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Use of ethyl malonyl silybin derivant in preparing antioxidant medicine

A technology of ethylmalonyl and silybin ester, which is applied in the field of medicine, can solve problems such as oxidative damage, achieve the effects of inhibiting lipid peroxidation, facilitating large-scale production, and effectively scavenging free radicals

Inactive Publication Date: 2011-01-19
WENZHOU MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, free radicals can also cause β-amyloid deposition, which reacts with cell membranes and leads to intracellular oxidative damage

Method used

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  • Use of ethyl malonyl silybin derivant in preparing antioxidant medicine
  • Use of ethyl malonyl silybin derivant in preparing antioxidant medicine
  • Use of ethyl malonyl silybin derivant in preparing antioxidant medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 : Compound malonic acid [3-(4-hydroxy-3-methoxyphenyl)-6-(2,3-dihydro-3,5,7-trihydroxy-4-oxo-benzopyran -2) Preparation of -2,3-dihydro-1,4-benzodioxane-2]-methyl ethyl ester

[0017]

[0018] Add 1 gram of silibinin (purchased from Liaoning Panjin Tianyuan Pharmaceutical Co., Ltd., HPLC detection purity 98%), 0.56 gram of monoethyl malonate and 1.6 gram of triphenylphosphine in the dry reaction bottle, use 20 Dissolve milliliters of anhydrous tetrahydrofuran, add 1 gram of diethyl azodicarboxylate, stir at room temperature for 10 hours after the addition is complete, distill off the solvent under reduced pressure, add 5 milliliters of chloroform, filter to remove the white solid, and the mother liquor is subjected to column chromatography to obtain shallow 0.46 g of yellow powder, yield 37%.

[0019] R f (chloroform / ethyl acetate / acetic acid=50:1:0.25): 0.11; H NMR 1 H NMR (400MHz, deuterated chloroform) δ: 1.28 (triplet, J=7.2Hz, 3H, CH 3 ), 3.41 (si...

Embodiment 2

[0026] Example 2 Malonic acid [3-(4-hydroxy-3-methoxyphenyl)-6-(2,3-dihydro-3,5,7-trihydroxy-4-oxo-benzopyran-2 )-2,3-dihydro-1,4-benzodioxane-2]-methyl ethyl ester in vitro scavenging activity of superoxide anion free radical

[0027] 2.1 Experimental materials and samples

[0028] 2.1.1 Experimental reagents:

[0029] 2.1.1.1 Phenazine methosulfate (PMS), nitrobluetetrazolium (NBT), and phenanthrozine (ferrozine) were purchased from Sigma;

[0030] 2.1.1.2 Quercetin (quercetin) was provided by the Laboratory of Traditional Chinese Medicine and Natural Medicine, School of Pharmacy, Zhejiang University (purity: 99%); silybin (Silybin) was purchased from Panjin Tianyuan Pharmaceutical Co., Ltd., Liaoning, and detected by HPLC 98% purity.

[0031] 2.1.1.3 Tris base, DMEM medium was purchased from Gibco;

[0032] 2.1.1.4 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and NADH (reduced coenzyme I) were purchased from Amresco;

[0033] 2.1.1.5 Other reage...

Embodiment 3

[0048] Example 3 Compound malonate [3-(4-hydroxy-3-methoxyphenyl)-6-(2,3-dihydro-3,5,7-trihydroxy-4-oxo-chromene- 2) -2,3-dihydro-1,4-benzodioxane-2]-methyl ethyl ester to hydrogen peroxide H 2 o 2 Protective activity test of induced PC12 cell injury

[0049] 3.1 Experimental materials and samples

[0050] 3.1.1 Cells: Rat adrenal pheochromoma cells (PC12) were purchased from Shanghai Institute of Cells, Chinese Academy of Sciences.

[0051] 3.1.2 Experimental reagents:

[0052] 3.1.2.1 Hydrogen peroxide (H 2 o 2 ), nitroblue tetrazolium (NBT), and phenanthrozine (ferrozine) were purchased from Sigma;

[0053] 3.1.2.2 Quercetin (quercetin) was provided by the Laboratory of Traditional Chinese Medicine and Natural Medicine, School of Pharmacy, Zhejiang University (purity: 99%); silybin (Silybin) was purchased from Liaoning Panjin Tianyuan Pharmaceutical Co., Ltd., and detected by HPLC 98% purity.

[0054] 3.1.2.3 Tris base, DMEM medium was purchased from Gibco;

[00...

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Abstract

The invention relates to use of ethyl malonyl silybin derivant in preparing antioxidant medicine, particularly relates to uses of a silybin esters with a replacement of ethyl malonyl in the 23 position in preparing medicine for preventing and curing senile dementia or gout. Pharmacodynamic experiments showing that the compound has function of cleaning superoxide anion free-radical, repressing generation of lipoperoxide reduced by free-radical, and has antioxidation damage protection action to PC12 cell damage caused by free-radical namely PC12 cell for simulating brain nerve cell, for this reason, it is expected to be developed as medicine for protecting brain nerve and curing senile dementia caused by free-radical damage. The compound can also be used for repressing cativity of xanthine oxidase, so it is expected to be developed as medicine for curing gout.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a 23-ethyl malonyl substituted silybin ester derivatives that is the compound malonic acid [3-(4-hydroxyl-3-methoxy Phenyl)-6-(2,3-dihydro-3,5,7-trihydroxy-4-oxo-benzopyran-2)-2,3-dihydro-1,4-benzobis Oxyhexane-2]-methyl ethyl ester or pharmaceutically acceptable salt thereof is used for the pharmaceutical application of preparing antioxidant. Pharmacological tests on the compound showed that the compound has the activity of scavenging superoxide anion free radicals in vitro and inhibiting the generation of lipid peroxide induced by free radicals; The damage effect of adrenal pheochromoma PC12 cells, that is, it has an anti-oxidative damage protection effect on PC12 cells that simulate brain nerve cells, indicating that it has a positive effect on protecting brain cell tissue from oxidation and cranial nerves, and preventing and treating Alz...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61P39/06A61P25/28A61P19/06
Inventor 黄可新汪峰李校堃伍义行杨雷香郝小江巫秀美赵昱瞿佳
Owner WENZHOU MEDICAL UNIV