title: Analgesic potential of standardized methanol stem bark extract of Ficus platyphylla in mice: Mechanisms of action.
abstract: BACKGROUND
  Extracts of the stem bark of Ficus platyphylla (FP) have been used in traditional the Nigerian medicine to treat psychoses, depression, epilepsy, pain and inflammation. Previous studies have revealed the analgesic and anti-inflammatory effects of FP in different assays including acetic acid-induced writhing, formalin-induced nociception, and albumin-induced oedema.
  
  
  OBJECTIVE
  In this study, we assessed the effects of the standardised extract of FP on hot plate nociceptive threshold and vocalisation threshold in response to electrical stimulation of the tail root in order to confirm its acclaimed analgesic properties. We also investigated the molecular mechanisms underlying these effects, with the focus on opiate receptor binding and the key enzymes of eicosanoid biosynthesis, namely cyclooxygenase (COX) and 5-lipoxygenase (5-LO).
  
  
  RESULTS
  FP (i) increased the hot plate nociceptive threshold and vocalisation threshold. The increase in hot plate nociceptive threshold was detectable over a period of 30min whereas the increase in vocalisation threshold persisted over a period of 90min. (ii) FP showed an affinity for µ opiate receptors but not for δ or κ opiate receptors, and (iii) FP inhibited the activities of COX-2 and 5-LO but not of COX-1.
  
  
  CONCLUSIONS
  We provided evidence supporting the use of FP in Nigerian folk medicine for the treatment of different types of pain, and identified opioid and non-opioid targets. It is interesting to note that the dual inhibition of COX-2 and 5-LO appears favourable in terms of both efficacy and side effect profile.
authors.affiliation: Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria; Institute of Pharmacology and Toxicology, Faculty of Medicine, Otto-von-Guericke University, Leipziger Str. 44, 39120 Magdeburg, Germany; Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development, P. M. B. 21, Abuja, Nigeria.
authors.forename: Ben A
authors.initials: BA
authors.lastname: Chindo
authors.affiliation: Institute of Pharmacology and Toxicology, Faculty of Medicine, Otto-von-Guericke University, Leipziger Str. 44, 39120 Magdeburg, Germany.
authors.forename: Helmut
authors.initials: H
authors.lastname: Schröder
authors.affiliation: Chair of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich-Schiller-University Jena, Philosophenweg 14, 07743 Jena, Germany.
authors.forename: Andreas
authors.initials: A
authors.lastname: Koeberle
authors.affiliation: Chair of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich-Schiller-University Jena, Philosophenweg 14, 07743 Jena, Germany.
authors.forename: Oliver
authors.initials: O
authors.lastname: Werz
authors.affiliation: Institute of Pharmacology and Toxicology, Faculty of Medicine, Otto-von-Guericke University, Leipziger Str. 44, 39120 Magdeburg, Germany. Electronic address: axel.becker@med.ovgu.de.
authors.forename: Axel
authors.initials: A
authors.lastname: Becker
mesh_terms: D000700:Analgesics / Q000494:pharmacology* / Q000627:therapeutic use*; D000818:Animals; D001094:Arachidonate 5-Lipoxygenase / Q000235:genetics / Q000378:metabolism; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D051545:Cyclooxygenase 1 / Q000378:metabolism; D051546:Cyclooxygenase 2 / Q000378:metabolism; D004558:Electric Stimulation; D030681:Ficus; D057809:HEK293 Cells; D006358:Hot Temperature / Q000009:adverse effects; D006801:Humans; D008297:Male; D000432:Methanol / Q000737:chemistry; D051379:Mice; D010146:Pain / Q000188:drug therapy*; D024301:Plant Bark / Q000737:chemistry; D010936:Plant Extracts / Q000494:pharmacology* / Q000627:therapeutic use*; D011957:Receptors, Opioid / Q000235:genetics / Q000378:metabolism; D012997:Solvents / Q000737:chemistry; D014828:Vocalization, Animal / Q000187:drug effects
chemical_list: D000700:Analgesics; D010936:Plant Extracts; D011957:Receptors, Opioid; D012997:Solvents; D001094:Arachidonate 5-Lipoxygenase; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human; D000432:Methanol
keywords: 5-Lipoxygenase; Cyclocoxygenase; Ficus platyphylla; Mouse; Opiate receptor; Pain threshold