In the rural communities of sub-Saharan African (sSA) countries, malaria is being managed using phytocompounds. Artesunate is reported to inhibit Gephyrin E, a central, multi-domain scaffolding protein of inhibitory post-synapses. Neem plant and its metabolites like azadirachtin are being indicated for management of malaria by traditional healers. The present study was aimed to cheminformatically analyse the binding potential of artesunate and azadirachtin with various reactive moieties of Gephyrin E, to reduce malaria scourge. With molecular dynamics (MD), binding free energy estimation and binding affinity of artesunate and azadirachtin to Gephyrin E was done. GRIP docking was done to study the interactions of these test ligands with Gephyrin E (6FGC). MD simulation gave insights to structural changes upon binding of artesunate and azadirachtin in the ligand-binding pocket of Gephyrin E. Root mean square deviation (RMSD) and root mean square fluctuation (RMSF) were calculated. From the estimation, azadirachtin had a total binding energy of −36.97 kcal/mol; artesunate had a binding energy of −35.73 kcal/mol. The GRIP docking results provided a clearer evidence that artesunate has comparatively better binding affinity to Gephyrin E than azadirachtin, and the critical binding sites (in activity order) were cavity 3, 2, 8, and 6 for artesunate while for azadirachtin, it was cavity 6, 3, 8, and 2. The GRIP docking provided detailed interactions at the atomic levels, providing evidence; both compounds have chances to overcome the drug resistance problem, albeit higher for artesunate. Our findings added another piece of evidence that azadirachtin may be effective as an anti-malarial agent. The results herein may provide impetus for more studies into bioactive components of plant origin towards the effective management of malaria disease phenotype.
Malaria is a major global health problem with the greatest burden in sub-Saharan Africa (sSA). Unfortunately, Nigeria accounts for 25 percent of the world’s malaria burden and it accounts for more deaths than HIV/AIDS. The causative agent of malaria is plasmodium species. This paper reviews the current approaches to inhibiting plasmodium transmission, and the phyto active compound currently in use in the sSA (particularly in Nigeria) with the goal to ameliorate the high incidence of malaria and to correlating it with recent progress and scientific understanding. Using search engines, several databases including Google scholar, Pub Med, Academic Resource Index, Scopus, etcetera, were utilized to source for relevant publications and literatures. The complex life cycle of the Plasmodium species (causative agent of malaria) gives room for measures that can disrupt its completion. Several methods are currently being tested and experimented on to disrupt the parasite transmission. The disruption of a cell surface transport protein, Feline Leukemia Virus subgroup C Receptor (FLVCR) that pumps heme out of the cell; Gene silencing-techniques used to reduce the levels of FLVCR in the mosquito gut; Prevention of the interaction between the plasmodium TRAP and the Anopheles Saglin protein, which aid the malaria parasite invasion of the mosquito salivary gland; Prevention of the Interaction of Surface Enolase and Plasminogen of Mammalian Blood, disrupting an important role in ookinete invasion of the mosquito midgut; the use of Plants with antimicrobial peptides(cyclotide), that possess structural similarities to SM1 peptide, an inhibitor of plasmodium TRAP-saglin binding;and Use of Phyto-Active Compounds to Block Plasmodium Transmission. These approaches are novel methods in the control and transmission of plasmodium species/malaria. Chemically, phytochemicals with structural similarities to artemisinin, (asesquiteterpene lactone containing an unusual peroxide bridge) is thought of to be present in certain plants with antimalarial and other medicinal value.
A preliminary survey on the knowledge, attitude, and practice of the COVID-19 pandemic among residence in North Central Nigeria, was conducted. An anonymous electronic network sampling survey designed by e-survey was employed. The result showed that on the level of knowledge and practice, 76.83% opined that people may be sick for 1-14 days without developing the symptoms. On the viral transmission, 94.41% agreed that the transmission of the virus can be through direct contact with contaminated surfaces through eyes, nose, and mouth, as well as 78.35%, responded that the virus doesn't penetrate the skin. More so 92.04% of the respondents showed that older and sick people are more vulnerable to the disease with 98.86% showing that the most common symptoms may include fever, tiredness, dry cough, and sometimes difficulty in breathing. Only 24.43% asserted that COVID-19 cannot be transmitted through social gatherings, going put often, making direct physical contact with people. Meanwhile, 21.02% showed COVID-19 is a punishment for immoral behavior. On the rate of the outbreak, 94.32% said it is scary. Only 55.11% asserted approval of the control approach by the government. However, 82.29% would agree with the response of the masses to government measures to control the spread. On the way forward, 98.87% advised the need for more research and 87.08% would approve of vaccination against the disease. This implies that the respondents have a good level of knowledge and practice about COVID-19 and necessary adjustments are needed to control or manage the spread of the pandemic.
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