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豚鼠尿液中17-羟基皮质类固醇葡萄糖醛酸苷作为水杨酰胺葡萄糖醛酸化指标的意义。

Significance of 17-hydroxycorticosteroid glucuronide in urine as an index of salicylamide glucuronidation in guinea pigs.

作者信息

Sawada Y, Hayashi M, Awazu S, Hanano M

出版信息

J Pharmacobiodyn. 1981 Nov;4(11):893-900. doi: 10.1248/bpb1978.4.893.

Abstract

The glucuronidation of 17-hydroxycorticosteroids (17-OHCS) and its effectiveness as an index of salicylamide (SAM) glucuronidation were examined in guinea pigs, the same cortisol type animals as man, treated with carbon tetrachloride (CCl4), D-galactosamine, phenobarbital, D,L-ethionine and alloxan. There was not a statistically significant correlation between the plasma clearance of SAM glucuronidation (CLglu) and the urinary excretion ratio of 17-OHCS glucuronide to total 17-OHCS in the intact, and CCl4, D-galactosamine, alloxan and D,L-ethionine treated guinea pigs (r = 0.158). However, there was a statistically significant correlation between the CLglu and the clearance of 17-OHCS glucuronidation obtained as urinary 17-OHCS glucuronide/plasma cortisol concentration (r = 0.738, p less than 0.1). It was proposed that the clearance of 17-OHCS glucuronide metabolized from endogenous cortisol could be used as an index to assess the drug glucuronidation activity.

摘要

在豚鼠(与人类同属皮质醇类型动物)中,研究了17-羟皮质类固醇(17-OHCS)的葡萄糖醛酸化及其作为水杨酰胺(SAM)葡萄糖醛酸化指标的有效性。这些豚鼠分别用四氯化碳(CCl4)、D-半乳糖胺、苯巴比妥、D,L-乙硫氨酸和四氧嘧啶进行处理。在完整的、经CCl4、D-半乳糖胺、四氧嘧啶和D,L-乙硫氨酸处理的豚鼠中,SAM葡萄糖醛酸化的血浆清除率(CLglu)与17-OHCS葡萄糖醛酸苷与总17-OHCS的尿排泄率之间没有统计学上的显著相关性(r = 0.158)。然而,CLglu与以尿17-OHCS葡萄糖醛酸苷/血浆皮质醇浓度表示的17-OHCS葡萄糖醛酸化清除率之间存在统计学上的显著相关性(r = 0.738,p < 0.1)。有人提出,内源性皮质醇代谢产生的17-OHCS葡萄糖醛酸苷的清除率可用作评估药物葡萄糖醛酸化活性的指标。

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