Application of SB-743921 to preparation of antifungal drugs

A technology of SB-743921, 1. SB-743921 is applied in the field of preparing antifungal drugs, and can solve problems such as no reports on the antifungal effect of SB-743921

Active Publication Date: 2020-11-27
SHAANXI UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there is no report on the antifungal effect of SB-743921 at home and abroad

Method used

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  • Application of SB-743921 to preparation of antifungal drugs
  • Application of SB-743921 to preparation of antifungal drugs
  • Application of SB-743921 to preparation of antifungal drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1, the effect of SB-743921 on different fungi

[0019] Materials and methods

[0020] 1. Test drug:

[0021] SB-743921 (CAS No. 940929-33-9): purchased from Shanghai Kairui Biotechnology Co., Ltd., purity ≥ 99%.

[0022] Fluconazole: sigma company, batch number 036M4709V.

[0023] Dimethylsulfoxide (DMSO): Tianjin Tianli Chemical Reagent Co., Ltd.

[0024] Each reagent was prepared in DMSO and stored at -20°C. Before the experiment, the drug was taken out and placed in a 35°C incubator to melt, and mixed thoroughly.

[0025] 2. Strains:

[0026] Strains Used: Including:

[0027] 1. Sensitive strains (sensitive to fluconazole): sensitive Candida albicans (SC5314), Candida parapsilosis (22019), Cryptococcus neoformans (32609);

[0028] 2. Drug-resistant strains (resistant to fluconazole): drug-resistant Candida albicans (103), drug-resistant Candida tropicalis, naturally drug-resistant Candida krusei (ATCC2340), naturally drug-resistant Candida glabrata (AT...

Embodiment 2

[0055] Example 2, the effect of SB-743921 on the survival of different fungi

[0056] experimental method:

[0057] 1, medicine, bacterial strain, material are with embodiment 1

[0058] 2. Experimental steps:

[0059] Before the experiment, a small number of bacterial clones were picked from the SDA medium stored at 4°C, inoculated into 1mL YEPD medium, and cultured at 35°C, 200rpm shaking for 16h, so that the fungus was in the late exponential growth phase.

[0060] Dilute with RPMI1640 liquid culture medium and adjust the bacterial concentration to 1×10 5 CFU / mL. Add fluconazole and compound SB-743921 to the above bacterial liquid respectively, so that the final concentration of fluconazole is 1 μg / mL, the final concentration of compound SB-743921 is 64 μg / mL, 32 μg / mL and 16 μg / mL, and the blank control is added with the same volume of DMSO, the content of DMSO in all bacterial solutions was lower than 0.5%. In a 35°C incubator, shake culture at 200rpm, take samples at ...

Embodiment 3

[0064] Example 3, the effect of SB-743921 combined with fluconazole on different fungi

[0065] experimental method:

[0066] 1, medicine, bacterial strain, material are with embodiment 1

[0067] 2. Experimental steps:

[0068] Before the experiment, a small number of bacterial clones were picked from the SDA medium stored at 4°C, inoculated into 1mL YEPD medium, and cultured at 35°C, 200rpm shaking for 16h, so that the fungus was in the late exponential growth phase.

[0069] Add 1.3ml of each bacterial solution to five 5ml EP tubes. The concentration of the original drug SB-743921 solution was 6.4 mg / ml, and 3.25 μl, 1.625 μl, 0.812 μl, 0.406 μl, and 0.203 μl of the original drug solution were added to each of the five EP tubes so that the drug contents in the tubes were 16 μg / ml, 8μg / ml, 4μg / ml, 2μg / ml, 1μg / ml.

[0070] Take a sterile 96-well plate for each strain, and add 100 μL of RPMI 1640 liquid medium to the No. 1 well of each row as a blank control; add 100 μL of...

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Abstract

The invention provides an application of SB-743921 to preparation of antifungal drugs. In vitro cell experiments show that SB-743921 has different degrees of antifungal and even fungicidal effects ondrug-resistant candida albicans 103, sensitive candida albicans SC5314, candida krusei ATCC2340, candida parapsilosis 22019, candida glabrata ATCC2281 and drug-resistant candida tropicalis. Combined with fluconazole, SB-743921 has a synergistic effect on the drug-resistant candida albicans 103, candida glabrata ATCC2281 or candida tropicalis, and has an additive effect on the candida parapsilosis22019. A novel application is opened up for SB-743921, SB-743921 can be used for preparing antifungal drugs, new candidate drugs are provided for treatment of fungal infections. SB-743921 has broad antifungal spectrum and fungicidal activity, and provides a novel curative approach for clinical efficient treatment of fungal infection and even drug-resistant fungal infection.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the use of SB-743921 for preparing antifungal drugs. Background technique [0002] SB-743921 is a highly effective spindle kinesin inhibitor. Modern pharmacological studies have shown that SB-743921 has anti-tumor functions. [0003] At present, there is no report on the antifungal effect of SB-743921 at home and abroad. Contents of the invention [0004] To solve the problems in the prior art, the present invention provides the use of SB-743921 for preparing antifungal drugs. [0005] The present invention is achieved through the following technical solutions: [0006] Use of SB-743921 for the preparation of antifungal drugs. [0007] Preferably, the fungi include sensitive fungal strains and drug-resistant fungal strains. [0008] Further, the sensitive fungal strains include sensitive Candida albicans SC5314 and Candida parapsilosis 22019. [0009] Still fur...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/4196A61P31/10
CPCA61K31/352A61K31/4196A61P31/10A61K2300/00
Inventor 刘伟韩磊王胜正
Owner SHAANXI UNIV OF SCI & TECH
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