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Synthesis,antimicrobial, antiquorum-sensing and cytotoxic activities of new series of benzothiazole derivatives

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Chinese Chemical Letters 2015年第12期26卷 1522-1528页

作者： Moustafa T.Gabr Nadia S.el-Gohary eman r.el-bendary Mohamed M.el-Kerdawy Nanting Ni Mona I.Shaaban Department of Medicinal Chemistry Faculty of Pharmacy Mansoura University Department of Chemistry Georgia State University Department of Microbiology Faculty of Pharmacy Mansoura University Department of Microbiology College of Pharmacy Taibah University

New series of benzothiazole derivatives were designed and synthesized. The newly synthesized compounds were screened for their antibacterial activity against Escherichia coli, Staphylococcus aureus and Bacillus cereus. Compounds 6j and 6o showed the highest activity against E. coli and S. aureus. The antifungal activity of these compounds was also tested against Candida albicans and Aspergillus fumigatus293. Compounds 4c, 4g and 6j exhibited the highest activity against C. albicans. In addition, compounds4 a and 6j displayed promising activity against A. fumigatus 293. The same compounds were examined for their antiquorum-sensing activity against Chromobacterium violaceum ATCC 12472, whereas compounds4 a, 6j and 6p showed moderate activity. The in vitro cytotoxicity testing of the synthesized compounds was performed against cervical cancer（Hela） and kidney fibroblast cancer（COS-7） cell lines. results indicated that all tested compounds have IC50 values 〉50 mmol/L against both cell lines. Molecular properties, toxicities, drug-likeness, and drug score profiles of compounds 4a–c, 5a, 6g,h, 6j, 6l, 6o and7 c,d were also assessed.

关键词： antibacterial moiety antifungal antimicrobial cytotoxic screened moderate substituent Candida albicans

Agmatine induces gastric protection against ischemic injury by reducing vascular permeability in rats

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World Journal of Gastroenterology 2012年第18期18卷 2188-2196页

作者： Abeer A Al Masri eman el Eter Department of Physiology College of Medicine and King Khalid University HospitalKing Saud UniversityRiyadh 11461Saudi Arabia

AIM:To investigate the effect of administration of agmatine(AGM) on gastric protection against ischemia reperfusion(I/r) ***:Three groups of rats(6/group);sham,gastric I/r injury,and gastric I/r + AGM(100 mg/kg,*** 15 min prior to gastric ischemia) were *** injury was conducted by ligating celiac artery for 30 min and reperfusion for another 30 *** tissues were histologically studied and immunostained with angiopoietin 1(Ang-1) and *** endothelial growth factor(VEGF) and monocyte chemoattractant protein-1(MCP-1) were measured in gastric tissue *** assess whether AKt/phosphatidyl inositol-3-kinase(PI3K) mediated the effect of AGM,an additional group was pretreated with Wortmannin(WM)(inhibitor of Akt/PI3K,15 μg/kg,i.p.),prior to ischemic injury and AGM treatment,and examined histologically and *** set of experiments was run to study vascular permeability of the stomach using Evan's blue ***:AGM markedly reduced Evan's blue dye extravasation(3.58 ± 0.975 μg/stomach vs 1.175 ± 0.374 μg/stomach,P rotein vs 48.4 ± 6.53 pg/100 mg protein,P el(29.5 ± 7 pg/100 mg protein vs 41.17 ± 10.4 pg/100 mg protein,P reserved gastric histology and reduced ***-1 and Ang-2 immunostaining were reduced in stomach sections of AGM-treated *** administration of WM abolished the protective effects of AGM and extensive hemorrhage and ulcerations were ***:AGM protects the stomach against I/r injury by reducing vascular permeability and *** protection is possibly mediated by Akt/PI3K.

关键词： Ischemia reperfusion injury Agmatine Wortmannin Vascular permeability Monocyte chemoattractant protein-1 Stomach Vascular endothelial growth factor

Diffusion-weighted magnetic resonance imaging and micro-rNA in the diagnosis of hepatic fibrosis in chronic hepatitis C virus

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World Journal of Gastroenterology 2019年第11期25卷 1366-1377页

作者： Tarek Besheer Hatem elalfy Mohamed Abd el-Maksoud Ahmed Abd el-razek Saher Taman Khaled Zalata Wagdy elkashef Hossam Zaghloul Heba elshahawy Doaa raafat Wafaa elemshaty eman elsayed Abdel-Hady el-Gilany Mahmoud el-bendary Department of Tropical Medicine and Hepatology Mansoura Faculty of Medicine-Mansoura University Department of Diagnostic radiology Mansoura Faculty of Medicine-Mansoura University Department of Pathology Mansoura Faculty of Medicine-Mansoura University Department of Clinical Pathology Mansoura Faculty of Medicine-Mansoura University Department of Public Health and Preventive Medicine Mansoura Faculty of Medicine-Mansoura University

