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1.
Drug Des Devel Ther ; 18: 597-612, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38436040

RESUMO

Purpose: New bioactive anthraquinone derivatives are investigated for antibacterial, tyrosinase inhibitory, antioxidant cytotoxic activity, and molecular docking. Methods: The compounds were produced using the grindstone method, yielding 69 to 89%. These compounds were analyzed using IR, 1H, and 13C NMR and elemental and mass spectral methods. Additionally, the antibacterial, antioxidant, and tyrosinase inhibitory activities of all the synthesised compounds were evaluated. Results: Compound 2 showed remarkable tyrosinase inhibition activity, with an (IC50: 13.45 µg/mL), compared to kojic acid (IC50: 19.40 µg/mL). It also exhibited moderate antioxidant and antibacterial activities with respect to the references BHT and ampicillin, respectively. Kinetic analysis revealed that the tyrosinase inhibitory activity of compound 2 was non-competitive and competitive, whereas that of compound 1 was low. All compounds (1-8) were significantly less active than doxorubicin (LC50: 0.74±0.01µg/mL). However, compound 2 affinity for the 2Y9X protein was lower than kojic acid, with a lower docking score (-8.6 kcal/mol compared to (-4.7 kcal/mol), making it more effective. Conclusion: All synthesized compounds displayed remarkable antibacterial, tyrosinase inhibitory, antioxidant, and cytotoxic activities, with compound 2 showing exceptional potency as a multitarget agent. Anthraquinone substituent groups may offer the potential for the development of treatments. The derivatives were synthesized using the grindstone method, and their antibacterial, antioxidant, tyrosinase inhibitory, and cytotoxic activities were inspected. Molecular docking and molecular dynamics simulations were performed using compound 2 and kojic acid to validate the results and confirm the stability of the compounds.


Assuntos
Agaricales , Antineoplásicos , Ciclopentanos , Monofenol Mono-Oxigenase , Simulação de Acoplamento Molecular , Antioxidantes/farmacologia , Cinética , Antibacterianos/farmacologia , Antraquinonas/farmacologia
2.
PLoS One ; 18(12): e0284505, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38085717

RESUMO

BACKGROUND: Anemia is a significant public health problem in HIV/AIDS patients worldwide. This study is aimed to determine the prevalence of anemia and its risk factors among HIV-infected adults in Sawla General Hospital, southern Ethiopia. METHODS: A facility-based cross-sectional study involving HIV-infected adults was conducted in ART clinic of Sawla General Hospital from April 01 to May 31, 2019. A systematic random sampling technique was employed to recruit the study participants. Socio-demographic and clinical data were collected using a structured questionnaire and checklist. Hemoglobin concentration from venous blood was determined by HemoCue® 301 analyzer. Descriptive and inferential statistics, by Statistical Package for Social Science version 26.0, were applied; p-values ≤ 0.05 in the multivariable logistic regression analysis were considered statistically significant. RESULTS: A total of 220 HIV-infected adults participated in this study. The prevalence of anemia was 38.6%, from which 90.6, 7.1, and 2.3% are mild, moderate, and severe anemia, respectively. Anemia among HIV-infected adults was significantly associated with CD4 cell count below 200 cells/mm3 (AOR: 4.32; 95% CI: 2.10-8.86), clinical stage III or above (AOR: 4.20; 95% CI: 1.06-16.62), five or more years duration of HIV infection (AOR: 2.32; 95% CI: 1.08-4.94) and BMI below 18.5 kg/m2 (AOR: 3.82; 95% CI: 1.83-8.00). CONCLUSION: Anemia is a moderate public health problem among the study population. Longer duration of HIV infection, advanced clinical stage, lower CD4 cell count, and BMI are risk factors for anemia. Therefore, early ART enrolment for HIV-infected adults with nutritional support and rigorous monitoring of CD4 cell count are essential to lower the prevalence.


