title: The leaves of Ficus exasperata Vahl (Moraceae) generates uterine active chemical constituents.
abstract: BACKGROUND
  In the search for new, safe and efficacious uterine active agents, the plant Ficus exasperata was subjected to phytochemical screening and pharmacological analysis.
  
  
  METHODS
  Ethyl acetate and methanolic leaf extracts of Ficus exasperata were fractionated and purified by a series of chromatographic techniques. The isolation process was guided by in vitro functional uterine assays involving the use of C57Bl/6 female mice. Identification of the active chemical constituents was performed by several spectroscopic techniques which included 1D and 2D nuclear magnetic resonance (NMR) and high resolution mass spectrometry (HRMS). The uterine effects of these compounds were investigated on spontaneous, oxytocin-induced and high KCl-induced contractions using isolated uterine segments of non-pregnant female mice. The activity of different compounds on the amplitude (maximum tension above basal force) and frequency of uterine contractions were simultaneously measured and then statistically analysed. The structure-activity relationships were also examined where possible.
  
  
  RESULTS
  These studies led to the identification of some new phytochemical derivatives. Pharmacological assay revealed the presence of both uterine stimulatory and inhibitory constituents. The new pheophytin/pheophorbide derivatives, flavonoids, fatty acids and glycerol derivatives significantly reduced the frequency and amplitude of uterine contraction, while KCl salt, pyrimidine and pheophorbide-b derivatives significantly augmented both spontaneous and agonist-induced contractions.
  
  
  CONCLUSIONS
  This study has demonstrated that Ficus exasperata generates secondary metabolites which have proven effective in the significant inhibition of uterine contractions and thus a potential source of new tocolytic agents. Additionally, uterine stimulatory constituents were also generated some of which may be potential drugs for contraception and/or labour facilitation. Lead compounds generated from this study are the pheophytin/pheophorbide derivatives, pyrimidine derivatives and flavonoid derivatives.
authors.affiliation: Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, The John Arbuthnott Building, 161 Cathedral Street, Glasgow G4 0RE, United Kingdom. tomebafor@yahoo.com
authors.forename: Enitome E
authors.initials: EE
authors.lastname: Bafor
authors.forename: Chiew V
authors.initials: CV
authors.lastname: Lim
authors.forename: Edward G
authors.initials: EG
authors.lastname: Rowan
authors.forename: Ruangelie
authors.initials: R
authors.lastname: Edrada-Ebel
mesh_terms: D000818:Animals; D005260:Female; D030681:Ficus; D066298:In Vitro Techniques; D051379:Mice; D008810:Mice, Inbred C57BL; D010121:Oxytocin; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves / Q000737:chemistry; D011189:Potassium Chloride; D015149:Tocolytic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D014590:Uterine Contraction / Q000187:drug effects*; D014599:Uterus / Q000187:drug effects* / Q000502:physiology
chemical_list: D010936:Plant Extracts; D015149:Tocolytic Agents; D010121:Oxytocin; D011189:Potassium Chloride