ABSTRACT
Through our screening for novel antifungal compounds, YM-215343 was found in the culture extract of Phoma sp. QN04621. The structure of YM-215343 was determined by several spectroscopic experiments as a novel compound closely related to apiosporamide and fischerin. YM-215343 exhibited antifungal activity against the pathogenic fungi, Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus with MIC values of 2 to approximately 16 microg/ml. It also showed cytotoxicity against HeLa S3 cells with an IC50 of 3.4 microg/ml.
Subject(s)
Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Heterocyclic Compounds, 4 or More Rings/chemistry , Heterocyclic Compounds, 4 or More Rings/pharmacology , Mitosporic Fungi/metabolism , Naphthalenes/chemistry , Naphthalenes/pharmacology , Pyridones/chemistry , Pyridones/pharmacology , Antifungal Agents/isolation & purification , Chromatography, Gel , Fermentation , HeLa Cells , Heterocyclic Compounds, 4 or More Rings/isolation & purification , Humans , Inhibitory Concentration 50 , Microbial Sensitivity Tests , Mitosporic Fungi/chemistry , Naphthalenes/isolation & purification , Nuclear Magnetic Resonance, Biomolecular , Plants/microbiology , Pyridones/isolation & purification , Spectrometry, Mass, Fast Atom BombardmentSubject(s)
Benzoates/pharmacology , Enzyme Inhibitors/pharmacology , Fungi/metabolism , Neuraminidase/antagonists & inhibitors , Sulfates/pharmacology , Benzoates/chemistry , Benzoates/metabolism , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/metabolism , Magnetic Resonance Spectroscopy , Mass Spectrometry , Molecular Structure , Spectrophotometry, Ultraviolet , Sulfates/chemistry , Sulfates/metabolismABSTRACT
Massadine, a highly oxygenated alkaloid, was isolated from the marine sponge Stylissa aff. massa as an inhibitor of geranylgeranyltransferase type I (GGTase I). The structure of massadine has been deduced from spectral data. Massidine inhibited GGTase I from Candida albicans with an IC(50) value of 3.9 microM. [structure: see text]
Subject(s)
Alkaloids/chemistry , Alkaloids/pharmacology , Alkyl and Aryl Transferases/antagonists & inhibitors , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Porifera/chemistry , Pyrroles/chemistry , Pyrroles/isolation & purification , Alkaloids/isolation & purification , Animals , Candida albicans/enzymology , Enzyme Inhibitors/isolation & purification , Inhibitory Concentration 50 , Magnetic Resonance Spectroscopy , Molecular Structure , Protein PrenylationABSTRACT
The brefeldin A (BFA) derivatives 4-O-acetyl BFA, 7-O-acetyl BFA, and 4-O-D-glucosyl BFA were found by the microbial conversion of BFA. 4-O-D-Glucosyl BFA is a novel compound produced by the conversion of BFA with Streptomyces sp. Q53834. The cytotoxicity and antifungal activity of all of the compounds were markedly less than those of BFA.
ABSTRACT
Two new polyacetylenic acids, corticatic acids D (2) and E (3), have been isolated from the marine sponge Petrosia corticata along with the known corticatic acid A (1) as geranylgeranyltransferase type I (GGTase I) inhibitors. Their structures were elucidated on the basis of spectroscopic and chemical methods. Compounds 1-3 inhibited GGTase I from Candida albicans with IC(50) values of 1.9-7.3 microM.
