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Synergistyczne działanie flukonazolu i laktonów ftalidowych jako czynnik ograniczający stosowanie leków azolowych w leczeniu kandidoz

Olejniczak Teresa

Wiadomości Chemiczne

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2023

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[Z] 77, 5-6

555-567

EN

The resistance of Candida albicans and other pathogenic yeasts to azole antifungal drugs has increased rapidly in recent years and is a significant problem in clinical therapy. The current state of pharmacological knowledge precludes the withdrawal of azole drugs, as no other active substances have yet been developed that could effectively replace them. Therefore, one of the anti-yeast strategies may be therapies that can rely on the synergistic action of natural compounds and azoles, limiting the use of azole drugs against candidiasis. Synergy assays perperformed in vitro were used to assess drug interactions Fractional Inhibitory Concentration Index. The synergistic effect of fluconazole (1) and three synthetic lactones identical to those naturally occurring in celery plants—3-n-butylphthalide (2), 3-n-butylidenephthalide (3), 3-n-butyl-4,5,6,7-tetrahydrophthalide (4)—against Candida albicans ATCC 10231, C. albicans ATCC 2091, and C. guilliermondii KKP 3390 was compared with the performance of the individual compounds separately. MIC90 (the amount of fungistatic substance (in µg/mL) inhibiting yeast growth by 90%) was determined as 5.96–6.25 µg/mL for fluconazole (1) and 92–150 µg/mL for lactones 2–4. With the simultaneous administration of fluconazole (1) and one of the lactones 2–4, it was found that they act synergistically, and to achieve the same effect it is sufficient to use 0.58–6.73 µg/mL fluconazole (1) and 1.26–20.18 µg/mL of lactones 2–4. Based on biological research, the influence of the structure on the fungistatic activity and the synergistic effect were determined.

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Wpływ pola elektromagnetycznego na przeżywalność, wrażliwość na antybiotyki, i przepuszczalność błony Candida Albicans

Sztafrowski Dariusz, Muraszko Jakub, Jasiura Adam, Urbanek Aneta K., Krasowska Anna

Przegląd Elektrotechniczny

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2022

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R. 98, nr 12

254--257

PL

Candida albicans jest patogenem oportunistycznym wywołującym grzybice powierzchni (skóry, błon śluzowych) i narządów wewnętrznych. Grzyb ten m.in. przylega do nabłonka i powierzchni abiotycznych (zastawki, protezy) i tworzy trudno gojące się biofilmy. Obecnie lekarze borykają się z ogromnym problemem narastania odporności na szeroko stosowane związki przeciwgrzybicze. Chociaż grzyby z rodzaju Candida są wiodącym czynnikiem etiologicznym zakażeń oportunistycznych, liczba dostępnych i skutecznych leków przeciwgrzybiczych jest ograniczona. Poszukiwanie nowych antybiotyków i sposobów zwalczania C. albicans ma obecnie ogromne znaczenie. Nasze wcześniejsze badania wykazały pozytywny wpływ statycznego pola magnetycznego na komórki C. albicans. Komórki hodowane w polu magnetycznym wykazywały zmniejszoną intensywność wzrostu i zwiększoną wrażliwość na stosowane antybiotyki – flukonazol i amfoterycynę B. W związku z tym postanowiono kontynuować badania z wykorzystaniem pola magnetycznego 50 Hz.

EN

Candida albicans is an opportunistic pathogen that causes mycoses of the surface (skin, mucosa) and internal organs. This fungus, among others, adheres to the epithelium and abiotic surfaces (valves, prostheses) and creates difficult-to-heal biofilms. Currently, doctors struggle with the great problem of growing resistance to the widely used antifungal compounds. Although fungi of the genus Candida are the leading etiological agent of opportunistic infections, the number of available and effective antifungal drugs is limited. The search for new antibiotics and ways to combat C. albicans is now of great importance. Our earlier research showed a positive effect of a static magnetic field on C. albicans cells. Cells grown in a DC magnetic field showed reduced growth intensity and increased sensitivity to the antibiotics used - fluconazole and amphotericin B. Therefore, it was decided to continue the research using an 50 Hz magnetic field.

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A brief review of fluconazole as an antifungal agent and the need for research into its nanoformulation

Nagaraj S.

Journal of Achievements in Materials and Manufacturing Engineering

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2022

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Vol. 114, nr 2

81--85

EN

Purpose: Antifungals compounds have gained significant attention, and in this context, fluconazole as an antifungal is used predominantly, and the use of a nanoformulated form of this is discussed. Design/methodology/approach: Fluconazole, an FDA-approved antibiotic, is an effective antimicrobial especially used to treat fungal infections. Its uniqueness lies in the fact that it contains fluoride with triazole functionality. Its efficacy against various types of fungus is demonstrated. Findings: Although it is one of the effective antibiotics, its side effects are well documented, and due to this, many techniques are tried to improve its efficacy with lesser side effects. Research limitations/implications: In this respect, nanoparticles play a crucial role, and many studies worldwide are carried out on this aspect. Among many nano techniques use of chitosan as well as lipid carriers of fluconazole are being considered. However, systematic studies are warranted to take this aspect into clinical trials. Practical implications: Nano-based platforms seem to be an alternating hope to combat resistance and side effect. Originality/value: A thorough study is the need of the hour to devise a proper nano-based strategy of fluconazole.