title: Anthelmintic activity of aporphine alkaloids from Cissampelos capensis.
abstract: Two known aporphine alkaloids, (S)-dicentrine (1) and (S)-neolitsine (2), have been isolated from the MeOH extract of the aerial parts of Cissampelos capensis (Menispermaceae). The structures of these compounds were elucidated by NMR and MS analysis and comparison to literature data. These compounds were isolated by bioassay-guided fractionation using the Haemonchus contortus larval development assay. Compounds 1 and 2 exhibited EC90 values (concentration at which 90% loss of larval motility is observed) of 6.3 and 6.4 microg/mL, respectively. In an IN VIVO assay, administration of 1 resulted in 67% reduction of worm counts in mice at 25 mg/kg when dosed orally.
authors.affiliation: Natural Products Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors.forename: Sloan
authors.initials: S
authors.lastname: Ayers
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Zink
authors.forename: Kenneth
authors.initials: K
authors.lastname: Mohn
authors.forename: Joanne Staats
authors.initials: JS
authors.lastname: Powell
authors.forename: Christine M
authors.initials: CM
authors.lastname: Brown
authors.forename: Terry
authors.initials: T
authors.lastname: Murphy
authors.forename: Robert
authors.initials: R
authors.lastname: Brand
authors.forename: Seef
authors.initials: S
authors.lastname: Pretorius
authors.forename: Dennis
authors.initials: D
authors.lastname: Stevenson
authors.forename: Donald
authors.initials: D
authors.lastname: Thompson
authors.forename: Sheo B
authors.initials: SB
authors.lastname: Singh
mesh_terms: D000470:Alkaloids / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D001060:Aporphines / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D031606:Cissampelos; D006189:Haemonchus / Q000187:drug effects*; D007814:Larva / Q000187:drug effects; D021261:Parasitic Sensitivity Tests; D008517:Phytotherapy; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000470:Alkaloids; D000871:Anthelmintics; D001060:Aporphines; D010936:Plant Extracts; C081279:aporphine