2-Methoxyoestradiol inhibits glucose transport in rodent skeletal muscle

Exp Physiol. 2010 Aug;95(8):892-8. doi: 10.1113/expphysiol.2010.053405. Epub 2010 May 14.

Abstract

2-Methoxyoestradiol (2-ME) is an oestrogen derivative that inhibits superoxide dismutase (which converts superoxide anions to H(2)O(2)). Since reactive oxygen species have been implicated in glucose transport, we determined the effect of 2-ME on glucose transport in skeletal muscle. Experiments were performed on isolated mouse extensor digitorum longus (EDL, glycolytic, fast-twitch) muscle. Glucose uptake was measured using 2-deoxy-d-[1,2-(3)H]glucose. 2-Methoxyoestradiol (50 microm) reduced glucose uptake induced by insulin, contraction and hypoxia by approximately 60%. Exogenous H(2)O(2) activated glucose uptake, and this effect was also blocked by 2-ME, demonstrating that 2-ME was exerting its inhibitory effect on glucose uptake at a site other than superoxide dismutase. When glucose uptake was stimulated by insulin, followed by addition of 2-ME, there was also an attenuation of the effect of insulin (approximately 60%). Moreover, basal glucose uptake was decreased by 2-ME (approximately 50%). In contrast, insulin-mediated translocation of glucose transporter type 4 protein to the plasma membrane was not affected by 2-ME. Similar results were obtained in soleus (oxidative, slow-twitch) muscle. In conclusion, 2-ME appears to decrease glucose transport in skeletal muscle by directly interfering with the function of glucose transport proteins in surface membranes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2-Methoxyestradiol
  • Animals
  • Deoxyglucose / metabolism
  • Estradiol / analogs & derivatives*
  • Estradiol / pharmacology
  • Glucose / metabolism*
  • Glucose Transporter Type 4 / metabolism
  • Hydrogen Peroxide / pharmacology
  • Hypoxia / physiopathology
  • Insulin / pharmacology
  • Male
  • Mice
  • Muscle Contraction
  • Muscle, Skeletal / drug effects
  • Muscle, Skeletal / metabolism*
  • Rats

Substances

  • Glucose Transporter Type 4
  • Insulin
  • Estradiol
  • 2-Methoxyestradiol
  • Deoxyglucose
  • Hydrogen Peroxide
  • Glucose