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大鼠肠黏膜中脑啡肽样寡肽转运的研究。

Studies on the transport of enkephalin-like oligopeptides in rat intestinal mucosa.

作者信息

Kerchner G A, Geary L E

出版信息

J Pharmacol Exp Ther. 1983 Jul;226(1):33-8.

PMID:6345754
Abstract

Transport of [D-Ala2, D-Leu5]enkephalin (DADLE(], Tyr-D-Ala-Gly-Phe (TDAGP) and tyrosine into rat jejunum mucosal cells was investigated in vitro. Active transport of either the pentapeptide (DADLE) or the tetrapeptide (TDAGP) into jejunal villi was not detected. Because substantial degradation of these peptides occurred during incubation, the proteolytic enzyme inhibitors, bestatin (30 microM) or D-phenylalanine (20 mM), were added during uptake studies of DADLE or TDAGP, respectively. The presence of these inhibitors significantly reduced degradation of the oligopeptides; however, no accumulation of peptides occurred in the mucosal tissue. Tyrosine was actively transported by the jejunum mucosal cells demonstrating the viability of the transport mechanisms of this in vitro preparation. The results suggest that there are no active transport systems for enkephalin-like oligopeptides.

摘要

在体外研究了[D-丙氨酸2,D-亮氨酸5]脑啡肽(DADLE)、酪氨酰-D-丙氨酸-甘氨酸-苯丙氨酸(TDAGP)和酪氨酸进入大鼠空肠黏膜细胞的转运情况。未检测到五肽(DADLE)或四肽(TDAGP)向空肠绒毛的主动转运。由于在孵育过程中这些肽发生了大量降解,因此在分别进行DADLE或TDAGP摄取研究时,加入了蛋白水解酶抑制剂贝司他汀(30微摩尔)或D-苯丙氨酸(20毫摩尔)。这些抑制剂的存在显著降低了寡肽的降解;然而,黏膜组织中未出现肽的积累。酪氨酸可被空肠黏膜细胞主动转运,这表明该体外制备物的转运机制具有活性。结果表明不存在脑啡肽样寡肽的主动转运系统。

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