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- Title
Canavanine increases glucose uptake in C<sub>2</sub>C<sub>12</sub> cells through the activation of imidazoline I-2B receptors.
- Authors
Chao, Pin‐Chun; Chang, Chin‐Hong; Niu, Ho‐Shan; Huang, Gin‐Chi; Chen, Li‐Jen; Cheng, Juei‐Tang
- Abstract
Canavanine is a guanidinium derivative that contains the basic structure of the ligand(s) of imidazoline receptor (I-R). Canavanine has been reported to activate the imidazoline I-3 receptor (I-3R) both in vivo and in vitro. Additionally, the activation of the imidazoline I-2B receptor (I-2 BR) by guanidinium derivatives may increase glucose uptake. Therefore, the effect of canavanine on the I-2 BR was investigated in the present study. Glucose uptake into cultured C2C12 cells was determined using the radio-ligated tracer 2-[14C]-deoxy-glucose. The changes in 5′ AMP-activated protein kinase ( AMPK) expression were also identified using Western blotting analysis. The canavanine-induced glucose uptake was inhibited in a dose-dependent manner by BU224 (0.01-1 μmol/L), which is a specific I-2 BR antagonist, in the C2C12 cells. Additionally, the canavanine-stimulated AMPK phosphorylation and glucose transporter ( GLUT4) expression were also sensitive to BU224 inhibition in the C2C12 cells. Moreover, both canavanine-stimulated glucose uptake and AMPK phosphorylation were attenuated by high concentrations of amiloride (1-2 μmol/L), which is another established I-2 BR inhibitor, in a dose-dependent manner in C2C12 cells. Additionally, compound C abolished the canavanine-induced glucose uptake and AMPK phosphorylation at a concentration (0.1 μmol/L) sufficient to inhibit AMPK. In conclusion, these data demonstrated that canavanine has an ability to activate I-2 BR through the AMPK pathway to increase glucose uptake, which indicates I-2 BR as a new target for diabetic therapy.
- Subjects
CANAVANINE; IMIDAZOLINES; GLUCOSE; BIOTECHNOLOGY; SMALL molecules; PHARMACOLOGY
- Publication
Clinical & Experimental Pharmacology & Physiology, 2015, Vol 42, Issue 10, p1045
- ISSN
0305-1870
- Publication type
Article
- DOI
10.1111/1440-1681.12464