Analysis of the oxidative stress inhibition potentials of Artemisia annua and its bioactive compounds through in vitro and in silico studies

Oxidative stress overwhelms the antioxidant mechanisms of living systems, with active involvement in the pathogenesis of several diseases. Natives of Gangnim in the Plateau State of Nigeria may be unknowingly endowed with some protective advantages against oxidative stress for their habitual consumption of Artemisia annua tea. The antioxidant activities of A. annua extracts were determined using in vitro methods and the inhibitory potentials of twenty-nine (29) bioactive compounds of the plant against oxidative stress target proteins were assessed through molecular docking analysis. These extracts showed significantly high activities in scavenging nitric oxide, 2,2-diphenyl-1-picrylhydrazyl (DPPH) and reducing ferric (Fe3+) to ferrous (Fe2+) iron. Virtually, none of the bioactive compounds binds to the active site of the antioxidant protein targets. Rather, 72.41, 93.10 and 75.86% of these compounds bind with high binding affinity to the activator binding sites of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and catalase (CAT) respectively. 7,8-dimethylalloxazine (-8.10 kcal/mol) ranked highest as a prospective inhibitor of xanthine oxidase (XOX). The antioxidant activity exhibited by the extracts of the locally cultivated A. annua and the molecular interactions of its bioactive compounds against the protein targets used predict that oxidative stress inhibition could be effectively achieved with these phytochemicals.

Herbal mouthwash formulated with the leaf extract of Jatropha gossypiifolia Linn. (Euphorbiaceae) exhibited in vitro antimicrobial activity against selected oral pathogens

Increase in the incidence of oral disease, resistance to antibiotics and adverse effect to synthetic medicines has made search for alternative safe, effective and cheaper treatment options imperative, preferably from plant sources. This study evaluated the antimicrobial profile of ethanol extracts of leaf and root bark of Jatropha gossypiifolia and mouthwash formulation containing the leaf extract. Extraction of plant parts was done by cold maceration with 70% ethanol. The antimicrobial activities of the extracts and the formulated mouthwash were evaluated againstStaphylococcus aureus, Escherichia coli, Klebsiella pneumonia, Bacillus subtilis and Candida albicans using Agar well diffusion method. The minimum inhibitory concentration of the extracts on susceptible organisms was determined according to the Clinical Laboratory Standards Institute protocol. The physicochemical parameters of the formulated mouthwash were assessed using standard methods. J. gossypiifolia leaf and root bark extracts exhibited a concentration dependent antimicrobial activity and MIC ranging from 50 to 260 mg/ml against test organisms. The formulated herbal mouthwash showed effective antimicrobial activity and suitable cosmetics properties. This study indicates that the leaf extracts of J. gossypiifolia possess bioactive metabolites with strong antimicrobial activities and its herbal mouthwash formulation has potential in the treatment of various diseases caused by oral pathogens.

Exploring patients’ viewpoints on uncomplicated malaria and its management in primary healthcare facilities of Plateau State, Nigeria: a qualitative study

Malaria infection is a major public health problem in Nigeria. The present study explored patients’ thoughts and feelings on uncomplicated malaria and its management practices in some primary healthcare (PHC) facilities of Plateau state, Nigeria. An in-depth interview was conducted on patients receiving treatment in some of the facilities in the state, who were recruited through purposive sampling method up to saturation point. All the information was audio-recorded and transcribed verbatim before analysis using the principles of thematic content analysis of inductive method. Generally, their views on malaria-related issues were categorised into four main themes based on their relevancies as: patients’ perceptions on malaria infection and anti-malarial drugs, the role of healthcare workers and family during treatment, medications taken and socio-economic-related factors, as well as their general views on healthcare facilities-related factors. The study showed patients’ perceptions of the aforementioned factors as influencing their treatment and management practices of the disease in the study area. Necessary interventions that would improve patients’ quality of management of the disease toward achieving the desired outcome of therapy are recommended.

