Background: Hypoestes rosea, an evergreen shrub belonging to the Acanthaceae family possess antiulcer potential amongst its several other medicinal properties, including usefulness as anti-diabetic and anti-inflammatory agents. Objective: In this study, we investigated the anti-secretory effect of aqueous leaf extract of H. rosea as the possible mechanism for its antiulcer activity in gastric ulcer induced rats. Methods: 40 rats were divided into 2 experimental phases of 20 rats each. They were further separated into 5 groups as follows: Group 1 (Normal control: rat chow and water only). Group 2 Ulcer control: Indomethacin-induced (40mg/kg bw). Group 3: Low dose (100mg/kg bw). Group 4: Medium dose (200mg/kg bw). Group 5: High dose (300mg/kg bw). Phase 1 involved determination of ulcer lesion index and % inhibition. Phase 2 involved estimation of gastric acid secretion using the method of continuous perfusion with 10minutes aliquots titrated against 0.01N NaOH. Results: Aqueous extract of Hypoestes rosea produced a significant (P<0.05) dose-dependent decrease in ulcer lesion score with an accompanying increase in percentage inhibition at the various doses used in the study (100, 200 and 300 mg/kg bw). Also, there was a significant decrease in basal and histamine-induced acid secretion at all doses with the greatest effect observed at the high dose (300mg/kg bw). Conclusion: Results obtained showed that aqueous extract of H. rosea decreased gastric acid secretion possibly due to inhibition of Histamine receptors and may thus be the mechanism for its anti-ulcer activity.
Background Escherichia coli like other Enterobactericeae are frequent isolates implicated in food-borne diseases. The prevalence of multi-drug resistant E. coli isolates from street vended fruits and its salad is on the increase across Nigeria. This study was designed to evaluate the antimicrobial activity Tetrapleura tetraptera (Uyayak) against E. coli as well as the druggability and pharmacokinetics of its bioactive compounds using in-silico and in-vitro approaches. Methods We utilized previously reported standard protocols in the isolation, characterization and the identification of the isolates, and the collection and preparation of the T. tetraptera pods. Antimicrobial activity of the extracts was done using the Kirby-Bauer disc diffusion method. Resulting bioactive compounds from gas chromatography coupled to mass spectrophotometry (GC-MS) were converted into canonical stings and used to for target prediction in humans and ADMET properties using the SWISSADME and pkCSM tools. Bioactive compounds that met Lipinski’s rule of five (ROF) were subjected to molecular docking against dihydropteroate synthase of E. coli using the AutoDock vina tool and the resulting interactions visualized in 2-D via Biovia Discovery Studio 21. Results The GC-MS analysis returned a total of twenty-eight (28) bioactive compounds. The abundance of the E. coli isolates varied according to location and fruit types. At trimethoprim and extracts concentrations of < 100mg/ml and < 100% respectively, the isolates showed resistance. A total of 13 bioactive compound showed zero violations to Lipinski’s rule of five (ROF). ADMET analysis of the screened bioactive compounds showed favourable absorption (intestinal and water solubility) and toxicity (AMES and hepatoxicity) profiles than trimethoprim. Molecular docking revealed various amino residues interacting with dihydropteroate synthase and gave docking scores that ranged from − 4.0 to -5.3 kcal/mole for the bioactive compounds and − 6.5 5 kcal/mole for trimethoprim. Target prediction showed that all the bioactive are capable of reaching various targets with nuclear receptor being the most abundant target. Conclusion The bioactive compounds of T. tetraptera examined in this study showed favourable antimicrobial activity against E. coli, docking scores and pharmacokinetics, suggesting the need for further studies to validate their potential as antimetabolites for management of pathogenic E. coli infections.
Hyperuricemia is associated with ATDs, with treatment duration being a significant factor. The disorder should be closely monitored, especially during the intensive phase of treatment.
Objectives: Resistance of Gram-negative bacilli (GNB) to antimicrobial agents is increasing worldwide. This is fast becoming a serious public health concern as these bacteria display multiple antibiotic resistance mechanisms. This study was aimed at evaluating antibiotic resistance profiles of GNB from clinical samples in Cross River State, Nigeria. Material and Methods: Urine and stool samples of 600 randomly selected participants were analyzed. Samples were inoculated onto CLED agar and selenite-F broth, respectively, and enriched bacterial growth in selenite-F broth was subcultured on deoxycholate citrate agar. Gram stain procedure was used to determine the Gram reaction of isolates and identification was carried out using the Microbact 24E GNB identification kit. Antibiotic susceptibility testing was performed using the Kirby–Bauer disk diffusion method. Multiple antibiotic resistance indices (MARIs) for each isolate were calculated. Data analysis was carried out using Microsoft Excel Package 2016 and GraphPad Prism version 6. Results: A total of 129 non-repetitive GNB were isolated and categorized by their ability to ferment sugars. The lactose-fermenting Enterobacteriaceae (LFE) were the most predominant isolates (32 Klebsiella pneumoniae and 25 Escherichia coli). There were 50 non-sugar-fermenting Gram-negative bacilli (NSF-GNB) comprising Pseudomonas spp. (28), Acinetobacter spp. (15), Burkholderia cepacia (3), and one isolate each of Tatumella ptyseos, Alcaligenes faecalis, Aeromonas hydrophila, and Stenotrophomonas maltophilia. Non-lactose-fermenting Enterobacteriaceae comprised Proteus spp. (14), Providencia stuartii (4), and Serratia rubidaea (4). Antimicrobial susceptibility test results showed that tetracycline was the least effective with 71.3% of isolates showing resistance. About 65% of LFE and 95.5% of non-lactose-fermenting Enterobacteriaceae (NLFE) showed resistance to tetracycline. Resistance of all isolates to tigecycline, a member of a new class of antibiotics, was 31% (40/129); however, all isolates of E. coli, S. rubidaea, and Acinetobacter spp. were susceptible to tigecycline. Resistance profiles of LFE to tested antibiotics showed comparable resistance levels for ceftriaxone and tetracycline between K. pneumoniae and E. coli. However, the resistance of K. pneumoniae to ceftazidime, ciprofloxacin, and tigecycline was 50%, 44%, and 13% compared with E. coli – 32%, 32%, and 0%, respectively. E. coli showed, on average, higher resistance levels to carbapenems compared with K. pneumoniae. Among NLFE, Proteus spp. was more resistant than P. stuartii to cephalosporins, quinolones, and tigecycline. In contrast, P. stuartii isolates were twice as resistant to the carbapenems as Proteus spp. Except for ciprofloxacin, tetracycline, and gentamicin, S. rubidaea was susceptible to all other antibiotics. Among NSF-GNB, Acinetobacter spp. was the most resistant to all other carbapenems, except ertapenem. Pseudomonas spp. were the most resistant to fluoroquinolones. The mean of the total MARI was 0.45 ± 0.26, with 54.3% (70/129) of isolates having MARI above the total mean. About 73% (95/129) of the total GNB had MARI above 0.2. Multidrug resistance in Enterobacteriaceae, Pseudomonas aeruginosa, and Acinetobacter species was 53.2%, 100%, and 93.3%, respectively. Conclusion: The high level of antibiotic resistance of GNB, especially by NLFE and NSF-GNB, portends great danger for the health sector as these organisms are opportunistic pathogens and pose serious health risks as nosocomial pathogens and community-acquired pathogens in immunosuppressed individuals.
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