Pharmaceutical Microbiology
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Item Anti-measles potential of selected compounds from uvaria chamae P. beauv: a molecular docking approach(2024) Oluremi, B. B.; Osamudiamen, P. M.; Nwude, D. O.; Ajeoge, J. K.; Babatunde, A.Measles is an extremely contagious viral infection, reported to be responsible for most global childhood death. Plants have been proven to be very effective against viral diseases with an added advantage of less toxicity. Previous studies have reported the activities of Uvaria chamae extracts against measles virus. This study investigated the in silico anti-measles activities of bioactive compounds from Uvaria Chamae leaves extract. The in silico docking studies were carried out using four compounds isolated from U. chamae (stigmasterol, chrysin, chalcone, and dihydrochalcone) reported in literature. The pharmacokinetic properties of these selected compounds were also evaluated using ADMET studies. The compounds were docked to the measles virus nucleoprotein (PDB ID: 5E4V) and they had binding affinities ranging from -6.4 to -8.2 kcal/mol. Stigmasterol (-8.2 kcal/mol) and Chrysin (-8.0 kcal/mol) showed the greatest affinities for the protein target. These two compounds passed the Lipinski’s Rule of Five for leadlikeness. Stigmastrol and Chrysin showed promising pharmacological properties that indicate that they could be investigated as viable lead candidates for further anti-measles drug development studies.Item Antibacterial, antibiofilm activities and toxicity of uvaria chamae P. beauv (annonaceae)(2024) Oluremi, B. B.; Oloche, J. J.; Abiona, P. D.; Ofudi, C. B."Background: Bacteria biofilms are a serious global health concern. The rapid increase of antimicrobial resistance in diarrheagenic bacteria due to biofilm formation has limited the clinical usefulness of some antibiotics in circulation. Objectives: Uvaria chamae has shown broad spectrum antibacterial activity, hence the need to study its antibiofilm activity against enteroaggregative Escherichia coli (EAEC) strains implicated in paediatric diarrhoea. Methods: Samples of authenticated U. chamae root, stem and leaf were collected, air-dried, ground and extracted by cold maceration in dichloromethane and methanol separately. The EAEC strains tested were; O42, DH5α, MN5DE, D25D and D28I. The plant extracts were subjected to quantitative and qualitative phytochemical screening and the 50% lethality (LC50) brine shrimp assay carried out. Extracts were screened for antibacterial activity using agar diffusion method, while agar dilution and broth dilution methods were used to determine minimum inhibitory and bactericidal concentrations, respectively. Biofilm inhibition of the active extracts was investigated by crystal violet method. Results: All the EAEC strains were multi-drug resistant, but susceptible to gentamicin and azithromycin. Dichloromethane leaf extract (DLE) and methanol leaf extract (MLE) inhibited the growth of the tested EAEC strains with the MIC of MLE D28I being MIC 3.75 mg/mL. The percentage biofilm inhibition by MLE against EAEC strains O42, MND5E and D25D were 72%, 74.5%, and 63%, respectively. Alkaloids were the most abundant in the methanol leaf extract of U. chamae (MLE). The extracts had LC50 >1000 μg/mL. Conclusion: Uvaria chamae is non-toxic and possesses antibiofilm potential that could be further developed as a natural remedy for diarrhoea.Item Peptide-rich extracts from leaves of newbouldia laevis (P. Beauv.) seem. ex. bureau (bignoniaceae) with antimicrobial and brine shrimp lethality activities(Faculty of Pharmaceutical Sciences, University of Jos, Nigeria, 2024-05) Nkumah, A. O.; Kehinde, C. T.; Oluremi, B. B.; Attah, A. F.; Ogbole, O. O.Global concerns over antibiotic-resistant microbial pathogens have spurred a quest for innovative, stable, and target-specific molecules like bioactive peptides. This study evaluates the antimicrobial properties and toxicity of peptide-enriched extracts from Newbouldia laevis leaves. Aqueous extraction, thin