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1.
BMC Public Health ; 23(1): 642, 2023 04 04.
Article in English | MEDLINE | ID: mdl-37016374

ABSTRACT

BACKGROUND: Postnatal care (PNC) is crucial for maternal and newborn health. Healthcare-seeking practices within the postpartum period help healthcare providers in early detection of complications related to childbirth and post-delivery period. This study aims to investigate trends of PNC utilization from 2006 to 2018, and to explore the effects of multi-level determinants of both maternal and newborn PNC in Pakistan. METHODS: Secondary data analysis of the last three waves of the nationally representative Pakistan Demographic and Health Surveys (PDHSs) was conducted Analysis was limited to all those women who had delivered a child during the last 5 years preceding each wave of PDHS Bivariate and multivariate logistic regression was applied to determine the association of maternal and newborn PNC utilization with multi-level determinants at individual, community, and institutional levels. RESULTS: In Pakistan, an upward linear trend in maternal PNC utilization was found, with an increase from 43.5 to 63.6% from 2006 to 2018. However, a non-linear trend was observed in newborn PNC utilization, with an upsurge from 20.6 to 50.5% from 2006 to 2013, nonetheless a decrease of 30.7% in 2018. Furthermore, the results highlighted that the likelihood of maternal and newborn PNC utilization was higher amongst older age women, who completed some years of schooling, were employed, had decision-making and emotional autonomy, had caesarean sections, and delivered at health facilities by skilled birth attendants. Multivariate analysis also revealed higher odds for women of older age, who had decision-making and emotional autonomy, and had caesarean section deliveries over the period of 2006-2018 for both maternal and newborn PNC utilization. Further, higher odds for maternal PNC utilization were found with parity and size of newborn, while less for ANC attendance and available means of transportation. Furthermore, increased odds were recorded for newborn PNC utilization with the number of children, ANC attendance, gender of child and mass media exposure from 2006 to 18. CONCLUSION: A difference in maternal and newborn PNC utilization was found in Pakistan, attributed to multiple individual (socio-demographic and obstetrics), community, and institutional level determinants. Overall, findings suggest the need to promote the benefits of PNC for early diagnosis of postpartum complications and to plan effective public health interventions to enhance women's access to healthcare facilities and skilled birth assistance to save mothers' and newborns' lives.


Subject(s)
Maternal Health Services , Postnatal Care , Child , Pregnancy , Infant, Newborn , Female , Humans , Cesarean Section , Pakistan/epidemiology , Parity , Demography , Prenatal Care , Patient Acceptance of Health Care , Health Surveys
2.
Molecules ; 28(3)2023 Feb 01.
Article in English | MEDLINE | ID: mdl-36771037

ABSTRACT

Water contaminated with heavy metals constitutes an important threat. This threat is a real problem with a negative impact in some developing countries where untreated industrial effluents are used for irrigation. The present study examines heavy metals in wastewater-irrigated vegetables (apple gourd, spinach, cauliflower, sponge gourd, and coriander) water, and soil from Chenab Nagar, Chiniot, Pakistan. In particular, the metals quantified were cadmium (Cd), chromium (Cr), cobalt (Co), nickel (Ni), lead (Pb), and manganese (Mn). Among them, Cr and Co in crops irrigated -wastewater exceeded the levels recommended by the World Health Organization (WHO). In contrast, Ni, Cu, Pb, and Mn concentrations were in line with WHO standards. Compared with the limits established by the Food and Agriculture Organization of the United Nations (FAO), all the study vegetables presented higher (thus unsafe) concentrations of Cd (0.38 to 1.205 mg/Kg). There were also unsafe concentrations of Cr in coriander, sponge gourd, and cauliflower. Pb was found at an unsafe concentration (0.59 mg/Kg) in cauliflower. Conversely, Ni and Mn concentrations were below the maximum permissible limits by WHO, and FAO in all of the analyzed samples. The contamination load index (CLI) in soil, bioconcentration factor (BCF) in plants, daily intake of metals (DIM), and health risk index (HRI) have also been evaluated to estimate the potential risk to human health in that area. We have found an important risk of transitions of Pb, Cd, Cr, and Co from water/soil to the edible part of the plant. The highest HRI value associated with Cd (6.10-13.85) followed by Cr (1.25-7.67) for all vegetable samples presented them as high health risk metal contaminants. If the issue is not addressed, consumption of wastewater-irrigated vegetables will continue posing a health risk.


