- Title
- Selected alpha-pyrones from the plants Cryptocarya novoguineensis (Lauraceae) and Piper methysticum (Piperaceae) with activity against Haemonchus contortus in vitro
- Creator
- Herath, Dilrukshi; Preston, Sarah; Jabbar, Abdul; Garcia-Bustos, Jose; Addison, Russell; Hayes, Sasha; Rali, Topul; Wang, Tao; Koehler, Anson; Chang, Bill; Hofmann, Andreas; Davis, Rohan; Gasser, Robin
- Date
- 2019
- Type
- Text; Journal article
- Identifier
- http://researchonline.federation.edu.au/vital/access/HandleResolver/1959.17/170375
- Identifier
- vital:14154
- Identifier
-
https://doi.org/10.1016/j.ijpddr.2018.12.006
- Identifier
- ISBN:2211-3207
- Abstract
- Due to the widespread occurrence and spread of anthelmintic resistance, there is a need to develop new drugs against resistant parasitic nematodes of livestock animals. The Nobel Prize-winning discovery and development of the anti-parasitic drugs avermectin and artemisinin has renewed the interest in exploring natural products as anthelmintics. In the present study, we screened 7500 plant extracts for in vitro-activity against the barber's pole worm, Haemonchus contortus, a highly significant pathogen of ruminants. The anthelmintic extracts from two plants, Cryptocarya novoguineensis and Piper methysticum, were fractionated by high-performance liquid chromatography (HPLC). Subsequently, compounds were purified from fractions with significant biological activity. Four alpha-pyrones, namely goniothalamin (GNT), dihydrokavain (DHK), desmethoxyyangonin (DMY) and yangonin (YGN), were purified from fractions from the two plants, GNT from C. novoguineensis, and DHK, DMY and YGN (= kavalactones) from P. methysticum. The three kavalactones induced a lethal, eviscerated (Evi) phenotype in treated exsheathed third-stage larvae (xL3s), and DMY and YGN had moderate potencies (IC50 values of 31.7 +/- 0.23 mu M and 23.7 +/- 2.05 mu M, respectively) at inhibiting the development of xL3s to fourth-stage larvae (L4s). Although GNT had limited potency (IC50 of 200-300 mu M) at inhibiting L4 development, it was the only compound that reduced L4 motility (IC50 of 6.25-12.50 mu M). The compounds purified from each plant affected H. contortus in an irreversible manner. These findings suggest that structure-activity relationship studies of alpha-pyrones should be pursued to assess their potential as anthelmintics.
- Publisher
- Elsevier
- Relation
- International Journal for Parasitology-Drugs and Drug Resistance Vol. 9, no. (2019), p. 72-79
- Rights
- Copyright © 2019 The Authors. Published by Elsevier Ltd on behalf of Australian Society for Parasitology. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/BY-NC-ND/4.0/).
- Rights
- Open Access
- Rights
- http://creativecommons.org/licenses/BY-NC-ND/4.0/
- Rights
- This metadata is freely available under a CCO license
- Subject
- 1108 Medical Microbiology; Haemonchus contortus; Anthelmintic; Natural products; Cryptocarya novoguineensis; Piper methysticum; α-pyrones
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