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Application of magnolol and azole medicines to preparation of antifungal combined medicines

A magnolol and antifungal technology, applied in the field of medicine, can solve the problems of inability to achieve effective bactericidal concentration, treatment failure, etc., and achieve the effect of improving drug efficacy, reducing concentration, and increasing concentration

Inactive Publication Date: 2014-12-10
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the high expression of the efflux pump, the accumulation of drugs in the bacteria is reduced, so that the effective bactericidal concentration cannot be reached, and the treatment fails.

Method used

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  • Application of magnolol and azole medicines to preparation of antifungal combined medicines
  • Application of magnolol and azole medicines to preparation of antifungal combined medicines
  • Application of magnolol and azole medicines to preparation of antifungal combined medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1 in vitro synergy experiment

[0027]In vitro susceptibility test of antifungal drugs and checkerboard microdilution method refer to literature Clinical and Laboratory Standards Institute. M27-A3, Reference method for broth dilution antifungal susceptibility testing of yeasts: approved standard, 3rd ed., 2008. Wayne, PA. The specific operation is as follows:

[0028] (1) Bacterial solution preparation and sensitivity analysis

[0029] The Candida albicans strain stored at -70°C was thawed, inoculated on YPD solid medium, and cultured at 37°C for 24 hours. A well-developed single colony was inoculated on YPD again, and cultured at 35°C for 24 hours to obtain a pure culture. Five bacterial colonies with a diameter greater than 1mm were selected, and they were prepared into a bacterial suspension with 0.85% sterilized physiological saline. Shake the bacterial suspension on an oscillator for 15 seconds, count the number of bacteria with a hemocytometer, and a...

Embodiment 2

[0055] Embodiment 2: Research on Synergy Mechanism

[0056] Determination of Absorbance Value of Rhodamine 123 in Extracellular Fluid by Fluorescent Microplate Reader

[0057] Strain culture: Pick the monoclonal strain and inoculate it in RPMI-1640 culture medium, incubate at 35°C for 24 hours, centrifuge at 3000rpm for 10 minutes to collect the cells, transfer the cells to 100ml of fresh RPMI-1640 culture medium, and culture with shaking at 35°C After 4 hours, count the number of bacteria with a hemocytometer, and adjust the concentration of the bacterial suspension to 107 cfu / ml, take 100ml of bacterial suspension, centrifuge at 3000rpm for 10 minutes to collect fungal cells, wash twice with PBS.

[0058] Determination of Rhodamine 123 Concentration in Specimens

[0059] For the supernatant samples collected during the efflux process, the fluorescence values ​​were measured with a fluorescent microplate reader (excitation wavelength 488nm, emission wavelength 525nm). Deter...

Embodiment 3

[0071] Embodiment 3 Molecular Mechanism Research

[0072] (1) Fluorescent quantitative PCR method to measure the expression of related genes in the ergosterol biosynthetic pathway (ERG3, ERG5, ERG1, ERG25, ERG6, ERG11) and fungal cell membrane efflux pump related genes (MDR1, CDR1, CDR2) sample processing

[0073] Pick the single clone of drug-resistant strain CA10 and inoculate it in 30ml YPD culture medium, culture overnight at 37°C, centrifuge at 3000g for 5min, and resuspend with fresh YPD to adjust the bacterial density to 1.0×10 6 cfu / ml respectively drug group and control group. Incubate with shaking at 37°C for 12 hours, then centrifuge at 4°C.

[0074] TES preparation

[0075] 10mM Tris.Cl pH 7.5; 10mM EDTA; 0.5% (W / V) SDS was prepared with RNase-free water and stored at room temperature.

[0076] Extraction of RNA by thermal phenol method

[0077] The cell pellet was resuspended with 1ml of ice-cold PBS, transferred to a 1.5ml proteinase K-treated Eppendorf tube...

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Abstract

The invention provides application of magnolol and azole medicines to preparation of antifungal combined medicines. The application indicates that azole medicines such as fluconazole, ketoconazole, itraconazole, miconazole and voriconazole are used together with magnolol to generate a synergetic antifungal effect; the magnolol serving as an efflux pump Cdrlp substrate is utilized to compete with the azole medicines for an efflux system, so that the concentration of efflux medicines can be reduced, and the curative effect of medicines can be improved. Furthermore, magnolol acts on the synthetic pathway of ergosterol and is combined with azole medicines to form a double-edged sword to inhibit synthesis of ergosterol together.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the application of magnolol and azole drugs such as fluconazole, ketoconazole, itraconazole, miconazole and voriconazole in the preparation of antifungal combined drugs. Background technique [0002] In recent years, due to the widespread use of antibiotics and immunosuppressants, the incidence of organ transplantation and bone marrow transplantation, cancer chemotherapy, AIDS and diabetes has been increasing, and the morbidity and mortality of fungal infections, especially opportunistic fungal infections, have risen sharply[C.E. Linares, S.R.Giacomelli, D.Altenhofen, S.H.Alves, V.M.Morsch, M.R.Schetinger, Fluconazole and amphotericin-B resistance are associated with increased catalase and superoxide dismutase activity in Candida albicans and Candida dubliniensis, Rev 25 op 1 Bras Med (7) -758]. Fungal infectious diseases, including superficial fungal infections and ...

Claims

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Application Information

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IPC IPC(8): A61K31/4196A61K31/496A61K31/506A61K31/4174A61P31/10A61K31/05
Inventor 孙玲美廖凯
Owner SOUTHEAST UNIV
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