BACKGrOUND Diffusion-weighted magnetic resonance imaging has shown promise in the detection and quantification of hepatic fibrosis. In addition, the liver has numerous endogenous micro-rNAs(mirs) that play important roles in the regulation of biological processes such as cell proliferation and hepatic *** To assess diffusion-weighted magnetic resonance imaging and mirs in diagnosing and staging hepatic fibrosis in patients with chronic hepatitis *** This prospective study included 208 patients and 82 age-and sex-matched controls who underwent diffusion-weighted magnetic resonance imaging of the abdomen, mir profiling, and liver biopsy. Pathological scoring was classified according to the METAVIr scoring system. The apparent diffusion coefficient (ADC) and mir were calculated and cor.elated with pathological *** The ADC value decreased significantly with the progression of fibrosis, from controls(F0) to patients with early fibrosis(F1 and F2) to those with late fibrosis(F3 and F4)(median 1.92, 1.53, and 1.25 × 10^(-3) mm^2/s, respectively)(P = 0.001).The cut-off ADC value used to differentiate patients from controls was 1.83 × 10^(-3) mm^2/s with an area under the curve(AUC) of 0.992. Combining ADC and mir-200 b revealed the highest AUC(0.995) for differentiating patients from controls with an accuracy of 96.9%. The cut-off ADC used to differentiate early fibrosis from late fibrosis was 1.54 × 10^(-3) mm^2/s with an AUC of 0.866. The combination of ADC and mir-200 b revealed the best AUC(0.925) for differentiating early fibrosis from late fibrosis with an accuracy of 80.2%. The ADC cor.elated with mir-200 b(r =-0.61, P = 0.001), mir-21(r =-0.62, P = 0.001), and mir-29(r = 0.52,P = 0.001).CONCLUSION Combining ADC and mirs offers an alternative surrogate non-invasive diagnostic tool for diagnosing and staging hepatic fibrosis in patients with chronic hepatitis C.

关键词： Diffusion Magnetic resonance imaging Fibrosis Liver Hepatitis C virus Micro-rNA

Toxoplasma gondii infection can induce retinal DNA damage: an experimental study

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International Journal of Ophthalmology(English edition) 2014年第3期7卷 431-436页

作者： Nagwa Mostafa el-Sayed eman Mohamed Aly Department of Medical Parasitology Research Institute of Ophthalmology Department of Basic Science Biophysics and Laser Science Unit Research Institute of Ophthalmology

AIM:To detect whether Toxoplasma gondii(***)infection of mice can induce retinal DNA ***:A total of 20 laboratory-bred male Swiss albino mice were used and divided into four groups:control group(non-infected animals);*** infected group;immunosuppressed infected group;and infected group treated with sulfadiazine and *** eyes were collected 6wk post infection and retinas were *** retina was immediately processed for comet assay and the frequency of tailed nuclei(DNA damage)was *** addition,retinal DNA damage was revealed by various comet assay parameters that were provided by the image analysis software including tail length,percentage of DNA in the tail,percentage of tailed cells and tail ***:The obtained results showed that *** infection induced a statistically significant increase in the frequency of tailed nuclei,tail length,percentage of DNA in the tail,and tail moment in mice retinal cells compared to the control group(which showed some degree of DNA damage).In immunosuppressed infected group,retinal DNA damage was severing and there was significant increase in various comet assay parameters compared to both control and infected *** treatment with sulfadiazine and pyrimethamine,retinal DNA damage decreased and all comet assay parameters showed a statistical significant decrease compared to infected ***:*** infection can induce DNA damage in mice retinal cells.