Subject(s)
Metals, Heavy , Soil Pollutants , Humans , Vegetables , Wastewater , Cadmium , Lead , Environmental Monitoring , Metals, Heavy/toxicity , Metals, Heavy/analysis , Nickel , Chromium/toxicity , Cobalt , Soil , Manganese , Water , Soil Pollutants/toxicity , Soil Pollutants/analysis , Risk Assessment
3.
Molecules ; 27(22)2022 Nov 11.
Article in English | MEDLINE | ID: mdl-36431887

ABSTRACT

Currently the discovery and development of potent ß-glucuronidase inhibitors is an active area of research due to the observation that increased activity of this enzyme is associated with many pathological conditions, such as colon cancer, renal diseases, and infections of the urinary tract. In this study, twenty-seven 2-aminopyrimidine derivatives 1-27 were synthesized by fusion of 2-amino-4,6-dichloropyrimidine with a variety of amines in the presence of triethylamine without using any solvent and catalyst, in good to excellent yields. All synthesized compounds were characterized by EI-MS, HREI-MS and NMR spectroscopy. Compounds 1-27 were then evaluated for their ß-glucuronidase inhibitory activity, and among them, compound 24 (IC50 = 2.8 ± 0.10 µM) showed an activity much superior to standard D-saccharic acid 1,4-lactone (IC50 = 45.75 ± 2.16 µM). To predict the binding mode of the substrate and ß-glucuronidase, in silico study was performed. Conclusively, this study has identified a potent ß-glucuronidase inhibitor that deserves to be further studied for the development of pharmaceutical products.


Subject(s)
Enzyme Inhibitors , Glucuronidase , Structure-Activity Relationship , Molecular Docking Simulation , Enzyme Inhibitors/chemistry , Glucuronidase/metabolism
4.
Biomed Res Int ; 2022: 7537955, 2022.
Article in English | MEDLINE | ID: mdl-35880033

ABSTRACT

Diospyros kaki leaf extract was used in this study as a favorable basis for the synthesis of copper nanoparticles (Cu NPs). X-ray diffraction (XRD) and UV-visible spectroscopy approaches were used to characterize the biologically synthesized copper nanoparticles. The XRD analysis showed that copper nanoparticles were face-centered cubic structure. Various experimental levels like conc. of dye, concentration of Cu NPs, pH, reaction time, and temperature were optimized to decolorize reactive red 81 dye using the synthesized Cu NPs. Reactive red 81 dye was decolorized maximum using Cu NPs of 0.005 mg/L. Additionally, reactive red 81 dye was decolorized at its maximum at pH = 6, temperature = 50°C. Our study reported that chemical oxidation demand (COD) and total organic carbon (TOC) deduction efficacies were 74.56% and 73.24%. Further degradation study of reactive red 81 dye was also carried out. Cu NPs have the ability and promising potential to decolorize and degrade reactive red 81 dye found in wastewater.


Subject(s)
Metal Nanoparticles , Nanoparticles , Copper/chemistry , Metal Nanoparticles/chemistry , Nanoparticles/chemistry , Plant Extracts/chemistry , Wastewater , X-Ray Diffraction
5.
Curr Med Chem ; 29(41): 6288-6333, 2022.
Article in English | MEDLINE | ID: mdl-35838225

ABSTRACT

Pyranopyrazoles are bicyclic nitrogen-containing heterocycles having broadspectrum bioactivities, which may act as anti-cancer, anti-inflammatory, antibacterial, antifungal, insecticidal and molluscicidal agents. Pyranopyrazoles have become an attractive scaffold for the discovery of new drugs due to the diverse range of bioactivities associated with this nucleus. In this review, we have focused on the medicinal importance of pyranopyrazole derivatives and highlighted different routes for the synthesis of pyranopyrazole derivatives using inexpensive and commonly available starting materials.


