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Polyphenol derivative compound 6-CEPN as therapeutic agent for acute ischemic stroke

A technology of acute cerebral ischemia, derivatives, applied in biochemical equipment and methods, drug combinations, organic active ingredients, etc.

Pending Publication Date: 2020-03-17
THE UNIVERSITY OF HONG KONG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite decades of research, there are currently no approved drug therapies capable of stimulating neurological recovery in stroke patients (Endres, Engelhardt et al., 2008)

Method used

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  • Polyphenol derivative compound 6-CEPN as therapeutic agent for acute ischemic stroke
  • Polyphenol derivative compound 6-CEPN as therapeutic agent for acute ischemic stroke
  • Polyphenol derivative compound 6-CEPN as therapeutic agent for acute ischemic stroke

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Focal cerebral ischemia-reperfusion model in rats

[0025] Adult male Sprgue-Dawley rats weighing 250-280 g were provided by the Laboratory Animal Unit of the University of Hong Kong. The animal experiment protocol was approved and supervised by the Committee on the Use of Live Animals in Teaching and Research of the University of Hong Kong. SD rats were maintained at controlled temperature (22±2°C) with food and water supplies. Rats underwent MCAO (middle cerebral artery occlusion) followed by reperfusion to simulate cerebral ischemia / reperfusion injury. All rats were randomly divided into MCAO operation group and sham operation group. However, the investigators were aware of group assignments. Briefly, rats were anesthetized with 4% isoflurane (Abbott, IL, USA) and maintained with 1.5% isoflurane during induction of anesthesia. During surgery, rats were placed on a heating pad to maintain body temperature at 37°C. After shaving, the skin around the neck was steri...

Embodiment 2

[0027] medical treatement

[0028] To clarify ONOO - Effect in ischemic stroke, FeTMPyP (75854, Cayman, MI, USA) was used as positive control drug. At the beginning of reperfusion, 3 mg / kg of FeTMPyP was administered once intravenously from the rat femoral vein. Similar to FeTMPyP, 6-CEPN (5, 10 mg / kg), which was well dissolved in a mixture of PEG400, ethanol and saline, was also injected intravenously from the femoral vein. After injection, the skin was sutured and sterilized with 75% ethanol. Then, remove the monofilament for reperfusion. All animals received individual care after surgery.

Embodiment 3

[0030] behavior test

[0031] The modified neurological impairment score (mNSS) scale was used to assess neurological impairment after ischemic stroke. The mNSS scale is scored from 0 to 18 and includes motor, sensory, and reflex tests to assess neurological impairment. Before the MCAO operation, each rat was trained once with reference to the mNSS scale. The higher the score obtained, the more severe the nerve damage. Behavioral tests were assessed 24 hours after MCAO.

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Abstract

A novel flavonoid derivative compound 6-CEPN can protect a brain against ischemia / reperfusion (I / R) injury by attenuating peroxynitrite-mediated mitochondrial autophagy. The infarct volume and neurological impairment score of acute ischemic stroke is significantly improved by 6-CEPN. It is found that the 6-CEPN inhibites excess mitochondrial autophagy activation during brain I / R injury, accompanied by a reduction in the production of peroxynitrite. Specifically, the 6-CEPN inhibites the expression ratio of LC3-II / I and Drp1 in the mitochondrial fraction in a dose-dependent manner, as well as the protein expression of the iNOS and NADPPH oxidase subunit p47phox.

Description

technical field [0001] The present subject matter provides methods and therapeutics for acute ischemic stroke. Background technique [0002] Acute ischemic stroke (AIS) is a devastating cause of death and disability depending on the time from ischemic onset to treatment, the affected brain region and its size. Despite decades of research, there are currently no approved drug therapies capable of stimulating neurological recovery in stroke patients (Endres, Engelhardt et al., 2008). Tissue plasminogen activator (t-PA) is the only approved and widely used drug in clinical treatment. [0003] Many pharmacological drugs, such as eptifbatide (Adeoye et al., 2015), reteplase (Qureshi et al., 2005), lovastatin (Elkind et al., 2009), granulocyte colony-stimulating factor (Shyu et al., 2006), edaravone (Wada et al., 2014) and caffeinol (Martin-Schild et al., 2009) have been used in clinical trials for AIS by reducing ischemic injury and enhancing functional recovery. In addition, ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/366A61K31/4152A61K38/12A61K38/48A61P9/10A61P25/00
CPCA61K31/352A61K31/366A61K31/4152A61K38/12A61K38/482C12Y304/21068A61P9/10A61P25/00A61K2300/00
Inventor 沈剑刚王明福冯靖涵邓瑞霞杜巧辉
Owner THE UNIVERSITY OF HONG KONG
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