TETRONOTHIODIN, A NOVEL CHOLECYSTOKININ TYPE-B RECEPTOR ANTAGONIST PRODUCED BY Streptomyces sp. NR0489 II. ISOLATION, CHARACTERIZATION AND BIOLOGICAL ACTIVITIES

A novel cholecystokinin type-B receptor antagonist named tetronothiodin has been isolated by column chromatography and preparative HPLC from the fermentation broth of Streptomyces sp. NR0489. Tetronothiodin inhibited the binding of CCK8 (C-terminal octapeptide of cholecystokinin) to rat cerebral cor...

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Published inJournal of antibiotics Vol. 46; no. 1; pp. 11 - 17
Main Authors OHTSUKA, TATSUO, KOTAKI, HIROMICHI, NAKAYAMA, NOBORU, ITEZONO, YOSHIKO, SHIMMA, NOBUO, KUDOH, TSUTOMU, KUWAHARA, TOSHIKAZU, ARISAWA, MIKIO, YOKOSE, KAZUTERU, SETO, HARUO
Format Journal Article
LanguageEnglish
Published Tokyo JAPAN ANTIBIOTICS RESEARCH ASSOCIATION 01.01.1993
Japan Antibiotics Research Association
Subjects
Animals
Biological and medical sciences
Calcium - metabolism
Cell Line
Cerebral Cortex - drug effects
Chromatography, Gel
Chromatography, High Pressure Liquid
Furans - chemistry
Furans - isolation & purification
Furans - pharmacology
Magnetic Resonance Spectroscopy
Medical sciences
Miscellaneous
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pancreas - drug effects
Pharmacology. Drug treatments
Pituitary Gland, Anterior - drug effects
Rats
Receptors, Cholecystokinin - antagonists & inhibitors
Sincalide - antagonists & inhibitors
Streptococcus - chemistry
Streptomyces
Thiophenes - chemistry
Thiophenes - isolation & purification
Thiophenes - pharmacology
Actinomycetales
Cholecystokinine receptor B
Streptomycetaceae
Streptomyces
Bacteria
Isolation
Actinomycetes
Antagonist
In vitro
Biological activity
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Summary:A novel cholecystokinin type-B receptor antagonist named tetronothiodin has been isolated by column chromatography and preparative HPLC from the fermentation broth of Streptomyces sp. NR0489. Tetronothiodin inhibited the binding of CCK8 (C-terminal octapeptide of cholecystokinin) to rat cerebral cortex membranes (CCK type-B receptors) with an IC50 of 3.6nM, whereas it did not inhibit CCK8 binding to rat pancreatic membranes (CCK type-A receptors). It also inhibited CCK8 induced Ca2+ mobilization in GH3 cells, a rat anterior pituitary cell line, but was without effect on the basal cytosolic Ca2+ concentration. This finding indicated tetronothiodin was an antagonist of CCK type-B receptors.
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ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.46.11