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Engineered nanoparticles are known to boost membrane performance in membrane technology. Hitherto, tunable properties that lead to improved hydrophilicity due to increased surface oxygen functionalities upon oxidation of petrol soot have not been fully exploited in membrane filtration technology. Herein, the integration of oxidized petrol soot nanoparticles (PSN) into polyethersulfone ultrafiltration membranes produced via phase inversion technique for dye removal in wastewater is reported. The nanoparticles, as well as the composite membranes, were characterized with diverse physicochemical methods, particularly TEM, SEM, BET, AFM, contact angle, etc. The effect of varying the ratio of PSN (0.05–1.0 wt %) on the properties of the composite membrane was evaluated. The composite membranes displayed increased hydrophilicity, enhanced pure water flux, and antifouling properties relative to the pristine membrane. For example, the obtained pure water flux increased from 130 L·m−2·h−1 for base membrane to 265 L·m−2·h−1 for the best composite membrane (M4). The best flux recovery ratio (FRR) observed for the membranes containing PSN was ca. 80% in contrast to 49% obtained with the pristine membrane indicative of the positive influence of PSN on membrane antifouling behavior. Furthermore, the PSN composite membranes displayed relatively selective anionic dye rejection of ˃95% for Congo red and between 50–71% for methyl orange compared with 42–96% rejection obtained for cationic methylene blue dye with increasing PSN content. The successful fabrication of polyethersulfone–PSN composite membranes by a simple blending process opens a novel route for the preparation of economical, functional, and scalable water purification membranes capable of addressing the complex issue of water remediation of organic azo dyes.

The resistance of bacteria to current antibiotic drugs and the re-occurrence of different ailments after several therapeutic protocols continue to be a cause for concern. Arylated amino acids are vital synthons to many compounds; they serve as essential building blocks in the synthesis of nitrogen heterocycles with various biological activities. This research reports on the synthesis of some N-aryl amino acids and evaluates their antibacterial activities. The N-aryl amino acids 3a–3j were obtained by reacting different 4-substituted fluorobenzene 1a–1d with different amino acids 2a–2g via a metal-free base-induced aryl amination reaction of aryl halides. The antibacterial activities of the synthesized compounds were evaluated against eight bacterial strains (Four Gram-positive, Bacillus subtilis (ATCC 6633), Streptococcus pneumonia (ATCC 33400), Staphylococcus aureus (ATCC 25923), and Staphylococcus epidermidis (ATCC 14990), and four Gram-negative, Enterobacter cloacae (ATCC 43560), Escherichia coli (ATCC 25922), Proteus mirabilis (ATCC 43071), and Klebsiella oxytoca (ATCC 13182) using the agar well diffusion method with streptomycin as a reference drug. The biological screening indicates that the synthesized compounds 3a, 3e, and 3j have promising broad-spectrum antibacterial potential, as the N-aryl amino acid displayed activity that was comparable to the standard drug against Streptococcus pneumonia, Escherichia coli, and Proteus mirabilis.

Essential oils from plants have been proven safe as natural antioxidants, and few are already marketed as digestive enhancers as well as in prevention of several degenerative diseases. This study evaluated the antioxidant capacity of seed and shell essential oils of Abrus precatorius (L), a herb used for ethno-medicinal practices in Nigeria. The essential oils were obtained by hydro-distillation. The ability of the oils to act as hydrogen/electrons donor or scavenger of radicals were determined by in-vitro antioxidant assays using 2,2-diphenyl-2-picryl-hydrazyl free radical (DPPH.) scavenging; 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical scavenging; lipid peroxide and nitric oxide radicals scavenging assays. The IC50 of the seed and shell oils (2.10 mg/mL and 1.20 mg/mL respectively) showed that antioxidant activity is higher than that for the standard drugs (3.20 mg/mL and 3.40 mg/mL) for the nitric oxide scavenging assay. The lipid peroxidation radical activity of the oils were similar to vitamin C, weak DPPH and ABTS radical scavenging activities were discovered in comparison to vitamin C and rutin. Generally, in the four antioxidant assays, a significant correlation existed between concentrations of the oils and percentage inhibition of free radicals and lipid peroxidation. The composition of A. precatorius essential oils reported earlier may account for their antioxidant capacity.

Piliostigma thonningii (Schumach.) Milne-Redhead. (Leguminosae) is used for various medicinal purposes in African countries. Phytochemical investigation of P. thonningii yielded two compounds newly isolated from natural sources, 2 β -methoxyclovan-9 α -ol ( 1 ), and methyl- ent -3 β -hydroxylabd-8(17)-en-15-oate ( 2 ), along with 14 known compounds ( 3 – 16 ). Compounds 1 and 4 (alepterolic acid) showed potential selectivity towards Trypanosoma brucei brucei with IC 50 7.89 and 3.42 μM, respectively. Compound 2 showed activity towards T. brucei and Leishmania donovani Amastigote with IC 50 3.84 and 7.82 μM, respectively. The structure activity relationship (SAR) of the isolated metabolites suggested that hydroxylation at C-2 enhances the antiprotozoal activity towards T. brucei in sesquiterpenes 1 and 3 . Similarly hydroxylation at C-3 in labdane diterpenes elevates the antiprotozoal activity towards T. brucei .

