Cyclodextrin-complexed Ocimum basilicum leaves essential oil increases Fos protein expression in the central nervous system and produce an antihyperalgesic effect in animal models for fibromyalgia

Int J Mol Sci. 2014 Dec 29;16(1):547-63. doi: 10.3390/ijms16010547.

Abstract

O. basilicum leaves produce essential oils (LEO) rich in monoterpenes. The short half-life and water insolubility are limitations for LEO medical uses. β-Cyclodextrin (β-CD) has been employed to improve the pharmacological properties of LEO. We assessed the antihyperalgesic profile of LEO, isolated or complexed in β-CD (LEO/β-CD), on an animal model for fibromyalgia. Behavioral tests: mice were treated every day with either LEO/β-CD (25, 50 or 100 mg/kg, p.o.), LEO (25 mg/kg, p.o.), tramadol (TRM 4 mg/kg, i.p.) or vehicle (saline), and 60 min after treatment behavioral parameters were assessed. Therefore, mice were evaluated for mechanical hyperalgesia (von Frey), motor coordination (Rota-rod) and muscle strength (Grip Strength Metter) in a mice fibromyalgia model. After 27 days, we evaluated the central nervous system (CNS) pathways involved in the effect induced by experimental drugs through immunofluorescence protocol to Fos protein. The differential scanning analysis (DSC), thermogravimetry/derivate thermogravimetry (TG/DTG) and infrared absorption spectroscopy (FTIR) curves indicated that the products prepared were able to incorporate the LEO efficiently. Oral treatment with LEO or LEO-βCD, at all doses tested, produced a significant reduction of mechanical hyperalgesia and we were able to significantly increase Fos protein expression. Together, our results provide evidence that LEO, isolated or complexed with β-CD, produces analgesic effects on chronic non-inflammatory pain as fibromyalgia.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / administration & dosage
  • Analgesics / chemistry
  • Analgesics / isolation & purification
  • Analgesics / therapeutic use*
  • Animals
  • Central Nervous System / drug effects
  • Central Nervous System / metabolism
  • Central Nervous System / physiopathology
  • Fibromyalgia / drug therapy*
  • Fibromyalgia / genetics
  • Fibromyalgia / physiopathology
  • Hand Strength
  • Hyperalgesia / drug therapy
  • Hyperalgesia / genetics
  • Hyperalgesia / physiopathology
  • Male
  • Mice
  • Monoterpenes / administration & dosage
  • Monoterpenes / chemistry
  • Monoterpenes / isolation & purification
  • Monoterpenes / therapeutic use*
  • Motor Activity / drug effects
  • Ocimum basilicum / chemistry*
  • Oils, Volatile / administration & dosage
  • Oils, Volatile / chemistry
  • Oils, Volatile / isolation & purification
  • Oils, Volatile / therapeutic use*
  • Plant Leaves / chemistry
  • Proto-Oncogene Proteins c-fos / genetics*
  • Up-Regulation / drug effects
  • beta-Cyclodextrins / chemistry*

Substances

  • Analgesics
  • Monoterpenes
  • Oils, Volatile
  • Proto-Oncogene Proteins c-fos
  • beta-Cyclodextrins
  • betadex