Abstract:
:2'-Chloroflavone (CF) and 4'-CF were studied as inducers of cytochrome P-450-mediated monooxygenases in rat hepatic microsomes by comparison with phenobarbital (PB) and 3-methylcholanthrene (MC). As a result of interaction with the substrate 7-ethoxycoumarin (7-EC), 2'-CF-induced microsomes showed a difference spectrum different from usual type I, whereas 4'-CF-induced microsomes showed a typical type I spectrum. 2'-CF-induced microsomes increased the Vmax of aminopyrine (AM) N-demethylase activity about 1.6-fold while not affecting the apparent Km value. In contrast, 4'-CF-induced microsomes decreased the Km of 7-EC O-deethylase activity to about one fourth while significantly increasing the Vmax value. All the activities of AM N-demethylase, 7-EC O-deethylase and 6,7-dimethoxycoumarin O-demethylase in 2'-CF-induced microsomes were inhibited strongly by metyrapone and SKF 525-A, and significantly by diphenhydramine. The three enzyme activities in 4'-CF-induced microsomes were inhibited markedly by alpha-naphthoflavone and significantly by 2-bromo-4'-nitroacetophenone. These results further support the previous proposal that 2'-CF is a PB-type inducer of cytochrome P-450 while 4'-CF is a MC-type inducer.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Kato S,Yamamoto Kdoi
10.1248/bpb.16.90subject
Has Abstractpub_date
1993-01-01 00:00:00pages
90-2issue
1eissn
0918-6158issn
1347-5215journal_volume
16pub_type
杂志文章abstract::We examined the action mechanism of oleanolic acid 3-O-monodesmoside, momordin Ic (1), and oleanolic acid 3-O-glucuronide (2) for the inhibitory effect on the increase in serum glucose levels in oral glucose-loaded rats. Although 1 and 2 dose-dependently inhibited the increase in serum glucose levels in oral glucose-l...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2005-04-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:1998-06-01 00:00:00
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更新日期:2004-07-01 00:00:00
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pub_type: 杂志文章
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更新日期:1993-12-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2009-10-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2001-09-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b15-00997
更新日期:2016-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2003-10-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.1262
更新日期:2006-06-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2017-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.26.256
更新日期:2003-02-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b12-00228
更新日期:2012-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b20-00101
更新日期:2020-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:1995-05-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:1997-05-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2000-09-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2001-04-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.997
更新日期:1994-08-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:1995-12-01 00:00:00
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pub_type: 杂志文章
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2007-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.582
更新日期:1999-06-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b20-00631
更新日期:2020-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2002-03-01 00:00:00