L-Prolinamides are emerging as promising scaffolds in medicinal chemistry due to their favorable electronic properties and structural versatility. This study employed a comprehensive computational approach, including molecular docking, density functional theory (DFT), molecular dynamics (MD) simulations, and binding free energy calculations, to evaluate a series of L-prolinamides as potential multi-target inhibitors against key Type 2 diabetes (T2D) enzymes: α-amylase, α-glucosidase, and dipeptidyl peptidase-4 (DPP-4). Out of 27 screened compounds, six (Q10, Q14, Q19, Q22, Q24, and Q26) demonstrated superior binding profiles relative to standard inhibitors. Binding free energy calculations revealed that Q14 and Q10 interacted effectively with α-amylase, with ΔGbind values of − 49.51 and − 45.18 kcal/mol, respectively, closely approaching that of acarbose (− 55.20 kcal/mol). Against α-glucosidase, Q24 emerged as the most potent (− 55.79 kcal/mol), outperforming miglitol (− 48.05 kcal/mol), while Q22, Q26, and Q19 also showed competitive binding. Quantum chemical analysis computed at the B3LYP/6–311 +  + G(d,p) level of theory indicated Q10 had the lowest LUMO energy (− 2.43 eV), enhancing electron acceptance, while Q24 had the highest HOMO value (− 5.98 eV), promoting electron donation. MD simulations further confirmed the structural stability of the top ligand enzyme complexes. In silico pharmacokinetic assessments supported their drug-likeness and oral bioavailability. Collectively, these findings highlight L-prolinamides, particularly Q10 and Q24, as promising multi-target candidates for T2D therapy and warrant further experimental exploration.

BackgroundUlcer remains a health challenge worldwide with antibiotics and proton pump inhibitors as major management therapy. The study investigated the acute, sub-chronic toxicity and gastrointestinal protective activity of a polyherbal formulation (Mystomate4®) used locally in Nigeria.MethodsOral LD50 and the sub-chronic toxicity test were determined in mice and rats. Mice were grouped into 8 groups of 8 mice each. They were dosed a graded concentration of the formulation (1.28, 2.56; 5.12; 10.24; 20.48; 40.96; 81.92; 163.84 g/kg body weight). The graded dose used was arrived at after an initial pilot study. Thereafter doses were chosen around the dose obtained from the pilot study. Animal were dosed orally and observed for sign of toxicity and number of death recorded after 24 h. The sub-chronic toxicity study was carried out for 3 months in rats at a dose of 2.5 and 5.0 g/kg body weight arrived at by titrating down the LD50 value after which some vital tissues were harvested and assessed for toxicity using relevant biomarkers. Anti-ulcer activity was evaluated in rats using ethanol, indomethacin and pylorus ligation induced ulcer models. Data were analysed with Graph Pad Prism version 5.0 using appropriate statistical method and significant level placed at p ≤ 0.05.ResultsThe acute toxicity study showed an LD50 result of 22,837.21 g/kg. The sub-chronic toxicity study resulted in a significant reduction in body weight due to significant decrease (p ≤ 0.05) in feed consumption. Biochemical analyses of the blood samples showed a significant increase (p ≤ 0.05) in creatinine and albumin level in the 2.5 mg/kg female group. ALT was significantly increased in all the treated rats except in 2 mg/kg female rats. Alkaline phosphatase significantly increased in high dosed male (HM) group while blood urea:creatinine ratio was significantly lowered in all the treated groups. There was a significant increase in serum TGL in all rats while LDL was significantly increased and decreased in HM and high dosed female (HF) respectively.ConclusionMystomate4® showed significant protection against ethanol and indomethacin-induced ulcer models but did not modify the gastric parameters in pylorus ligation-induced ulcer model. The polyherbal formulation is nontoxic with promising potentials for treating experimental peptic ulcer.

Acalypha godseffiana is an important plant used as an ornamental and herbs; its leaves are used in the management of diseases like diabetes in Eastern Nigeria. The study aims at linking the hypoglycemic activity extracts of leaves of A. godseffiana to their polyphenolic contents. Fresh leaves of A. godseffiana were obtainedfrom Imo State, Nigeria, identified in University of Lagos Herbarium, air-dried, pulverized and kept for investigations. The phytochemical compositions and antioxidant potentials of acetone, aqueous, ethanol and methanol extracts of A. godseffiana were determined using adopted methods. An in-vitro approach was used to evaluate the hypoglycemic potentials of the extracts on α-amylase and α-glucosidase enzymes. The mechanism of inhibitions was studied using the Lineweaver-Burk plot. Antioxidant results revealed that total antioxidant capacity of the acetone extract (IC50: 0.34 mg/mL) showed better activity compared to the standards (silymarin 0.52 mg/mL; gallic acid 0.51 mg/mL). Thehypoglycemic findings confirmed that acetone extract demonstrated strong and mild inhibitory potential against α-amylase and α-glucosidase respectively, showing concentration dependent with IC[sub.50] values of 2.33 mg/mL and 0.13 mg/mL. The observed hypoglycemic and antioxidant potentials of acetone extract of A. godseffiana correlate to its high polyphenolic contents which include phenols (133.20 mg gallic acid g[sup.-1]), flavonoid (350.60 mg quercetin g[sup.-1]) and tannins (264.67 mg catechin g[sup.-1]). The mechanisms of action exhibited by the acetone extractwere uncompetitive and mixed non-competitive which can be attributed to its inhibitory properties on α-glucosidase and α-amylase respectively. The results obtained from this study validate the acetone leaves extract of A. godseffiana as potential agent in management of sugar related disorder.

