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Application of 3-O-methyl quercetin to resisting oxidation or reducing blood sugar

A methyl quercetin, anti-oxidation technology, applied in the field of medicine, can solve problems such as side effects and oxidative damage, and achieve a significant effect of inhibiting activity

Inactive Publication Date: 2020-05-19
ZHENGZHOU FRUIT RES INST CHINESE ACADEMY OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, continuous high-glucose stimulation will induce severe oxidative stress in the body, and produce excessive free radicals to react with some biomolecules, thereby causing oxidative damage to the body
Anti-diabetic drugs such as acarbose, voglibose, and miglibose have been used in clinical practice, but continued use can cause some side effects

Method used

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  • Application of 3-O-methyl quercetin to resisting oxidation or reducing blood sugar
  • Application of 3-O-methyl quercetin to resisting oxidation or reducing blood sugar
  • Application of 3-O-methyl quercetin to resisting oxidation or reducing blood sugar

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Inhibition of α-glucosidase activity by 3-O-methylquercetin in vitro

[0022] 1.1 Reagents: α-glucosidase (α-glucosidase, Sigma, 750U), 4-nitrophenyl-α-D-glucopyranoside (pNPG, TOKYO Chemica Industry Co., LTD), acarbose (Acarbose , TOKYO ChemicaIndustry Co., LTD), corosolic acid, Na 2 HPO 4 , NaH 2 PO 4 .

[0023] Comparator 1

[0024] Rhamnetin is a derivative of quercetin with the molecular formula C 16 h 12 o 7 ; Molecular weight: 316.26; CAS accession number: 90-19-7, structural formula:

[0025]

[0026] Comparator 2

[0027] Quercetin 3-rhamnoside is a kind of quercetin derivative with the molecular formula C 21 h 20 o 11 ; Molecular weight: 448.38; CAS accession number: 522-12-3, structural formula:

[0028]

[0029] Experimental equipment: microplate reader TECAN infinite M200 PRO (Teacan Group Ltd., Switzerland).

[0030] 1.2 Experimental steps

[0031] 1.2.1 Preparation of drug solution: first prepare 3-O-methyl quercetin, quercetin, acarb...

Embodiment 2

[0048] 3-O-Methylquercetin Antioxidative Ability Test in Vitro

[0049] 2.1 ORAC antioxidant experiment

[0050] 2.1.1 Reagents: vitamin E (Trolox), ABAP [2,2-Azobis (2-amidinopropane) dihydrochloride solution], DCFH–DA (2′,7′-Dichlorfluorescin diacetate), sodium fluorescein (Sodium Fluorescein), Na 2 HPO 4 , NaH 2 PO 4 . Experimental equipment: microplate reader TECAN infinite M200 PRO (Teacan Group Ltd., Switzerland).

[0051] 2.2 Experimental steps

[0052] 2.2.1 Preparation of drug solution: Prepare the sample to be tested from dimethyl sulfoxide (DMSO) into a 10 mg / mL mother solution; accurately weigh 20 mg of fluorescein sodium FL and dissolve it in 50 mL of PBS solution (pH=7.4), and prepare a concentration of 0.4mg / mL FLA solution, store in –20°C refrigerator; dissolve 200μL FLA solution in 50mL PBS solution to make FLB solution; dilute 500μL FLB solution to 50mL PBS solution to make FL working solution; weigh accurately Dissolve 2.5mg Trolox in 10mL PBS solutio...

Embodiment 3

[0065] Intracellular Antioxidant (CAA) Experiment of 3-O-Methylquercetin

[0066] 3.1 Reagents: DCFH–DA (2′,7′-Dichlorfluorescin diacetate), sodium fluorescein (Sodium Fluorescein), ABAP [2,2-Azobis (2-amidinopropane) dihydrochloride solution], HepG2 liver cancer cells (Kunming Institute of Zoology, Chinese Academy of Sciences), MEM medium (Gibco), methanol (Tianjin Damao), L-glutamine (Gibco), Hanks balanced salt solution (HBSS), fetal bovine serum (FBS, Gibco), double antibody (Gibco), trypsin (Gibco) ). Experimental instrument: microplate reader TECAN infinite M200 PRO (Teacan Group Ltd., Swizerland)

[0067] 3.2 Experimental steps

[0068] 3.2.1 Principle: The CAA method is a detection of active oxygen by using the fluorescent probe DCFH-DA. DCFH-DA itself has no fluorescence, can freely pass through the cell membrane, enter the cell, and can be hydrolyzed by intracellular esterase DCFH is generated, and DCFH cannot pass through the cell membrane, so that the probe is e...

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PUM

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Abstract

The invention discloses an application of 3-O-methyl quercetin to resisting oxidation or reducing blood sugar, and belongs to the technical field of pharmaceuticals. The invention aims to provide a quercetin derivative-3-O-methyl quercetin having activity of resisting oxidation and reducing blood sugar, and an application of the quercetin derivative-3-O-methyl quercetin as an alpha-glucosidase inhibitor and an antioxidant to preparation of medicines and / or health-care products for treating diabetes. The 3-O-methyl quercetin disclosed by the invention has favorable alpha-glucosidase restrainingactivity, and besides, has the activity of resisting oxidation. The in vitro alpha-glucosidase restraining experiment proves that the 3-O-methyl quercetin disclosed by the invention has significant restraining activity on the alpha-glucosidase, and the IC50 value for restraining the alpha-glucosidase is 1.38+ / -0.01 [mu]g / mL which is significantly better than that of quercetin.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the application of 3-O-methyl quercetin in antioxidation or hypoglycemia. Background technique [0002] Quercetin derivatives are widely found in plants such as fruits, vegetables, tea and medicinal materials, and are phenolic substances widely present in daily diet. Studies have shown that quercetin has anti-inflammatory, antibacterial, anti-cancer, hypoglycemic, anti-viral and other effects, and has a strong antioxidant function. In recent years, with quercetin as the lead compound, derivatives obtained through structural modification, some compounds with better activity than quercetin can be obtained through activity screening. Mulholland et al. synthesized a water-soluble quercetin prodrug 3′-O-N-carboxymethylformamidoquercetin, which has entered clinical phase I, and found that it inhibits the growth of ovarian cancer A2780 cells, mainly by blocking Proliferati...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P3/10A61P39/06
CPCA61K31/352A61P3/10A61P39/06
Inventor 张强焦中高刘杰超张春岭刘慧吕真真杨文博陈大磊
Owner ZHENGZHOU FRUIT RES INST CHINESE ACADEMY OF AGRI SCI
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