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Corynoxeine and application of isomer thereof in preparing medicines

A technology of dehydromenthomenine and isomer, applied in the field of traditional Chinese medicine, can solve the problems of abnormal contraction of blood supply arterioles, disturbance of arteriole diastolic and systolic function, damage to target organs and the like

Inactive Publication Date: 2011-03-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

2. The diastolic function of the arterioles in the target organ is disordered, which leads to abnormal contraction of the arterioles supplying blood to the organ, which reduces the blood flow of the organ and causes ischemic damage to the target organ
4. The primary disease causes oxidative stress, which releases a large amount of oxygen free radicals in the body and causes damage to target organs
So far, there have been no reports on the vasodilator, antihypertensive, and cardiac effects of the active ingredient of Uncaria: dehydrorhynchophylline (corynoxeine) and its isomers (isocorynoxeine, isocorynoxeine)

Method used

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  • Corynoxeine and application of isomer thereof in preparing medicines
  • Corynoxeine and application of isomer thereof in preparing medicines
  • Corynoxeine and application of isomer thereof in preparing medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Relaxation effect of dehydrorhynchophylline and isodehydrorhynchophylline on aortic ring in hypertensive rats

[0036] Take male spontaneously hypertensive rats, weighing 200-250 g. Animals were sacrificed after anesthesia, and the thoracic aorta was removed and placed in a mixed gas (95% O 2 , 5% CO 2 ) in the nutrient solution, wash the congestion inside and outside the blood vessels, and use tweezers to remove the surrounding fatty connective tissue. Cut the arterial strip into a vascular ring about 5 mm long, pass it through with two stainless steel wire hooks, and move it into the bath cavity with 10 ml of nutrient solution added in advance, and continue to pass the mixed gas, and the constant temperature water pump maintains the temperature in the bath at 37 °C . Composition of nutrient solution: NaCl 118 mmol / L, KCl 4.5 mmol / L, CaCl 2 2.5 mmol / L, MgSO 4 1.2 mmol / L, KH 2 PO 4 1.0 mmol / L, NaHCO 327 mmol / L, glucose 10 mmol / L. One hook is fixe...

Embodiment 2

[0044] Example 2 Effects of dehydrorhynchophylline and isodehydrorhynchophylline on the negative inotropic effect of the ventricular papillary muscle of hypertensive rats and the effect of increasing the excitation threshold

[0045] Male spontaneously hypertensive rats with a body weight of 200-250 g were killed after anesthesia, and the heart was taken out and placed in a mixed gas (95% O 2 , 5% CO 2 ) in the nutrient solution, gently flush out the congestion in the heart, cut off the right heart, cut the left heart from the apex to the aortic arch, and separate the papillary muscle. After the heart was opened, needles were used to fix and expand its surroundings, so that the papillary muscles were completely exposed. The tendons near the aortic arch were ligated with No. 0 surgical thread, and the tendons near the apex were also ligated. Fix the muscle on the tension transducer and make the muscle between the two electrodes of the bracket, move it to the bath cavity with...

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PUM

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Abstract

The invention belongs to the traditional Chinese medicine field, and relates to corynoxeine and an application of an isomer of the corynoxeine in preparing medicines. In the invention, the results of animal experiments prove that the corynoxeine and the isomer thereof have the effects of expanding vessels and lowering blood pressure, and can be used for preparing the medicines for expanding the vessels and lowering the blood pressure; the corynoxeine and isocorynoxeine have the effects of expanding the vessels, lowering heart afterload, lightening heart burden and decreasing myocardial oxygen consumption, and can be used for preparing anti-angina pectoris medicines; the corynoxeine has the effects of negative myodynamia, directly decreasing the myocardial oxygen consumption, and doubly lowering the myocardial oxygen consumption; the corynoxeine and the isocorynoxeine have the effects of improving the ventricular muscle excited threshold and lowering the ventricular muscle contraction frequency, can be used for treating ventricular tachycardia, and can be used as a quality identification uncaria and tagged molecules of the ffective parts of the corynoxeine and the isocorynoxeine.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine, and relates to the active ingredient of the traditional Chinese medicine Uncaria and its new application, in particular to the application of dehydrorhynchophylline and its isomer (isodehydrorhynchophylline) in the preparation of medicines, especially the preparation of dehydrorhynchophylline Use in blood pressure drugs, vasodilators, anti-anginal drugs or anti-ventricular arrhythmia drugs. Background technique [0002] Hypertension is a major disease that threatens human health. Its harmfulness lies in the damage of target organs caused by long-term hypertension, which is the root cause of disability and death of hypertensive patients. Studies have shown that target organ damage often involves important organs such as the heart and kidneys, and its mechanism includes multiple independent pathways. Hyperplasia of vascular smooth muscle cells induced by hypertension, diabetes, etc.; i...

Claims

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Application Information

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IPC IPC(8): A61K31/438A61P3/06A61P9/08A61P9/10A61P9/06A61P9/12A61P9/00
Inventor 朱依纯朱依谆丁滢泂陈莹
Owner FUDAN UNIV
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