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Studies on synergisidin

H Jinnouchi, K Yagishita

    The Japanese Journal of Antibiotics
    |January 1, 1981
    PubMed
    Summary

    A novel compound, synergisidin, isolated from Penicillium sp. exhibits weak antifungal activity but potent synergistic effects with imidazole antimycotics against Candida species. Its toxicity and cellular effects were also characterized.

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    Area of Science:

    • Mycology
    • Natural Product Chemistry
    • Antimicrobial Research

    Background:

    • Soil microorganisms are a rich source of novel bioactive compounds.
    • Fungal infections, particularly those caused by Candida species, pose a significant public health challenge.
    • The development of new antifungal strategies, including synergistic combinations, is crucial.

    Purpose of the Study:

    • To isolate and characterize a novel compound, synergisidin, from Penicillium sp. No. Y-11930.
    • To evaluate the antimicrobial and antifungal activities of synergisidin.
    • To investigate the synergistic potential of synergisidin in combination with existing antifungal agents.

    Main Methods:

    • Isolation and purification of synergisidin from Penicillium sp. culture broth.
    • Determination of chemical structure through physiochemical properties and comparison with known compounds.
    • Antimicrobial susceptibility testing against various bacteria and fungi.
    • Evaluation of synergistic effects with imidazole antimycotics against Candida species.
    • Acute toxicity studies (LD50) in mice and morphological effects on HeLa cells.

    Main Results:

    • Synergisidin was isolated and identified as identical to brefeldin A and ascotoxin.
    • The compound exhibited minimal antibacterial activity but weak antifungal activity against eumycetes.
    • Synergisidin demonstrated significant 30-125-fold synergistic effects with econazole, miconazole, and clotrimazole against Candida species.
    • Acute toxicity in mice was LD50 ≤ 250 mg/kg, with morphological degenerative effects on HeLa cells observed at concentrations > 0.122 µg/ml.

    Conclusions:

    • Synergisidin (brefeldin A) shows potent synergistic activity when combined with imidazole antimycotics, enhancing their efficacy against Candida species.
    • This synergistic combination represents a promising strategy for combating fungal infections.
    • Further research into the mechanism of synergy and potential therapeutic applications is warranted.

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