Identification of ten KB425796-A congeners from Paenibacillus sp. 530603 using an antifungal assay against Aspergillus fumigatus in combination with micafungin

  title={Identification of ten KB425796-A congeners from Paenibacillus sp. 530603 using an antifungal assay against Aspergillus fumigatus in combination with micafungin},
  author={Hirohito Kai and Midori Yamashita and Shigehiro Takase and Michizane Hashimoto and Hideyuki Muramatsu and Ikuko Nakamura and Koji Yoshikawa and Ryuichi Kanasaki and Masami Ezaki and Kumiko Nitta and Masato Watanabe and Noriaki Inamura and Akihiko Fujie},
  journal={The Journal of Antibiotics},
The discovery and characterization of natural congeners is one approach for understanding the relationship between chemical structure and biological function. We recently isolated the novel antifungal metabolite KB425796-A produced by the recently isolated bacterium Paenibacillus sp. 530603. On the basis of morphological changes of Aspergillus fumigatus induced by KB425796-A in combination with micafungin, we developed a highly sensitive screening method for the specific detection of KB425796-A… 
Synergistic antifungal activity of KB425796-C in combination with micafungin against Aspergillus fumigatus and its efficacy in murine infection models
The findings suggest that KB425796-C is a good candidate for the treatment of aspergillosis in combination with micafungin.
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Les bacteries qui sont des sources prolifiques d'antibiotiques et des fournisseurs importants d’agents pharmaceutiques peuvent produire une grande variete de metabolites. Ainsi, la decouverte de


KB425796-A, a novel antifungal antibiotic produced by Paenibacillus sp. 530603
The novel antifungal macrocyclic lipopeptidolactone, KB425796-A (1), was isolated from the fermentation broth of bacterial strain 530603, which was identified as a new Paenibacillus species based on
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Synergy, Pharmacodynamics, and Time-Sequenced Ultrastructural Changes of the Interaction between Nikkomycin Z and the Echinocandin FK463 against Aspergillus fumigatus
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FR901469, a novel antifungal antibiotic from an unidentified fungus No.11243. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological properties.
It is shown that FR901469 inhibited the activity of 1,3-beta-glucan synthase from Candida albicans with an IC50 value of 0.05 microg/ml, and displayed greater inhibitory activity than other 1, 3- beta-gluca synthase inhibitors such as, WF11899A, echinocandin B, aculeacin A, and papulacandin A.
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1,3-beta-Glucan synthase: a useful target for antifungal drugs.
It has been shown that the plasma membrane localization of this enzyme is essential for its activity, and inhibition of 1,3-beta-glucan synthase activity by anti-fungal drugs of the lipopeptide type triggers a cell cycle feedback mechanism leading to cell cycle arrest.
Efficacy of micafungin alone or in combination against experimental pulmonary aspergillosis.
Results indicate that MICA has moderate activity against pulmonary aspergillosis and might be useful in combination with conventional AMB and the combination of MICA and ICZ appeared to be potentially antagonistic.
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