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氨肽酶抑制剂贝他定的立体异构体在体内引起的不同酶促振荡。

Different enzymatic oscillations in vivo caused by the stereoisomers of an aminopeptidase inhibitor, bestatin.

作者信息

Aoyagi T, Wada T, Yamamoto K, Kojima F, Nagai M, Harada S, Umezawa H

出版信息

J Appl Biochem. 1984 Aug;6(4):212-21.

PMID:6520072
Abstract

The present study was undertaken to compare the enzymatic oscillations induced in three major organs, spleen, kidney, and liver, of mice by the active and inactive forms of an aminopeptidase inhibitor, bestatin. Although bestatin caused sine curve-type oscillations of enzymatic activities in spleen and kidney, its isomer, possessing no enzyme-inhibiting actions and no biological actions, did not show any typical enzymatic changes. Such typical oscillations were not elicited by either one of those two agents in liver, in spite of the apparent difference in the type of oscillations induced by them in this organ. These observations were taken to indicate that the enzymatic oscillations in vivo caused by bestatin are closely related to its aminopeptidase-inhibiting actions seen in vitro and that the immunomodifying actions of this agent are based on its effects on enzymes sensitive to it, possibly involving immunoresponsive cells.

摘要

本研究旨在比较氨肽酶抑制剂贝司他汀的活性形式和非活性形式在小鼠的三种主要器官(脾脏、肾脏和肝脏)中诱导的酶活性振荡。尽管贝司他汀在脾脏和肾脏中引起酶活性的正弦曲线型振荡,但其异构体不具有酶抑制作用和生物学作用,未表现出任何典型的酶变化。尽管这两种药物在肝脏中诱导的振荡类型存在明显差异,但它们均未在肝脏中引发这种典型振荡。这些观察结果表明,贝司他汀在体内引起的酶活性振荡与其在体外的氨肽酶抑制作用密切相关,并且该药物的免疫调节作用基于其对敏感酶的影响,可能涉及免疫反应细胞。

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