Methods: Three semi-synthetic series of compounds (C1-4, P1-4, and G1-4) were prepared and evaluated biologically as potential dual epidermal growth factor receptor (EGFR) and COX-2 inhibitors. The main phenolic constituents of Amaranthus spinosus L. (p-coumaric, caffeic and gallic) acids have been isolated and subsequently subjected to diazo coupling with various amines to get novel three chemical scaffolds with potential anticancer activities.
Results: Compounds C4 and G4 showed superior inhibitory activity against EGFR (IC50: 0.9 and 0.5 µM, respectively) and displayed good COX-2 inhibition (IC50: 4.35 and 2.47 µM, respectively). Moreover, the final compounds were further evaluated for their cytotoxic activity against human colon cancer (HT-29), pancreatic cancer (PaCa-2), human malignant melanoma (A375), lung cancer (H-460), and pancreatic ductal cancer (Panc-1) cell lines. Interestingly, compounds C4 and G4 exhibited the highest cytotoxic activity with average IC50 values of 1.5 µM and 2.8 µM against H-460 and Panc-1, respectively. The virtual docking study was conducted to gain proper understandings of the plausible-binding modes of target compounds within EGFR and COX-2 binding sites.
Discussion: The NMR of prepared compounds showed characteristic peaks that confirmed the structure of the target compounds. The synthesized benzoxazolyl scaffold containing compounds showed inhibitory activities for both COXs and EGFR which are consistent with the virtual docking study.
METHODS: On Ambae Island, blood samples were collected from 231 and 282 individuals in 2003 and 2007, respectively. Parasite prevalence was determined by microscopy. Antibodies to three Plasmodium falciparum (PfSE, PfMSP-119, and PfAMA-1) and three Plasmodium vivax (PvSE, PvMSP-119, and PvAMA-1) antigens, as well as the Anopheles-specific salivary antigen gSG6, were detected by ELISA. Age-specific seroprevalence was analysed using a reverse catalytic modelling approach to estimate seroconversion rates (SCRs).
RESULTS: Parasite rate decreased significantly (P
RESULTS: The overall prevalence of Schistosoma haematobium was 12.9%, whereas that of Schistosoma mansoni was 2.95%. Additionally, the males had higher prevalence (60%) of S. mansoni than females (40%). However, both gender were equally infected with S. haematobium (50%). With regard to risk factors, distance of residence from water source and source of drinking water are relatively associated with the infection.
OBJECTIVE: In order to investigate the influence between electron density in conjugated π-systems and biological activities, different withdrawing substituents, namely Nitro (NO2), Cyano (C≡N) and trifluoromethyl (CF3) were introduced in the chalcone-based molecular system.
METHODS: All the derivatives were then tested on MCF-7 cell line using the fluorescence microscopy-based cytotoxicity analyses.
RESULTS: The preliminary findings showed that both -NO2 and -CF3 substituents revealed their potential to inhibit the growth of MCF-7 with IC;50 values of 14.75 and 13.75 μg/ml, respectively. In addition, the morphological changes of MCF-7 cells were observed in response to alkoxy substituted chalcone treatment through an induction of apoptosis pathway with cell blebbing, phosphatidylserine exposure and autophagic activity with acidification of lysosomal structure. Intermolecular interaction based on in silico investigation on nitro, trifluoromethyl and cyano based chalcones exhibited several types of interactions with tumor necrosis factor receptor (PDB: 1EXT) protein and high hydrogen bond in the molecule-receptor interaction have given significant impact towards their toxicity on MCF-7 cells.
CONCLUSION: Significantly, these types of chalcones exhibited ideal and high potential to be further developed as anti-cancer agents.
Materials and Methods: A cross-sectional questionnaire-based research was conducted among 65 pediatric dentists in Malaysia. Online questionnaires were distributed to the pediatric dentists employed at public hospitals (MOH) and universities in Malaysia.
Result: It was found that over half of the respondents (65.6%) employed HTPMC. The analysis of the co-occurrence network frequency revealed that a high frequency of female pediatric dentists who were within the age group of 31-40 years old had fulfilled their postgraduation overseas and was employed in the university mainly applied HTPMC.
Conclusion: The application of HTPMC among respondent pediatric dentists in Malaysia was high. However, most respondents considered HTPMC a treatment option only to manage carious primary molar rather than a treatment of choice.
OBJECTIVES: To measure the level of COVID-19 information overload (COVIO) and assess the association between COVIO and sociodemographic characteristics among the general public.
