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Application of isopentenyl flavonoid compound in preparation of medicine

A prenyl flavonoid and prenyl technology, which is applied in the field of pharmaceutical research and development, can solve the problems of low curative effect, suppressing pulmonary edema, etc., and achieve the effects of low dosage, suppressing pulmonary edema, and reducing lung wet weight

Pending Publication Date: 2022-05-06
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Therefore, the object of the present invention is to solve the defects that the drugs in the prior art cannot suppress pulmonary edema while anti-inflammation and have the problems of high dosage and low curative effect, thereby providing a kind of prenyl flavonoids in the preparation of Use in a medicament useful for preventing or treating acute lung injury and / or acute respiratory distress syndrome

Method used

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  • Application of isopentenyl flavonoid compound in preparation of medicine
  • Application of isopentenyl flavonoid compound in preparation of medicine
  • Application of isopentenyl flavonoid compound in preparation of medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053]

[0054] Commercially available flavescens 20kg, crushed to 100-200 mesh, stirred and extracted with 80% ethanol (80L) at 55°C for 3 hours, filtered, and the residue was extracted with 50% ethanol (60L) at 55°C for 2 hours, filtered, and combined twice The filtrate was concentrated under reduced pressure to no alcohol smell (solid content 3.3kg), and the concentrated solution was extracted 4 times with 2 times the amount of petroleum ether, ethyl acetate, and water-saturated n-butanol successively to obtain 507g of petroleum ether layer and 923g of ethyl acetate layer , n-butanol layer 596g, water layer 1256g, get petroleum ether part, ethyl acetate part and n-butanol part and concentrate respectively, obtain 3 components Fr.A (petroleum ether layer), Fr.B (ethyl acetate layer) , Fr.C (n-butanol layer).

[0055]Fr.B was subjected to column chromatography on a silica gel column (column diameter 6cm×height 60cm, column volume 1.7L), using volume ratios of 70:1, 50:1, 3...

Embodiment 2

[0064]

[0065]

[0066] 20kg of commercially available licorice was crushed into coarse powder, heated (60°C) with 85% and 50% ethanol, respectively, and extracted with stirring, for 2 hours each time, filtered, combined extracts, and concentrated under reduced pressure to obtain 8.3kg of extract. After suspending with 5L of water, extract 3 times with petroleum ether and ethyl acetate respectively, 10L each time, collect the ethyl acetate and concentrate under reduced pressure (solid content 770g), and the concentrate is passed through a silica gel column for column chromatography (column diameter 6cm × height 60cm, column volume 1.7L), followed by petroleum ether-ethyl acetate (volume ratio is 50:1, 30:1, 20:1, 10:1, 5:1, 1:1), dichloromethane - Methanol (volume ratios 20:1, 10:1, 5:1, 1:1) 3 column volumes per gradient yielding 10 fractions Fr.A-J.

[0067] Fr.B (eluent with petroleum ether-ethyl acetate volume ratio of 30:1) was subjected to silica gel column chroma...

Embodiment 3

[0082]

[0083]

[0084] 25kg of jackfruit roots and rhizomes were crushed into coarse powder, added 150kg of 95% ethanol to extract at 60°C for 2 hours, extracted 3 times, combined the filtrates, concentrated to no alcohol smell (solid content 3.7kg), passed through D101 macroporous resin, and washed with pure water respectively , 25% ethanol, 95% ethanol for elution, 3 column volumes for each gradient, collect 95% ethanol eluted parts, concentrate until there is no alcohol smell, add pure water to 10L, and use petroleum ether, chloroform, ethyl acetate and normal Extract with butanol twice, 15L each time, collect the extracts from each part and concentrate to obtain the extracts Fr.A-D of different polar parts.

[0085] Take the chloroform part Fr.B, and go through silica gel column chromatography (column diameter 8cm×height 70cm, column volume 3.5L), and the volume ratio is 20:1, 10:1, 8:1, 6:1, 5: 1, 4:1, 3:1, 2:1 and 1:1 mixture of n-hexane and ethyl acetate and pur...

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Abstract

The invention relates to the technical field of medicine research and development, in particular to application of an isopentenyl flavonoid compound in preparation of a medicine, the medicine can be used for preventing or treating acute lung injury and / or acute respiratory distress syndrome, the isopentenyl flavonoid compound has a structure as shown in a formula 1, and definitions of R1-R10, M, X and k are recorded in the specification. The isopentenyl flavonoid compound provided by the invention can obviously inhibit inflammatory response, inhibit release of inflammatory factors, reduce the content of inflammatory factors in alveolar lavage fluid and serum, and also can obviously inhibit pulmonary edema, reduce generation of pulmonary effusion and reduce wet weight of lungs, so that the lung quality is improved. The increasing degree of the ratio of wet weight to dry weight of lung caused by acute lung injury is inhibited, so that the effects of resisting inflammation and inhibiting lung edema are achieved.

Description

technical field [0001] The invention relates to the technical field of medicine research and development, in particular to the application of a prenyl flavonoid compound in the preparation of medicines. Background technique [0002] Acute lung injury (ALI) / acute respiratory distress syndrome (ARDS) is a common clinical critical illness with a very high mortality rate, which seriously threatens the lives of critically ill patients. According to statistics, more than 10% of ALI / ARDS patients need to be admitted to the intensive care unit for treatment, and the fatality rate is as high as about 55%. The basic physiological change of ALS / ARDS is non-cardiogenic pulmonary edema caused by increased permeability of pulmonary capillary endothelium and alveolar epithelial cells, severe ventilation / blood flow imbalance due to alveolar edema and alveolar collapse, especially intrapulmonary shunt Significantly increased, resulting in severe hypoxemia, leading to acute hypoxic respirato...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/36A61K31/12A61K31/353A61K31/335A61K31/216A61K31/343A61P11/00A61P9/10A61P31/04A61P31/12A61P31/14A61P31/16A61P31/22A61P7/08
CPCA61K31/352A61K31/36A61K31/12A61K31/353A61K31/335A61K31/216A61K31/343A61P11/00A61P9/10A61P31/04A61P31/12A61P31/14A61P31/16A61P31/22A61P7/08
Inventor 温尧林陈佳玲
Owner CATCH BIO SCI & TECH
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