layer chromatography (TLC), and Phenomenex's Stratum Giant Tube C18-E were used to obtain partly purified fraction (PPF) and crude peptide extracts (CPE). Antimicrobial inhibitory capacity was determined using p-INT dye, with gentamicin and fluconazole as standards. Cytotoxicity was assessed with Artemia salina nauplii. Microsoft Excel and GraphPad Prism 5 was used in analysing the data. Peptides were detected in CPE and PPF via TLC and modified G-250. PPF demonstrated more efficacy (IC50: 5.89μg/mL to 33.94μg/mL) against bacteria and fungi, with low toxicity (LC50: 5964.87μg/mL for PPF and 1094.20μg/mL for CPE) in the Brine shrimp lethality assay. The study presents the discovery of bioactive peptides from the leaves of Newbouldia laevis. Consequently, bioactive peptides extracted from this plant hold potential as foundational compounds for the development of novel broad-spectrum antibiotics aimed at combating microbial infections.Item The role of viruses in the development of cancer(2024) Oluremi, B. B.; Omobolade, E. S.Cancer continues to be a leading cause of death globally. According to the World Health Organisation, it ranked second most common cause of death globally, claiming millions of lives with millions of new cases diagnosed yearly. Despite recent advances in cancer research and availability of several therapies, severe adverse effects, multi-drug resistance and cost of management are drawbacks of available therapies. Hence, the need for novel approaches that will mitigate the limitations of these conventional treatment options. Cancer has been linked to several factors and while the focus is usually on carcinogenic substances, viruses have been found to account for 15-20% of cancer cases. Oncolytic viruses are viruses that are used in cancer treatment. These viruses have the ability to selectively infect and replicate within tumor cells making them specific in their action against them. This promising approach is also effective when combined with other cancer treatment options such as chemotherapy and radiation.Item Molecular modeling identification of key secondary metabolites from xylopia aethiopica as promising therapeutics targeting tssential measles viral proteins(Hindawi, 2023-02) Oloche, J. J.; Oluremi, B. B.; Aruwa, C. E.; Sabiu, S.This study computationally screened three key compounds (vanillin (VAN), oxophoebine (OPB), and dihydrochalcone (DHC)) derived from Xylopia aethiopica (Guinea pepper), a medicinal plant with known antiviral activity, against key druggable measles virus (MV) proteins (fusion protein (FUP), haemagglutinin protein (HMG), and phosphoprotein (PSP)). Each molecular species was subjected to a 100 ns molecular dynamics (MD) simulation following docking, and a range of postdynamic parameters including free binding energy and pharmacokinetic properties were determined. The docking scores of the resulting OPB-FUP (-5.4kcal/mol), OPB-HMG (-8.1 kcal/mol), and OPB-PSP (-8.0kcal/mol) complexes were consistent with their respective binding energy values (-25.37, -28.74, and -40.68 kcal/mol), and higher than that of the reference standard, ribavirin (RBV) in each case. Furthermore, all the investigated compounds were thermodynamically compact and stable, especially HMG of MV, and this observation could be attributed to the resulting intermolecular interactions in each system. Overall, OPB may possess inhibitory properties against MV glycoproteins (FUP and HMG) and PSP that play important roles in the replication of MV and measles pathogenesis. While OPB could serve as a scaffold for the development of novel MV fusion and entry inhibitors, further in vitro and in vivo evaluation is highly recommended.Item Anti-streptococcus mutans, anti-adherence and anti-acidogenic activity of uvaria chamae P. beauv(Elsevier B.V., 2023-01) Madiba, M.; Oluremi, B. B.; Gulube, Z.; Oderinlo, O. O.; Marimani, M.; Osamudiamen, P. M.; Patel, M.Ethnopharmacological relevance. Streptococcus mutans a key pathogen, produces biofilm, acids and extracellular polysaccharides in the oral