Subject(s)
Anti-Bacterial Agents , Antifungal Agents , Humans , Antifungal Agents/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Inflammatory Agents , Nitrogen
6.
BMC Womens Health ; 22(1): 118, 2022 04 14.
Article in English | MEDLINE | ID: mdl-35421973

ABSTRACT

BACKGROUND: Pakistan has been showing consistently the highest prevalence of consanguinity. The popularity of consanguineous marriages is not declining in the country, because of social, cultural, and religious beliefs as well as economic advantages. However, couples also face various health-related implications, such as poor pregnancy outcomes or multiple reproductive and fertility consequences, having adverse effects on mothers and their children. This research investigated the trend of consanguineous marriages and their association with women's reproductive health and fertility behavior in Pakistan from 1990 to 2018. METHODS: This study is based on secondary data analysis, using all four waves of the Pakistan Demographic Health Surveys carried out from 1990 to 2018. The analysis is limited to women aged 15-49 years, who had given birth in the previous five years preceding each survey. Sampling weights were calculated and subsequently weighted analysis was conducted. Descriptive statistics, bivariable and multivariable logistic regression analysis were performed to determine the association of consanguinity with multiple characteristics related to socio-demographics, co-variates, and women's reproductive health and fertility behaviors. RESULTS: The findings revealed a high but overall stable trend of consanguinity prevalence of about 63% during the last three decades. Consanguineous marriages were more prevalent amongst young and uneducated women, living in rural areas, with poorer wealth status and having less exposure to mass media to access information. A strong association of consanguinity was observed with women's reproductive health and fertility behavior, particularly for women who gave first birth at a younger age, had multi-gravida pregnancies, multi-parity, pregnancy termination, ANC visits, and higher fertility. CONCLUSION: Consanguineous marriages are predominant in the patriarchal society of Pakistan. Findings revealed that consanguinity contributes significantly to women's reproductive health and fertility behaviors. Appropriate counseling, educational, and health promotional programs related to consanguinity should be designed and launched at the community level to raise awareness about risks towards women's reproductive health and fertility.


Subject(s)
Data Analysis , Reproductive Health , Child , Consanguinity , Female , Fertility , Health Surveys , Humans , Pakistan/epidemiology , Pregnancy , Prevalence
7.
Med Chem ; 18(6): 667-678, 2022.
Article in English | MEDLINE | ID: mdl-34931966

ABSTRACT

INTRODUCTION: Antioxidants are known to prevent oxidative stress-induced damage to the biomolecules and thus, delay the onset of cancers and many age-related diseases. Therefore, the development of novel and potent antioxidants is justified. METHODS: During this study, we synthesized symmetrical Bis-Schiff bases of carbohydrazide 1-27, and evaluated their in vitro antioxidative activity and cytotoxic activity. RESULTS: Among synthesized compounds, six compounds 20 (IC50 = 12.89 ± 0.02 µM), 16 (IC50 = 14.32 ± 0.43 µM), 17 (IC50 = 18.52 ± 0.83 µM), 19 (IC50 = 22.84 ± 0.62 µM), 24 (IC50 = 35.1 ± 0.82 µM) and 15 (IC50 = 40.03 ± 1.06 µM) showed an excellent 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, better than the standard butylatedhydroxyanisole (BHA) (IC50 = 44.6 ± 0.6 µM). Likewise, two compounds 16 (IC50 = 4.3 ± 1.3 µM) and 20 (IC50 = 6.6 ± 1.6 µM) showed oxidative burst scavenging activity better than the standard drug ibuprofen (IC50 = 11.2 ± 1.9 µM). Some synthesized compounds showed good to moderate toxicity against prostate cancer (PC-3) cell lines. CONCLUSION: This study has identified potent antioxidants and good cytotoxic agents with the potential to further investigate.


Subject(s)
Antioxidants , Schiff Bases , Antioxidants/chemistry , Cytotoxins , Hydrazines/pharmacology , Schiff Bases/chemistry
8.
BMC Public Health ; 21(1): 2328, 2021 12 30.
Article in English | MEDLINE | ID: mdl-34969379