Assuntos
Anemia , Infecções por HIV , Adulto , Humanos , Infecções por HIV/complicações , Infecções por HIV/epidemiologia , HIV , Estudos Transversais , Hospitais Gerais , Etiópia/epidemiologia , Prevalência , Fatores de Risco , Anemia/complicações , Anemia/epidemiologia
3.
Infect Drug Resist ; 16: 6405-6426, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37789841

RESUMO

Background: Bacterial otitis media (OM) is a common infection among the pediatric community worldwide and is the first reason for prescribing antibiotics in pediatric practices. However, if not promptly diagnosed and appropriately treated, it may persist and cause severe intra- and extra-cranial hard-to-cure complications. Hence, knowing the magnitude, etiology, and antibiotic susceptibility profile is very important for the proper management. Methods: A cross-sectional study was carried out in 312 pediatrics (1 to 18 years) attending the Ear Nose Throat outpatient departments of the two title hospitals from 25 February to 30th August 2022. Patients were chosen through a systematic random sampling method. Data were obtained by means of a semi-structured questionnaire. Samples were collected to identify the causative bacteria as per microbiological guidelines. The antibiotic susceptibility test was done according to the Kirby-Bauer disc diffusion; SPSS version 25 was used for the analysis. Results: The overall prevalence of otitis media was 67.3% (n=210); CSOM showed a slight preponderance (n=107) Gram-negative bacteria and Gram-positive bacteria were present in 59.8% (n=137) and 40.1% (n=92), respectively. Otitis media was predominantly caused by S. aureus (n=52, 56.5%), followed by Proteus spp. (n=33, 24%). Gram-negative bacteria were highly resistant to co-trimoxazole, amoxicillin-clavulanic acid, piperacillin, and tetracycline, whereas their positive counterparts were considerably penicillin and co-trimoxazole resistant. Overall, 61.5 and 19.2% of the isolates were MDR and XDR, respectively. MRSA, MR-CoNs, and VRE were 38.4% (n=20), 17.1% (n=5), and 58.3% (n=12), respectively; 19.7% (n=25) of Gram-negative bacteria produced ESBL, and 7% (n=9) were carbapenem-resistant. History of exposure to loud noise [AOR=3.4; CI=1.14-10.23; P-value=0.028] and family history of smoking at home [AOR=2.9; CI=1.18-7.25; P-value=0.020] have the greatest odds of otitis media. Conclusion: Overall, the prevalence of otitis media is showing an upward trend, and MDR among bacterial isolates is increasing alarmingly.

4.
J Health Popul Nutr ; 42(1): 46, 2023 05 26.
Artigo em Inglês | MEDLINE | ID: mdl-37231498

RESUMO

BACKGROUND: Microbial contamination of baby bottle food has been identified as a significant public health concern, especially in developing countries, but it remains overlooked. Therefore, this study aimed to determine microbiological hazards, compliance with hygiene practices, and critical control points of contamination in baby bottle food in Arba Minch, southern Ethiopia. OBJECTIVE: To evaluate the bacteriological quality and prevalence of foodborne pathogens in baby bottle food and to identify associated factors among bottle-fed babies attending three government health institutions in Arba Minch, southern Ethiopia. METHODS: A cross-sectional study was conducted between February 24 and March 30, 2022. A total of 220 food samples, comprising four types prepared with different sources of materials, were collected from systematically selected bottle-fed babies attending health facilities. The data on sociodemographic characteristics, food hygiene, and handling practices were solicited by face-to-face interview using a semi-structured questionnaire. Food samples (10 mL) were quantitatively analyzed for total viable counts (TVC) and total coliform count (TCC) and qualitatively for the presence of common foodborne bacterial pathogens. Data were analyzed using SPSS; ANOVA and multiple linear regression analyses were done to identify factors influencing microbial counts. RESULTS: Results revealed that the means and standard deviations of TVC and TCC were 5.3 ± 2.3 log10 colony forming units (CFU)/mL and 4.1 ± 2.6 log10 CFU/mL, respectively. Of the various food samples analyzed, 57.3 and 60.5% had a TVC and TCC above the maximum acceptable limits, respectively. The result of the ANOVA showed that there was a significant difference in the mean score of TCV and TCC among the four types of food samples (p < 0.001). Enterobacteriaceae were found in the majority of positive food samples (79.13%), followed by Gram-positive cocci (20.8%). Salmonella spp., diarrheagenic Escherichia coli, and Staphylococcus aureus were the common foodborne pathogens detected in 8.6% of tested foods. The regression result revealed that the type of baby food, hand washing practices of mothers or caregivers, and sterilizing and disinfecting procedures of feeding bottles are independent determinants of bacterial contamination (p < 0.001). CONCLUSION: The high microbial load and the presence of potential foodborne bacterial pathogens in the bottle food samples analyzed indicate unsanitary practices and the potential risk of exposure to foodborne pathogens in bottle-fed babies. Thus, interventions such as educating parents about proper hygiene practices, sterilizing feeding bottles and limiting bottle feeding practices are critical to reducing the risk of foodborne to bottle-fed infants.


