BIOLOGICAL EFFECTS OF ACETOMYCIN: II. INACTIVATION BY ESTERASES IN VITRO

Acetomycin has antitumor activity in vitro but not in vitro. HCT-8 human colon adenocarcinoma assays in the presence of a drug metabolizing system (rat liver S9 fraction) demonstrated that liver enzymes inactivated acetomycin. The structure of acetomycin suggested that an esterase could be the key i...

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Bibliographic Details
Published in:Journal of antibiotics 1987/01/25, Vol.40(1), pp.77-80
Main Authors: MAMBER, S. W., MITULSKI, J. D., BORONDY, P. E., TUNAC, J. B.
Format: Article
Language:English
Subjects:
Adenocarcinoma
Animals
Anti-Bacterial Agents - pharmacology
Antineoplastic agents
Biological and medical sciences
Biotransformation
Cell Line
Chemotherapy
Colonic Neoplasms
Esterases - metabolism
Furans - metabolism
Furans - pharmacology
Humans
Kinetics
Liver - enzymology
Medical sciences
Microsomes, Liver - metabolism
Mixed Function Oxygenases - metabolism
Pharmacology. Drug treatments
Rats
Swine
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Summary:Acetomycin has antitumor activity in vitro but not in vitro. HCT-8 human colon adenocarcinoma assays in the presence of a drug metabolizing system (rat liver S9 fraction) demonstrated that liver enzymes inactivated acetomycin. The structure of acetomycin suggested that an esterase could be the key inactivating enzyme. Assays with porcine liver esterase (EC 3.1.1.1) showed that this enzyme rapidly abolishes the activity of acetomycin against HCT-8 cells. The potential utility of acetomycin as an antitumor agent thus depends on finding a means of preventing esterase inactivation.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.40.77