DEPARTMENT OF PHARMACEUTICAL CHEMISTRY

Plasmodium falciparum malaria, contributing 26.8% of global malaria deaths in 2022, drives Nigeria's health burden, with artemisinin resistance necessitating novel natural product-derived treatments. This study bridges Nigeria's ethnobotanical heritage with modern pharmacognosy to evaluate the extracts of Alchornea cordifolia (Ogwu obi) and Enantia chlorantha (Awopa). This study aims to assess the antiplasmodial potential of a combined A. cordifolia and E. chlorantha extract via molecular docking against P. falciparum Plasmepsin II and evaluate its acute toxicity in mice. Leaves of A. cordifolia and stem bark of E. chlorantha were extracted with methanol, freeze-dried, and concentrated using a rotary evaporator at 40℃, respectively. Molecular docking targeted Plasmepsin II (PDB ID: 1LEE) using PyRx 0.9.8, with dihydroartemisinin (standard antimalarial drug) and R36 (co-crystallized ligand) as comparators. Compounds with binding affinities ≤ -6.5 kcal/mol were prioritised. Acute toxicity was assessed in Swiss mice using Lorke's method (10–5000 mg/kg). Drug-likeness was evaluated via SwissADME 2025.2 and ProTox-3.0. Binding affinity trends were analysed descriptively. Docking revealed 10 A. cordifolia compounds (e.g., CID:236432, -9.1 kcal/mol) and 15 E. chlorantha compounds (e.g., CID:91710667, -8.6 kcal/mol) with binding affinities ≤ -6.5 kcal/mol, comparable to dihydroartemisinin (-7.1 kcal/mol) and R36 (-10.0 kcal/mol), indicating strong Plasmepsin II inhibition. No toxicity was observed at a dose of 5000 mg/kg. Most compounds showed favourable drug-likeness.

This study investigated the phytochemical composition, antioxidant capacity, andantimicrobial activity of the methanol leaf extract of Bryophyllumpinnatum(Crassulaceae), a plant widely used in traditional medicine for the treatment of infections, inflammation, and wounds. The crude extract was prepared by maceration in methanol and screened for secondary metabolites using standard phytochemical tests. The extract showed the presence of alkaloids, saponins, flavonoids, terpenoids, phenols, carbohydrates, and anthraquinones, while tannins were absent. Quantitative analysesrevealed a total phenolic content of 0.040 ± 0.008 mg GAE/g and a total flavonoidcontent of 0.197 ± 0.005 mg QE/g, confirming the predominance of flavonoidconstituents.The antioxidant potential of the extract was evaluated using DPPHandFRAP assays. The DPPH radical scavenging test showed concentration-dependent activity with an IC₅₀ value of 189 µg/mL compared to 120 µg/mL for ascorbic acid, whilethe FRAP assay demonstrated moderate reducing power. Antimicrobial screeningusingthe agar well diffusion method against selected bacterial and fungal isolates (S. aureus, E. coli, P. aeruginosa, K. pneumoniae, B. subtilis, C. albicans, and A. niger) revealedthat the methanol extract exhibited no detectable inhibitory zones at 1000 mg/mL, whereasstandard drugs ciprofloxacin and ketoconazole showed significant activity. The findings indicate that Bryophyllum pinnatum contains bioactive secondarymetabolites with measurable antioxidant capacity but limited antimicrobial effect underthe tested conditions. Nonetheless, its strong phytochemical and antioxidant profilesupports its ethnomedicinal use and suggests potential for further purificationandevaluation of its individual constituents as sources of novel therapeutic agents.

