 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 Figure 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-ca...

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Abstract

The present invention relates to the use of LB2G as a novel and effective method for blocking key cardiac hypertrophy and fibrosis-promoting signaling pathways in vivo, thereby inhibiting cardiac hypertrophy and cardiac fibrosis during the progression of heart failure, delaying or / and reversing heart failure course of disease. The invention provides the application of LB2G in the treatment of heart failure, which has remarkable curative effect and no obvious toxic and side effects. Therefore, the LB2G described in the present invention can be prepared as a pharmaceutical preparation for treating 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 Patents(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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