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海藻糖酶抑制剂曲二唑醇在飞蝗(Locusta migratoria)中的命运和效应。

Fate and effects of the trehalase inhibitor trehazolin in the migratory locust (Locusta migratoria).

机构信息

Institute of Zoology, Molecular Physiology, Johannes Gutenberg-University, D-55099 Mainz, Germany.

出版信息

J Insect Physiol. 2010 Jun;56(6):567-74. doi: 10.1016/j.jinsphys.2009.11.021. Epub 2009 Dec 10.

Abstract

Trehalose is the main haemolymph sugar in many insect species. To be utilized trehalose must be hydrolysed into its glucose units by trehalase (EC 3.2.1.28). Inhibitors of trehalase have attracted interest as possible pesticides and tools for studying the regulation of trehalose metabolism in insects. To make full use of these inhibitors requires knowledge of their fate and effects in vivo. To this end we have measured trehazolin in locusts using a method based on the specific inhibition of a trehalase preparation. After injection of 20 microg, trehazolin decreased in haemolymph with a half-life of 2.6 days and after 10 days almost 95% had disappeared. Trehazolin did not reach the intracellular water space of locust tissues, but appeared with full inhibitory potency in locust faeces, suggesting that it was not metabolized, but quantitatively eliminated via the gut. Haemolymph trehalose increased transiently upon trehazolin injection, it was maximal after 3 days, then decreased and reached control level after 10 days. Inhibition of flight muscle trehalase by trehazolin was prolonged and still conspicuous 21 days post injection, suggesting that trehazolin inhibits trehalase activity irreversibly in vivo and that recovery requires de novo enzyme synthesis.

摘要

海藻糖是许多昆虫物种血淋巴中的主要糖。要利用海藻糖,必须通过海藻糖酶(EC 3.2.1.28)将其水解成葡萄糖单位。海藻糖酶抑制剂作为可能的杀虫剂和研究昆虫中海藻糖代谢调节的工具引起了人们的兴趣。要充分利用这些抑制剂,需要了解它们在体内的命运和作用。为此,我们使用基于对海藻糖酶制剂的特异性抑制的方法测量了蝗虫中的 trehazolin。在注射 20μg 后,trehazolin 在血淋巴中的半衰期为 2.6 天,10 天后几乎 95%消失。trehazolin 未到达蝗虫组织的细胞内水空间,但在蝗虫粪便中以完全抑制效力出现,表明它没有被代谢,而是通过肠道被定量消除。在注射 trehazolin 后,血淋巴海藻糖短暂增加,在 3 天后达到最大值,然后下降并在 10 天后达到对照水平。飞行肌海藻糖酶被 trehazolin 抑制的时间延长,在注射后 21 天仍很明显,这表明 trehazolin 在体内不可逆地抑制海藻糖酶活性,并且恢复需要新酶的合成。

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