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Use of mangiferin calcium salt as peroxisome proliferator-activated receptor agonist

A peroxidase and receptor agonist technology, applied in the field of mangiferin calcium salt as a peroxidase proliferator-activated receptor agonist, can solve problems such as adverse reactions

Inactive Publication Date: 2009-06-24
HAINAN DEZE DRUG RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the gradual deepening of the research on the above various drugs, the existing drugs show one or another adverse reaction, which limits the clinical application of the existing drugs, so finding and developing new PPARs agonists has great clinical and market value
[0006] Tom Hsun-Wei Huang et al [Tom Hsun-Wei Huang, Gang Peng, George Qian Li, et al. Salacia oblonga root improves postprandial hyperlipidemia and hepatic steatosis in Zucker diabetic fatty rats: Activation of PPAR-α. Toxicology and Applied Pharmacology, 210 (2006) : 225-235] It was reported that mangiferin (mangiferin) has an agonistic effect on PPAR-α in vitro, but whether mangiferin has an agonistic effect on PPAR-γ, and whether mangiferin has a dual agonistic effect on PPAR-α / γ has not been reported.

Method used

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  • Use of mangiferin calcium salt as peroxisome proliferator-activated receptor agonist
  • Use of mangiferin calcium salt as peroxisome proliferator-activated receptor agonist
  • Use of mangiferin calcium salt as peroxisome proliferator-activated receptor agonist

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Embodiment 1: the preparation of mangiferin

[0027] 100kg Anemarrhena decoction pieces were added with 80% ethanol to reflux extraction twice, each time for 1 hour, the ethanol was recovered under reduced pressure, adsorbed by macroporous resin, washed with water, eluted with 20% ethanol, and the eluate was concentrated under reduced pressure to obtain crude neomangiferin; Then eluted with 40% ethanol, and the eluate was concentrated under reduced pressure to obtain crude mangiferin. The crude mangiferin was recrystallized and refined to obtain pure mangiferin, and the mangiferin sample was identified with the mangiferin reference substance to confirm that the obtained sample was mangiferin, and the purity was greater than 90% as determined by HPLC. Embodiment 2: the preparation of mangiferin calcium salt

Embodiment 2

[0027] 100kg Anemarrhena decoction pieces were added with 80% ethanol to reflux extraction twice, each time for 1 hour, the ethanol was recovered under reduced pressure, adsorbed by macroporous resin, washed with water, eluted with 20% ethanol, and the eluate was concentrated under reduced pressure to obtain crude neomangiferin; Then eluted with 40% ethanol, and the eluate was concentrated under reduced pressure to obtain crude mangiferin. The crude mangiferin was recrystallized and refined to obtain pure mangiferin, and the mangiferin sample was identified with the mangiferin reference substance to confirm that the obtained sample was mangiferin, and the purity was greater than 90% as determined by HPLC. Embodiment 2: the preparation of mangiferin calcium salt

[0028] Mangiferin calcium salt can be prepared according to the preparation method contained in the patent [PCT / CN2007 / 071112] applied by the inventor. Here, only one method is provided to illustrate the acquisition ...

Embodiment 3

[0044] Example 3: Preparation of mangiferin calcium salt freeze-dried powder injection

[0045] Weigh 40g of mannitol, put it in an appropriate container, add 1000ml of water for injection, add 0.2g (0.1% w / v) of charcoal for needles, heat to 80°C, stir for 30min, filter through a 0.22μm microporous membrane, and set aside the filtrate.

[0046] Weigh 10g of mangiferin calcium salt, add it into the mannitol solution, and stir to dissolve completely. Add water for injection to 2000ml, check the content and pH value, filter with a 0.22μm microporous membrane, sub-package, each tube contains G10mg, and freeze-dry. Vacuum plugging, capping, labeling, and packaging.

[0047]In order to illustrate the pharmacological activity of the calcium salt of mangiferin described in the summary of the invention, the inventors conducted experimental research in a combination of in vivo and in vitro, using representative disease models as representatives of various diseases. That is, to study ...

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Abstract

The invention provides use of a mangiferin calcium salt as a PPARs excitant. The structural formula of the mangiferin calcium salt is as shown on the right.

Description

technical field [0001] The invention relates to the use of mangiferin calcium salt as a peroxidase proliferator-activated receptor agonist. Background technique [0002] Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors, which belong to the type II nuclear receptor superfamily. After being activated by activators, PPARs can regulate the expression of a variety of target genes in the nucleus, thus in many physiological and pathological processes, such as energy balance, glucose and lipid metabolism, improving insulin resistance, regulating inflammation and immune response, cell differentiation, and inhibiting tumor formation etc., play a very crucial role. [0003] PPARs include three phenotypes: PPAR-α, PPAR-β / δ, and PPAR-γ. Among them, PPAR-α is mainly distributed in tissues with high metabolic activity, such as liver, kidney, heart, and muscle tissue, and is also expressed in vascular endothelial cells, smooth muscle cells, monocytes and macrophag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P43/00
Inventor 徐广爱
Owner HAINAN DEZE DRUG RES
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