- 【Updated on May 12, 2025】 Integration of CiNii Dissertations and CiNii Books into CiNii Research
- Trial version of CiNii Research Automatic Translation feature is available on CiNii Labs
- Suspension and deletion of data provided by Nikkei BP
- Regarding the recording of “Research Data” and “Evidence Data”
Biotransformation of coumarin derivatives (2). Oxidative metabolism of 7-alkoxycoumarin by microsomal enzymes and a simple assay procedure for 7-alkoxycoumarin O-dealkylase.
-
- MATSUBARA Takashi
- Shionogi Research Laboratories, Shionogi & Co., Ltd.
-
- OTSUBO Shigemi
- Shionogi Research Laboratories, Shionogi & Co., Ltd.
-
- YOSHIHARA Emiko
- Shionogi Research Laboratories, Shionogi & Co., Ltd.
-
- TOUCHI Akira
- Shionogi Research Laboratories, Shionogi & Co., Ltd.
Bibliographic Information
- Other Title
-
- Biotransformation of Coumarin Derivatives-2-Oxidative Metabolism of 7-Alkoxycoumarin by Microsomal Enzymes and а Simple Assay Procedure for 7-Alkoxycoumarin 0-Dealkylase
- Biotransformation of Coumarin Derivativ
Search this article
Description
The in vitro biotransformation of 7-alkoxycoumarin by rat liver microsomes was studied to develop a simple and accurate assay procedure for 7-alkoxycoumarin O-dealkylase. 7-Alkoxycoumarin was converted to the O-dealkylated metabolite, 7-hydroxycoumarin, by aerobic incubation of the parent compound with microsomes and NADPH, but the decreased amount of 7-alkoxycoumarin in the reaction mixture was several times higher than that of the 7-hydroxycoumarin produced during the incubation. The thin-layer chromatogram of the ether extractable metabolites in the reaction mixture showed the existence of several fluorescent metabolites including 7-hydroxycoumarin. Fluorescent properties of the parent compound, 7-alkoxycoumarin, and most of the metabolites differed from that of 7-hydroxycoumarin, but the reaction cofactor, NADPH, showed similar properties. Treatment of the reaction mixture with perchloric acid resulted in conversion of NADPH to the non-fluorescent form without any effect upon the fluorescent properties of 7-hydroxycoumarin and its related compounds. Based on these properties, an improved and simple in vitro fluorometric assay of the O-dealkylation of 7-alkoxycoumarin was developed. The method is applicable to routine determination of O-dealkylase activity in both isolated microsomes and whole homogenate. Species differences in the substrate specificity of the O-dealkylation reaction and in the responsiveness of animals to the inducer were observed even with use of the liver homogenate obtained from untreated and phenobarbital- or β-naphthoflavone-pretreated animals, similar to what was observed with the microsomal system.
Journal
-
- The Japanese Journal of Pharmacology
-
The Japanese Journal of Pharmacology 33 (1), 41-56, 1983
The Japanese Pharmacological Society
- Tweet
Keywords
Details 詳細情報について
-
- CRID
- 1390282679263595904
-
- NII Article ID
- 130000835320
-
- NII Book ID
- AA00691188
-
- COI
- 1:CAS:528:DyaL3sXhtl2gu7Y%3D
-
- ISSN
- 13473506
- 00215198
- http://id.crossref.org/issn/00215198
-
- NDL BIB ID
- 2623195
-
- PubMed
- 6603543
-
- Text Lang
- en
-
- Article Type
- journal article
-
- Data Source
-
- JaLC
- NDL Search
- Crossref
- PubMed
- CiNii Articles
-
- Abstract License Flag
- Disallowed