FR209602 and Related Compounds, Novel Antifungal Lipopeptides from Coleophoma crateriformis No. 738

  title={FR209602 and Related Compounds, Novel Antifungal Lipopeptides from Coleophoma crateriformis No. 738},
  author={Ryuichi Kanasaki and Fumie Abe and Shigetada Furukawa and Koji Yoshikawa and Akihiko Fujie and Motohiro Hino and Seiji Hashimoto and Yasuhiro Hori},
  journal={The Journal of Antibiotics},
The biological activities of the novel echinocandin-like lipopeptides, FR209602, FR209603 and FR209604, were evaluated. These compounds showed antifungal activity against Candida albicans and Aspergillus fumigatus attributed to inhibition of 1,3-β-glucan synthesis. The minimum effective concentrations of these compounds against C. albicans and A. fumigatus ranged from 0.02 to 0.04 µg/ml by microbroth dilution assay, and the IC50 values on C. albicans 1,3-β-glucan synthase were 0.49, 0.64 and 0… 
FR209602 and Related Compounds, Novel Antifungal Lipopeptides from Coleophoma crateriformis No. 738
Novel antifungal lipopeptides, FR209602, FR209603 and FR209604, were isolated from the fermentation broth of a fungal strain No. 738 which was identified as Coleophoma crateriformis from
FR227673 and FR190293, Novel Antifungal Lipopeptides from Chalara sp. No. 22210 and Tolypocladium parasiticum No. 16616
Novel antifungal lipopeptides, FR227673 and FR190293, were isolated from the fermentation broths of fungal strains Chalara sp. No. 22210 and Tolypocladium parasiticum No. 16616, respectively. These
Micafungin: a sulfated echinocandin
  • S. Hashimoto
  • Biology, Chemistry
    The Journal of Antibiotics
  • 2009
Micafungin is the second approved antifungal agent in the echinocandin series and is now used worldwide in chemotherapy for life-threatening fungal infections. It is water-soluble and is
Emergence of Candida spp. and exploration of natural bioactive molecules for anticandidal therapy –status quo
The exploration of drugs from natural resources serves as a better alternative source in anticandidal therapeutics, having great scope for drug discovery in the future.
Non-β-Lactam Antibiotics
Some classes of fungal metabolites which are presently used as medicinal, veterinary or agricultural antibiotics, as well as some newer candidates for development are reviewed.
Antimicrobial lipopeptides : in vivo and in vitro synthesis
This review starts with general comments on antimicrobial peptides (AMPs), a large family of compounds that includes non-ribosomally assembled lipopeptides that have potential environmental and medical applications, but limited productivity.
Enhancement of Echinocandin B Production by a UV- and Microwave-Induced Mutant of Aspergillus nidulans with Precursor- and Biotin-Supplying Strategy
A stable mutant Aspergillus nidulans ZJB12073, which can use fructose as optimal carbon source instead of expensive mannitol, was selected from thousand isolates after several cycles of UV and microwave irradiation and showed 1.9-fold improvement in echinocandin B production.
Genomics‐driven discovery of a novel self‐resistance mechanism in the echinocandin‐producing fungus Pezicula radicicola
It is concluded that prfks1a is primarily responsible for protecting the fungus against extracellular echinocandin toxicity and is consistently transcribed at low levels and is upregulated in the presence of exogenous echinOCandin, but not during growth conditions promoting endogenous production of sporiofungin.
Use of a serum‐based antifungal susceptibility assay to predict the in vivo efficacy of novel echinocandin compounds
The data indicate that determination of serum‐MIC values will facilitate prediction of the in vivo potency of new antifungal compounds such as novel echinocandins, as well as previously uncharacterized echinOCandin compounds.


WF11899A, B and C, novel antifungal lipopeptides. II. Biological properties.
WF11899A, B and C, novel water-soluble lipopeptides related to the echinocandins, possess potent anti-Candida activities and mildly suppressed the growth of Aspergillus fumigatus and A. niger.
WF11899A, B and C, novel antifungal lipopeptides. I. Taxonomy, fermentation, isolation and physico-chemical properties.
WF11899A, B and C, novel antifungal lipopeptide antibiotics were isolated from the culture broth of Coleophoma empetri F-11899 and showed good solubility in water.
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.
Micafungin: a therapeutic review
Micafungin is expected to increase the efficacy rate of treatment in patients with severe aspergillosis or candidiasis when used in combination with amphotericin B or mold azoles.
The first echinocandin: caspofungin
In invasive aspergillosis casp ofungin resulted in higher response rates compared to a historic control under standard therapy, and in several multicenter randomised double blind trials on candida infections caspofungin proved to be at least non‐inferior to standard therapies.
Echinocandin inhibition of 1,3-beta-D-glucan synthase from Candida albicans.
The cyclic peptide antibiotic echinocandin was found to inhibit 1,3-beta-D-glucan synthase activity present in a mixed membrane fraction from Candida albicans and GTP stimulated enzyme activity approximately 4-fold, but did not affect the percentage inhibition of the enzyme by echinOCandin.
IPC synthase as a useful target for antifungal drugs.
Current progress in the development of IPC synthase inhibitors with antifungal activities are reviewed, and structure-activity relationships (SAR), physicochemical and structural properties, and synthetic methodology for chemical modification are presented.
Amphotericin B: 30 years of clinical experience.
The clinical uses of amphotericin B are discussed, including its application in AIDS-related fungal infections, in neutropenic cancer patients who are persistently febrile, and in infections of the central nervous system, lung, peritoneum, genitourinary system, eye, and skin.
Clinically significant azole cross‐resistance in Candida isolates from HIV‐positive patients with oral candidosis
Clinically significant cross-resistance to other azoles may occur in fluconazole-resistant isolates of C. albicans, although initially most isolates are not cross-resistant and the detection of cross- resistant isolates is associated with a history of greater prior azole exposure.
Treatment of fungal and other opportunistic infections in immunocompromised patients.
  • J. Wade
  • Medicine, Biology
  • 1997
Significant improvements have been made with regard to infection-related mortality in patients with underlying immune deficiencies, but the mortality rate continues to be very high for immunocompromised patients who develop infection with Candida and Aspergillus.