Assuntos
Mães , Salmonella , Feminino , Lactente , Criança , Humanos , Etiópia/epidemiologia , Estudos Transversais , Escherichia coli , Instituições de Assistência Ambulatorial
5.
Molecules ; 26(21)2021 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-34771072

RESUMO

The synthesis of nanoparticles is most important in the context of cancer therapy, particularly copper nanoparticles, which are widely used. In this work, copper(II)-tyrosinase was isolated from potato peel powder. Copper nanoparticles (Tyr-Cu(II)-AEEA NPs) were synthesized via the reaction of tyrosinase with N-aminoethylethanolamine to produce Cu(II)-NPs and these were characterized by means of FT-IR, UV-Spectroscopy, XRD, SEM, TEM and a particle size analyzer. These Tyr-Cu(II)-AEEA NPs were tested as anticancer agents against MCF-7 breast cancer cells. Fluorescence microscopy and DNA fragmentation were also performed, which revealed the inhibiting potentials of Cu(II)-AEEA NPs and consequent cell death; Tyr-Cu(II)-AEEA NPs show potential cytotoxicity activity and this nano material could be contemplated as an anticancer medicament in future investigations.


Assuntos
Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Cobre/farmacologia , Etanolaminas/farmacologia , Nanopartículas Metálicas/química , Monofenol Mono-Oxigenase/metabolismo , Solanum tuberosum/metabolismo , Antineoplásicos/química , Antineoplásicos/metabolismo , Proliferação de Células/efeitos dos fármacos , Complexos de Coordenação/química , Complexos de Coordenação/metabolismo , Cobre/química , Cobre/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Etanolaminas/química , Etanolaminas/metabolismo , Feminino , Humanos , Células MCF-7 , Microscopia de Fluorescência , Solanum tuberosum/química
6.
Infect Drug Resist ; 14: 2883-2894, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34335034

