Abstract:
:The inhibitory effects of N-(4-hydroxyphenyl)retinamide (HPR) and its glucuronide derivative on the growth of MCF-7 human breast cancer cells in vitro were compared. The results indicate that the glucuronide had slightly greater potency and much less cytotoxicity than the free retinoid. At a concentration of 10(-6) M, HPR inhibited MCF-7 cell growth by approximately 25%, whereas an equimolar concentration of the glucuronide caused a 40% growth inhibition. Higher concentrations of HPR were highly cytotoxic. At a 10(-5) M concentration of the glucuronide, cell viability was 77%, and 65% of the cells were able to resume growth. On the other hand, at 10(-5) M HPR, cell viability dropped to 49%, and only 15% of the cells were capable of resuming growth. The lower cytotoxicity and higher potency of the retinoid glucuronide compared to the parent retinamide suggest that the conjugate may have a chemotherapeutic advantage over the parent compound. The apparent higher efficacy of HPR in combination with glucarate (GT) compared to the single agents could be due to increased net formation of HPR glucuronide conjugate following conversion of GT to the beta-glucuronidase inhibitor, D-glucaro-1,4-lactone. However, HPLC analysis of the cell metabolites did not show any detectable levels of the retinoid glucuronide upon treatment of MCF-7 cells with HPR and GT.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Bhatnagar R,Abou-Issa H,Curley RW Jr,Koolemans-Beynen A,Moeschberger ML,Webb TEdoi
10.1016/0006-2952(91)90563-ksubject
Has Abstractpub_date
1991-05-15 00:00:00pages
1471-7issue
10eissn
0006-2952issn
1873-2968pii
0006-2952(91)90563-Kjournal_volume
41pub_type
杂志文章abstract::The effect of the bisdioxopiperazine cardioprotector ICRF-187 (ADR-529, dexrazoxan) on drug-induced DNA damage and cytotoxicity was studied. Using alkaline elution assays, ICRF-187 in a dose-dependent manner inhibited the formation of DNA single strand breaks (SSBs) as well as DNA-protein cross-links induced by drugs ...
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doi:10.1016/0006-2952(93)90514-w
更新日期:1993-08-03 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(84)90320-4
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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journal_title:Biochemical pharmacology
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pub_type: 杂志文章
doi:10.1016/0006-2952(92)90039-l
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journal_title:Biochemical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1999-04-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章,评审
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更新日期:2017-10-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:1994-06-01 00:00:00
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pub_type: 杂志文章
doi:10.1016/j.bcp.2007.02.009
更新日期:2007-06-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:1994-10-07 00:00:00
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更新日期:2010-10-15 00:00:00
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pub_type: 杂志文章
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更新日期:1986-09-15 00:00:00
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更新日期:2014-05-15 00:00:00
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pub_type: 杂志文章
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更新日期:1986-12-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(89)90238-4
更新日期:1989-03-01 00:00:00
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pub_type: 杂志文章
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:2009-09-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:2020-11-06 00:00:00
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更新日期:2011-05-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:1989-10-01 00:00:00
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更新日期:2008-04-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:2000-06-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:2004-05-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:1984-12-01 00:00:00
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更新日期:1999-07-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:2014-03-15 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/j.bcp.2005.07.001
更新日期:2005-10-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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更新日期:2007-05-15 00:00:00