ABSTRACT

BACKGROUND: In 2019, around 5 million and 10 million people were affected by hepatitis B virus (HBV) and hepatitis C virus (HCV) respectively in Pakistan. On World Hepatitis Day 2019, Pakistan's Government announced the Prime Minister's Plan to eliminate HBV and HCV from the country by 2030. In order to achieve this goal, adequate knowledge about HBV and HCV regarding mode of transmission, symptoms of the disease, and awareness about available treatments and vaccines is imperative. The present study aims to investigate the determinants related to overall knowledge about and behaviour in relation to HBV and HCV amongst married women in Pakistan. METHODS: Secondary data analysis was carried out using the Pakistan Demographic and Health Survey (PDHS) 2017-18. A series of questions regarding women's knowledge about how to avoid HBV and HCV and their health behaviour in relation to HBV and HCV were posed to 12,364 ever-married women of reproductive age (15-49 years). Bivariate and multivariable logistic and linear regression was applied to examine the effects of sociodemographic characteristics and covariates on women's overall knowledge and health behaviour regarding HBV and HCV. RESULTS: The findings highlight that the majority of women (88.3%) have heard of HBV and HCV. Nonetheless, only 34.8% had comprehensive knowledge about how to avoid HBV and HCV. Few women (11.3%) had been tested for HBV or HCV during the year preceding the survey. Furthermore, the results indicate that women living in urban areas, being older, and having more than 10 years of schooling, reported better knowledge and health behaviours regarding HBV and HCV. CONCLUSION: This study provides evidence that women's sociodemographic characteristics create differences in their overall knowledge about and attitudes towards HBV and HCV. This research emphasized that there is a need to create awareness about the causes and prevention of HBV and HCV in order to achieve the goal of eliminating these diseases in Pakistan by 2030.


Subject(s)
Hepatitis B , Hepatitis C , Adolescent , Adult , Female , Health Behavior , Hepatitis B/diagnosis , Hepatitis B/epidemiology , Hepatitis B/prevention & control , Hepatitis C/diagnosis , Hepatitis C/epidemiology , Humans , Marriage , Middle Aged , Pakistan/epidemiology , Young Adult
9.
Front Psychol ; 12: 620838, 2021.
Article in English | MEDLINE | ID: mdl-34177688

ABSTRACT

Digital media is a common phenomenon in contemporary societies. Recognizing the popularity of digital and online devices among the younger generation, the subject of parental internet mediation is of utmost significance for avoiding the adverse effects of digital media on the physical, cognitive, and social wellbeing of youngsters. Taking insights from an informed review of multi-grounded theories, we propose an extended framework of socio-ecological predictors concerning parental internet mediation. This contribution offers an innovative methodological and analytical perspective to consider both psychological and behavioral predictors for promoting resilience. This review acknowledged resilience as a strength-based measure to ensure online safety among young individuals. This review suggests that an integrated socio-ecological approach is critical to formulating the basis for a theoretical framework to fully comprehend the socio-ecological predictors of parental internet mediation.

10.
Article in English | MEDLINE | ID: mdl-33920404

ABSTRACT

Amid the COVID-19 pandemic, digital health literacy (DHL) has become a significant public health concern. This research aims to assess information seeking behavior, as well as the ability to find relevant information and deal with DHL among university students in Pakistan. An online-based cross-sectional survey, using a web-based interviewing technique, was conducted to collect data on DHL. Simple bivariate and multivariate linear regression was performed to assess the association of key characteristics with DHL. The results show a high DHL related to COVID-19 in 54.3% of students. Most of the Pakistani students demonstrated ~50% DHL in all dimensions, except for reliability. Multivariate findings showed that gender, sense of coherence and importance of information were found to be significantly associated with DHL. However, a negative association was observed with students' satisfaction with information. This led to the conclusion that critical operational and navigations skills are essential to achieve COVID-19 DHL and cope with stress, particularly to promote both personal and community health. Focused interventions and strategies should be designed to enhance DHL amongst university students to combat the pandemic.


Subject(s)
COVID-19 , Health Literacy , Cross-Sectional Studies , Humans , Information Seeking Behavior , Pakistan , Pandemics , Reproducibility of Results , SARS-CoV-2 , Students , Surveys and Questionnaires , Universities
11.
BMC Public Health ; 21(1): 317, 2021 02 08.
Article in English | MEDLINE | ID: mdl-33557795