关键词： Toxoplasma gondii retinochoroiditis DNA damage comet assay

Mesenchymal stem cells transplantation attenuates experimentally induced brain injury after neonatal hypoxia by different two routes of administrations

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BIOCelL 2019年第1期43卷 21-28页

作者： Nesrine EBrAHIM eman EHSAN eman Abd el GHANY Dina SABrY Ashraf SHAMAA Histology and Cell Biology Department Faculty of MedicineBenha UniversityBenhaEgypt Pediatrics Department Faculty of MedicineCairo UniversityGizaEgypt Medical Biochemistry and molecular biology Department Faculty of MedicineCairo UniversityGizaEgypt Surgical and radiology Department Faculty of Veterinary MedicineCairo UniversityGizaEgypt

The neonatal hypoxic-ischemic encephalopathy(HIE)is an important cause of neurological morbidity and mortality in *** therapy is considered a promising method for treating severe neurological disorders such as this *** cells have the capacity for self-renewal and differentiation into certain cell *** present study was aimed to find out the most beneficial route of bone marrow-derived mesenchymal stem cells(BMSCs)administration for the attenuation of experimentally induced HIE in neonatal *** neonatal rats were divided randomly into four *** 1:control *** 2:rats were exposed to bilateral ligation of cephalic *** 3:rats were exposed to bilateral ligation of cephalic arteries and then underwent intravenous(IV)BMSC *** 4:rats were exposed to bilateral ligation of cephalic arteries and then underwent intracerebroventricular(ICV)BMSC *** animals were evaluated by(a)neurobehavioral tests;(b)histopathology,i.e.,histological and immuno-histochemical studies;and(3)gene expression *** BMSC treated groups(3 and 4)showed improvement in neurobehavioral tests,histopathological studies,and gene expression,as compared to non-injected lesioned rats(Group 2)with better improvement in Group 4(ICV injections)than in Group 3(IV injections).

关键词： Cerebral cortex Neonatal hypoxic ischemia Stem cells

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World Journal of Gastroenterology 2016年第30期22卷 6800-6816页

作者： Mahmoud Fathy Dondeti eman Anwar.el-Maadawy roba Mohamed Talaat Genetic Engineering and Biotechnology research Division National Research Centre Molecular Biology Department Genetic Engineering and Biotechnology Research Institute University of Sadat City

Hepatocellular carcinoma(HCC) is a primary liver cancer, which is one of the most prevalent cancers among humans. Many factors are involved in the liver carcinogenesis as lifestyle and environmental factors. Hepatitis virus infections are now recognized as the chief etiology of HCC; however, the precise mechanism is still enigmatic till now. The inflammation triggered by the cytokine-mediated immune response, was reported to be the closest factor of HCC development. Cytokines are immunoregulatory proteins produced by immune cells, functioning as orchestrators of the immune response. Genes of cytokines and their receptors are known to be polymorphic, which give rise to variations in their genes. These variations have a great impact on the expression levels of the secreted cytokines. Therefore, cytokine gene polymorphisms are involved in the molecular mechanisms of several diseases. This piece of work aims to shed much light on the role of cytokine gene polymorphisms as genetic host factor in hepatitis related HCC.

关键词： Hepatocellular carcinoma Hepatitis C virus Hepatitis B virus Cytokines Polymorphism

Validation and application of Vierordt’’s spectrophotometric method for simultaneous estimation of tamoxifen/coenzyme Q10 in their binary mixture and pharmaceutical dosage forms

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Asian Journal of Pharmaceutical Sciences 2016年第2期11卷 318-325页

作者： eman S. el-Leithy rania S. Abdel-rashid Department of Pharmaceutics Faculty of Pharmacy Helwan University

For the sake of improving patient compliance and sustainability of chemotherapy healthcare system, both TC and CoQ10 were formulated as solid lipid nanoparticles (SLNs). The study was focused on establishing and validating a simple and reproducible spectrophotometric method for simultaneous determination of TC and CoQ10 in their binary mixture or pharmaceutical dosage forms. A new method based on simultaneous estimation of drug mixture without prior separation was developed. Validation parameters were checked with International Conference on Harmonization (ICH) guidelines. The accuracy and reproducibility of proposed method was statistically compared to HPLC. The TC and CoQ10 were quantified at absorptivity wavelengths of 236 nm and 275 nm, respectively. Calibration curves obeyed Beer’s law in range of 2–14 μg/ml with a cor.elation coefficient (r^2) of 0.999 in both methanol and simplified simulated intestinal fluid (SSIF). The %means recovery of TC and Co Q10 in pure state or binary mixture at various concentration levels were all around 100%.The low values of SD and %rSD (rm high precision and accuracy of the proposed method. Formulated SLNs showed different %means recovery in range 81–92% for TC and 32–59% for CoQ10. The data obtained by applying simultaneous Vierordt’s equations showed no statistical significance in comparison to HPLC. Vierordt’s method was successfully applied as a simple, accurate, precise, and economical analysis method for estimating TC and CoQ10 concentrations in pure state, binary mixture and pharmaceutical dosage forms.

