Thirty-five years (1986–2021) of HIV/AIDS in Nigeria: bibliometric and scoping analysis

Background Acquired immunodeficiency syndrome (AIDS) is an acquired defect of the cellular immunity associated with the infection by the human immunodeficiency virus (HIV). The disease has reached pandemic proportion and has been considered a public health concern. This study is aimed at analyzing the trend of HIV/AIDS research in Nigeria. Method We used the PUBMED database to a conduct bibliometric analysis of HIV/AIDS-related research in Nigeria from 1986 to 2021 employing “HIV”, “AIDS”, “acquired immunodeficiency syndrome”, “Human immunodeficiency virus”, and “Nigeria” as search description. The most common bibliometric indicators were applied for the selected publications. Result The number of scientific research articles retrieved for HIV/AIDS-related research in Nigeria was 2796. Original research was the predominant article type. Articles authored by 4 authors consisted majority of the papers. The University of Ibadan was found to be the most productive institution. Institutions in the United States dominated external production with the University of Maryland at the top. The most utilized journal was PLoS ONE. While Iliyasu Z. was the most productive principal author, Crowel TA. was the overall most productive author with the highest collaborative strength. The keyword analysis using overlay visualization showed a gradual shift from disease characteristics to diagnosis, treatment and prevention. Trend in HIV/AIDS research in Nigeria is increasing yet evolving. Four articles were retracted while two had an expression of concern. Conclusion The growth of scientific literature in HIV/AIDS-related research in Nigeria was found to be high and increasing. However, the hotspot analysis still shows more unexplored grey areas in future

Synthesis of some esters of cinnamic acid and evaluation of their in vitro antidiabetic and antioxidant properties

Purpose: To synthesize various ester derivatives of cinnamic acid and to evaluate their in vitro antidiabetic and antioxidant properties. Methods: Esters of cinnamic acid were synthesized by refluxing the parent compound (cinnamic acid) with different alcohols using concentrated sulphuric acid as a catalyst. Physicochemical analyses (solubility, boiling point, refractive index) and spectrophotometric analyses (ultraviolet-visible spectroscopy (UV-VIS), Fourier-transform infrared spectroscopy (FT-IR) and gas chromatography-mass spectroscopy (GC-MS)) were carried out on the synthesized products. The antioxidant inhibitory property, uptake of glucose by yeast, and haemoglobin glycosylation of the synthesized products were also evaluated using standard methods. Results: The identities of methylcinnamate, ethylcinnamate, propylcinnamate, 2-propylcinnamate, butylcinnamate and 2-butylcinnamate were confirmed, at m/z ratios of (131,103,77 and M+ of162), (131,103,77 and M+ of 176), (147,103,77and M+ of 190), (147,103,77 and M+ of 204), (143, 103, 77 and M+ of 190), and finally (147,103,77 and M+ of 204) respectively. FT-IR results revealed the following important bonds for the synthesized compounds: C=O, C-C, C-O, C=H, C-H and adjacent H. The results for glucose uptake by yeast and of haemoglobin glycosylation test indicate that all the products facilitated the transport and detachment of glucose at varying concentrations, respectively. The DPPH scavenging activity of propylcinnamate, 2-butylcinnamate and methylcinnamate with the absorbance of 63.06, 56.85 and 53.06 at 50 μg/mL - 250 μg/mL, respectively, recorded the highest values when compared with the control (ascorbic acid). Conclusion: The results reveal that the six ester derivatives of cinnamic acid exhibit a certain degree of antidiabetic activity by facilitating the uptake of glucose by yeast and reducing glycation of haemoglobin; thus, showing a reasonable level of inhibition against free radicals

Evaluation of Annona muricata extract against Staphylococcus aureus isolate and in-silico activity of bioactive compounds against Capsular protein (Cap5O)

