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A kind of pharmaceutical composition and application thereof for Candida albicans echinocandins drug-resistant bacteria

A technology of echinocandin and Candida albicans, which is applied in pharmaceutical formulations, antifungal agents, medical preparations containing active ingredients, etc., can solve the problems of inability to effectively inhibit the activity, and achieve the effect of treating invasive infections

Active Publication Date: 2021-08-10
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compound L-269289 is a specific inhibitor of GGTase 1, which is highly specific and cannot effectively inhibit the activity of this enzyme in human cells

Method used

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  • A kind of pharmaceutical composition and application thereof for Candida albicans echinocandins drug-resistant bacteria
  • A kind of pharmaceutical composition and application thereof for Candida albicans echinocandins drug-resistant bacteria
  • A kind of pharmaceutical composition and application thereof for Candida albicans echinocandins drug-resistant bacteria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Chemical structural formula of Camoen Net and Compound L-269289 figure 1 As shown, the present embodiment verifies the bactericidal activity of the combined drug resistant strain by in vitro experiments, and the specific operation is as follows:

[0023] (1) Measurement of Cantonese Phase Pharmaceutical Experiment: The determination of alcoholic pharmacokinese experiments were completed in 96-well plates, and 100 ul of yeast leaching glucose culture solution was added to each well. Kumole is net by dilution according to the set concentration (concentration setting figure 2 A) Place in the hole, the designated strain (wild-type alcohol colors; alcoholine drug resistant strains, including FKS1 F641S And FKS1 S645F Cultivate to approximately 10 per well after cultivating 3 The bacteria; after cultivating 48 hours in the dark for 48 hours, the strain concentration was measured by the enzyme gauge, and the data was indicated, such as figure 2 (A) shown. figure 2 The results of (...

Embodiment 2

[0026] Concentration gradient detection of combined medication: 100 ul of yeast leaching glucose culture solution (YPD), carpoff and compound L-269289 were added to the 96-well plate, and the compound L-269289 was added to set concentration (concentration setting) image 3 Placed in the well, combined with alcoholicobacterium drug resistant strain (including FKS1) F641S And FKS1 S645F Cultivate to approximately 10 per well after cultivating 3 The bacteria; after cultivating 48 hours in the dark for 48 hours, the strain concentration was measured by the enzyme gauge, and the data was indicated, such as image 3 Indicated. image 3 The results show that the net carbaclasin drug resistant strain is used alone with the net in 0.5 μg / ml ~ 4 μg / ml high concentration, including FKS1 F641S And FKS1S645F The inhibitory effect is weak. However, 1.5 μg / ml ~ 4μg / ml kapopen net and 25 ~ 35 um l-269289 combined drugs for drug resistant strains FKS1 F641S Growth has a significant inhibitory...

Embodiment 3

[0028] Compound L-269289 is verified to the toxicity of the human renal cell line 293, which includes the following operations:

[0029] (1) Human renal cell line 293 is provided by China Typical Culture Safety Center (CCTCC), which is negative by PCR to detect mycoplasma pollution;

[0030] (2) 293 cells with 5.0 × 10 per hole 4 The concentration of cells were inoculated in 96-well plates, and 10% fetal bovine serum was added, with DMSO (MP biomedicine) and compound L-269289, the concentration was set to 10 μm, 20 μm, 30 μm, 40 μm, 50 μM culture for 72 h, The cultured surviving cells were detected with a cell count kit 8 (APEXBIO), and the cell survival rate of the non-L-269289 treatment was 100% as a control.

[0031] Experimental results Figure 4 (A) shown, Figure 4 (A) The results show that the L-269289 will show inhibition of 293 cell viability when the concentration is greater than 40 μm.

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Abstract

The invention belongs to the field of medicaments, and in particular relates to a pharmaceutical composition for treating invasive infection of Candida albicans echinocandin drug-resistant bacteria and application thereof. The active component of the pharmaceutical composition is composed of caspofungin and compound L-269289, and in vitro inhibits Echinocandin drug-resistant strains of Candida albicans, the caspofungin and compound L-269289 The mass ratio is 1:3~1:36; for the treatment of the invasive infection of Candida albicans echinocandins drug-resistant strains to mice, the mass ratio of the caspofungin and the compound L-269289 is 1:10. The present invention has verified in vitro experiments that the combined use of caspofungin and compound L‑269289 can effectively kill echinocandin drug-resistant strains of Candida albicans, and is suitable for treating echinocandin drugs of Candida albicans Invasive infection of mice by drug-resistant strains.

Description

Technical field [0001] The invention belongs to the sect of the pharmaceutical field, and in particular to a pharmaceutical composition for alcoholic bacteria drug resistant bacteria and its application thereof. Background technique [0002] Candida Albicans, also known as white candida or white forsythics, is the most common fungi and pathogens currently recognized in human beings, exotic, epidermis, upper respiratory tract, Gastrointestinal tract and vagina, etc. In healthy humans, this symbiotic is usually benign, generally not caused disease or only slight superfur infection, but when the human immune system is impaired or in the body's normal microbial flora, the excessive growth of the bacteria caused More severe shallow infections (such as thrush and vaginitis), may even lead to fatal deep invasive infections (such as sepsis). Although there are currently a variety of antifungal treatment, the invasional candida disease still has a higher fatal rate. At present, the invasi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/12A61P31/10A61K31/496
CPCA61K31/496A61K38/12A61P31/10A61K2300/00
Inventor 苏畅逯杨孙强强
Owner WUHAN UNIV
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