ABSTRACT

BACKGROUND: The internet has become the most widely used medium among teenagers, who spend much of their time online, which raises parental concerns. Notwithstanding teens' increased internet use and exposure to online risks, little is yet known about parental internet mediation in local settings. The present research aimed to assess the various dimensions of parental mediation to regulate teens' use of the internet and their predictors. METHODS: A cross-sectional survey was conducted in the district of Lahore, Pakistan, among mothers/female caregivers of teens (aged 13-19 years). Only women were interviewed because they are more frequently engaged as primary caregivers than fathers or male caregivers. Furthermore, only qualified and working mothers from the top two professions among women, i.e. academia and medicine, were interviewed. A stratified random sampling technique was adopted, and 347 mothers were interviewed using face-to-face interviews at 11 universities and 11 hospitals/medical colleges. Data were entered and analysed using descriptive, bivariate and multivariate logistic regression analyses. RESULTS: The findings highlighted that more than 65% of respondents applied highly active mediation of internet safety, around 60% used highly active co-use mediation and more than 56% applied restrictive mediation. In addition, 36% of respondents monitored and 15.3% technically mediated to regulate their teens' use of the internet. The results of the multivariate logistic regression revealed that the majority of respondents were more inclined to adopt active internet safety mediation if they had teens aged 16-19 years, with medium internet addiction, possessed good digital skills, felt confident about their teens' coping appraisal to perform online protection, and considered their teens to have high self-esteem and resilience. CONCLUSIONS: This research found that parental internet mediation is a multifaceted concept used to regulate teens' online activity and enhance a resilient approach to reduce the risks associated with use of the internet. The researchers recommend developing parental guidelines, e-safety resource material, local support networks and community programmes to educate parents, teachers and teens in order to raise awareness and promote resilient pathways amongst teens.


Subject(s)
Caregivers , Internet Use , Adolescent , Adult , Cross-Sectional Studies , Female , Humans , Internet , Male , Pakistan , Parents , Young Adult
12.
Environ Sci Pollut Res Int ; 27(26): 32998-33007, 2020 Sep.
Article in English | MEDLINE | ID: mdl-32519107

ABSTRACT

In current years, pollution caused by synthetic dyes has become one of the most serious environmental issues. By rapidly developing industrial units, effluents having synthetic dyes are directly or indirectly being discharged into the environment. Bio-sorption is cost-effective way for the eradication of toxic dyes present in textile effluent. The present study involves the synthesis of nickel nanoparticles using Citrullus colocynthis stem extract. The characterization of synthesized nickel nanoparticles (Ni-NPs) was done by SEM. The synthesized Ni-NPs were used to degrade the Reactive Yellow 160 dye following the optimization of different experimental parameters. The maximum decolorization (91.4%) was obtained at 0.02% dye conc., 9 mg/L conc. of Ni-NPs, pH 7 at 40 °C. TOC and COD were used to assess the efficiency of this experiment. Percent reduction in COD and TOC was found to be 84.35% and 83.24% respectively. The degradation pathway of dye under study confirmed the formation of non-toxic end-products.


Subject(s)
Citrullus colocynthis , Nanoparticles , Coloring Agents , Nickel , Plant Extracts , Textile Industry
13.
Med Chem ; 16(2): 244-255, 2020.
Article in English | MEDLINE | ID: mdl-30987574

ABSTRACT

BACKGROUND: Peptic ulcer and urolithiasis are largely due to infection caused by ureaseproducing bacteria. Therefore, the discovery of urease inhibitors is an important area of medicinal chemistry research. OBJECTIVE: The main aim of the work was to identify novel urease inhibitors with no cytotoxicity. METHODS: During the current study, a series of ß-ketosulfones 1-26 was synthesized in two steps and evaluated for their in vitro urease inhibition potential. RESULTS: Out of twenty-six compounds, seventeen have shown good to significant urease inhibitory activity with IC50 values ranging between 49.93-351.46 µM, in comparison to standard thiourea (IC50 = 21 ± 0.11 µM). Moreover, all compounds found to be non-cytotoxic against normal 3T3 cell line. CONCLUSION: This study has identified ß-ketosulfones as novel and non-cytotoxic urease inhibitors.


Subject(s)
Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Sulfones/chemical synthesis , Sulfones/pharmacology , Urease/antagonists & inhibitors , Animals , Chemistry Techniques, Synthetic , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/toxicity , Inhibitory Concentration 50 , Mice , Molecular Docking Simulation , NIH 3T3 Cells , Protein Conformation , Structure-Activity Relationship , Sulfones/chemistry , Sulfones/toxicity , Urease/chemistry , Urease/metabolism
14.
BMC Public Health ; 19(1): 793, 2019 Jun 21.
Article in English | MEDLINE | ID: mdl-31226969

