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本文引用的文献

1
Diurnal rhythmicity in glucose uptake is mediated by temporal periodicity in the expression of the sodium-glucose cotransporter (SGLT1).葡萄糖摄取的昼夜节律由钠-葡萄糖协同转运蛋白（SGLT1）表达的时间周期性介导。
Surgery. 2008 Jun;143(6):813-8. doi: 10.1016/j.surg.2008.03.018.
2
Capsaicin-sensitive vagal afferents modulate posttranscriptional regulation of the rat Na+/glucose cotransporter SGLT1.辣椒素敏感的迷走神经传入纤维调节大鼠钠/葡萄糖协同转运蛋白SGLT1的转录后调控。
Am J Physiol Gastrointest Liver Physiol. 2008 Apr;294(4):G1078-83. doi: 10.1152/ajpgi.00591.2007. Epub 2008 Feb 28.
3
The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability.肠道和肝脏中药物转运的基础知识：限制药物吸收和生物利用度的外排蛋白。
Eur J Pharm Sci. 2004 Jan;21(1):25-51. doi: 10.1016/j.ejps.2003.07.003.
4
ABC of oral bioavailability: transporters as gatekeepers in the gut.口服生物利用度基础：转运体作为肠道的守门人
Gut. 2003 Dec;52(12):1788-95. doi: 10.1136/gut.52.12.1788.
5
P-glycoprotein-mediated intestinal and biliary digoxin transport in humans.P-糖蛋白介导的人体肠道和胆汁中地高辛的转运
Clin Pharmacol Ther. 2003 Mar;73(3):223-31. doi: 10.1067/mcp.2003.27.
6
Diurnal rhythm of H+-peptide cotransporter in rat small intestine.大鼠小肠中氢离子-肽共转运体的昼夜节律
Am J Physiol Gastrointest Liver Physiol. 2002 Jul;283(1):G57-64. doi: 10.1152/ajpgi.00545.2001.
7
Correlation of gene expression of ten drug efflux proteins of the ATP-binding cassette transporter family in normal human jejunum and in human intestinal epithelial Caco-2 cell monolayers.正常人类空肠及人肠上皮Caco-2细胞单层中ATP结合盒转运体家族十种药物外排蛋白的基因表达相关性
J Pharmacol Exp Ther. 2001 Oct;299(1):164-70.
8
Diurnal rhythmicity in intestinal SGLT-1 function, V(max), and mRNA expression topography.肠道SGLT-1功能、V(max)及mRNA表达拓扑结构的昼夜节律性。
Am J Physiol Gastrointest Liver Physiol. 2001 Feb;280(2):G209-15. doi: 10.1152/ajpgi.2001.280.2.G209.
9
Functional polymorphisms of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo.人类多药耐药基因的功能多态性：多个序列变异以及一个等位基因与体内P-糖蛋白表达和活性的相关性
Proc Natl Acad Sci U S A. 2000 Mar 28;97(7):3473-8. doi: 10.1073/pnas.97.7.3473.
10
Circadian periodicity of intestinal Na+/glucose cotransporter 1 mRNA levels is transcriptionally regulated.肠道钠/葡萄糖协同转运蛋白1 mRNA水平的昼夜节律性是由转录调控的。
J Biol Chem. 1998 Apr 17;273(16):9510-6. doi: 10.1074/jbc.273.16.9510.

空肠药物转运体转录的昼夜节律性。

Diurnal rhythmicity in the transcription of jejunal drug transporters.

作者信息

Stearns Adam T, Balakrishnan Anita, Rhoads David B, Ashley Stanley W, Tavakkolizadeh Ali

机构信息

Department of Surgery, Brigham & Women's Hospital/Harvard Medical School, 75 Francis Street, Boston, MA 02115, USA.

出版信息

J Pharmacol Sci. 2008 Sep;108(1):144-8. doi: 10.1254/jphs.08100sc. Epub 2008 Sep 11.

DOI:10.1254/jphs.08100sc
PMID:18787306
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4109053/
Abstract

Intestinal drug efflux proteins play a major role in the pharmacokinetics of many drugs. We assessed diurnal rhythmicity in the expression of ten major drug transporters. We acquired male Sprague-Dawley rats and harvested jejunal mucosa at 3-h intervals across a 24-h period. qPCR was performed for ten transporters: Mdr1, Mdr3, Mrp1 - 3, Mct1, Brcp, Pept1, Octn2, and Oatp-b. Rhythmicity was assessed with the cosinor procedure. Diurnal rhythmicity was observed for Mdr1, Mct1, Mrp2, Pept1, and Bcrp (1.6 - 5.4-fold-changes). Acrophases occurred during fasting hours. We conclude that many drug transporters display profound diurnal rhythms in transcription, which may underlie diurnal rhythms in drug pharmacokinetics.

摘要

肠道药物外排蛋白在许多药物的药代动力学中起主要作用。我们评估了十种主要药物转运蛋白表达的昼夜节律性。我们获取了雄性Sprague-Dawley大鼠，并在24小时内每隔3小时采集空肠黏膜。对十种转运蛋白进行了qPCR检测：Mdr1、Mdr3、Mrp1 - 3、Mct1、Brcp、Pept1、Octn2和Oatp-b。采用余弦分析程序评估节律性。观察到Mdr1、Mct1、Mrp2、Pept1和Bcrp有昼夜节律性（变化倍数为1.6 - 5.4倍）。峰值相位出现在禁食期间。我们得出结论，许多药物转运蛋白在转录过程中表现出显著的昼夜节律，这可能是药物药代动力学昼夜节律的基础。