Free radicals have been implicated in the occurrence of oxidative stress. They have also been found to be important in the pathophysiology of a number of disease conditions. This therefore, underlies the need for very effective antioxidants. Ficus exasperata has been used traditionally for the treatment and management of numerous disease conditions. Assessment of antioxidant properties creates opportunities for further research into the pharmacological, toxicological properties and clinical relevance of Ficus exasperata. The plant sample was collected, identified, dried, and extracted. Plant sample was assessed for its phytochemical constituents, Total Phenolic Content (TPC) and Total Flavonoid Content (TFC), using spectrophotometric methods. Using the DPPH (2,2-diphenyl-1-picrylhydrazyl) assay, and Total Antioxidant Capabilities (TAC), the antioxidant properties of the plant extract was assessed using specified methods. Glycosides, alkaloids, flavonoids, phenols were among the phytochemicals observed to be present. Total Phenolic Content (TPC) was -1.82±47 mg GAE/g of exteract, Total Flavonoid Content (TFC) was found to be 47.69±23.2 mg QE/g of extract. The IC50 of ascorbic acid and extract for DPPH scavenging activity was determined to be 1.31 µg/mL and 1.91 µg/mL, respectively. The IC50 for TAC of the extract was determined to be 1.23 µg/mL, while that of the standard (ascorbic acid) was found to be 8.82𝑥10−9 µg/mL.

Background: .The tetracycline class of antimicrobials demonstrates a broad spectrum of activity against various pathogens, encompassing Gram-positive and Gram-negative bacteria, as well as atypical organisms.However, their use for bacterial infections has been restricted in recent years due to the emergence of resistant organisms employing efflux and ribosomal protection mechanisms.However tetracycline has been used for therapeutic reasons in both humans and animals
Aim: The primary aim is to perform a quantitative and qualitative analysis on various brands of tetracycline found in pharmacies in Benin city. Method: Visual inspection was performed according to World health Organisation Visual Inspection of Medicines Template while the dissolution test was performed using the United State Pharmacopoeia modified method of spectrometry according to Ahmed et al was used and absorbance was taken at 362nm.
Results: The visual inspection showed that 90% of the brand inspected met the required standard according to the USP. The dissolution test showed that the percentage content in 20 40 and 60 minutes was within the range of 91.31 - 99.53, 92.62 - 99.53 and 97.83 - 99.57 respectively the spectrometry test shows that all the brands met up to the 90 -125% (USP).
Conclusion: The conclusion of this research shows that the analysed tetracycline brands follow the official monographs, except for the color deviation that was noted in the T7 tablets.

Schiff bases are synthesized through condensation reactions between primary amines and aldehydes or ketones. They have been identified as promising lead compounds for drug design and development. The study aims to synthesize, characterize, and assess the physicochemical and pharmacological properties of Schiff base derivatives. Para-aminophenol (3.0 g) was reacted with benzaldehyde (3.0 g), 4-methoxybenzaldehyde (3.2 g), 3-OH-4-methoxybenzaldehyde (4 g), methylene-dioxybenzaldehyde (4 g), 4- chlorobenzaldehyde (4 g), 4-nitrobenzaldehyde (4 g), 3,4-dimethyl-aminobenzaldehyde (4 g), and cinnamaldehyde (3.3 g). The reaction was microwaved at 140 W (20 % intensity) after 3-5 drops of glacial acetic acid for 5 minutes. The mixture was cooled to room temperature, then filtered and recrystallized using either methanol or ethanol to produce samples BS1 to BS8. The reaction was monitored via TLC. Elemental composition was confirmed with spectroscopic analysis. Antimicrobial activity was evaluated using the agar diffusion method, toxicity was determined following the Lorke method, and analgesic properties were assessed using the hot plate model. In silico analyses were also performed on all products to determine their potential protein-ligand binding interactions. Antimicrobial screening indicated that BS1, BS2, BS5, BS6, and BS8 exhibited moderate inhibitory activity against Escherichia coli, Staphylococcus aureus, and Candida albicans. BS3 showed zones of inhibition for E. coli and S. aureus, 14 mm and 13 mm, respectively. The MIC was determined to be 62.5 µg/ml, while the MBC for BS1 and BS2 was 125 µg/ml. Acute toxicity studies revealed an LD₅₀ of 316 to 1265 mg/kg. Analgesic evaluation demonstrated promising activity when compared to pethidine. In silico analyses showed BS3 and BS7 favorable binding affinities with cyclooxygenase-1 (COX-1) and COX-2 enzymes (-8.62 and -8.49 kcal/mol, respectively). The findings suggest that these derivatives have potential therapeutic applications, particularly as analgesics and antimicrobial agents, with further optimization of their structural efficiency, pharmacological efficacy, pharmacokinetic parameters, and safety

