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A kind of scutellarin aglycon derivative and its preparation method and application

A technology of scutellarin aglycone and derivatives, applied in the field of medicinal chemistry research, can solve the problems of unsatisfactory clinical application of scutellarin, low bioavailability of scutellarin, unfavorable drug efficacy, etc.

Inactive Publication Date: 2017-06-30
CENTRAL SOUTH UNIVERSITY OF FORESTRY AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the clinical application of scutellarin is not ideal. There are two main reasons: (1) scutellarin has poor water solubility and fat solubility; (2) scutellarin has low bioavailability and is easy to metabolize in the body, which is not conducive to exerting the drug effect

Method used

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  • A kind of scutellarin aglycon derivative and its preparation method and application
  • A kind of scutellarin aglycon derivative and its preparation method and application
  • A kind of scutellarin aglycon derivative and its preparation method and application

Examples

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Embodiment 1

[0029] A kind of scutellarin aglycon derivative provided by the present invention, its structural formula is as follows:

[0030]

[0031] The specific preparation process of the scutellarin aglycon derivative in this example is as follows: take 1 kg of the whole Vernonia herb, dry it naturally, soak it in 20 liters of ethanol with a concentration of 50% for 30 days; filter the leaching solution, and obtain the filtrate Concentrate to dryness at 50°C to obtain extract I; extract extract I with 5 liters of ethyl acetate to obtain extract, then concentrate the extract to obtain extract II; dissolve extract II with 3 liters of methanol, add 100g of silica gel was stirred to obtain a column sample; the column sample was subjected to silica gel column chromatography, eluted with petroleum ether, acetone and n-propanol in sequence, and the n-propanol eluate was collected, and the obtained n-propanol eluate was concentrated , to obtain a concentrated solution; adopt D101 macroporo...

Embodiment 2

[0036] A scutellarin aglycon derivative provided by the present invention, the structural formula of which is the same as that of Example 1.

[0037] The specific preparation process of the scutellarin aglycone derivative in this example is as follows: take 1 kg of the whole Vernonia herb, dry it naturally, soak it in 10 liters of ethanol with a concentration of 90% for 30 days; filter the leaching solution, and obtain the filtrate Concentrate to dryness at 60°C to obtain extract I; extract extract I with 5 liters of ethyl acetate to obtain extract, then concentrate the extract to obtain extract II; dissolve extract II with 3 liters of methanol, add 100g of silica gel was stirred to obtain a column sample; the column sample was subjected to silica gel column chromatography, eluted with petroleum ether, acetone and n-propanol in sequence, and the n-propanol eluate was collected, and the obtained n-propanol eluate was concentrated , to obtain a concentrated solution; adopt D101 ...

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Abstract

The invention discloses a scutellarin aglycone primer with a novel structure, and a preparation method and application of the scutellarin aglycone primer in preparing oxidation resisting medicine. The preparation method of the scutellarin aglycone primer comprises the steps that whole vernonia esculenta is soaked in ethyl alcohol to obtain leaching liquid, the leaching liquid is filtered and concentrated to obtain extract I, and the extract I is extracted through ethyl acetate and then concentrated to obtain extract II; a column passing sample is prepared from the extract II, subjected to chromatography through a silicagel column and concentrated to obtain a concentrated solution; the concentrated solution is subjected to adsorption and desorption, and then a crude scutellarin aglycone primer is obtained; the crude scutellarin aglycone primer is recrystallized through ethyl alcohol, filtered and dried to obtain the refined scutellarin aglycone primer. The experimental result of in-vitro detection on free radical scavenging by antioxidant shows that the antioxidant activity of the scutellarin aglycone primer is higher than that of scutellarin, and the scutellarin aglycone primer is expected to be widely applied as the oxidation resisting medicine.

Description

technical field [0001] The invention relates to the field of medicinal chemistry research, in particular to a novel scutellarin aglycone derivative, a preparation method thereof and an application in preparation of antioxidant drugs. Background technique [0002] Scutellarin (also known as scutellarin) is a flavonoid compound extracted and isolated from the dried whole herb of the Compositae plant Erigeronbreviscapus (Van.t) Hand.-Mazz. The main component of flower element, its structural formula is as follows: [0003] [0004] Scutellarin [0005] Scutellarin is mainly used clinically to treat cardiovascular and cerebrovascular diseases, rheumatoid arthritis and sequelae of stroke. Modern pharmacological studies have proved that scutellarin can increase cerebral blood flow, reduce cerebrovascular resistance, improve cerebral circulation, relieve arteriolar spasm, improve blood-brain barrier permeability, antagonize myocardial ischemia-reperfusion injury, inhibit plate...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/30C07D311/40A61K31/352A61P39/06
CPCC07D311/30C07D311/40
Inventor 郭鑫吴义强胡云楚
Owner CENTRAL SOUTH UNIVERSITY OF FORESTRY AND TECHNOLOGY