UK-2A, B, C, and D, Novel Antifungal Antibiotics from Streptomyces sp. 517-02. VII. Membrane Injury Induced by C9-UK-2A, a Derivative of UK-2A, in Rhodotorula mucilaginosa IFO 0001.

DOI PubMed Open Access

Bibliographic Information

Other Title
  • VII. Membrane Injury Induced by C9-UK-2A, a Derivative of UK-2A, in <i>Rhodotorula mucilaginosa</i> IFO 0001

Search this article

Description

UK-2A is a potent antifungal antibiotic and its structure is highly similar to that of antimycin A3 (AA). UK-2A and AA inhibit mitochondrial electron transport at complex III. However, the antifungal activities of UK-2A and AA disappear after 48-hour treatment. In an attempt to improve the duration of the antifungal activity of UK-2A, several UK-2A derivatives were prepared by substituting its nine-membered dilactone ring with an n-alkyl or an isoprenyl moiety. Among all the derivatives tested, C9- and C10-UK-2A showed the most potent and durable antifungal activities against a strict aerobic yeast, Rhodotorula mucilaginosa IFO 0001. C9-UK-2A, in particular, continued to demonstrate its broad-spectrum antifungal activity after 120-hour treatment. Therefore, we focused on C9-UK-2A to further examine its mode of action against the yeast. Interestingly, C9-UK-2A did not inhibit cellular respiration of the cells even at concentrations greater than 100μg/ml. C9-UK-2A gradually induced the efflux of potassium ions from the cells. Moreover, C9-UK-2A gradually induced the release of glucose from glucose-encapsulating liposomes. The patterns of efflux and release induced by C9-UK-2A were not as rapid as those seen with amphotericin B. These results suggest a membrane injury caused by C9-UK-2A in R. mucilaginosa IFO 0001.

Journal

Keywords

Details 詳細情報について

  • CRID
    1390282679127851136
  • NII Article ID
    130003503966
  • DOI
    10.7164/antibiotics.55.315
  • COI
    1:CAS:528:DC%2BD38Xis1aisbc%3D
  • ISSN
    18811469
    00218820
  • PubMed
    12014448
  • Text Lang
    en
  • Article Type
    journal article
  • Data Source
    • JaLC
    • Crossref
    • PubMed
    • CiNii Articles
    • OpenAIRE
  • Abstract License Flag
    Disallowed

Report a problem

Back to top