Persea americana (avocado) leaves are reported to exhibit antimicrobial properties. As herbal products become increasingly popular, it is crucial to investigate whether formulation excipients affect the antimicrobial efficacy of plant extracts such as avocado leaves. This study investigates the antimicrobial efficacy of Persea americana leaf extract formulated into balms, comparing its effectiveness to that of the crude n-hexane extract. Fresh leaves of Persea americana were harvesteddried, pulverized and macerated in n- hexane.The extract obtained was subjected to phytochemical screening, then formulated into balms (0,100 and 200 mg/mL) and tested against clinical strains of Staphylococcus aureus Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Bacillussubtilis using the ditch method. Ciprofloxacin was used as a positive control. Statistical significance was determined using a One Way ANOVA, with a significance level set at p≤ 0.05.The hexane extract contained alkaloids, triterpenoids, steroids, phenolics, and proteins. At 100 mg/mL, the balm exhibited antimicrobial activity against Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus,while the hexane extract showed no activity. At 200 mg/mL, the extract showed broader antimicrobial activity against the five test organisms compared to the balm.The balm containing no extract showed no activity against any of the test organisms.The crude n-hexane extract exhibited dose-dependent antibacterial activity, producing inhibition zones of 17–20 mm at 200 mg/mL and 22–24 mm at 400 mg/mL, corresponding to approximately 50–77% of ciprofloxacin (4 mg/mL) activity.When formulated into a balm, antimicrobial potency of the extract decreased slightly, indicating possible interactions between the plant extract and the components of the balm. Formulating the n-hexane extract of Persea americana leaves into balm reduced the extract's antimicrobial activity. This suggests that excipient-extract interactions are essential factors to consider in the development of herbal formulations.

The outbreak of COVID-19, caused by SARS-CoV-2, has created an urgent need for new and more effective antiviral agents, particularly those derived from natural sources. Andrographis paniculata (Burm.f.) Nees (Acanthaceae), commonly known as the King of bitters, is a medicinal plant valued for its antiviral and immunomodulatory properties. This study aimed to investigate the therapeutic potential of phytochemicals from Andrographis paniculata as inhibitors of the SARS-CoV-2 virus (PDB ID:7BV2) using molecular docking and ADMET predictions. The 3D structure of the SARS-CoV-2 protein was obtained from the RCSB PDB. Amino acids at the binding site of the protein were identified using PLIP. The protein was prepared for docking in BIOVIA Discovery Studio. Phytochemicals isolated from the plant and identified using GC-MS were downloaded from PubChem as SDF files and imported into PyRx for molecular docking. Post-docking interaction was analysed in BIOVIA Discovery Studio. The ADMET predictions of the phytochemicals were done using the Swiss ADME web server and ProTox-3.0. Molecular docking results from 90 isolated compounds and 23 compounds from GC-MS analysis revealed 27 isolated compounds with a binding affinity range of -6.9 to -8.5 kcal/mol against the target protein, as compared to the standard drug (Remdesivir Triphosphate) and co-crystallized ligand (F86) with binding affinities of -7.7 and -6.8 kcal/mol, respectively. These 27 compounds were selected for post-docking analysis and ADMET profiling. Andrographis paniculata (Burm.f.) Nees (Acanthaceae) possesses phytoconstituents with potential inhibitory activity against the SARS-CoV-2 protein. Methyl 3,4-dicaffeoylquinate, identified as the top compound, along with 5-Hydroxy-7,2',6'-trimethoxyflavone, 5,7,2',6'- Tetrahydroxyflavone, and Apigenin showed good absorption, distribution, metabolism, elimination (ADME), and a comparatively safe toxicity profile. Therefore, further experimental validation is required to confirm their therapeutic potential as antiviral agents against SARS-CoV-2