cavity; which leads to the development of dental caries. Control of these pathogenic markers can prevent dental caries. Uvaria chamae P. Beauv. is a medicinal plant traditionally used for many ailments including oral infections. Root, leaves and bark extracts has proven antibacterial activity including activity against caries causing S. mutans. However, its effect on the virulence properties of S. mutans, responsible for the development of dental caries, has not been studied. Aim of the study This study investigated the phytochemical constituents, anti-S. mutans, anti-adherence and antiacidogenic activity of U. chamae root extract. Materials and methods Extracts were prepared and phytochemical analysis was performed. Minimum inhibitory concentrations (MIC) were determined, and MIC and sub-MIC concentrations of the best solvent were selected for their effect on the virulence factors of S. mutans. The results were analysed using one-way ANOVA and Wilcoxon Rank Sum Tests. Results The ichloromethane extract, with proanthocyanidin as a major chemical constituent, produced an MIC of 0.02 mg/ml. At 6 h, exposure to 0.005, 0.01, and 0.02 mg/ml extract significantly reduced S. mutans adherence by 39, 59, and 77% respectively (p < 0.05). Uvaria chamae also significantly inhibited acid production in S. mutans at 10, 12, 14 and 16 h (p < 0.05). At ½ MIC, the plant extract caused remarkable downregulation of the virulence genes responsible for the adherence, biofilm formation, extracellular polysaccharide synthesis and acid production. Conclusions This suggests that U. chamae extract may potentially be used to inhibit the proliferation of S. mutans and silencing the expression of pathology-related genes, which will prevent the development of dental caries.Item Anti-measles virus activity of 4-hydroxy-3-methoxy benzaldehyde (Vanillin) isolated from xylopia aethiopica (Dunal) A. rich(Elsevier B.V., 2023) Oluremi, B. B.; Osamudiamen, P. M.; Adeniji, J. A.; Aiyelaagbe, O. O.Xylopia aethiopica is a plant used ethnomedicinally for the treatment of several infections in Nigeria. This study was carried out to isolate the active compound(s) in Xylopia aethiopica and evaluate their anti-measles virus activity. The Dichloromethane (DCM) fraction of Xylopia aethiopica was fractionated using chromatographic techniques, which led to the isolation of a compound characterized using spectroscopic techniques, FT-IR, 1D and 2D NMR in addition to in vitro anti-measles evaluation in adsorption and post-infection inhibition assays. The isolated compound characterized as 4-Hydroxy-3-methoxy benzaldehyde (Vanillin) was active on measles virus and has minimum nontoxic dose of 10 μg with cytotoxic and inhibitory activity of CC 50 = 84.18 μg/mL, IC 50 = 0.71 μg/mL and selectivity index (SI) = 118.56 (r 2 = 0.979) and interfered with viral attachment and fusion. This is the first report of the isolation of Vanillin from Xylopia aethiopica leaf and its high antiviral activity shows it could be developed further into a promising antiviral lead compound.Item Ethnobotanical appraisal and in-silico investigation of plants used for the management of COVID-19 in Southwestern Nigeria(2021) Oderinlo, O. O.; Adenekan, O. A.; Alawode, T. T.; Osamudiamen, P. M.; Oluremi, B. B.; Oyeneyin, O. E.; Ngoepe, M. P.The continued spread of 2019 novel coronavirus disease is a serious threat to global health. Currently, no approved vaccines or antiviral agents for treatment exist, but, there are many anecdotal accounts of the use of herbal concoctions for the management of this disease in many low-income settings, including Nigeria abound. Using a combination of a web-based survey, and face-to-face interviews with local herbal sellers, this study documents the herbal flora used in the management of COVID-19 in Southwestern Nigeria, and also probes their potential as inhibitors of SARS-CoV-2 proteins. The preliminary in-silico studies identified taraxerol, vernonioside D2, nimbolide and mangiferoleanone as potential hit candidates for COVID-19. The current findings