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抗癌药物6-MP对小白鼠血清损伤DNA的影响和EMX的效果
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作者 郭志宏 《青海畜牧兽医杂志》 2008年第4期19-20,共2页
5周龄的DDY系小白鼠40只,分无处理的对照组、抗癌药物6-巯基嘌呤(6-MP)腹腔注射组(6-MP组)、6-MtP+EMX饮水组(EMX饮水组)、6-MP+EMX腹腔注射组(EMX注射组)4个组,每组10只。3周后断头宰杀,采取血清测定各组小白鼠血清中8-羟基脱氧鸟苷(8-... 5周龄的DDY系小白鼠40只,分无处理的对照组、抗癌药物6-巯基嘌呤(6-MP)腹腔注射组(6-MP组)、6-MtP+EMX饮水组(EMX饮水组)、6-MP+EMX腹腔注射组(EMX注射组)4个组,每组10只。3周后断头宰杀,采取血清测定各组小白鼠血清中8-羟基脱氧鸟苷(8-OHdG)的含量。结果表明:抗癌药物6-MP能提高小白鼠血清中损伤DNA的含量,EMX饮水和腹腔注射能显著减少血清中8-羟基脱氧鸟苷(8-OHdG)的含量(P<0.0 1),有效抑制抗癌药物对机体DNA的损伤。 展开更多
关键词 抗癌药物 6硫基嘌呤 8-羟基脱氧鸟苷(8-OHdG) EMX
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9-乙酰氧基乙基-6-烷氨基-2-烷硫基嘌呤的合成及抗血小板凝集活性评估 被引量:6
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作者 何琦文 杜洪光 《有机化学》 SCIE CAS CSCD 北大核心 2012年第9期1678-1683,共6页
以2-氨基-6-氯嘌呤(1)为原料,与2-溴乙基乙酸酯反应得到9-乙酰氧基乙基-2-氨基-6-氯嘌呤(2);2经重氮-烷硫化得到9-乙酰氧基乙基-2-烷硫基-6-氯嘌呤(3);3经胺解反应得到14个未见报道的9-乙酰氧基乙基-6-烷氨基-2-烷硫基嘌呤化合物4.这些... 以2-氨基-6-氯嘌呤(1)为原料,与2-溴乙基乙酸酯反应得到9-乙酰氧基乙基-2-氨基-6-氯嘌呤(2);2经重氮-烷硫化得到9-乙酰氧基乙基-2-烷硫基-6-氯嘌呤(3);3经胺解反应得到14个未见报道的9-乙酰氧基乙基-6-烷氨基-2-烷硫基嘌呤化合物4.这些化合物的结构经IR,1H NMR,13C NMR及HRMS得到表征,同时进行了抗血小板凝集活性测试. 展开更多
关键词 6-烷胺基-2-烷硫基 合成 结构表征 抗血小板凝集
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On tolerability and safety of a maintenance treatment with 6-thioguanine in azathioprineor 6-mercaptopurine intolerant IBD patients 被引量:4
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作者 Nanne KH de Boer Luc JJ Derijks +10 位作者 Lennard PL Gilissen Daniel W Hommes Leopold GJB Engels Sybrand Y de Boer Gijsbertus den Hartog Piet M Hooymans Anja BU M(?)kelburg Barend D Westerveld Anton HJ Naber Chris JJ Mulder Dirk J de Jong 《World Journal of Gastroenterology》 SCIE CAS CSCD 2005年第35期5540-5544,共5页
AIM: To determine the tolerability and safety profile of a low-dose maintenance therapy with 6-TG in azathioprine (AZA) or 6-mercaptopurine (6-MP) intolerant inflammatory bowel disease (IBD) patients over a treatment ... AIM: To determine the tolerability and safety profile of a low-dose maintenance therapy with 6-TG in azathioprine (AZA) or 6-mercaptopurine (6-MP) intolerant inflammatory bowel disease (IBD) patients over a treatment period of at least 1 year.METHODS: Database analysis.RESULTS: Twenty out of ninety-five (21%) patients discontinued 6-TG (mean dose 24.6 mg; mean 6-TGN level 540 pmol/8×108 RBC) within 1 year. Reasons for discontinuation were GI complaints (31%), malaise (15%)and hepatotoxicity (15%). Hematological events occurred in three patients, one discontinued treatment. In the 6-TG-tolerant group, 9% (7/75) could be classified as hepatotoxicity. An abdominal ultrasound was performed in 54% of patients, one patient had splenomegaly.CONCLUSION: The majority of AZA or 6-MP-intolerant IBD patients (79%) is able to tolerate maintenance treatment with 6-TG (dosages between 0.3 and 0.4 mg/kg per d). 6-TG may still be considered as an escape maintenance immunosuppressant in this difficult to treat group of patients, taking into account potential toxicity and efficacy of other alternatives. The recently reported hepatotoxicity is worrisome and 6-TG should therefore be administered only in prospective trials. 展开更多
关键词 6-THIOGUANINE AZATHIOPRINE 6-MERCAPTOPURINE Crohn's disease Ulcerative colitis Side effects Tolerance SAFETY
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Efficacy of 6-mercaptopurine treatment after azathioprine hypersensitivity in inflammatory bowel disease 被引量:2
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作者 Ferenc Nagy Tamás Molnár +3 位作者 Zoltán Szepes Klaudia Farkas Tibor Nyári János Lonovics 《World Journal of Gastroenterology》 SCIE CAS CSCD 2008年第27期4342-4346,共5页
AIM:To investigate the efficacy of 6-mercaptopurine (6-MP) in cases of azathioprine (AZA) hypersensitivity in patients with inflammatory bowel disease. METHODS: Twenty nine previously confirmed Crohn’s disease (CD) (... AIM:To investigate the efficacy of 6-mercaptopurine (6-MP) in cases of azathioprine (AZA) hypersensitivity in patients with inflammatory bowel disease. METHODS: Twenty nine previously confirmed Crohn’s disease (CD) (n = 14) and ulcerative colitis (UC) (n = 15) patients with a known previous (AZA) hypersensitivity reaction were studied prospectively. The 6-MP doses were gradually increased from 0.5 up to 1.0-1.5 mg/kg per day. Clinical activity indicies (CDAI/CAI), laboratory variables and daily doses of oral 5-ASA, corticosteroids, and 6-MP were assessed before and in the first, sixth and twelfth months of treatment. RESULTS: In 9 patients, 6-MP was withdrawn in the first 2 wk due to an early hypersensitivity reaction. Medication was ineffective within 6 mo in 6 CD patients, and myelotoxic reaction was observed in two. Data were evaluated at the end of the sixth month in 12 (8 UC, 4 CD) patients, and after the first year in 9 (6 UC, 3 CD) patients. CDAI decreased transiently at the end of the sixth month, but no significant changes were observed in the CDAI or the CAI values at the end of the year. Leukocyte counts (P = 0.01), CRP (P = 0.02), and serum iron (P = 0.05) values indicated decreased inflammatory reactions, especially in the UC patients at the end of the year, making the possibility to taper oral steroid doses. CONCLUSION: About one-third of the previously AZA- intolerant patients showed adverse effects on taking 6MP. In our series, 20 patients tolerated 6MP, but it was ineffective in 8 CD cases, and valuable mainly in ulcerative colitis patients. 展开更多
关键词 Inflammatory bowel disease AZATHIOPRINE 6-MERCAPTOPURINE Side effects EFFICACY
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