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15-(邻-123/131I-苯基)-十五烷酸(oPPA)和15-(对-123/131I-苯基)-十五烷酸(pPPA)在动物和人体中的示踪动力学

Tracer kinetics of 15-(ortho-123/131I-phenyl)-pentadecanoic acid (oPPA) and 15-(para-123/131I-phenyl)-pentadecanoic acid (pPPA) in animals and man.

作者信息

Kaiser K P, Geuting B, Grossmann K, Vester E, Lösse B, Antar M A, Machulla H J, Feinendegen L E

机构信息

Institute of Medicine, Nuclear Research Center, Jülich, FRG.

出版信息

J Nucl Med. 1990 Oct;31(10):1608-16.

PMID:2213181
Abstract

The human myocardium retains oPPA as opposed to pPPA. Therefore turnover of oPPA was compared with that of pPPA in rat hearts and in man, the latter by using substrates double-labeled with 123/131I and 14C. Moreover, substrate binding to coenzyme-A was tested in vitro. In rats, oPPA remained mainly in the pool of free fatty acids, as opposed to pPPA, which was metabolized by mitochondrial beta-oxidation. Binding to coenzyme-A at maximum was 62% for oPPA, 81% for pPPA and 90% for palmitic acid. In man, after i.v. and intracoronary injection of double-labeled oPPA, the two radionuclides reappeared together in venous blood and in coronary sinus respectively, in an unchanged ratio but at a significantly lower rate than with pPPA. It can be concluded that oPPA is bound to coenzyme-A and is retained in the cytosolic lipid pool, while pPPA is metabolized by mitochondrial beta-oxidation. A dual-tracer application of oPPA and pPPA has the potential of being a specific probe for the function of the carnitine shuttle.

摘要

与对羟基苯丙酮酸(pPPA)不同,人心肌保留了邻羟基苯丙酮酸(oPPA)。因此,在大鼠心脏和人体中比较了oPPA与pPPA的周转情况,在人体中使用了用123/131I和14C双标记的底物。此外,还在体外测试了底物与辅酶A的结合情况。在大鼠中,与通过线粒体β氧化代谢的pPPA不同,oPPA主要保留在游离脂肪酸池中。oPPA与辅酶A的最大结合率为62%,pPPA为81%,棕榈酸为90%。在人体中,静脉内和冠状动脉内注射双标记的oPPA后,两种放射性核素分别在静脉血和冠状窦中一起重新出现,比例不变,但速率明显低于pPPA。可以得出结论,oPPA与辅酶A结合并保留在细胞质脂质池中,而pPPA通过线粒体β氧化代谢。oPPA和pPPA的双示踪剂应用有可能成为肉碱穿梭功能的特异性探针。

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