highlight that nature can be a source for the discovery of medicinal agents active against COVID-19. These preliminary results necessitate further in-vitro and in-vivo experimental evidence.Item In vitro inhibition of multi-drug resistant pseudomonas efflux pump by xylopia aethiopica (dunal) A. rich(African Research Opinion Communication (AROC), 2021-09) Oloche, J. J.; Oluremi, B. B.; Koya, T. O.Global health is under constant threat due to antimicrobial drug resistance. Bacterial Infections caused by Pseudomonas aeruginosa are of importance because of their antibiotics resistance. This study aimed at evaluating the effects of extracts of Xylopia aethiopica (XA) on multidrug-resistant (MDR) Pseudomonas isolates. Fresh samples of XA leaf, stem bark and roots were collected from the botanical garden, University of Ibadan, Nigeria. Dried and pulverized samples were extracted with methanol and partitioned into n-hexane, dichloromethane and ethyl acetate. Phytochemical screening of the extracts was performed by standard methods. Antimicrobial activity and synergistic interaction were determined using microdilution and checkerboard broth dilution methods, respectively. The results revealed that crude methanol extracts of XA leaf, stem bark and root significantly (p<0.05) inhibited the growth of all tested MDR Pseudomonas isolates at 10 mg/mL. At 1 mg/mL, the ethyl acetate fraction of the leaf, and dichloromethane fraction of the roots produced clear zones of inhibition of 12 – 20 mm, and minimum inhibitory concentrations (MICs) of 1 μg/mL and 0.5 mg/mL, respectively. The modulation factor (MF) of ciprofloxacin, dichloromethane fraction of XA roots and ethyl acetate fraction of XA leaf were 4, 8, and 4 on MDR isolates E01006, OAU058 and P. aeruginosa ATCC 27853, respectively. In all tested isolates, but not E01006 and E01024, the fractional MICs of ciprofloxacin/ethylacetate fraction of XA leaf extract combination was not significantly different (p>0.05) compared with ciprofloxacin/verapamil combination. In conclusion, the root and leaf fractions Xylopia aethiopica that demonstrated antimicrobial activity against MDR P. aeruginosa and synergised with ciprofloxacin have the potential to rejuvenate the antimicrobial activity of ciprofloxacin in MDR P. aeruginosa.Item Anticancer and antibacterial activities of solanum aethiopicum L., solanum macrocarpon L. and garcinia kola heckel(2021-05) Oluremi, B. B.; Oloche, J. J.; Aden, A. J.Cancer and infectious diseases are among the top ten leading causes of death in developing countries. The discovery and development of newer agents for combating these global health problems cannot be overemphasized. This study was designed to investigate the activities of extracts of Solanum aethiopicum, Solanum macrocarpon and Garcinia kola on cancer and antibacterial pathogens. The Agar well diffusion method was used to evaluate antibacterial activity of the extracts. In vitro anticancer activity against cervical cancer (HeLa), breast cancer (MCF-7) and epidermoid carcinoma of the larynx (HEp-2) was done by microscopic evaluation of morphology and by determination of 50% cytotoxic concentrations (CC50). The CC50 of ethyl acetate extracts of Solanum aethiopicum and Solanum macrocarpon against MCF-7 were 38.79 μg/mL and 41.30 μg/mL respectively, and were significantly lower (p < 0.05) compared to the CC50 of the other extracts. Dichloromethane extract of Garcinia kola was significantly cytotoxic (p<0.05) on cervical cancer (CC50 = 38.13 μg/mL) compared to DCM extracts from Solanum aethiopicum and Solanum macrocarpon. The minimum concentration of methanol extracts of Solanum aethiopicum, Solanum macrocarpon and Garcinia kola that inhibited the growth of Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Klebsiella pneumoniae was 1.56 mg/mL. Solanum aethiopicum, Solanum macrocarpon and Garcinia kola extracts demonstrated significant (p < 0.05) anticancer and antibacterial activities and as such are promising sources of novel plant-derived anticancer and antibacterial drugs.