Literature DB >> 28211632

AMP-activated protein kinase (AMPK) activator A-769662 increases intracellular calcium and ATP release from astrocytes in an AMPK-independent manner.

Julia M Vlachaki Walker1,2, Josephine L Robb1, Ana M Cruz1, Amrinder Malhi1, Paul G Weightman Potter1, Michael L J Ashford2, Rory J McCrimmon2, Kate L J Ellacott1, Craig Beall1,2.   

Abstract

AIM: To test the hypothesis that, given the role of AMP-activated protein kinase (AMPK) in regulating intracellular ATP levels, AMPK may alter ATP release from astrocytes, the main sources of extracellular ATP (eATP) within the brain.
MATERIALS AND METHODS: Measurements of ATP release were made from human U373 astrocytoma cells, primary mouse hypothalamic (HTAS) and cortical astrocytes (CRTAS) and wild-type and AMPK α1/α2 null mouse embryonic fibroblasts (MEFs). Cells were treated with drugs known to modulate AMPK activity: A-769662, AICAR and metformin, for up to 3 hours. Intracellular calcium was measured using Fluo4 and Fura-2 calcium-sensitive fluorescent dyes.
RESULTS: In U373 cells, A-769662 (100 μM) increased AMPK phosphorylation, whereas AICAR and metformin (1 mM) induced a modest increase or had no effect, respectively. Only A-769662 increased eATP levels, and this was partially blocked by AMPK inhibitor Compound C. A-769662-induced increases in eATP were preserved in AMPK α1/α2 null MEF cells. A-769662 increased intracellular calcium in U373, HTAS and CRTAS cells and chelation of intracellular calcium using BAPTA-AM reduced A-769662-induced eATP levels. A-769662 also increased ATP release from a number of other central and peripheral endocrine cell types.
CONCLUSIONS: AMPK is required to maintain basal eATP levels but is not required for A-769662-induced increases in eATP. A-769662 (>50 μM) enhanced intracellular calcium levels leading to ATP release in an AMPK and purinergic receptor independent pathway.
© 2017 John Wiley & Sons Ltd.

Entities:  

Keywords:  A-769662; AMPK; ATP; BV-2; C2C12; GT1-7; H4IIE; INS-1; SH-SY5Y; U373; cortical astrocytes; hypothalamic astrocytes; intracellular calcium

Mesh:

Substances:

Year:  2017        PMID: 28211632     DOI: 10.1111/dom.12912

Source DB:  PubMed          Journal:  Diabetes Obes Metab        ISSN: 1462-8902            Impact factor:   6.577


  7 in total

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  7 in total

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