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Compound capable of reducing blood pressure and relaxing blood vessels and application of the compound

A technology for dilating blood vessels and compounds, applied in the field of medicine, can solve the problems of strong biological toxicity, low bioavailability, reduced research and clinical application value, etc.

Pending Publication Date: 2019-11-26
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the strong biotoxicity and low bioavailability of emodin, its research and clinical application value in cardiovascular diseases such as heart disease, stroke, and hypertension have been reduced.

Method used

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  • Compound capable of reducing blood pressure and relaxing blood vessels and application of the compound
  • Compound capable of reducing blood pressure and relaxing blood vessels and application of the compound
  • Compound capable of reducing blood pressure and relaxing blood vessels and application of the compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The pharmacodynamic study of compound (Kanglexin, KLX) shown in embodiment 1 formula I to reduce arterial blood pressure in spontaneously hypertensive rats (SHR)

[0025] 1. Drug preparation: Accurately weigh the compound represented by Formula I (Kanglexin) and dissolve it in distilled water to prepare 4, 8, and 16 mg / mL respectively, and prepare it immediately before use.

[0026] 2. Select 40 SPF grade spontaneously hypertensive rats (spontaneously hypertensive rats, SHR) and 10 common Sprague Dawley rats (purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd., batch number: No. 11400700341202).

[0027] 3. The blood pressure level of SHR was measured by rat tail method, and randomly divided into model control group (Model, 10 rats), Kanglexin low-dose group (10mg / kg / d, 10 rats), and Kanglexin middle-dose group according to the blood pressure value (20mg / kg / d, 10 rats), Kanglexin high-dose group (40mg / kg / d, 10 rats). Ordinary SD rats were used...

Embodiment 2

[0030] Example 2 Pharmacodynamic study of the compound represented by formula I (Kanglexin, KLX) relaxing isolated mesenteric arterioles

[0031] 1. Drug preparation: Accurately weigh the compound represented by Formula I (Kanglexin) and dissolve it in DMSO, vortex and mix well to make the concentration 2, 4, 14, 20, 40, 60 mM, store in the dark, and use immediately Ready to match.

[0032] 2. Select ordinary SD rats, weigh them, and inject 3% sodium pentobarbital solution into the abdominal cavity at 1.2 mL / kg to make them anesthetized. Rapidly open the abdominal cavity of the animal, separate the mesenteric artery, and place it in low-temperature Kreb's-Henseleit solution saturated with 95% oxygen in advance (Kreb's-Henseleit solution formula: NaCl 118mM, NaHCO 3 25mM, D-glucose 11mM, KCl 4.7mM, KH 2 PO 4 1.2mM, MgSO 4 1.17mM, CaCl 2 2.5 mM, pH 7.4).

[0033] 3. Place the blood vessel under a stereo microscope, use micro tweezers and micro scissors to quickly remov...

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Abstract

The invention discloses a compound capable of reducing blood pressure and relaxing blood vessels and application of the compound. The compound has a structure as shown in a formula I which is described in the specification, and can be synthesized and produced on a large scale as a monomeric compound with a clear chemical structure. Experiments prove that arterial blood pressure of spontaneously hypertensive rats can be effectively reduced and the mesenteric microarterial blood vessels of the rats can be relaxed by singly giving the compound (Kanglexin) disclosed by the invention, and the effect is remarkable. The compound disclosed by the invention can be prepared into tablets, powder, capsules, granules, suspensions, injections and the like together with pharmaceutically acceptable carriers, and can be used for relaxing blood vessels and reducing blood pressure in an independent administration mode or a combined treatment mode. The invention provides a new technical means for the treatment of hypertension.

Description

technical field [0001] The invention relates to a medicine and its application, in particular to a compound capable of lowering blood pressure and relaxing blood vessels and its application. The invention belongs to the technical field of medicine. Background technique [0002] The "China Cardiovascular Disease Report 2017" shows that cardiovascular and cerebrovascular diseases have become the leading cause of death in the world. Cardiovascular disease deaths account for more than 40% of residents' deaths, far higher than tumors and ranking first. The World Health Organization (WHO) predicts that the number of patients with cardiovascular diseases will continue to increase rapidly in the next ten years, and the burden of treatment will increase day by day. [0003] Studies have shown that high blood pressure is an independent risk factor for cardiovascular and cerebrovascular diseases. In 2017, about 17.3 million people died of cardiovascular and cerebrovascular diseases i...

Claims

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Application Information

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IPC IPC(8): A61K31/225A61P9/12A61P9/08
CPCA61K31/225A61P9/12A61P9/08
Inventor 杨宝峰杜智敏张妍
Owner HARBIN MEDICAL UNIVERSITY
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