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Branched chain fatty acid compound and derivative thereof for preventing and curing ischemical reperfusion injury

A reperfusion injury, compound technology, applied in the direction of organic chemistry, drug combination, ester active ingredients, etc., to achieve the effect of reducing reperfusion injury, strong anti-ischemia and reperfusion injury, and good therapeutic effect

Inactive Publication Date: 2009-10-14
福州永康生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

End group must be isopropyl or sec-butyl or tert-butyl

Method used

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  • Branched chain fatty acid compound and derivative thereof for preventing and curing ischemical reperfusion injury
  • Branched chain fatty acid compound and derivative thereof for preventing and curing ischemical reperfusion injury
  • Branched chain fatty acid compound and derivative thereof for preventing and curing ischemical reperfusion injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: the synthesis of 13-methyl-tetradecanoic acid

[0029] 139 grams of monomethyl dodecanedioate, 56 grams of isovaleric acid, and 0.65 grams of sodium metal were electrolyzed in 1400 ml of anhydrous methanol and a direct current of 2 A until the reaction solution was alkaline, distilled to remove methanol, and washed with water. Vacuum fractional distillation gave 21 grams of 13-methyl-tetradecanoic acid methyl ester. The above was mixed with 54ml of 10% NaOH and 60ml of methanol, refluxed for 2 hours, distilled off the methanol, adjusted to pH=2 with 10% HCl, cooled and filtered, washed with water until neutral to obtain a white solid, which was fractionated in vacuum and recrystallized from ethanol to obtain 13 - Methyl-tetradecanoic acid 14 g. Add 14 grams of 13-methyl-tetradecanoic acid into a round-bottomed flask, add 40ml of isopropanol and 1ml of concentrated sulfuric acid, heat to 90°C and reflux for 2 hours, distill off excess isopropanol, and vacu...

Embodiment 2

[0030] Embodiment 2: the preparation of 13-methyl-myristate isopropyl ester fat emulsion injection

[0031] 6% 13-methyl-myristate isopropyl ester 20% fat emulsion injection prescription composition: soybean oil for injection 200g, 13-methyl-myristate isopropyl ester 60g, lecithin for injection 12g, injection Add 25g of glycerin and water for injection to 1000mL.

[0032] The preparation process of the drug-containing fat emulsion injection is as follows: Weigh the prescribed amount of soybean oil and the drug in a liquid mixing pot, mix them evenly with a high-speed masher, heat to 80°C, add lecithin, and mash at a high speed until it is completely dissolved. into a homogeneous clear solution. Take another prescribed amount of water for injection and add glycerin, put it in another liquid mixing pot, stir and mix evenly under the condition of nitrogen protection, and heat to 60°C. Slowly add the drug-containing phospholipid oil solution into the aqueous glycerin solution un...

Embodiment 3

[0034] Example 3: Effects of 13-methyl-tetradecanoic acid and 13-methyl-tetradecanoic acid isopropyl ester on focal cerebral ischemia-reperfusion injury rat model

[0035] Model preparation: a rat model of acute middle cerebral artery ischemia-reperfusion injury by suture embolization (prepared according to Longa's method). Rats were anesthetized with 2% pentobarbital sodium (40 mg / kg, ip) and then the arteries of the neck were separated, and a nylon thread with a diameter of 0.205 mm was inserted into the right internal carotid artery from the right external carotid artery, and slowly advanced for about ( 18.5±0.5) mm (measured from the bifurcation), until resistance is encountered, a model of middle cerebral artery embolism (MCAO) is made. After 2 hours of ischemia, pull out the embroidered thread under anesthesia to form reperfusion, and at the same time give medicine or solution. Animals were kept warm during and after anesthesia before waking up from anesthesia. The sig...

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Abstract

The invention relates to an application of a compound with the tail end being branched chain fatty acid and a compound of a derivative for preparing medicine curing ischemia and reperfusion injury of tissues or organs of people. The ischemia and reperfusion injury comprises cerebral ischemia and reperfusion injury caused by operations of cerebrovascular disorder, cardiac arrest and cardio-pulmonary resuscitation, and ischemia and reperfusion injury of therapy of miocardial infarction, ischemia of intestine, hepatic ischemia and thrombolysis, operations on vessels of heart, and histoorgan transplantation.

Description

technical field [0001] The invention relates to a drug for resisting tissue and organ ischemia and reperfusion injury, which takes terminal branched chain fatty acid compounds and derivatives thereof as active ingredients, and its application in the field of cardiovascular and cerebrovascular diseases. Background technique [0002] Long-term ischemia and subsequent reperfusion of human tissues or organs can cause tissue damage or even necrosis in the ischemic area. Ischemia is usually the immediate cause of tissue hypoxia and lack of supply of energy substances. For the brain, heart and other organs that consume a lot of oxygen and are sensitive to energy substances, the length of ischemic time is usually the decisive factor to determine whether the damage is reversible. Taking acute cerebral infarction as an example, the nerve tissue is mainly caused by ischemic injury at first, and with the prolongation of ischemia time, more serious damage of nerve tissue and function wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C53/128C07C69/22C07C69/52A61K31/23A61P9/10
Inventor 林泽辉翁绳美
Owner 福州永康生物技术有限公司
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