Kaempferitrin inhibits GLUT4 translocation and glucose uptake in 3T3-L1 adipocytes

Biochemical and Biophysical Research Communications
C N Vishnu PrasadAnilkumar Gopalakrishnapillai

Abstract

Insulin stimulated GLUT4 (glucose transporter 4) translocation and glucose uptake in muscles and adipocytes is important for the maintenance of blood glucose homeostasis in our body. In this paper, we report the identification of kaempferitrin (kaempferol 3,7-dirhamnoside), a glycosylated flavonoid, as a compound that inhibits insulin stimulated GLUT4 translocation and glucose uptake in 3T3-L1 adipocytes. In the absence of insulin, we observed that addition of kaempferitrin did not affect GLUT4 translocation or glucose uptake. On the other hand, kaempferitrin acted as an inhibitor of insulin-stimulated GLUT4 translocation and glucose uptake in 3T3-L1 adipocytes by inhibiting Akt activation. Molecular docking studies using a homology model of GLUT4 showed that kaempferitrin binds directly to GLUT4 at the glucose transportation channel, suggesting the possibility of a competition between kaempferitrin and glucose during the transport. Taken together, our data demonstrates that kaempferitrin inhibits GLUT4 mediated glucose uptake at least by two different mechanisms, one by interfering with the insulin signaling pathway and the other by a possible competition with glucose during the transport.

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Citations

May 19, 2010·International Journal of Molecular Sciences·Kati HanhinevaKaisa Poutanen
Dec 8, 2009·FEBS Letters·C N Vishnu PrasadAnilkumar Gopalakrishnapillai
Dec 25, 2012·Journal of Molecular Graphics & Modelling·Hasthi V AnnapurnaArumugam Nagarajan
Feb 1, 2011·Molecular Nutrition & Food Research·Melina ClaussnitzerManuela J Rist
Jul 24, 2012·Journal of Ethnopharmacology·Rolffy Ortiz-AndradeAlejandro García-Carrancá
Sep 16, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Sonia Marlen Escandón-RiveraAdolfo Andrade-Cetto
Apr 28, 2019·International Journal of Molecular Sciences·Benedetta RussoSimona Frontoni
Oct 31, 2018·International Journal of Molecular Sciences·Wenxian JiangWanzhong Li
May 6, 2017·Journal of Agricultural and Food Chemistry·Sohyun KimJee-Young Imm

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