Journal article
Aminoguanidines: New leads for treatment of Giardia duodenalis infection
International Journal for Parasitology: Drugs and Drug Resistance, Vol.10, pp.38-44
2019
Abstract
Giardia duodenalis is an ubiquitous parasitic pathogen that causes significant morbidity and mortality worldwide. Failures in drug therapy are commonly due to poor patient compliance as a result of the need for repeated administration, off target drug effects and increasing parasite drug resistance. In this study the in vitro efficacy and selectivity of the aminoguanidine compound robenidine and 2 structural analogues against Giardia were determined. After 5 h exposure to each compound the IC50 was as low as 0.2 μM with corresponding MLCs as low as 2.8 μM. This is in contrast to metronidazole which required 24 h to exhibit inhibitory activity. A modified adherence assay, developed for this study, demonstrated that three of the compounds inhibited in vitro adherence of the parasite. The lead compound exhibited rapid giardicidal activity (<5hr). In addition, microscopy studies demonstrated damage to the plasma membrane of trophozoites. In conclusion, a class of aminoguanidines, represented by robenidine, has shown antigiardial activity warranting further investigation.
Details
- Title
- Aminoguanidines: New leads for treatment of Giardia duodenalis infection
- Authors/Creators
- R.J. Abraham (Author/Creator)S. Abraham (Author/Creator)A.J. Stevens (Author/Creator)S.W. Page (Author/Creator)A. McCluskey (Author/Creator)D.J. Trott (Author/Creator)R.M. O'Handley (Author/Creator)
- Publication Details
- International Journal for Parasitology: Drugs and Drug Resistance, Vol.10, pp.38-44
- Publisher
- Elsevier BV
- Identifiers
- 991005544851307891
- Copyright
- © 2019 Published by Elsevier Ltd on behalf of Australian Society for Parasitology
- Murdoch Affiliation
- School of Veterinary and Life Sciences
- Language
- English
- Resource Type
- Journal article
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- Collaboration types
- Domestic collaboration
- Citation topics
- 1 Clinical & Life Sciences
- 1.246 Diarrheal Diseases
- 1.246.985 Cryptosporidium
- Web Of Science research areas
- Parasitology
- Pharmacology & Pharmacy
- ESI research areas
- Microbiology