Sawada Y, Hayashi M, Awazu S, Hanano M
J Pharmacobiodyn. 1981 Nov;4(11):893-900. doi: 10.1248/bpb1978.4.893.
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.
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。