Abstract：
:The mechanism of action of the cyclopentenyl analogue of 3-deazaadenosine (3-deazaneplanocin A or c3Nep) was investigated in the human colon carcinoma cell line HT-29. Upon exposure of cells for 24 hr to 3-deazaneplanocin A (c3Nep), neplanocin A (Nep) or 3-deazaaristeromycin (c3Ari), significant toxicity was noted only for Nep, wherein an 87% reduction in viability was produced at a 100 microM concentration. c3Nep and c3Ari at 100 microM reduced viability by 34 and 21%, respectively. Intracellular levels of S-adenosylhomocysteine (AdoHcy) were elevated by a 24-hr exposure to 100 microM c3Nep, Nep and c3Ari and were 120, 75 and 25 pmoles/10(6) cells respectively. Only Nep was metabolized to an S-adenosylmethionine-like metabolite, and its formation was dose-related to its cytotoxicity. The t1/2 for the disappearance of elevated levels of AdoHcy following drug removal was 1.6 to 2.5 hr for all drugs. rRNA and tRNA methylation was inhibited significantly by Nep, but c3Nep and c3Ari inhibited tRNA methylation but not rRNA methylation to a lesser degree. These results demonstrate that c3Nep is a potent inhibitor of AdoHcy synthesis with a low degree of cytotoxicity.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Glazer RI,Knode MC,Tseng CK,Haines DR,Marquez VEdoi
10.1016/0006-2952(86)90774-4subject
Has Abstractpub_date
1986-12-15 00:00:00pages
4523-7issue
24eissn
0006-2952issn
1873-2968pii
0006-2952(86)90774-4journal_volume
35pub_type
杂志文章abstract：:Incubation of rat peritoneal mast cells with hydrogen peroxide results in a marked release of histamine. Maximal release is observed with 0.05-0.1 mM H(2)O(2), but higher concentrations of H(2)O(2) instead suppresses the release. Histamine release starts after about 2 min of lag time and reaches a plateau in about 10 ...
journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(80)90550-x
更新日期：1980-03-01 00:00:00
abstract：:In this study we compared two methods, electron spin resonance (ESR) spectroscopy and high performance liquid chromatography (HPLC), which are currently used to detect directly hydroxyl radical (OH.) formation in the ischemic and reperfused heart. Isolated buffer-perfused rat hearts were subjected to 30 min of normoth...
journal_title：Biochemical pharmacology
pub_type： 杂志文章
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(99)00008-8
更新日期：1999-05-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(84)90364-2
更新日期：1984-01-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(95)00265-2
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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pub_type： 杂志文章
doi：10.1016/0006-2952(87)90141-9
更新日期：1987-07-01 00:00:00
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pub_type： 杂志文章
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更新日期：2001-09-15 00:00:00
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更新日期：2003-11-01 00:00:00
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pub_type： 杂志文章
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更新日期：2016-02-01 00:00:00
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pub_type： 杂志文章
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更新日期：2017-08-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90052-9
更新日期：1987-05-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2006.03.026
更新日期：2006-04-18 00:00:00
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pub_type： 杂志文章
doi：10.1016/0006-2952(96)00476-5
更新日期：1996-10-25 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90091-8
更新日期：1987-04-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(94)00401-3
更新日期：1995-01-18 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2004.01.017
更新日期：2004-05-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(03)00149-7
更新日期：2003-06-15 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：2017-04-01 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：1994-02-11 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(94)90199-6
更新日期：1994-10-18 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(97)82443-4
更新日期：1997-05-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2011.09.025
更新日期：2012-01-01 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：1990-02-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2014.10.008
更新日期：2014-12-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(81)90336-1
更新日期：1981-09-01 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：1992-03-03 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(82)90415-4
更新日期：1982-06-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2016.01.013
更新日期：2016-03-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(82)90105-8
更新日期：1982-07-01 00:00:00
