Anti-onchocerca Metabolites from Cyperus articulatus: Isolation, In Vitro Activity and In Silico 'Drug-Likeness'
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Nat Prod Bioprospect. 2014 Aug;4(4):243-9. doi: 10.1007/s13659-014-0023-5. Epub 2014 Jun 10.
Anti-onchocerca Metabolites from Cyperus articulatus: Isolation, In Vitro Activity and In Silico 'Drug-Likeness'.
Metuge JA1, Babiaka SB2, Mbah JA3, Ntie-Kang F2, Ayimele GA3, Cho-Ngwa F1.
- 1ANDI Centre of Excellence, Department of Biochemistry and Molecular Biology, Faculty of Science, University of Buea, P. O. Box 63, Buea, Cameroon.
- 2Department of Chemistry, Faculty of Science, University of Buea, P. O. Box 63, Buea, Cameroon ; Chemical and Bioactivity Information Centre, Chemistry Department, Faculty of Science, University of Buea, P. O. Box 63, Buea, Cameroon.
- 3Department of Chemistry, Faculty of Science, University of Buea, P. O. Box 63, Buea, Cameroon.
The aims of this investigation were to isolate active ingredients from the roots/rhizomes of Cyperus articulatus used as herbal medicine in Cameroon for the treatment of human onchocerciasis and to assess the efficacy of the metabolites on the Onchocerca worm.
The antifilarial activity was evaluated in vitro on microfilariae (Mfs) and adult worms of the bovine derived Onchocerca ochengi, a close relative of Onchocerca volvulus.
Cytotoxicity was assessed in vitro on monkey kidney epithelial cells. The structures of the active compounds were determined using spectroscopic methods and their drug-likeness evaluated using Lipinski parameters.
Two secondary metabolites, AMJ1 [containing mustakone (1) as the major component] and linoleic acid or (9Z,12Z)-octadeca-9,12-dienoic acid (2) were isolated. Both compounds were found to kill both the microfilariae and adult worms of O. ochengi in a dose dependent manner.
The IC50s for AMJ1 were 15.7 µg/mL for Mfs, 17.4 µg/mL for adult males and 21.9 µg/mL for adult female worms while for linoleic acid the values were, 15.7 µg/mL for Mfs, 31.0 µg/mL for adult males and 44.2 µg/mL for adult females. The present report provides the first ever evidence of the anti-Onchocerca efficacy of AMJ1 and linoleic acid.
Cyperus articulates; Linoleic acid; Microfilariae; Mustakone; Onchocerca ochengi; Onchocerca volvulus