In pursuit of new anti-malarial candidates: novel synthesized and characterized pyrano-benzodioxepin analogues attenuated Plasmodium berghei replication in malaria-infected mice
| Autor: | Simbiat Oloriegbe, Olubunmi Atolani, Abdulmumeen Amao Hamid, Abraham Cornelius Akina, Azeezat Alayo, Adenike Faoziyat Sulaiman, Basheer Ajibola Balogun, Gabriel Ademola Olatunji, Learnmore Kambizi |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Science (General)
Plasmodium berghei Pharmacology Pyrano-benzodioxepin Parasite load Plasmodium Q1-390 In vivo medicine Artemisinin H1-99 Multidisciplinary biology Chemistry Acid phosphatase Aminobenzoic acid biology.organism_classification medicine.disease Social sciences (General) Toxicity biology.protein Chemosuppression Anti-malarial Malaria medicine.drug |
| Zdroj: | Heliyon, Vol 7, Iss 12, Pp e08517-(2021) |
| ISSN: | 2405-8440 |
| Popis: | Malaria, a parasitic disease of the tropics, is one of the major cause of morbidity and mortality, particularly in the tropics. Following the increased resistance of the primary causative parasites, Plasmodium sp, to the mainstream drug, artemisinin combination therapies (ACTs), combating malaria incidences, morbidity and mortality have remained elusive. Novel pyrano-benzodioxepin derivatives (DHA-PABA and DHA-LEVO) were synthesized and characterized using Fourier transform infrared (FT-IR) and nuclear magnetic resonance (NMR) spectrometries. The compounds were subjected to standard in vivo antimalarial screening (using chloroquine-sensitive strain) in mice, and the toxicity was also determined using a standard assay. The observed elevation in serum alkaline phosphatase and acid phosphatase activity in the untreated and the group administered lower doses of DHA-LEVO is an indication of the hepatic stage of the parasite in the experimental animal, which is accompanied by significant perturbation in the membrane of the hepatocyte leading to leakage of this enzyme out of the liver cells. The semisynthetic pyrano-benzodioxepin derivatives act rapidly by clearing the parasite load from the blood. The novel pyrano-benzodioxepin candidates containing endoperoxide functionality hold promise in the pursuit of new monotherapy drug candidates against the virulent strain of the plasmodium. |
| Databáze: | OpenAIRE |
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