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Use and preparation method of flavonoid derivatives

A technology of derivatives and flavonoids, which is applied in the directions of medical preparations containing active ingredients, food preparation and application, can solve problems such as loss of consciousness and damage, and achieve the effect of novel structure

Inactive Publication Date: 2012-02-22
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the blood and oxygen supply to the brain is completely interrupted, one will lose consciousness in 8 to 15 seconds, and irreversible damage will be caused in 6 to 10 minutes

Method used

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  • Use and preparation method of flavonoid derivatives
  • Use and preparation method of flavonoid derivatives
  • Use and preparation method of flavonoid derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] (1) Pulverize 4.2 kg of dried whole herb of Selaginella uncinata (Desv.) Spring, extract by heating and refluxing three times with 60% ethanol 10 times the weight of Selaginella uncinata (Desv.) Spring, 2 hours each time, and combine Extraction solution;

[0044] (2) Remove insoluble matter by filtration, and dry the filtrate under reduced pressure to obtain ethanol extract.

[0045] (3) The ethanol extract was extracted 3 times with equal volumes of ethyl acetate and n-butanol respectively;

[0046] (4) Take the ethyl acetate extract and dry it under reduced pressure in vacuo to obtain the ethyl acetate extract.

[0047](4) The ethyl acetate extract was subjected to open silica gel column chromatography, and the chloroform:methanol ratios were 99:1, 98:2, 97:3, 95:5, 9:1, 8:2, 7:3 , 6:4 solvent gradient elution. Using comprehensive separation methods such as gel Sephadex LH-20 column chromatography, ODS column chromatography, and RP-18 high-performance liquid phase ...

Embodiment 2

[0052] Compounds 1-16 prepared in Example 1 were formulated into liquids with a concentration of 180 μmol / L, 90 μmol / L, and 45 μmol / L respectively as the drug group, and 10% DMSO was used as the control group to protect PC12 cells from hypoxia. test, and calculate the survival percentage of PC12 cells. The experimental results were calculated by Student's ttest, expressed as: mean ± SD. The results are shown in Table 1.

[0053] Effects of compounds in table 1 on PC12 cell hypoxic injury (x ± SD)

[0054]

[0055] Note: Compared with the control group * P** P<0.01

[0056] Conclusion: It can be seen from Table 9 that compared with the blank solvent group, compound 1-16 has a strong protective effect on hypoxic PC12 cells at different concentrations, and has anti-hypoxic activity in vitro. It shows that these 16 compounds can be used as anti-hypoxic drugs.

Embodiment 3

[0058] The compounds 1-16 prepared in Example 1 were formulated into liquids with a concentration of 40 mg / mL as the drug group, and 20% DMSO was used as the control group to carry out the airtight hypoxic endurance test in mice, and observe the mice in the airtight condition. The following survival time. The results are shown in Table 2.

[0059] Survival of mice under table 2 hypoxic conditions (x±SD, n=10)

[0060]

[0061] Note: Compared with the control group * P** P<0.01

[0062] Conclusion: As can be seen from Table 10, compared with the control group, compound 1-16 can significantly improve the survival time of mice under airtight hypoxic conditions, has certain anti-hypoxic activity in vivo, and can be used as an anti-hypoxic drug .

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Abstract

The invention relates to the medicine field and provides an application of flavone derivative as anti-oxidation and anti-anoxia drugs or food. The compound has the structural formula on the right. The preparation method of the flavone derivative comprises the following operation steps: the whole herb of Uncinata Spikemoss Herb is ground and extracted by solvent or water in a reflux way; an initial extract is obtained by filtering or centrifugally removing undissolved substances and decompression drying; the initial extract is dispersed in water of equal volume and again extracted by chloroform, ethyl acetate and normal butanol sequentially; ethyl acetate extract liquor is taken and decompressed and dried in vacuum to obtain the ethyl acetate extract; and the flavone derivative is obtained by chromatography separation and refining.

Description

technical field [0001] The invention relates to the use and preparation method of flavonoid derivatives, belonging to the field of medicine. Background technique [0002] Selaginella uncinata (Desv.) Spring is the whole plant of Selaginella uncinata (Desv.) Spring. Taste slightly bitter, cold in nature. It has the effects of clearing away heat and dampness, detoxifying, eliminating blood stasis and stopping bleeding. Indications for jaundice, dysentery, edema, rheumatic arthralgia, cough and vomiting blood, sore throat, hemorrhoids, cuts, burns. [0003] Flavonoids generally refer to a series of compounds in which two benzene rings are connected to each other through three carbon atoms. Biflavonoids are compounds formed by linking two flavonoids, with many linking modes and complex structures. Biflavonoids have significant anti-tumor, anti-virus, anti-inflammatory and other pharmacological effects, and also have certain curative effects on cardiovascular system diseases,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P39/06A23L1/30A23L33/10
Inventor 姚新生王乃利范明郑俊霞吴丽颖刘宏伟丁爱石高昊戴毅
Owner JINAN UNIVERSITY
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