METHODS: A cross-sectional online survey was conducted between April and May 2020 using a modified Cancer Information Overload scale. The survey was developed and posted on four social media platforms. The data were only collected from those who consented to participate. COVIO score was classified into high vs. low using the asymmetrical distribution as a guide and conducted a binary logistic regression to examine the factors associated with COVIO.
RESULTS: A total number of 584 respondents participated in this study. The mean COVIO score of the respondents was 19.4 (± 4.0). Sources and frequency of receiving COVID-19 information were found to be significant predictors of COVIO. Participants who received information via the broadcast media were more likely to have high COVIO than those who received information via the social media (adjusted odds ratio ([aOR],14.599; 95% confidence interval [CI], 1.608-132.559; p = 0.017). Also, participants who received COVID-19 information every minute (aOR, 3.892; 95% CI, 1.124-13.480; p = 0.032) were more likely to have high COVIO than those who received information every week.
CONCLUSION: The source of information and the frequency of receiving COVID-19 information were significantly associated with COVIO. The COVID-19 information is often conflicting, leading to confusion and overload of information in the general population. This can have unfavorable effects on the measures taken to control the transmission and management of COVID-19 infection.
METHODS: Pre-dosed urine samples were collected from male Sprague-Dawley rats. The rats were treated with either LDA (10 mg/kg) or 1% methylcellulose (10 mL/kg) per oral for 28 days. The rats' stomachs were examined for gastric toxicity using a stereomicroscope. The urine samples were analyzed using a proton nuclear magnetic resonance spectroscopy. Metabolites were systematically identified by exploring established databases and multivariate analyses to determine the spectral pattern of metabolites related to LDA-induced gastric toxicity.
RESULTS: Treatment with LDA resulted in gastric toxicity in 20/32 rats (62.5%). The orthogonal projections to latent structures discriminant analysis (OPLS-DA) model displayed a goodness-of-fit (R2Y) value of 0.947, suggesting near-perfect reproducibility and a goodness-of-prediction (Q2Y) of -0.185 with perfect sensitivity, specificity and accuracy (100%). Furthermore, the area under the receiver operating characteristic (AUROC) displayed was 1. The final OPLS-DA model had an R2Y value of 0.726 and Q2Y of 0.142 with sensitivity (100%), specificity (95.0%) and accuracy (96.9%). Citrate, hippurate, methylamine, trimethylamine N-oxide and alpha-keto-glutarate were identified as the possible metabolites implicated in the LDA-induced gastric toxicity.
CONCLUSION: The study identified metabolic signatures that correlated with the development of a low-dose Aspirin-induced gastric toxicity in rats. This pharmacometabolomic approach could further be validated to predict LDA-induced gastric toxicity in patients with coronary artery disease.
Methods: The proposed study will be conducted in three phases: Phase I will involve the development of the item-pool to be included in the tool, followed by a face, content validity and construct validity. The tool reliability, readability and difficulty index will be determined. Phase II will involve the utilization of the tool to assess baseline SAV knowledge among the HCPs followed by an educational intervention. Multiple Linear Regression analysis will be used to determine the factors associated with SAV knowledge among the HCPs. Lastly, Phase III which will be a repeat of Phase II to assess and evaluate the knowledge after the intervention.
Discussion: The study design and findings may guide future implementation and streamline the intervention of improving SAV knowledge in HCPs training and practice.
Lay Summary: Knowledge assessment and educational intervention of snake antivenom among healthcare practitioners in northern Nigeria: a study protocol Snakebite envenoming (SBE) is an important occupational and public health hazard especially in sub-Saharan Africa. For optimum management of SBE, adequate knowledge of snake antivenom (SAV) is very critical among the healthcare practitioners. The baseline knowledge SAV dosage, mode of administration, availability, and logistics is very relevant among healthcare professionals, particularly those that are directly involved in its logistics. It is paramount that SAV is handled and used appropriately. The efforts and advocacy for the availability for more SAV will be in vain if not handled appropriately before they are used. This study protocol aims to develop a tool, to assess SAV knowledge and effects of educational interventions among healthcare professionals (HCPs) in northern Nigeria. This protocol suggests conducting studies in three phases: (a) Development and validation of SAV knowledge assessment tool, (b) Baseline assessment of SAV knowledge assessment tool among HCPs, and (c) Development, implementation and evaluation of an educational intervention to improve SAV knowledge among HCPs in northern Nigeria.