OPENIBO, JOHN OLUWAYOMI and Covenant University, Theses (2017) PRECLINICAL IN VITRO STUDY ON AMIDINE-HYDROXAMIC ACID BASED ANTIMALARIAL DRUG CANDIDATE. Masters thesis, COVENANT UNIVERSITY.
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Abstract
The emergence of drug resistant strains of malaria parasite has led to increased efforts to discover and develop new antimalarial drugs that are structurally distinct from already existing ones.This study was conducted to evaluate the antiplasmodial activity of novel amidine-hydroxamic acid derivatives. Chloroquine-sensitive – Pyrimethamine resistant Plasmodium falciparum 3D7 strain was cultured in vitro in O+ human red blood cells in RPMI 1640 medium supplemented with 10% heat inactivated O human serum, 25mM HEPES buffer, 50μg/ml penicillin and 50μg/ml streptomycin under a condition of 90% N2, 5% O2 and 5% CO2. Serially diluted drugs were seeded into 96-well microtitre plates and incubated with aliquots of parasite from 3D7 culture medium containing asynchronized stage of parasite at a parasitemia of 0.2% and an haematocrit of 4% and the asynchronized wild type P. falciparum blood sample at a parasitemia of 1% and 4% haematocrit. The results obtained from the inhibitory concentrations (IC50) analyses performed for the novel antimalarial drug candidate compound revealed that the test compound with the code OA2 has IC50 values of 15,960nM against Plasmodium falciparum 3D7 and 0.3941nM against the wild type Plasmodium falciparum, while the standard drugs Artemisinin and Chloroquine were 68.86nM and 68.24nM and 164.5nM and 59.0nM for the wild type and typed strain Plasmodium falciparum. From the result obtained, It can be inferred that OA2 is moderately active against the viability of P. falciparum in human blood cultures and hence may be promising antimalarial drug candidates.
| Item Type: | Thesis (Masters) |
|---|---|
| Uncontrolled Keywords: | Pre-clinical, In vitro, Plasmodium resistance, Novel Drug, Antimalarial. |
| Subjects: | Q Science > Q Science (General) Q Science > QH Natural history > QH301 Biology |
| Divisions: | Faculty of Medicine, Health and Life Sciences > School of Biological Sciences |
| Depositing User: | Mrs Hannah Akinwumi |
| Date Deposited: | 30 Jun 2020 17:16 |
| Last Modified: | 30 Jun 2020 17:16 |
| URI: | http://eprints.covenantuniversity.edu.ng/id/eprint/13441 |
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