Doc number: 168 Abstract Background: The leaves and root of Flabellaria paniculata (Malpighiaceae) are frequently used in the treatment of wounds and ulcers in Nigerian folk medicine. The purpose of this study was to compare the effect of ethanolic extracts from the leaves (FPL) and root (FPR) of F. paniculata on gastric ulcers in rats. Methods: The effect of FPL and FPR (100, 200 and 400 mg/kg) was evaluated in ethanol and indomethacin gastric ulcer models. Control groups for FPL and FPR were orally treated with 3% Tween 20 and distilled water respectively. FPL was further investigated in pylorus ligation model. Misoprostol and cimetidine were used as reference. Results: FPL significantly (P < 0.05) reduced gastric lesions by 82.22% and 67.32% in ethanol and indomethacin induced ulcer models at 100 mg/kg respectively while FPR (100, 200 and 400 mg/kg) did not exert significant effect in the two models. In pylorus ligation model, FPL exerted a significant preventive antiulcer effect as indicated by reduction in gastric volume at 200 and 400 mg/kg doses. Only 400 mg/kg of the extract exerted a significant reduction in ulcer index when compared with the control group. The oral route LD50 of FPL was estimated to be 4570 mg/kg while that of FPR was 2754 mg/kg. The LD50 in intraperitoneal injection was estimated to be 1202.26 and 1380.38 mg/kg for FPL and FPR respectively. The phytochemical investigation showed that both extracts possess triterpenoids and saponin, while the presence of flavonoid was detected only in FPL. Conclusions: The results of this study indicated that FPL and not FPR is effective against experimentally induced gastric ulcers. The presence of varied phytochemical constituents probably influenced the pharmacological differences between the two extracts.

Alzheimer’s disease (AD) presents a significant global health challenge, with its prevalence expected to rise sharply in the coming years. Despite extensive research, effective treatments addressing the multifaceted pathophysiology of AD remain elusive. This study investigates the therapeutic potential of twenty-seven prolinamides (P1 – P27), with the focus on their interactions with key proteins implicated in AD pathogenesis. Four of the compounds, namely; 10-((4-nitrophenyl)prolyl)-10 H-phenothiazine (P14), 2-((4-nitrophenyl)prolyl)isoindoline (P19), 1-(4-formylphenyl)-N-(p-tolyl)pyrrolidine-2-carboxamide (P22), and N,1-bis(4-nitrophenyl)pyrrolidine-2-carboxamide (P27) showed promising potential as Alzheimer’s drug. In-silico approaches including molecular docking, molecular dynamic (MD) simulation, post md study, physicochemical and drug-likeness parameters were employed to ascertain the potential of these compounds as inhibitors of certain proteins implicated in the pathophysiology of Alzheimer’s disease. Molecular docking and dynamics simulations demonstrated that P14, P19, P22 and P27 exhibited promising binding affinities towards crucial AD-associated proteins, including Beta-Secretase 1 (BACE1), Butyrylcholinesterase (BuChE), and Tau-tubulin kinase 2 (TTBK2). Structural stability analyses revealed that prolinamides, particularly P22 and P27 for BACE1 and P14 and P19 for BuChE, exhibited greater stability than their reference ligands, indicated by lower RMSD, RoG, and RMSF values. For BuChE, Rivastigmine had a docking score of -7.0 kcal/mol, a binding free energy (ΔGbind) of -22.19 ± 2.44 kcal/mol, RMSD of 1.361 ± 0.162 Å, RMSF of 9.357 ± 3.212 Å, and RoG of 22.919 ± 0.064 Å, whereas P19 exhibited a superior docking score of -10.3 kcal/mol, a significantly better ΔGbind of -33.74 ± 2.84 kcal/mol, RMSD of 1.347 ± 0.132 Å, RMSF of 8.164 ± 2.748 Å, and RoG of 22.868 ± 0.070 Å. Physicochemical and pharmacokinetic assessments affirmed the drug-likeness and bioavailability of P19 notably capable of penetrating the blood-brain barrier. Compounds P19 and P22, emerged as multi-targeted ligands, offering the potential for simultaneous modulation of multiple AD-related pathways. These findings highlight the possibilities of these compounds to be explored as novel therapeutic agents for AD. They also highlight the need for further experimental validation to confirm their efficacy and safety profiles, advancing them toward clinical application in AD management.