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Coumarin spermidine derivative and its extraction method and application

A technology of coumarinyl spermidine and its derivatives, which is applied in the field of preparation of coumarinyl spermidine derivatives, can solve problems such as the extraction of coumarinyl spermidine derivatives and unclear action mechanism, and achieve a simple preparation method Convenience, inhibition of apoptosis, and convenient operation

Active Publication Date: 2022-04-19
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of this application is to provide a kind of coumarin spermidine derivative and its extraction method and application, aiming at solving the problem of ambiguous extraction and action mechanism of coumarin spermidine derivative in the prior art

Method used

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  • Coumarin spermidine derivative and its extraction method and application
  • Coumarin spermidine derivative and its extraction method and application
  • Coumarin spermidine derivative and its extraction method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Extraction method of coumarin spermidine derivatives of roses

[0107] Adopt rose as the medicinal flower of experiment, extract the coumarin spermidine derivative of rose, comprise the steps:

[0108] (1) After 10 g of dried roses were crushed by a pulverizer, 100 mL of ethanol was added for ultrasonic extraction at room temperature for 1 hr. The filtrate was collected by filtration through filter paper, and the filter residue was extracted with 100 mL of ethanol for 1 hr, the extraction was repeated three times, the filtrate was combined, and the filtrate was evaporated to dryness by vacuum rotary evaporation at 45°C to obtain the initial extract of the coumarimide derivative;

[0109] (2) After dissolving the primary extract of coumarin spermidine derivatives with 5 mL of methanol, add a 100-200 mesh silica gel column (35 × 2.5 cm), and use 500 mL of ethyl acetate and n-hexane mixture (1:1 ), 500mL dichloromethane and methanol mixture (1:4) and 500mL acetone were el...

Embodiment 2

[0112] LC-MS analysis was performed on the SG-3 provided in step (2) of Example 1 and the SLs provided in step (3).

[0113] experimental method:

[0114] Among them, the LC parameters are reversed-phase YMC C18 column (150mm×2mm, 5μm pore size), the injection volume is 10μL, the mobile phase is 0.1% formic acid solution and acetonitrile, 5-80% acetonitrile gradient elution, and the flow rate is 0.4mL / min. The MS parameter is that the machine is SCIEXX500R Quadrupole Time-of-Flight (QTOF) system (AB Sciex LLC), IDA positive ion mode, gas1, gas 2 are both 40psi, curtain gas is 30psi, turbine injection temperature is 450°C, injection pressure is At 5500V, the CE values ​​of TOF / MS and TOF / MS / MS are 10V and 40V, respectively. MS scan 100-1000m / z, product ions scan 50-1000m / z.

[0115] Result analysis:

[0116] The SG-3 provided in step (2) of Example 1 was analyzed by LC-MS, as shown in Table 1 below, a total of 11 kinds of coumarimide derivatives were obtained, including ...

Embodiment 3

[0123] Analysis of the anti-apoptotic ability of the coumarin spermidine derivatives provided in Example 1

[0124]The cell apoptosis rate of the cells treated with the coumarin spermidine derivatives provided in Example 1 was measured by a flow cytometer, and the anti-apoptosis ability of the coumarin spermidine derivatives was analyzed. At the same time, Western blot was used to measure the expression of apoptosis-related proteins to determine the anti-apoptotic activity of the coumarin spermidine derivatives.

[0125] experimental method:

[0126] Cell experiment method

[0127] (1) Cell culture: HepG2 cell line is prepared with DMEM medium plus 10% FBS, 1% antibiotics, at 37°C, 5% CO 2 cultured in a constant temperature humidified incubator. Cells used in all experiments were at passage 12-20.

[0128] (2) Determination of cell activity: HepG2 cells were inoculated in a 96-well plate and cultured overnight, and then various concentrations of test compounds / extracts w...

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Abstract

The present application relates to the technical field of preparation of coumarin spermidine derivatives, in particular to a coumarin spermidine derivative and its extraction method and application. The coumarin spermidine derivatives provided by the application can significantly inhibit the apoptosis induced by alcohol, increase the expression of anti-apoptotic factor Bcl-2 and inhibit the expression of pro-apoptotic factors Bax, Caspase-3 and PARP, and have relatively Good anti-alcoholic, liver-protecting, and liver-protecting effects; the obtained coumarin spermidine derivatives have a wide range of applications in anti-alcohol, liver-protecting, and liver-protecting drugs or health foods; at the same time, the preparation method is simple and convenient , the operation is convenient, and the preparation and application of the coumarin spermidine derivatives can be realized.

Description

technical field [0001] The application belongs to the technical field of preparation of coumarin spermidine derivatives, in particular to a coumarin spermidine derivative and its extraction method and application. Background technique [0002] Among medicinal plants, some medicinal plants such as roses and jasmine have rich chemical components, including aromatic alcohols, aldehydes, fatty acids, phenols, and oils and fats containing flavors, which have effective functions when eaten. So far, the research on the medicinal plants of flowers has mainly focused on the research on their dietotherapy, and there are no detailed reports on the biological activities and specific mechanisms of the compounds therein. Among them, the coumarin spermidine derivative is a newly discovered polyphenol substance with antioxidant activity, but no relevant research has been carried out on its mechanism of action. Contents of the invention [0003] The purpose of this application is to provi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C235/34C07C231/24A61K31/165A61P1/16A61P39/02A23L33/105
CPCC07C235/34A61P1/16A61P39/02A23L33/105A23V2002/00A23V2200/30A23V2250/21A23V2300/10A23V2300/14A23V2300/38
Inventor 王明福周倩陈峰刘宾郑家荣
Owner SHENZHEN UNIV
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