Cardiovascular disorders, particularly hypertension, continue to pose major health challenges worldwide, necessitating the search for new therapeutic agents with improved efficacy and safety. Imidazole-based compounds have gained attention due to their diverse pharmacological profiles, including notable antibacterial, antifungal and antihypertensive properties. This study employed a computational screening approach to evaluate selected imidazole derivatives for potential antihypertensive activity, followed by the synthesis of a lead derivative (2,4,5-triphenyl-1H-imidazole). Molecular docking was conducted using PyRx (AutoDock Vina) to predict binding affinities and interaction profiles with key hypertension-related protein targets1O86, 4ZUD, 5XPR and 6L88). Several screened derivatives demonstrated strong binding affinities comparable to or higher than the reference drug, suggesting potential inhibitory activity through similar interaction mechanisms at the active site residues. In particular, 2,4,5-triphenyl-1H-imidazole, 1-benzoyl- 4,5-diphenyl-1H-imidazole, and 2-(2-methoxyphenyl)-4,5 diphenyl-1H-imidazole showed the most favorable binding energies and stable protein–ligand interactions across all target proteins. ADMET profiling further indicated acceptable pharmacokinetic behavior for these candidates. The synthesized 2,4,5-triphenyl-1H-imidazole was obtained in a yield of 81.28% and was subjected to preliminary characterization, exhibiting a melting point of 269–272 °C.. The findings highlight promising imidazole structural features with potential antihypertensive relevance and support further synthesis, and biological evaluation of these compounds to advance drug development in hypertension management.

Colorectal cancer (CRC) remains a major global health challenge characterized by high incidence and mortality rates. Emerging evidence supports the use of plant-derived bioactive compounds as promising agents in cancer therapeutics. This study aimed to assess the anticancer potential of phytoconstituents from Moringa oleifera, Olea europaea, Brassica oleracea, and Vitis vinifera against key colorectal cancer protein targets using in silico methods. Phytochemical constituents from these plants were compiled from literature and chemical databases, with their three-dimensional structures retrieved from PubChem. Target proteins implicated in colorectal carcinogenesis, including Human Thymidylate Synthase enzyme, 1HVY, and epidermal growth factor receptor (EGFR), 1XKK, were prepared for docking using Biovia discovery studio. Molecular docking simulations were performed with AutoDock Vina in PyRx, evaluating binding affinities and ligand interactions at active sites. Post-docking analysis and ADMET predictions were done using Biovia discovery studio and ADMETLAB, respectively.

Species belonging to the Cola genus (Malvaceae) are common across tropical regions of Africa and are well known for their use in traditional medicine, particularly for managing infections, inflammatory conditions, and disorders linked to oxidative stress. Several species are also valued in folk practices for their stimulating, antiemetic, and antiproliferative effects. This study investigates the phytochemical profile, as well as the antioxidant and antimicrobial activities, of the 70% ethanolic stem bark extract of Cola rostrata. The plant material was collected from Amapu-Igbengwo village, Umuakpara, Abia State, Nigeria. It was air-dried,
pulverized, and extracted using 70% ethanol by maceration. Identification and quantification studies were achieved via high-performance liquid chromatography (HPLC) on a C-12 column with a water–acetonitrile gradient, using 280 nm as detection wavelength. Gas chromatography-mass spectrometry (GC-MS) analysis employed a DB-5MS column with helium as a carrier gas and compound identification was supported by NIST library matching. Antioxidant capacity was evaluated using DPPH, ABTS, FRAP, and TAC assays. Antibacterial activity was determined through agar well diffusion and dilution techniques
against Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis,, and Enterobacter cloacae. The mode of antibacterial action was determined by calculating the MBC/MIC ratio for susceptible isolates.