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51.
Anti‐inflammatory and analgesic activities of cupressuflavone from Cupressus macrocarpa: Impact on pro‐inflammatory mediators 下载免费PDF全文
Eman Al‐Sayed Haidy A. Gad Mohamed El‐Shazly Mohamed M. Abdel‐Daim Abdel Nasser Singab 《Drug development research》2018,79(1):22-28
Hit, Lead & Candidate Discovery |
52.
El-Sayed I. El-Desoky Eman M. Keshk Aya A. El-Sawi Mohamed A. Abozeid Laila A. Abouzeid Abdel-Rahman H. Abdel-Rahman 《Saudi Pharmaceutical Journal》2018,26(6):852-859
The versatile precursor 2-acetyl-4-allyl-1-hydroxy naphthalene was synthesized efficiently via Claisen rearrangement 2-acetyl-1-allyloxynaphthalene. The Claisen-Schmidt condensation of latter precursor afforded the corresponding chalcones which were exploited to synthesize a series of potential heterocycles such as pyrazoline, isoxazoline, benzocoumarin and benzoflavone. The synthesized products showed potent antioxidant and antimicrobial activities. Chalcone 3c, naphthyl pyrazoline 6b and hydroxycoumarin 13 exhibited the highest activity as antioxidants. Their binding mode showed specialized recognition of hydroxycoumarin 13 with the triad key amino acids at the active site of the oxidoreductase enzyme (PDB code 1DXO). 1-Hydroxynaphth-2-yl pyrazoline (6b) revealed the highest efficacy against both Gram positive and negative bacterial species. In silico molecular docking of pyrazoline 6b endorsed its proper binding at the active site of the 2EX6 enzyme which explains its potent antibacterial activity in comparison with standard ampicillin. 相似文献
53.
Eman M. Alfadhli 《Saudi Pharmaceutical Journal》2018,26(7):965-969
Background
Patients with uncontrolled type 1 diabetes mellitus (T1DM) are at a high risk for Ramadan fasting and are exempt from fasting; however, most still insist on fasting. The aim of this study was to examine glucose level fluctuations in those patients during Ramadan fasting using a real-time continuous glucose monitoring system (RT-CGMS).Methods
This pilot study involved adult patients with uncontrolled T1DM (HbA1c?>?7%) who insisted on fasting during Ramadan in 2014 from Maternity and Children’s Hospital, Medina, Saudi Arabia. A Medtronic RT-CGMS was used to monitor the participants’ glucose levels for 3 consecutive days during fasting.Results
The study included 22 patients (mean age 22?±?6?years, duration of diabetes 10.9?±?7.2?years, HbA1c level 9.3?±?1.2). All participants were using the basal-bolus insulin regimen, except for one patient who was on an insulin pump. Sensor glucose (SG) profiles typically followed a pattern that was characterized by an exaggerated increase after iftar, which was sustained overnight, and a second rapid rise after suhoor, with a prolonged glucose decay over the daylight hours. The average SG was 199?±?104.1?mg/dl, which was lower during fasting 188.4?±?103.41?mg/dl than during the eating hours 212.5?±?103.51?mg/dl (P?=?0.00). There was a higher rate of hyperglycemia (48%) than hypoglycemia (10%).Conclusions
Patients with uncontrolled T1DM who fasted during Ramadan experienced a wide fluctuation of glucose levels between fasting and eating hours, exhibiting a greater tendency toward hyperglycemia. The long-term effects for this finding are not known and warrant further investigation. 相似文献54.
A 5′ AMP‐Activated Protein Kinase Enzyme Activator,Compound 59, Induces Autophagy and Apoptosis in Human Oral Squamous Cell Carcinoma 下载免费PDF全文
Jing‐Ru Weng Eman M. E. Dokla Li‐Yuan Bai Ching‐Shih Chen Shih‐Jiuan Chiu Tzong‐Ming Shieh 《Basic & clinical pharmacology & toxicology》2018,123(1):21-29
5′ AMP‐activated protein kinase enzyme (AMPK), a master regulator of cellular metabolism, is recognized for its association with various metabolic diseases, inflammation and cancer. In this study, we aimed to investigate the role of compound 59, an AMPK activator, in a panel of oral squamous cell carcinoma (OSCC) cell lines. The antiproliferative effects of compound 59 were assessed by MTT assays, flow cytometry, Western blotting, confocal microscopy and transmission electron microscopy. Relative to OSCC cells, normal human oral keratinocytes were almost insensitive to compound 59 treatment. Compound 59 induced apoptosis as indicated by caspase activation and PARP cleavage. In addition, it inhibited JAK/STAT3 signalling, arrested cells in the G1 phase, increased reactive oxygen species (ROS) generation and promoted autophagy. Interestingly, pre‐treatment with a protein tyrosine phosphatase (PP2A) inhibitor, cantharidin, partially reversed compound 59‐induced down‐regulation of p‐JAK2 and p‐STAT3, thereby suggesting the involvement of a protein tyrosine phosphatase. Together, these findings substantiate the potential of compound 59 for the treatment of OSCC patients. 相似文献
55.
56.
Ahmed Abd El Wahab Saleh Eman Mahmoud Amin Asmaa Adel Elfallah Ahmed Mohamed Hamed 《Andrologia》2020,52(11):e13773
Among various health issues, infertility has been always considered as one of the major health problems. Idiopathic infertility is still a matter of debate since the underlying mechanisms stay obscure. Idiopathic infertility is related to expanded chance of metabolic syndrome components, obesity and increased risk of cardiovascular diseases. This study aimed to assess insulin resistance and serum levels of irisin as one of the adipokines in patients with idiopathic infertility. This study included 50 male patients aged 25–50 years old suffering from idiopathic infertility, together with 50 healthy individuals of matched age as controls. Patients showed significantly increased homeostasis model assessment for insulin resistance values than controls. For irisin results, idiopathic infertility patients had significantly decreased values than controls indicating the potential effect of irisin in development of insulin resistance in idiopathic infertility patients. 相似文献
57.
