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Rottlerin activates AMPK possibly through LKB1 in vascular cells and tissues

Kanou Kojima1, Hiroyuki Motoshima, Atsuyuki Tsutsumi

  • 1Department of Metabolic Medicine, Graduate School of Medical Sciences, Kumamoto University, 1-1-1 Honjo, Kumamoto, Japan.

Biochemical and Biophysical Research Communications
|September 16, 2008
PubMed

Insights

Rottlerin activates AMP-activated protein kinase (AMPK) in vascular cells by involving LKB1, not protein kinase Cdelta. This study reveals a new mechanism for AMPK activation in vascular smooth muscle cells and aorta.

Area of Science:

  • Biochemistry
  • Cell Biology
  • Vascular Biology

Background:

  • AMP-activated protein kinase (AMPK) is a critical cellular energy sensor.
  • AMPK plays a role in numerous cell signaling pathways and is a therapeutic target for vascular diseases.
  • The effect of rottlerin, a protein kinase Cdelta inhibitor, on AMPK in vascular cells was previously unclear.

Purpose of the Study:

  • To investigate whether rottlerin activates AMPK in vascular smooth muscle cells (VSMCs) and rabbit aorta.
  • To determine the role of protein kinase Cdelta and LKB1 in rottlerin-mediated AMPK activation.

Main Methods:

  • Treatment of VSMCs and isolated rabbit aorta with rottlerin.
  • Measurement of cellular ATP levels.
  • Inhibition of protein kinase Cdelta and LKB1.
  • Assessment of AMPK activation.

Main Results:

  • Rottlerin reduced cellular ATP and activated AMPK in VSMCs and aorta.
  • Inhibition of protein kinase Cdelta did not lead to AMPK activation.
  • LKB1 was expressed in VSMCs and aorta.
  • Overexpression of dominant-negative LKB1 attenuated rottlerin-induced AMPK activation.

Conclusions:

  • Rottlerin activates AMPK in vascular cells and tissues.
  • LKB1 mediates rottlerin-induced AMPK activation, independent of protein kinase Cdelta inhibition.
  • This finding provides novel insights into the upstream regulation of AMPK in vascular biology.

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