RRC ID 2650
Author Ikeda Y, Furumai T, Igarashi Y.
Title Nocardimicins G, H and I, siderophores with muscarinic M3 receptor binding inhibitory activity from Nocardia nova JCM 6044.
Journal J Antibiot (Tokyo)
Abstract In the screening for muscarinic M3 receptor binding inhibitors from microbial secondary metabolites, the extract of Nocardia nova JCM 6044 was found to be highly active. Bioassay-guided isolation led to the identification of three siderophores, nocardimicins G (1), H (2) and I (3). Their chemical structures were determined by spectroscopic analysis using NMR and MS. 1 and 2 inhibited the binding of tritium-labeled N-methylscopolamine to the muscarinic M3 receptor with Ki values of 0.44 microM and 0.37 microM, respectively, whereas 3 showed no inhibition at 10 microM. 1 and 2 also showed weak binding inhibitory activity to the M5 receptor but not to the M1, M2 and M4 receptors at 10 microM.
Volume 58(9)
Pages 566-72
Published 2005-9-1
DOI 10.1038/ja.2005.77
PMID 16320761
MeSH Hydroxamic Acids / isolation & purification Hydroxamic Acids / pharmacology Molecular Structure Muscarinic Antagonists / chemistry Muscarinic Antagonists / isolation & purification Muscarinic Antagonists / pharmacokinetics Muscarinic Antagonists / pharmacology Nocardia / chemistry* Oxazoles / isolation & purification Oxazoles / pharmacology Receptor, Muscarinic M3 / antagonists & inhibitors* Receptor, Muscarinic M3 / metabolism Siderophores / chemistry Siderophores / isolation & purification* Siderophores / pharmacology
IF 2.668
Times Cited 11
WOS Category PHARMACOLOGY & PHARMACY BIOTECHNOLOGY & APPLIED MICROBIOLOGY IMMUNOLOGY MICROBIOLOGY
Resource
Pathogenic microorganisms JCM 6044