Abstract Background Staphylococcus aureus has prevailed against the majority of antibiotics currently in clinical use, making it a significant global public health problem. As a safer alternative, bioactive compounds have been explored. Annona muricata has been shown to possess antimicrobial activity. However, there are few reports on the molecular activity of A. muricata bioactive compounds against S. aureus. Thus, this study was aimed at evaluating the antimicrobial activity of its crude extract as well as investigating the potential of its bioactive compounds against the Cap5O capsular polysaccharides (CPS) of S. aureus via molecular docking. Methods Collection of plant leaves, preparation of extracts, anti-nutrient analysis, phytochemical screening via crude method and gas chromatography-mass spectrophotometer (GC-MS), isolation and characterization of S. aureus and the antimicrobial activity test were all done using standard protocols. Molecular docking was done using the MCULE online tool with emphasis on docking scores, toxicity, and other properties. Results Crude screening of the extracts showed the presence of polyphenols, hydroxyanthraquinones, reducing compounds, flavonoids, saponins, glycosides, alkaloids, anthraquinones, phlobatannins and tannins in different concentrations. Anti-nutrient analysis showed the presence of allowable levels of evaluated anti-nutrients. GC-MS revealed a total of twenty-nine (29) bioactive compounds, out of which only 4 (13.80%) docked without toxicity and these were bicyclo[4.1.0]heptan-2-one 6-methyl, trichloromethane, carbonic acid 2-dimethylaminoethyl propyl ester, and 1-methyl-4-phenyl-5-thioxo-1,2,4-triazolidin-3-one on either the NAD-binding or C-terminal substrate binding domain of Cap5O. Conclusion Results obtained show that Cap5O could be a potential drug target for multi-drug resistant S. aureus, however, further studies aimed at evaluating these bioactive compounds individually and in combination are highly needed

Betulinic and ursolic acids from Nauclea latifolia roots mediate their antimalarial activities through docking with PfEMP-1 and PfPKG proteins

Abstract Background Chemotherapies target the PfEMP-1 and PfPKG proteins in Plasmodium falciparum, the parasite that causes malaria, in an effort to prevent the disease’s high fatality rate. This work identified the phytochemical components of Nauclea latifolia roots and docked the chemical compounds against target proteins, and examined the in vivo antiplasmodial effect of the roots on Plasmodium berghei-infected mice. Methods Standard protocols were followed for the collection of the plant’s roots, cleaning, and drying of the roots, extraction and fraction preparation, assessment of the in vivo antiplasmodial activity, retrieval of the PfEMP-1 and PfPKG proteins, GCMS, ADME, and docking studies, chromatographic techniques were employed to separate the residual fraction’s components, and the Swis-ADME program made it possible to estimate the drug’s likeness and pharmacokinetic properties. The Auto Dock Vina 4.2 tool was utilized for molecular docking analysis. Results The residual fraction showed the best therapeutic response when compared favorably to amodiaquine (80.5%) and artesunate (85.1%). It also considerably reduced the number of parasites, with the % growth inhibition of the parasite at 42.8% (D2) and 83.4% (D5). Following purification, 25 compounds were isolated and characterized with GCMS. Based on their low molecular weights, non-permeation of the blood–brain barrier, non-inhibition of metabolizing enzymes, and non-violation of Lipinski’s criteria, betulinic and ursolic acids were superior to chloroquine as the best phytochemicals. Hence, they are lead compounds. Conclusion In addition to identifying the bioactive compounds, ADME, and docking data of the lead compounds as candidates for rational drug design processes as observed against Plasmodium falciparum target proteins (PfEMP-1 and PfPKG), which are implicated in the pathogenesis of malaria, the study has validated that the residual fraction of N. latifolia roots has the best antiplasmodial therapeutic index

Antimicrobial analysis of honey against Staphylococcus aureus isolates from wound, ADMET properties of its bioactive compounds and in-silico evaluation against dihydropteroate synthase

One of the main challenges of wound healing is infection with multi-drug resistant (MDR) bacteria such as Staphylococcus aureus. The spectrum of antibiotics used to treat them is declining; thus, there is a need for alternatives. Our study was designed to evaluate the antimicrobial properties of honey, its pharmacokinetics (ADMET) properties and in-silico analysis of its bioactive compounds against dihydropteroate synthase of S. aureus using trimethoprim as control. Methods: Standard protocols were employed in collection and preparation of samples, generation of canonical strings, and conduction of microbiological analyses. Bioactive compounds’ ADMET properties were evaluated using the SWISSADME and the MCULE toxicity checker tools. The MCULE one-click docking tool was used in carrying out the dockings. Results: The gas chromatography-mass spectrophotometry revealed twenty (20) bioactive compounds and was dominated by sugars (> 60%). We isolated a total of 47 S. aureus isolates from the wound samples. At lower concentrations, resistance to trimethoprim (95.74 to 100.00%) was higher than honey (70.21 to 96.36%). Only seven (7) isolates meet Lipinski’s rule of five and ADMET properties. The docking scores of the bioactive compounds ranged from -3.3 to -4.6 while that of trimethoprim was -6.1, indicating better binding or interaction with the dihydropteroate synthase. The bioactive compounds were not substrates to P450 cytochrome enzymes (CYP1A2, CYP2CI9 and CYP2D6) and p glycoprotein, indicating better gastrointestinal tract (GIT) absorption. Conclusion: The favourable docking properties shown by the bioactive compounds suggest they could be lead compounds for newer antimetabolites for management of MDR S. aureus