ABSTRACT

BACKGROUND: HIV/AIDS has emerged as a serious public health issue across the globe, and particularly in developing countries. Comprehensive knowledge and positive attitudes are cornerstones for the prevention, control and treatment of HIV/AIDS. However, there are various misconceptions associated with HIV/AIDS transmission, which lead to negative attitudes towards people living with AIDS. The present study aims to explore the effects of these determinants, related to socio-demographic characteristics and autonomy, on women's overall knowledge and attitudes regarding HIV/AIDS in Pakistan. METHODS: Secondary data analysis was carried out using the national representative dataset of the 2012-13 Pakistan Demographic and Health Survey. A series of questions related to HIV/AIDS was asked of 13,558 ever-married women aged 15-49 years to assess respondents' knowledge regarding modes of HIV/AIDS transmission and preventative measures, as well as their attitudes towards people living with HIV/AIDS. Descriptive and bivariate statistics were used to identify associations with socio-demographic and autonomy-related variables. Furthermore, bivariate and multivariate logistic regression analyses were performed to assess the association between multiple factors and overall HIV/AIDS knowledge as well as attitudes towards people living with AIDS. RESULTS: The results show that only 42% of Pakistani women have heard about HIV/AIDS. Amongst these women, the majority (68%) have good overall knowledge of HIV/AIDS and more than 55% have positive attitudes towards people living with AIDS. Furthermore, women residing in urban areas, having at least secondary-level education, with high autonomy, belonging to the richest wealth quintile and having exposure to mass media had high overall knowledge and positive attitudes towards people living with AIDS. CONCLUSION: The findings of this research support the relevance of women's autonomy, education and exposure to mass media, particularly in rural areas of Pakistan, to address the lack of knowledge and eliminate various myths and stigmatisation of people living with HIV/AIDS. Furthermore, it reveals a need to increase focused and targeted interventions to enhance women's knowledge and positive attitudes towards people living with HIV/AIDS. In this regard, the media can play a proactive role to gauge wider audience in creating awareness and eradicating the myths and misconceptions regarding HIV/AIDS.


Subject(s)
HIV Infections/transmission , Health Knowledge, Attitudes, Practice , Marriage/statistics & numerical data , Adolescent , Adult , Demography , Female , Humans , Male , Mass Media/statistics & numerical data , Middle Aged , Pakistan , Socioeconomic Factors , Young Adult
15.
Org Biomol Chem ; 17(22): 5615-5632, 2019 06 05.
Article in English | MEDLINE | ID: mdl-31120090

ABSTRACT

Routes to bicyclic tetramates derived from cysteine permitting ready incorporation of functionality at two different points around the periphery of a heterocyclic skeleton are reported. This has enabled the identification of systems active against Gram-positive bacteria, some of which show gyrase and RNA polymerase inhibitory activity. In particular, tetramates substituted with glycosyl side chains, chosen to impart polarity and aqueous solubility, show high antibacterial activity coupled with modest gyrase/polymerase activity in two cases. An analysis of physicochemical properties indicates that the antibacterially active tetramates generally occupy physicochemical space with MW of 300-600, clog D7.4 of -2.5 to 4 and rel. PSA of 11-22%. This work demonstrates that biologically active 3D libraries are readily available by manipulation of a tetramate skeleton.


Subject(s)
Anti-Bacterial Agents/pharmacology , Bridged Bicyclo Compounds/pharmacology , Cysteine/pharmacology , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Bridged Bicyclo Compounds/chemical synthesis , Bridged Bicyclo Compounds/chemistry , Cysteine/chemistry , Microbial Sensitivity Tests , Molecular Structure
16.
Med Chem ; 14(8): 818-830, 2018.
Article in English | MEDLINE | ID: mdl-29793412

ABSTRACT

BACKGROUND: Glucuronidation is essential for the metabolism and excretion of toxic substances. ß-Glucuronidase enzyme slows down the process of glucuronidation, and thus plays an important role in the on-set of colorectal carcinoma, and many other diseases. Inhibition of ß- glucuronidase activity is thus identified as an important approach for the treatment of several diseases. OBJECTIVE: Current study was aimed to synthesize a library of 2-oxo-1,2,3,4-tetrahydropyrimidine and to evaluate their ß-glucuronidase inhibitory activity, and their mode of enzyme inhibition. METHOD: We synthesized a series of 2-oxo-1,2,3,4-tetrahydropyrimidines 1-25 by fusing urea, ethyl acetoacetate, and a variety of aldehydes using copper nitrate trihydrate as catalyst. All synthesized compounds were evaluated for their in vitro ß-glucuronidase inhibitory activity. In addition, molecular docking studies were also performed by using MOE docking tools. RESULTS: Eighteen compounds showed inhibitory activity better than the standard D-saccharic acid 1,4-lactone, a well known ß-glucuronidase inhibitor (IC50 = 45.75 ± 2.16 µM). Compound 20 (IC50 = 1.36 ± 0.03 µM) showed an excellent inhibitory activity, thirty-five folds superior to the standard. Docking results highlighted the role of various chemical moieties at different positions on 2- oxo-1,2,3,4-tetrahydropyrimidine skeleton in enzyme inhibitory activity. CONCLUSION: This study has identified a class of potent ß-glucuronidase inhibitors with the potential to be investigated further.