RESUMO

INTRODUCTION: Catheter-associated urinary tract infections (CAUTIs) are the most common nosocomial infection and a leading cause of morbidity. The aim of this study was to determine the prevalence, associated factors and antibiogram of the bacterial isolates among CAUTIs patients. METHODS: A facility-based, cross-sectional study was conducted from March to December 2019 at Arba Minch General Hospital, Southern Ethiopia. Clinical and socio-demographic data were obtained using a questionnaire. Clean catch midstream urine samples were collected and inoculated onto blood agar, MacConkey agar, and cysteine lactose electrolyte deficient agar (CLED). The inoculated culture media were incubated in an aerobic atmosphere at 37°C for 24 h. After overnight incubation, the bacterial growth on the respective media was inspected visually and graded for the presence of significant bacteriuria. A significant bacteriuria was considered, if pure culture at a concentration of ≥105 colony forming unit (CFU)/mL. All isolates were further identified using colony morphology and biochemical tests. Antimicrobial sensitivity was determined by modified Kirby-Bauer disc diffusion method. Data were analyzed using SPSS version 25. P-value less than 0.05 was used as statistical significance. RESULTS: The overall incidence of symptomatic CAUTIs was 39/231 (16.8%). Independent predictors of CAUTIs were prolonged (≥7 days) catheterization (AOR = 3.6, 95% CI = 1.0-12.2), diabetes mellitus (AOR = 5.3, 95% CI = 1.4-19.6) and insertion of catheter in surgical ward (AOR = 3.6, 95% CI = 1.08-12.28). The most common bacterial isolates were E. coli 17/42 (40.5%), Klebsiella species 9/42 (21.4%) and Enterococcus species 5/42 (11.9%). High (>80%) drug resistance was observed against cotrimoxazole, cefoxitin and tetracycline. Ciprofloxacin and nitrofurantoin were the most active drugs. The overall prevalence of MDR among isolates was 37/42 (88.1%). Most bacterial isolates 30/42 (71.4%) were biofilm producers. CONCLUSION: High levels of drug resistance were observed to commonly used antibiotics. In our study, biofilm-producing bacterial isolates were the predominant cause of CAUTIs. Therefore, continuous surveillance of antimicrobial resistance patterns is necessary to help physicians in treatment and management of CAUTIs.

7.
Mol Divers ; 23(1): 35-53, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29974311

RESUMO

Novel pyrazolidine-3,5-dione derivatives (2a-g, 4a-g, and 6a-g) were synthesized by an easy-to-perform Mg(II) acetylacetonate-catalyzed reaction with high yields using water as the reaction medium. Synthesized compounds were screened for anticancer and antimicrobial activities. The compound 6c (LD50 19.1 µg/mL) showed anticancer activity higher than that of all other compounds against MCF-7 breast cancer cell line. Results of antimicrobial activities revealed that the compound 4d (MIC 0.5 µg/mL) had higher activity than ciprofloxacin against Staphylococcus aureus, whereas the compound 2b (MIC 0.5 µg/mL) had higher activity than clotrimazole against Candida albicans. Overall results of this study envisaged that the compounds 2b, 4d, and 6c have the potential to be developed as anticancer and antimicrobial agents. Novel pyrazolidine-3,5-dione derivatives (2a-g, 4a-g, and 6a-g) were synthesized via an easy-to perform Mg(II) catalysis in water medium. The synthesized compounds were screened for anticancer and antimicrobial activities.


Assuntos
Anti-Infecciosos/síntese química , Antineoplásicos/síntese química , Pirazóis/síntese química , Anti-Infecciosos/farmacologia , Antineoplásicos/farmacologia , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Catálise , Humanos , Células MCF-7 , Magnésio/química , Testes de Sensibilidade Microbiana , Pirazóis/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento , Relação Estrutura-Atividade , Água/química
8.
Open Microbiol J ; 12: 163-171, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29997701

RESUMO

BACKGROUND: Tuberculosis (TB) is an extremely contagious disease detrimentally affecting virtually every organ, most importantly the lungs. Pulmonary complications have been one of the commonest causes of morbidity and mortality since the advent of AIDS (Acquired Immune Deficiency Syndrome) pandemic. The AIDS virus has considerably reshape the epidemiology of TB by widening the risk of reactivating latent TB, increasing the possibility of TB infection once contracted to tubercle bacilli (re-infection) and by elevating the risk of rapid progression instantly after the infection. In this background, this study is intended to understand the prevalence of pulmonary tuberculosis and associated factors amongst Human Immunodeficiency Virus (HIV) positive patients attending antiretroviral therapy (ART) clinic in Arba Minch General hospital during the study period (March to May, 2016). METHODS: A cross-sectional study was carried out at Arba Minch Hospital from March to May, 2016. To assess the associated factors, a pre-tested structured questionnaire has been used. Sputum samples were collected and examined microscopically by using acid fast staining. The data was analyzed using Statistical Package for Social Services, version 20. RESULTS: Totally, 291 HIV positive patients were included in this study of which 71.5% were females and 28.5% were males. It was found that 42.3% of respondents were in the age ranged between 31-40 years. Of the 291 patients screened, 21 were positively diagnosed with pulmonary TB making the overall prevalence rate of 7.2%. From this study, it was revealed that CD4 count, previous history of tuberculosis and smoking were the significant predictors of tuberculosis (p˂0.05) in HIV patients. CONCLUSION: The results of the present study envisaged that the prevalence of HIV/TB co-infection was 7.2%. Previous history of TB, CD4 count less than 200/µl, and smoking habit were the possible risk factors elucidated. Therefore, TB screening among HIV-positive patients, public awareness, and community mobilization should be encouraged.

