In vivo modulation of the behavioral effects of nicotine by the coumarins xanthotoxin, bergapten, and umbelliferone

Psychopharmacology (Berl). 2016 Jun;233(12):2289-300. doi: 10.1007/s00213-016-4279-9. Epub 2016 Apr 14.

Abstract

Rationale: Nicotine, a dominant alkaloid found in tobacco, is responsible for physical dependence, as well as addiction to cigarette smoking; consequently, smoking cessation is a very difficult process. Hepatic cytochrome P-450 2A6 (CYP2A6) is involved in the 70-80 % of the initial metabolism of nicotine and its co-metabolites. As this metabolism is slowed by inhibitors of CYP2A6, this kind of enzymatic inhibition has been proposed as a novel target for smoking cessation.

Objectives: Nicotine administered alone improved memory acquisition and consolidation as well as exerted antidepressive activity in animal models. These effects persist for 24 h. However, they are completely extinguished 48 h after administration.

Methods: To investigate if the coumarins prolong the behavioral effects of nicotine, the forced swimming test (FST)-animal models of depression, and passive avoidance (PA) test-memory and learning paradigm were used.

Results: This study revealed that three CYP2A6 inhibitors: two furanocoumarins, xanthotoxin (15 mg/kg) and bergapten (25 mg/kg), and the simple coumarin umbelliferone (25 mg/kg), prolonged the antidepressive and procognitive effects of nicotine.

Conclusions: These natural products may offer a new approach to the treatment of nicotinism as antidepressant and memory improvement actions are one of the main factors of nicotine dependence.

Keywords: Coumarins; Depression; Memory; Mice; Nicotine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 5-Methoxypsoralen
  • Animals
  • Antidepressive Agents / pharmacology
  • Avoidance Learning / drug effects
  • Behavior, Animal / drug effects*
  • Coumarins / pharmacology*
  • Cytochrome P-450 CYP2A6 / antagonists & inhibitors
  • Depression / psychology
  • Locomotion / drug effects
  • Male
  • Memory / drug effects
  • Methoxsalen / analogs & derivatives*
  • Methoxsalen / pharmacology*
  • Mice
  • Nicotine / pharmacology*
  • Nicotinic Agonists / pharmacology*
  • Nootropic Agents / pharmacology
  • Swimming / psychology
  • Umbelliferones / pharmacology*

Substances

  • Antidepressive Agents
  • Coumarins
  • Nicotinic Agonists
  • Nootropic Agents
  • Umbelliferones
  • 5-Methoxypsoralen
  • 7-hydroxycoumarin
  • Nicotine
  • Cytochrome P-450 CYP2A6
  • Methoxsalen