Direct measurement of pyrimidine C6-hydrate stability

Direct measurement of pyrimidine C6-hydrate stability
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DOI:
10.1016/s0968-0896(01)00137-7
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发表时间:
2001-09-01
影响因子:
3.5
通讯作者:
Greenberg, MM
Greenberg, MM
中科院分区:
医学3区
文献类型:
--
作者:
Carter, KN;Greenberg, MM

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嘧啶 C6 水合物通过紫外线照射产生,静置后脱水。这些化合物的稳定性与其遗传毒性有直接关系。通过HPLC直接测量5,6-二氢-5-羟基胸苷(6)和5,6-二氢-5-羟基-2'-脱氧尿苷(9)的5'-苯甲酰化衍生物的消除速率常数。脱水速率常数从 pH 6.0 增加到 8.0。 6和9在pH 7.4和37℃下的半衰期分别为46.5和24.4小时。即使在 90 摄氏度下加热,也未观察到去糖基化。这些观察结果证实了嘧啶水合物的寿命足够长,可以对生物系统产生重大影响。 (C) 2001 Elsevier Science Ltd. 保留所有权利。
Pyrimidine C6-hydrates are produced via UV-irradiation and undergo dehydration upon standing. The stability of these compounds has a direct bearing on their genotoxicity. The rate constants for elimination from 5 ' -benzyoylated derivatives of 5,6-dihydro-5-hydroxythymidine (6) and 5,6-dihydro-5-hydroxy-2 ' -deoxyuridine (9) were measured directly via HPLC. The rate constants for dehydration increase from pH 6.0 to 8.0. The half-lives for 6 and 9 at pH 7.4 and 37 degreesC are 46.5 and 24.4 h, respectively. Deglycosylation is not observed, even upon heating at 90 degreesC. These observations reinforce proposals that pyrimidine hydrates are sufficiently long-lived that they can exert significant effects on biological systems. (C) 2001 Elsevier Science Ltd. All rights reserved.