9.
Open Microbiol J ; 11: 352-359, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29399216

RESUMO

BACKGROUND: Controlling infectious disease using medicinal plants is the oldest healthcare known to mankind. Regardless of the enormous advances observed in modern medicine, medicinal plants are still playing vital roles. However, only a small proportion of medicinal plants are examined for bioactive compounds which may vary in different factors. This study aimed to evaluate phytochemical constituent and antimicrobial activities of Nicotiana tabacum L. extracted by different solvents against three set of bacteria. METHODS: Nicotiana tabacum L. was collected from the Western Ethiopia and extracted in seven organic solvents. An in-vitro anti-bacterial activity of plant extracts was carried out by agar well diffusion assay against microbial type culture collection of human pathogens, clinical bacterial isolates, and biofilm forming bacteria. Gas Chromatographic and Mass Spectroscopic (GC-MS) analysis was used to determine the phytochemical constituents. RESULTS: Antimicrobial activities of plant extract vary by extraction solvents; and ethyl acetate based extracts showed better antimicrobial activities. Of the experimental organisms, biofilm forming uropathogens were the most sensitive while clinical isolates were quite resistant. Analysis of the active ethyl acetate extract by GC-MS evinced a mixture of five volatile compounds; and Pyridine, 3-(1-methyl-2-pyrrolidinyl)-, (S) was the major compound detected. The overall results of the present study revealed that N. tabacum L extract has high antimicrobial activities against biofilm forming uropathogens. CONCLUSION: High antimicrobial activity was observed in ethyl acetate extract of N. tabacum against the biofilm forming bacteria whereas the clinically isolated bacteria were the most resistant group. The antibacterial property demonstrated could be due to Pyridine, 3-(1-methyl-2-pyrrolidinyl)-(S) with a broad spectrum of activity.

10.
Bioorg Med Chem Lett ; 27(1): 66-71, 2017 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-27889456

RESUMO

A simple and convenient one-pot four-component synthesis of morpholine-connected pyrazolidine derivatives 2a-f and 4a-f was developed using direct metal-free catalysis, with the identities of the synthesized compounds confirmed by IR, NMR (1H and 13C), mass spectrometry, and elemental analysis. The prepared compounds were inspected for antimicrobial, antioxidant, and cytotoxic activities. Antimicrobial and antifungal activities against five bacterial and four fungal pathogens, respectively, were investigated using the disc diffusion technique. In antibacterial activity, compounds 2d and 2f (MIC=2µg/mL) exhibited significantly higher activity than the standard ciprofloxacin. The results of antifungal assay showed that the activity of compound 4a (MIC=0.5µg/mL) was significantly higher than the standard clotrimazole. Antioxidant activity was screened based on ABTS+ radical scavenging and linoleic acid peroxidation performance. Compound 4a showed substantial antioxidant (91.3%) activities, as compared with the Trolox standard. Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for 2b (GI50=12.2µm) and 4a (GI50=07.8µm).


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Morfolinas/farmacologia , Pirazóis/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Antioxidantes/síntese química , Antioxidantes/química , Bactérias/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Fungos/efeitos dos fármacos , Células HeLa , Células Hep G2 , Humanos , Células MCF-7 , Testes de Sensibilidade Microbiana , Estrutura Molecular , Morfolinas/síntese química , Morfolinas/química , Pirazóis/síntese química , Pirazóis/química , Relação Estrutura-Atividade
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