title: Cinnamoylphenethyl amides from Polygonum hyrcanicum possess anti-trypanosomal activity.
abstract: A methanolic extract from aerial parts of Polygonum hyrcanicum (Polygonaceae) showed high activity against Trypanosoma brucei rhodesiense (IC50 = 3.7 microg/mL). Bioassay-guided fractionation of the extract resulted in isolation of cinnamoylphenethyl amides, including N-trans-caffeoyltyramine (1), N-trans-p-coumaroyltyramine (7), and N-trans-feruloyltyramine (8) as the main active constituents (IC50s ranging from 2.2 to 13.3 microM). Some structurally related, but less active compounds, such as cannabisin B (2), tyrosol (3), p-coumaric acid (4), ferulic acid (5), and N-cis-feruloyltyramine (6) were also identified, along with N-trans-3,4-dimethoxycinnamoyldopamine (9). Cytotoxicity of the active compounds in L6 cells was determined, and selectivity indices (SI) of 7.9 to 33.4 were calculated.
authors: Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
authors: Fahimeh
authors: F
authors: Moradi-Afrapoli
authors: Nargues
authors: N
authors: Yassa
authors: Stefanie
authors: S
authors: Zimmermann
authors: Soodabeh
authors: S
authors: Saeidnia
authors: Abbas
authors: A
authors: Hadjiakhoondia
authors: Samad N
authors: SN
authors: Ebrahimi
authors: Matthias
authors: M
authors: Hamburger
mesh_terms: D003373:Coumaric Acids / Q000737:chemistry / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry* / Q000494:pharmacology*; D019664:Polygonaceae / Q000737:chemistry*; D028502:Polygonum / Q000737:chemistry*; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology*; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects*; D014439:Tyramine / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D003373:Coumaric Acids; D010936:Plant Extracts; D014344:Trypanocidal Agents; C074004:feruloyltyramine; D014439:Tyramine