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Application of chondriokinesis inhibitor in preparation of medicines for preventing and treating hypertension

A mitochondrial and high blood pressure technology, applied in the field of biomedicine, can solve the problems such as the difficulty of new antihypertensive drugs and the lack of anti-hypertension

Active Publication Date: 2015-05-27
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above drugs have decades of history. Due to the lack of discovery of new antihypertensive targets, new antihypertensive drugs have been difficult to come out in recent years

Method used

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  • Application of chondriokinesis inhibitor in preparation of medicines for preventing and treating hypertension
  • Application of chondriokinesis inhibitor in preparation of medicines for preventing and treating hypertension
  • Application of chondriokinesis inhibitor in preparation of medicines for preventing and treating hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Application of Mitochondrial Splitting Inhibitors in Prevention and Treatment of Hypertension

[0022] 1. Animals and experimental reagents:

[0023] SD rats (strain: SD, purchased from Beijing Jingweitong Lihua Experimental Animal Technology Co., Ltd.), Mdivi-1, Dynasore (Selleck China, Shanghai)

[0024] 2. Experimental method:

[0025] 2.1. Establishment of rat mesenteric artery constriction model induced by phenylephrine and high potassium

[0026] Healthy SD male rats, weighing 300-350g. The mesenteric artery was placed in a DMT microvascular tensiometer (Denmark) to balance for 1 hour, and different treatments were given, and the change of vascular tension was measured at the same time. The contraction was induced by phenylephrine and high potassium, the concentration of phenylephrine was 5 μM, and the high potassium solution was 60 mM high potassium phosphate buffer solution (KPSS).

[0027] 2.2 Effects of Mdivi-1 and Dynasore on rat mesenteric arte...

experiment example 1

[0042] Experimental Example 1 Mechanism Research

[0043] In order to confirm that the vasoconstriction effect of mitochondrial fission inhibitors comes from the inhibition of mitochondrial fission rather than the effect of the drug structure itself, this experimental example further studied the mechanism:

[0044] Mitochondrial fission produces reactive oxygen species derived from mitochondria. We pretreated rat mesenteric arteries with MitoTEMPO (Sigma-Aldrich), a specific antioxidant for mitochondrial reactive oxygen species, and found that it could also inhibit the contraction induced by phenylephrine and high potassium. Figure 6 It was shown that MitoTEMPO pretreatment of rat mesenteric artery inhibited the constriction of rat mesenteric artery induced by phenylephrine and high potassium. After MitoTEMPO pretreatment of rat mesenteric artery for 30 minutes, phenylephrine and high potassium were administered respectively to induce contraction, such as Figure 6 A, 10, 20...

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Abstract

The invention discloses an application of a chondriokinesis inhibitor in preparation of medicines for preventing and treating hypertension, belonging to the technical field of biological medicines. The research proves that the chondriokinesis activity of blood vessels participates in vasotonia generation, and due to inhibition of chondriokinesis of blood vessels, vasoconstriction induced by phenylephrine and high potassium fluid can be obviously relaxed. According to a chondriokinesis inhibitor Mdivi-1 of which the structural formula is shown in a formula I, the vasoconstriction induced by phenylephrine and high potassium fluid can be obviously relaxed, so that the animal blood pressure is reduced. On the basis, the invention provides a method for screening novel hypotensive drugs and a novel application of the chondriokinesis inhibitor serving as a novel hypotensive drug. According to the application provided by the invention, a novel technical means is provided for prevention and treatment of hypertension. The structural formula is as shown in the specification.

Description

technical field [0001] The invention relates to a new application of a mitochondrial fission (mitochondrial fission) inhibitor, in particular to the application of the mitochondrial fission inhibitor in the preparation of antihypertensive drugs. The invention belongs to the technical field of biomedicine. Background technique [0002] Hypertension disease is a common cardiovascular disease that seriously threatens human health. If hyperbaric disease cannot be effectively controlled, it will cause damage to target organs such as the heart, brain, and kidneys, causing disability and death. At present, antihypertensive drugs mainly include the following categories: 1. Diuretic and antihypertensive drugs: such as hydrochlorothiazide. 2. Sympathetic nerve depressants: (1) central antihypertensive drugs: such as clonidine, etc.; (2) ganglion blocking drugs: such as camphedrine, etc.; (3) noradrenergic nerve ending blocking drugs : such as reserpine; (4) adrenergic receptor bloc...

Claims

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Application Information

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IPC IPC(8): A61K49/00A61K31/517A61K31/166A61P9/12
Inventor 董德利
Owner HARBIN MEDICAL UNIVERSITY
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