Anti-trypanosomal, antioxidant and antimicrobial activities of the fruiting bodies of Ganoderma lucidum (W. Curt.: Fr) (Ganodermataceae) aqueous extract

Human African Trypanosomiasis (HAT) infection is caused by sub species of Trypanosoma brucei. The clinically licensed drugs have unacceptable toxicities and variable efficacies. The prognosis is influenced by the level of circulating free radicals and opportunistic infections. Many plants have been screened for activity in different models of HAT but the same is not true of mushrooms. This study screened the aqueous extract of the fruiting bodies of Ganoderma lucidum for trypanocidal, antioxidant and antimicrobial activities. Fruiting bodies of the mushroom were extracted sequentially with n – hexane, ethyl acetate, absolute ethanol and distilled water. The extracts were screened for phytochemical constituents and in vitro trypanocidal activity, the most active of which was further subjected to in vivo trypanocidal, anti-oxidant and anti-microbial screening. Alkaloids, carbohydrates, flavonoids, saponins and anthraquinones were present. In vitro trypanocidal screening showed the aqueous extract as the most active (IC50 = 14.65 μg/μl). It also dose-dependently inhibited parasitaemia and prolonged survival in parasite - infected mice (50, 100, 200 and 400 mg/kg). DPPH radical scavenging activity gave an IC50 of 131.00 ± 0.03 mg/ml. The extract demonstrated broad spectrum antimicrobial activity at 250 mg/ml. The fruiting bodies of G. lucidum is a potential source of trypanocidal compounds.

Central nervous system depressant activity of fractions of Globimetula braunii Engl. (Loranthaceae) growing on Terminalia catappa L. (Combretaceae) and isolation of lupeol

Globimetula braunii is a parasitic plant belonging to the family Loranthaceae. Traditionally, the plant has been reported to be used in the treatment of insomnia. The study was carried out to investigate the central nervous system (CNS) depressant activity of the fractions of Globimetula braunii growing on Terminalia catappa and to isolate the phytochemical compound(s) present in the most active fraction. The CNS depressant activity of all the fractions was investigated using diazepam induced sleep. The most active fraction was further subjected to the hole board test and beam walk assay. The chromatographic technique was used for the isolation of phytochemical compound. Hexane fraction significantly (p<0.05) reduced latency to sleep and prolonged the sleeping time. Both chloroform and ethylacetate fractions at highest and median doses showed significant increase in the duration of sleep compared to normal saline. The n-butanol fraction at all doses tested do not have any effect on time of onset and duration of sleep when compared with normal saline treated group. Hexane fraction significantly (p<0.05) decreased the number of head dip in a dose dependent manner and delayed the time to reach the goal box compared to normal saline treated group. Lupeol was isolated from n-hexane fraction.

Quality assessment of nine brands of metformin hydrochloride tablets marketed in Abuja, Nigeria

Metformin is a drug of first choice in management of type II diabetes mellitus and the Nigerian market is flooded with many brands of metformin tablets. The aim of this study is to assess the pharmaceutical quality of nine brands of metformin tablets circulating in pharmacy outlets in Abuja. The brands were assessed for uniformity in weight, hardness, friability, disintegration time and in vitro dissolution using official methods. The content of active ingredient was also determined spectrophotometrically. All the brands had weights within the official limits, hardness was found to differ across the brands with values ranging between 1.20 and 11.50 kgF. Friability values were between 0.00 and 2.25%, disintegration time was between 2.06 and 10.36 min and within official specifications for film-coated tablets. Drug release within 60 min was between 93 and 103%, however, one of the brands fell outside the lower limit of the official specification and therefore, failed the dissolution test. Similarly, all but one of the brands were within the official specification of the percent content of active ingredient. The results highlight the need to routinely carry out market surveillance on drug products so as to safeguard the health of patients.

Use of Rasch Wright map to understand the quality of Healthcare Workers’ Knowledge, Attitudes, and Practices for Uncomplicated Malaria (HKAPIUM)

The present study assessed the dimensionality and item difficulty targeting to person ability of HKAPIUM scale using Rasch Wright map approach. A HKAPIUM instrument (Cronbach’s alpha = 0.71) containing eighteen (18)-items was administered to 121 trained healthcare professionals involved in the management of uncomplicated malaria in 24 selected primary health care (PHC) facilities in Plateau state, Nigeria. The respondents filled and returned the instrument and the data was analyzed using Bond&Fox software®. The Rasch principal components analysis (Rasch-PCA) of the item residuals indicated variance explained values of 52 (knowledge), 41.1 (attitudes), and 55.4 (practices) and eigenvalues of the first contrast as 1.2, 1.8, and 1.5, respectively, which were within acceptable values thatindicated the unidimensionality of the three constructs of the HKAPIUM scale. The result showed moderate items difficulty levels for all the three constructs. The mean person ability levels of respondents with-respect-to knowledge-related items were low, while their mean person ability levels in endorsing the attitudes and practices-related items were good. The study revealed unidimensionality of the 3 constructs of HKAPIUM scale, with observed mismatch between item difficulty levels of the constructs with most of the person ability levels of the respondents.