Subject(s)
Enzyme Inhibitors/chemistry , Glucuronidase/antagonists & inhibitors , Pyrimidinones/chemistry , Small Molecule Libraries/chemistry , Enzyme Inhibitors/chemical synthesis , Molecular Docking Simulation , Pyrimidinones/chemical synthesis , Small Molecule Libraries/chemical synthesis , Structure-Activity Relationship
17.
Global Health ; 14(1): 17, 2018 02 06.
Article in English | MEDLINE | ID: mdl-29409528

ABSTRACT

BACKGROUND: South Asia is experiencing a dismal state of maternal and newborn health (MNH) as the region has been falling behind in reducing the levels of maternal and neonatal mortality. Most of the efforts are focused on enhancing coverage of MNH services; however, quality remains a serious concern if the region is to achieve expected outcomes in terms of standardised MNH services within healthcare delivery systems. This research consists of a review of South Asian quality improvement (QI) approaches/interventions, specifically implemented for MNH improvement. METHODS: A literature review of QI approaches/interventions was conducted using the PRISMA guidelines. Online databases, including PubMed, the Cochrane Library and Google Scholar, were searched. Primary studies published between 1998 and 2013 were considered. Studies were initially screened and selected based upon the selection criteria for data extraction. A thematic synthesis/analysis was performed to organise, group and interpret the key findings according to prominent themes. RESULTS: Thirty studies from six South Asian countries were included in the review. Findings from these selected studies were grouped under eight broad, cross-cutting themes, which emerged from a deductive approach, representing the most commonly employed QI approaches for improving MNH services within different geographical settings. These consist of capacity building of healthcare providers on clinical quality, clinical audits and feedback, financial incentives to beneficiaries, pay-for-performance, supportive supervision, community engagement, collaborative efforts and multidimensional interventions. CONCLUSIONS: Employing and documenting QI approaches is essential in order to measure the potential of an intervention, considering its cost-effectiveness, feasibility and acceptability to communities. This research concluded that QI approaches are very diverse and cross-cutting, because they are subject to the varied requirements of regional health systems. This high level of variability leads to implementation and knowledge-management challenges for MNH programme planners and managers in the countries of the South Asia region.


Subject(s)
Delivery of Health Care/organization & administration , Maternal Health Services/standards , Quality Improvement/organization & administration , Asia , Female , Humans , Infant, Newborn , Pregnancy
18.
Med Chem ; 14(5): 524-535, 2018.
Article in English | MEDLINE | ID: mdl-29189174

ABSTRACT

BACKGROUND: Xanthine oxidase is an important enzyme which catalyzes the production of uric acid and superoxide anion from xanthine. The over-production of these products leads to different disease conditions. For instance, uric acid is responsible for hyperuricemia, gout, and arthritis, while superoxide anion contributes to the oxidative stress, and related diseases. Hence XO is an important pharmacological target for the treatment of a range of diseases. METHODS: Based on the structural resemblance of pyrimidines with xanthine, a series of previously synthesized ethyl 6- methyl-2-oxo-1, 2, 3, 4-tetrahydro-5-pyrimidinecarboxylate derivatives were evaluated for XO inhibitory activity. RESULTS: Among 25 pyrimidone derivatives, 22 were found to be good to weak inhibitors with IC50 values in the range of 14.4 - 418 µM. Compounds 3, 14, 15, 18, and 21-23 were significant inhibitors, and thus analyzed for their kinetic parameters. Among them compounds 14, 15, 18, and 23 were competitive, 21 and 22 showed non-competitive, while 23 was a mixed-type of inhibitor. Molecular docking studies highlighted the interactions of these inhibitors with critical amino acids of XO, such as Val1011, Phe649, Lys771, and others. Moreover, the cytotoxicity studies on these selected inhibitors showed all these compounds to be non-cytotoxic. CONCLUSION: These non-cytotoxic, significant XO inhibitors can thus be further investigated for the treatment of hyperuricemia, and gout.


