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Succinic acid derivative and preparation method and application thereof

A technology of derivatives and succinic acid is applied in the application field of preparing Candida albicans inhibitor, and can solve the problems such as no drugs.

Active Publication Date: 2018-04-24
NINGBO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are no reports on the chemical structure and anti-Candida albicans activity of this compound, so there is no drug related to it on the market

Method used

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  • Succinic acid derivative and preparation method and application thereof
  • Succinic acid derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A kind of succinic acid derivative structural formula is as shown in I:

[0023] (I).

Embodiment 2

[0025] The preparation method of the succinic acid derivative shown in I formula specifically comprises the steps:

[0026] (1) Fermentation production

[0027] Trichoderma with preservation number CGMCC No: 12969 Trichoderma Sp. was revived by streaking, transferred to a 250mL Erlenmeyer flask containing 100 mL of PDB medium, and cultured at 25°C and 180 r / min for 4 days to obtain a seed culture solution; after that, the seeds were inoculated according to an inoculum volume of 10% by volume. The solution was inoculated into a 1000mL Erlenmeyer flask equipped with PDB medium (2g of potato extract and 8g of glucose, dissolved in 400mL of seawater), and fermented on a shaking table at 25°C and 150rpm for 14 days to obtain a fermentation broth;

[0028] (2) Obtaining the extract

[0029] The above-mentioned fermented liquid was extracted 3 times with an equal volume of ethyl acetate, and the extract was concentrated under reduced pressure to remove the ethyl acetate to obtain ...

Embodiment 3

[0037] Anti-Candida albicans activity test in vitro (96-well plate antibacterial method)

[0038] (1) Experimental samples

[0039] Preparation of the test sample solution: the test sample is the pure compound I isolated and purified in Example 1 above, and an appropriate amount of sample is accurately weighed, and prepared into a solution of the required concentration with DMSO for testing the activity.

[0040] (2) Experimental method

[0041] 96-well plate anti-Candida albicans test method: The compound to be tested was serially diluted in 20% DMSO / saline, and transferred 10 µL to a 96-well flat-bottomed microplate. Under aerobic conditions, the Candida albicans strain was cultured on Sabouraud agar medium (SDA) at 30° C. for 16-20 hours. A series of compounds with different concentrations were added to RPMI1640 medium, and Candida albicans strains were inoculated, and cultured at 35°C for 46 hours. 8 μg / ml fluconazole was used as a positive control, and DMSO solution wa...

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PUM

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Abstract

The invention discloses a succinic acid derivative and preparation and application thereof. The succinic acid derivative is characterized in that the structural formula of the succinic acid derivativeis as shown in formula I. The preparation method of the succinic acid derivative comprises the following steps: acquiring fermentation liquid of a novel succinic acid derivative by fermental cultivation through marine trichoderma strains with the preservation number of CGMCC No: 12969; then extracting fermentation liquid with ethyl acetate to obtain a crude extract; and separating and purifying the crude extract to obtain the succinic acid derivative by reduced pressure column chromatography on silica gel and inversed-phase semi-preparative high performance liquid chromatography. The succinicacid derivative has effect of resisting candida albicans, and has the advantage that the succinic acid derivative can be used as a novel drug ingredient of a candida albicans inhibitor or a lead compound.

Description

technical field [0001] The invention relates to a succinic acid derivative, in particular to a method for preparing a succinic acid derivative with marine Trichoderma and the application of the compound in the preparation of a Candida albicans inhibitor. Background technique [0002] Candida albicans ( Candida albicans ) is a normal flora that resides on the mucous membranes of the normal human digestive tract, respiratory tract and female genital tract, and is also the most common conditional pathogenic bacteria in the genus Candida. In recent years, due to the extensive application of immunosuppressants, the development of tumor radiotherapy, chemotherapy, invasive treatment, organ transplantation, and the widespread application of a large number of broad-spectrum antibiotics, the normal flora is imbalanced, making the infection rate and incidence of Candida albicans relatively high. There has been a marked increase in the past. Due to the lack of existing antifungal dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C59/76A61P31/10C12P7/50C12R1/885
CPCC07C59/76C12P7/50
Inventor 姚佳晓丁立建何山孙晴镁任湛群斯拉瓦·爱泼斯坦
Owner NINGBO UNIV
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