OFFOR, GLORIA NWABUGWU and Covenant University, Theses (2017) IN VITRO AND EX VIVO ACTIVITIES OF NOVEL HYDROXAMIC ACID DERIVATIVE AGAINST Plasmodium falciparum. Masters thesis, COVENANT UNIVERSITY.
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Abstract
Emergence of drug-resistant strains of Plasmodium has recently led to increased efforts to discover and develop new antimalarial drugs both for the prophylaxis and treatment of malaria infection. The present study was conducted to evaluate the antiplasmodial activity of novel hydroxamic acid derivative against Plasmodium falciparum 3D7 strain and the wild type isolate from malaria infected patients. Chloroquine-sensitive P. falciparum 3D7 was grown in vitro in O+ human red blood cells in RPMI 1640 medium supplemented with 10% heat inactivated AB human serum, 25 mM HEPES buffer, 50 μg/ml penicillin and 50 μg/ml streptomycin under an atmosphere of 90% N2, 5% O2 and 5% CO2. Serially diluted drugs were placed in the wells of 96 well micro titre plates and incubated with aliquots of parasite culture medium containing asynchronized rings at a parasitemia of 0.2% and a haematocrit of 4%. For the ex vivo assay, aliquots of the washed infected red blood cells in complete medium were incubated with varying concentrations of the drugs. The parasitemia for both assays were determined microscopically using Giemsa-stained smears. Chloroquine and artemisinin used as the positive controls as well as the drug-free negative control were all assayed in duplicates simultaneously with the test compound (OA4). Results from the half maximal inhibitory concentrations (IC50) analyses showed the in vitro and ex vivo IC50 values of OA4 to be 28200 nM and 154.2 nM respectively. OA4 lowered the parasitemia across all the drug-treated wells when compared to the drug-free negative control wells. The result from the erythrocyte stabilization assay revealed that OA4 did not induce any alteration on the morphology of red blood cells. In conclusion, these results demonstrated that the hydroxamic acid derivative OA4 could be a promising antimalarial drug candidate
| Item Type: | Thesis (Masters) |
|---|---|
| Subjects: | Q Science > Q Science (General) Q Science > QD Chemistry Q Science > QH Natural history > QH301 Biology |
| Divisions: | Faculty of Engineering, Science and Mathematics > School of Civil Engineering and the Environment |
| Depositing User: | Mrs Hannah Akinwumi |
| Date Deposited: | 05 Feb 2020 15:05 |
| Last Modified: | 05 Feb 2020 15:05 |
| URI: | http://eprints.covenantuniversity.edu.ng/id/eprint/13106 |
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