FR207944, an antifungal antibiotic from Chaetomium sp. no. 217 I. Taxonomy, fermentation, and biological properties.
An antifungal antibiotic, FR207944, was isolated from the culture broth of a fungal strain Chaetomium sp. no. 217. FR207944 is a triterpene glucoside with antifungal activity against Aspergillus fumigatus and Candida albicans. Specifically, FR207944 exhibits in vitro and in vivo antifungal activity against A. fumigatus. The effects of FR207944 on the morphology of A. fumigatus were shown to be similar to those of FR901379, a known 1,3-beta-glucan synthase inhibitor. The MECs of FR207944 against A. fumigatus FP1305 and C. albicans FP633 in micro-broth dilution test were 0.039 and 1.6 mug/ml respectively. FR207944 showed good potency by subcutaneous injection and oral administration against A. fumigatus in a murine systemic infection model, with ED(50)s of 5.7 and 17 mg/kg respectively.
Kobayashi
Motoo
M
Fermentation Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Tokodai, Tsukuba, Ibaraki, Japan. motoo_kobayashi@po.fujisawa.co.jp
Kanasaki
Ryuichi
R
Sato
Ikuko
I
Abe
Fumie
F
Nitta
Kumiko
K
Ezaki
Masami
M
Sakamoto
Kazutoshi
K
Hashimoto
Michizane
M
Fujie
Akihiko
A
Hino
Motohiro
M
Hori
Yasuhiro
Y
D000818:Animals; D000935:Antifungal Agents / Q000145:classification / Q000302:isolation & purification* / Q000378:metabolism / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D005285:Fermentation; D006027:Glycosides / Q000302:isolation & purification* / Q000378:metabolism / Q000494:pharmacology; D051379:Mice; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D014315:Triterpenes / Q000302:isolation & purification* / Q000378:metabolism / Q000494:pharmacology
D000935:Antifungal Agents; C503272:FR207944; D006027:Glycosides; D014315:Triterpenes