Identification of a Naturally Occurring Quinazolin-4(3H)-one Firefly Luciferase Inhibitor

A prefractionated Streptomyces-derived extract was initially identified as being active using a luciferase-based AMP-activated protein kinase (AMPK) assay. Bioassay-guided fractionation led to the isolation of the new compound quinazolin-4(3H)-one (1) as the active component. However, 1 was shown to...

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Veröffentlicht in:	Journal of natural products (Washington, D.C.) D.C.), 2011-06, Vol.74 (6), p.1500-1502
Hauptverfasser:	Somanadhan, Brinda, Leong, Chungyan, Whitton, Stephen R, Ng, Siewbee, Buss, Antony D, Butler, Mark S
Format:	Artikel
Sprache:	eng
Schlagworte:	AMP-Activated Protein Kinases - metabolism Analytical, structural and metabolic biochemistry Animals Biological and medical sciences Biological Products - chemistry Biological Products - isolation & purification Biological Products - pharmacology Fundamental and applied biological sciences. Psychology Luciferases, Firefly - antagonists & inhibitors Luciferases, Firefly - metabolism Molecular Structure Non peptidic neurotransmitters, polyamines Other biological molecules Quinazolinones - chemistry Quinazolinones - isolation & purification Quinazolinones - pharmacology Streptomyces - chemistry
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Zusammenfassung:	A prefractionated Streptomyces-derived extract was initially identified as being active using a luciferase-based AMP-activated protein kinase (AMPK) assay. Bioassay-guided fractionation led to the isolation of the new compound quinazolin-4(3H)-one (1) as the active component. However, 1 was shown to have potent firefly luciferase inhibitory activity with no effect on AMPK. This is the first report of a natural luciferase inhibitor.
ISSN:	0163-3864 1520-6025
DOI:	10.1021/np1006179