关键词： Tamoxifen citrate Coenzyme Q10 Binary mixture Solid lipid nanoparticles Validation

Effects of Nigella sativa on outcome of hepatitis C in Egypt

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World Journal of Gastroenterology 2013年第16期19卷 2529-2536页

作者： eman Mahmoud Fathy Barakat Lamia Mohamed el Wakeel radwa Samir Hagag Department of Tropical Medicine Faculty of Medicine Ain Shams University Department of Clinical Pharmacy Faculty of Pharmacy Ain Shams University Department of Clinical Pharmacy Faculty of Pharmacy Egyptian Russian University

AIM: To evaluate the safety, efficacy and tolerability of Nigella sativa (N. sativa ) in patients with hepatitis C not eligible for interferon (IFN)-α. METHODS: Thirty patients with hepatitis C virus (HCV) infection, who were not eligible for IFN/ribavirin therapy, were included in the present study. Inclusion criteria included: patients with HCV with or without cirrhosis, who had a contraindication to IFN-α therapy, or had refused or had a financial constraint to IFN-α therapy. Exclusion criteria included: patients on IFN-α therapy, infection with hepatitis B or hepatitis Ⅰ virus, hepatocellular carcinoma, other malignancies, major severe illness, or treatment non-compliance. Various parameters, including clinical parameters, complete blood count, liver function, renal function, plasma glucose, total antioxidant capacity (TAC), and polymerase chain reaction, were all assessed at baseline and at the end of the study. Clinical assessment included: hepato and/ or splenomegaly, jaundice, palmar erythema, flapping tremors, spider naevi, lower-limb edema, and ascites. N. sativa was administered for three successive months at a dose of (450 mg three times daily). Clinical response and incidence of adverse drug reactions were assessed initially, periodically, and at the end of the study. rESULTS: N. sativa administration significantly improved HCV viral load (380808.7 ± 610937 vs 147028.2 ± 475225.6, P = 0.001) and TAC (1.35 ± 0.5 vs 1.612 ± 0.56, P = 0.001). After N. sativa administration, the following laboratory parameters improved: total protein (7.1 ± 0.7 vs 7.5 ± 0.8, P = 0.001), albumin (3.5 ± 0.87 vs 3.69 ± 0.91, P = 0.008), red blood cell count (4.13 ± 0.9 vs 4.3 ± 0.9, P = 0.001), and platelet count (167.7 ± 91.2 vs 198.5 ± 103, P = 0.004). Fasting blood glucose (104.03 ± 43.42 vs 92.1 ± 31.34, P = 0.001) and postprandial blood glucose (143.67 ± 72.56 vs 112.1 ± 42.9, P = 0.001) were significantly decreased in both diabetic and non-diabetic HCV patients. Patients

关键词： Hepatitis C virus Nigella sativa Oxidative stress Viral load

Non-alcoholic fatty liver disease: The diagnosis and management

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World Journal of Hepatology 2015年第6期7卷 846-858页

作者： Shehab M Abd el-Kader eman M Salah el-Den Ashmawy Department of Physical Therapy Faculty of Applied Medical Sciences King Abdulaziz University Department of Physical Therapy for Cardiopulmonary Disorders and Geriatrics Faculty of Physical Therapy Cairo University

Non-alcoholic fatty liver disease(NAFLD) is now the most frequent chronic liver disease that occurs across all age groups and is recognized to occur in 14%-30% of the general population, representing a serious and growing clinical problem due to the growing prevalence of obesity and overweight. Histologically, it resembles alcoholic liver injury but occurs in patients who deny significant alcohol consumption. NAFLD encompasses a spectrum of conditions, ranging from benign hepatocellular steatosisto inflammatory nonalcoholic steatohepatitis, fibrosis, and cirrhosis. The majority of hepatocellular lipids are stored as triglycerides, but other lipid metabolites, such as free fatty acids, cholesterol, and phospholipids, may also be present and play a role in disease progression. NAFLD is associated with obesity and insulin resistance and is considered the hepatic manifestation of the metabolic syndrome, a combination of medical conditions including type 2 diabetes mellitus, hypertension, hyperlipidemia, and visceral adiposity. Confirmation of the diagnosis of NAFLD can usually be achieved by imaging studies; however, staging the disease requires a liver biopsy. Current treatment relies on weight loss and exercise, although various insulin-sensitizing agents, antioxidants and medications appear promising. The aim of this review is to highlight the current information regarding epidemiology, diagnosis, and management of NAFLD as well as new information about pathogenesis, diagnosis and management of this disease.

关键词： Non-alcoholic fatty liver disease Nonalcoholicsteatohepatitis Liver disease