Anthelmintic activity of aporphine alkaloids from Cissampelos capensis.
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.
Ayers
Sloan
S
Natural Products Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
Zink
Deborah L
DL
Mohn
Kenneth
K
Powell
Joanne Staats
JS
Brown
Christine M
CM
Murphy
Terry
T
Brand
Robert
R
Pretorius
Seef
S
Stevenson
Dennis
D
Thompson
Donald
D
Singh
Sheo B
SB
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
D000470:Alkaloids; D000871:Anthelmintics; D001060:Aporphines; D010936:Plant Extracts; C081279:aporphine