Novel magnesium-serinate compound and use thereof

A compound, serine technology, applied in the direction of magnesium organic compounds, heavy metal compounds active ingredients, applications, etc., can solve the problem of insufficient amount and so on

Pending Publication Date: 2021-03-26
アストロゲン カンパニーリミティド
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, under conditions of disease or stress, the amount of L-serine biosynthesized in the cell is insufficient compared to the amount of L-serine required by the cell, so it is classified as an essential condition requiring external supply through diet. Amino acid (conditionally essential amino acid)

Method used

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  • Novel magnesium-serinate compound and use thereof
  • Novel magnesium-serinate compound and use thereof
  • Novel magnesium-serinate compound and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0153] 1. Preparation of magnesium-serinate (Mg-Serinate)

[0154] 1.1. Preparation of magnesium-serinate (Mg-Serinate, AST-011)

[0155] Put 100 ml of distilled water in a 500 ml Erlenmeyer flask and heat up to a temperature of 70 to 80°C, then weigh 50 g (~0.48 moles) of L-serine (MW 105.1) in the distilled water while using a magnetic stirrer (magnetic stirrer) Stir to dissolve. After crushing MgO (MW 40.3) into small particles in a mortar, weigh 9.7g (~0.24moles) and add it in a small amount to L-serine aqueous solution while stirring at a temperature of 70~80°C. A reflux cooling device was attached in the medium, and the reaction was carried out for 2 hours under the same conditions.

[0156]In an uncooled state, centrifuge directly at 6000 rpm for 10 minutes, and recover 130 ml of supernatant. Ethanol was added to the supernatant so that the final concentration became 75 v / v%, and then stirred at room temperature for 14 hours with a magnetic stirrer to allow precipita...

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Abstract

The present invention pertains to a novel magnesium-serinate compound and a use thereof, and more specifically, to: a novel magnesium-serinate compound in which magnesium atoms are chelate-bonded to L-serine; and a pharmaceutical use thereof related to central nervous system diseases, etc. A novel magnesium-serinate compound obtained from the production method of the present invention was found toconsist of about 10% of magnesium and about 90% of serine on the basis of instrumental analysis results. The compound was found to be soluble in room temperature water at a concentration of about 500mg/ml within a pH range of 6.0-10.0 and remain in an aqueous solution state without sedimentation, was found to be soluble at a concentration of about 500 mg/ml without sedimentation even in a physiological saline (phosphate-buffered saline, PBS) solution at room temperature, and was thus confirmed to have properties suitable as an orally administrable and injectable substance to the human body.The compound activated mitochondrial function and neuronal cell proliferation by improving the mitochondrial oxygen consumption rate, exhibited a neuroprotective effect of inhibiting oxidative stress-induced mitochondrial membrane potential damage and/or endoplasmic reticulum stress-induced neuronal cell death, and exhibited improved vascular-brain barrier permeability. Thus, the compound is veryeffective in preventing, treating, and alleviating central nervous system diseases such as cognitive disorders, intellectual disorders, microencephaly, epilepsy, neurodevelopmental disorders, dementia, autism spectrum disorders, Down syndrome, Rett syndrome, fragile-X syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis. Therefore, the presentinvention is very useful for the pharmaceutical industry, etc.

Description

technical field [0001] The present invention relates to novel magnesium-serinate (magnesium-serinate) compound and application thereof, more specifically, relate to the novel magnesium-serinate compound of L-serine (serine) and magnesium atom to form chelate bond and central nervous system disease (centralnervous system disease) system diseases) and other related medical uses, etc. Background technique [0002] Magnesium is the fourth most abundant inorganic salt in the human body. About 50% is stored in the bone, whereas the remaining 50% is mainly stored inside the cells of body tissues and organs [Jahnen-Dechent and Ketteler, 2012; Farruggia et al., 2014]. In cells, magnesium acts as a cofactor for hundreds of enzymes and thus is involved in major cellular responses. In particular, magnesium is required for the stabilization of various enzymes associated with ATP-generating reactions associated with energy metabolism [Swaminathan, 2003; Saris et al., 2000; Romani, 2013]...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F3/02A61K31/28A61P25/28A23L33/10A23K20/24A23K20/10
CPCA61P25/28A23L33/10C07C229/76A23K20/10A23K20/24A23L33/16A23V2200/322A61K31/28C07F3/02A23L33/165
Inventor 黄寿卿李民龙徐民淑田桃连金敏珠金英浩赵英经
Owner アストロゲン カンパニーリミティド
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