Subject(s)
Enzyme Inhibitors/pharmacology , Pyrimidinones/pharmacology , Xanthine Oxidase/antagonists & inhibitors , 3T3 Cells , Animals , Catalytic Domain , Cattle , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/toxicity , Inhibitory Concentration 50 , Kinetics , Mice , Molecular Docking Simulation , Molecular Structure , Pyrimidinones/chemistry , Pyrimidinones/toxicity , Structure-Activity Relationship , Xanthine Oxidase/chemistry
19.
Nutr J ; 16(1): 78, 2017 Dec 06.
Article in English | MEDLINE | ID: mdl-29208001

ABSTRACT

BACKGROUND: Optimum nutrition and good feeding practices amongst infants and young children are the key determinants of growth for a healthy life. Dietary diversity is considered to be a reliable and easy-to-measure proxy variable to assess young children's feeding practices for dietary adequacy and nutritional intake. This research aims to examine the current practices of dietary diversity amongst infants and young children aged 6-23 months in Pakistan and the various associated factors at child, maternal, household and community levels. METHODS: Secondary data analysis was performed for this research using the nationally representative dataset of the Pakistan Demographic and Health Survey 2012-13. Data on the last-born infants and young children aged 6-23 months (n = 1102) was taken from their mothers' interviews, who reported on their child's consumption of 7 food groups during the 24 h immediately preceding the survey. Data was analysed, using IBM® SPSS® Complex Sample to measure the association between children's dietary diversity and various factors at child, maternal, household and community levels through multiple linear regressions. RESULTS: Our research uncovered positive associations between children's dietary diversity and other sociodemographic variables. Overall, a variation was observed in consumption of 7 food groups across the youngest, middle and oldest age-groups of children. Multivariate analysis revealed that the children's Dietary Diversity Score (scale from 0 to 7) increases to 0.56 (95% CI: 0.18-0.94) amongst children in the middle age-group (12-17 months). Furthermore, the children who were still breastfeeding, with mothers who had a primary level of schooling and whose mothers also received information/services from lady health workers (LHWs) on maternal and child health were found to be a statistically significant predictor of infants' and young children's dietary diversity. Nevertheless, amongst them, the DDS had a negative association with the children's status of still breastfeeding and mothers' primary level of schooling, whereas it had a positive association with children being in the middle age-group and with mothers who received information/services from LHWs. CONCLUSION: The dietary diversity of infants and young children aged 6-23 months has a modest, nevertheless statistically significant, relationship with sociodemographic characteristics in Pakistan. There is a need for practical efforts to change the behaviour of communities to encourage more diverse foods to promote the healthy growth of children.


Subject(s)
Diet , Infant Nutritional Physiological Phenomena , Nutritional Status , Breast Feeding , Cross-Sectional Studies , Educational Status , Feeding Behavior , Food , Health Education , Health Surveys , Humans , Infant , Mothers , Pakistan , Socioeconomic Factors
20.
Molecules ; 22(12)2017 Dec 16.
Article in English | MEDLINE | ID: mdl-29258168

ABSTRACT

The present study aimed to assess and compare the ability to remediate synthetic textile and industrial wastewaters by Fenton treatment, a biological system and sequential treatments using Aspergillus niger (A. niger). All studied treatments were found to be effective in decolorization of the effluents under study. Fenton treatment followed by A. niger showed excellent potential for the maximum decolorization of the synthetic and industrial effluents under study. The effectiveness of sequential treatment was evaluated by water quality parameters such as total organic carbon (TOC), Biological Oxygen Demand (BOD5) and Chemical Oxygen Demand (COD) before and after each treatment. The results indicated that A. niger is an effective candidate for detoxification of textile wastewaters.


Subject(s)
Aspergillus niger/growth & development , Water Pollutants, Chemical/analysis , Aspergillus niger/metabolism , Biodegradation, Environmental , Biological Oxygen Demand Analysis , Soil Microbiology , Soil Pollutants/analysis , Water Pollutants, Chemical/metabolism
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