Willaert Robin Shaheen Eman Deferm Julie Vermeersch Hubert Jacobs Reinhilde Mombaerts Ilse 《Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie》2020,258(7):1527-1532
Graefe's Archive for Clinical and Experimental Ophthalmology - Current methods to analyse the globe position, including Hertel exophthalmometry and computed tomography (CT), are limited to the... 相似文献
58.
Omnia Shafei Alyaa A. Kotby Mona M. El Ganzoury Nevin M. Habeeb Eman Elsayed 《Congenital heart disease》2022,17(2):173-185
Objectives: We aimed to evaluate the effect of percutaneous atrial septal defect (ASD) closure in children using
right heart indices and serum galectin-3 (Gal-3), as potential biomarkers of right heart remodeling. Methods: This
case–control prospective study included 40 children with ASD and 25 control subjects. An echocardiographic evaluation was performed before the procedure, as well as 24 h, 1 month, and 6 months after intervention. Serum
Gal-3 was measured before, and 1 month after the procedure. Results: Serum Gal-3 concentration, right atrial
(RA) dimensions, right ventricular (RV) dimensions, indexed RA area, and right index of myocardial
performance (RIMP) were significantly increased in children with ASD compared with control subjects while tricuspid annular plane systolic excursion (TAPSE) was significantly decreased. Six months after closure, RA, and
RV dimensions significantly decreased and RV function improved (RIMP decreased and TAPSE increased). Gal-3
oncentration significantly decreased 1 month after ASD closure, but it did not reach normal range compared with
control subjects. A positive correlation between Gal-3 and age at closure, RA area, RV dimensions, and RIMP was
observed. A positive correlation was observed between the decrease in Gal-3 concentration and the decrease in
RA area and RV dimensions 1 month after ASD closure. A significant negative correlation was observed between
TAPSE and Gal-3 concentration before and after intervention. Conclusions: Percutaneous ASD closure can
improve right-sided indices and decrease serum Gal-3 concentration. Gal-3 can be used as a sensitive biomarker
of right heart remodeling, with a decrease in Gal-3 concentration suggesting reversal of maladaptive remodeling. 相似文献
59.
Discovery of Novel Peptidomimetics as Irreversible CHIKV NsP2 Protease Inhibitors Using Quantum Mechanical‐Based Ligand Descriptors 下载免费PDF全文
Eman M. El‐labbad Mohammed A. H. Ismail Dalal A. Abou Ei Ella Marawan Ahmed Feng Wang Khaled H. Barakat Khaled A. M. Abouzid 《Chemical biology & drug design》2015,86(6):1518-1527
Chikungunya virus (CHIKV) is a mosquito‐borne alphavirus. Recent outbreaks of CHIKV infections have been reported in Asia, Africa, and Europe. The symptoms of CHIKV infection include fever, headache, nausea, vomiting, myalgia, rash, and chronic persistent arthralgia. To date, no vaccines or selective antiviral drugs against this important emerging virus have been reported. In this study, the design, synthesis, and antiviral activity screening of new topographical peptidomimetics revealed three potential prototype agents 3a , 4b, and 5d showing 93–100% maximum inhibition of CHIKV replication in cell‐based assay having EC90 of 8.76–9.57 μg/mL. Intensive molecular modeling studies including covalent docking, lowest unoccupied molecular orbital energies, and the atomic condensed Fukui functions calculations strongly suggested the covalent binding of peptidomimetics 3a , 4b, and 5d to CHIKV nsP2 protease leading to permanent enzyme inactivation via Michael adduct formation between α/β‐unsaturated ketone functionality in our designed peptidomimetics and active site catalytic cysteine1013. Furthermore, small molecular weight peptidomimetics 3a and 4b satisfied the Lipinski rule of five for drug‐likeness and showed promising intestinal absorption and aqueous solubility via computational admet studies making them promising hits for further optimization. 相似文献
60.
Fatma Abdellah Mohamed Sawsan Mahmoud El-Bana Eman Abd-Elaziz Mohamed Nagat Farouk Abolwafa 《Journal of neonatal nursing : JNN》2019,25(6):285-292
BackgroundNewborn infants have an increased sensitivity to pain and are more reactive to pain than older children and adults. Nurses play a crucial role in assessing pain, implementing and evaluating interventions to minimize neonatal pain using available resources especially nonpharmacologic techniques.Aim of the studyto develop and apply an educational program on pediatric nurses regarding selected nonpharmacologic techniques to relieve pain in neonates.Research designA pre/post quasi-experimental research design was utilized in the present study. The study was carried out at Minia University for Obstetric and Pediatric and General Hospitals at neonatal care units. A convenient sample of 41 nurses was included in this study. Educational program for nurses was done through using the following data collection tools 1) Pre-designed questionnaire sheet, 2) Observation checklists sheet and 3) Educational and training program.ResultsIt was revealed that there was an obvious increase in the total mean scores of knowledge and practice in post and follow up program phase compared with pretest phase, with a very highly significant difference (p < 0.001).ConclusionThe education program had a significant impact on pediatric nurses' knowledge and practices regarding selected nonpharmacologic techniques to relieve pain in neonates.RecommendationsA continuous training and educational program should be planned and offered on regular basis for nurses regarding nonpharmacologic techniques to relieve pain in neonates. 相似文献