Evaluation of knowledge, attitudes and practices of human healthcare students about antimicrobial drug use and resistance: a cross-sectional study in University of Maiduguri, Nigeria

Inappropriate consumption of antimicrobial drugs is the main cause of antibiotic resistance which is currently the most critical global public health challenge. This research aimed to evaluate knowledge, attitudes, and practices of antimicrobial drug use and resistance among 576 students. Data were collected through a questionnaire. Descriptive analyses were performed to characterize the sampled population. Ethical clearance and students’ informed consent were obtained. Most of the students were within the age range of 21-25 years and have excellent knowledge of antimicrobial use. Also, most of them had very good knowledge of antimicrobial resistance. From the data analysed 445 (77.3%) agreed that students should get special training on the use of antimicrobials; 120 (20.8%) students agreed that education on the use of the antimicrobial drugs is necessary; 115 (20.0%) believed that prohibiting the use of antimicrobials without a valid prescription is a solution. The knowledge level on antimicrobial drug use and resistance was excellent 329 (57.1%). Most of the students' attitude as regards the usage of antimicrobials was found to be average. High rates of incorrect antimicrobial usage practices were noticed and the attitude was average. The development of an effective antimicrobial stewardship program is a necessity.

One-pot synthesis of N-benzyl-2-aminobenzoic acid, via ring opening of isatoic anhydride derivative, and its antibacterial screening

2-(N-Benzyl) amino benzoic acid is a bifunctional molecule that could be produced from the reaction between isatoic anhydride and aryl halide. Analogues and derivatives of isatoic anhydride have wide application in pharmaceuticalsincluding antibacterial activity. The aim of this study is to synthesize, characterize and screen N-benzyl isatoic anhydride and 2-(N-benzyl) amino benzoic acid for antibacterial activity. The reaction of isatoic anhydride and benzyl bromide in the presence of potassium carbonate in DMSO at room temperature yielded N-benzyl isatoic anhydride, which under hydrolysis yielded 2-(N-benzyl) amino benzoic acid in which the anhydride ring is opened up. This compound was screened against Gram positive and negative bacteria. Moderate yield of 2-(N-benzyl) amino benzoic acid, a yellow crystal (melting point of 160-162oC, percentage yield 65 %, Rf 0.19) formed by ring opening of N-benzyl isatoic anhydride. The compound showed no antibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas pyocyanea, Salmonella typhimurium, Klebsiella aeruginosa and Bacillus subtilis. 2-(N-benzyl)amino benzoic was synthesized, characterized and showed no activity against bacteria.

Time-kill kinetics and antibacterial activity of root extract of Adenodolichos paniculatus (Hua) Hutch & Dalz (Fabaceae)

Medicinal plants have been used in treatment of illness from time immemorial. Adenodolichos paniculatus is a medicinal plant used for traditional remedy of sore throat infections. This study therefore, evaluated the antibacterial activities of the root extracts and time-kill kinetics of the most potent extract. Five extracts, obtained by maceration using n-hexane, chloroform, ethyl acetate, methanol and water sequentially were evaluated for antibacterial activities and time-kill kinetics against Streptococcus pyogenes, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Chloroform root extract at 100 mg/ml was active against Streptococcus pyogenes, Staphylococcus aureus and Pseudomonas aeruginosa with zones of inhibition 25.00, 21.00 and 14.75 mm respectively but not against Escherichia coli. Minimum inhibitory concentrations were 1.56, 6.25 and 25.00 mg/ml respectively and the minimum bactericidal concentrations were 3.12, 12.50 and 50.00 mg/ml. Complete elimination of S. pyogenes, S. aureus and P. aeruginosa was achieved at concentrations 1.56 mg/ml, 6.25 mg/ml and 25.00 mg/ml within 300, 720 and 960 minutes exposure respectively and at concentrations 3.12 mg/ml, 25.00 mg/ml and 50.00 mg/ml within 180, 300 and 720 minutes exposure respectively. Chloroform root extract has the potential to be used as antibacterial agent and was better than the other solvent extract two-fold. Keywords: Adenodolichos paniculatus; Antibacterial activity; Time-kill kinetics; Percentage reduction, Log reduction