615 results on '"Gouda"'
Search Results
2. Chemistry of 2-(Piperazin-1-yl) Quinoline-3-Carbaldehydes
- Author
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Mohammed A. Salem, Moustafa A. Gouda, and Ghada G. El-Bana
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chemistry.chemical_compound ,chemistry ,Organic Chemistry ,Quinoline ,Organic chemistry - Abstract
Abstract: This review described the preparation of 2- chloroquinoline-3-carbaldehyde derivatives 18 through Vilsmeier-Haack formylation of N-arylacetamides and the use of them as a key intermediate for the preparation of 2-(piperazin-1-yl) quinoline-3-carbaldehydes. The synthesis of the 2- (piperazin-1-yl) quinolines derivatives was explained through the following chemical reactions: acylation, sulfonylation, Claisen-Schmidt condensation, 1, 3-dipolar cycloaddition, one-pot multicomponent reactions (MCRs), reductive amination, Grignard reaction and Kabachnik-Field’s reaction.
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- 2022
3. Synthetic and Reactions Routes to Tetrahydrothieno[3,2-b]Quinoline Derivatives (Part IV)
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Hoda A. R. Hussein, Ameen A. Abu-Hashem, Moustafa A. Gouda, and Ahmed A. M. Abdelgawad
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chemistry.chemical_compound ,chemistry ,Organic Chemistry ,Quinoline ,Organic chemistry - Abstract
Abstract: This review describes the synthesis and chemical reactivity of tetrahydrothieno[3,2-b] quinoline derivatives from through many of the reagents such as; 1, 2-dihydropyridine-3-carbonitrile; 1,6-dihydropyrimidine-5-carbonitrile; 2,3-dihydropyridazine-4-carbonitrile; 3-amino-thiophene-2-carboxylate; 3-amino-thiophene-2-carbonitrile; 3,4-diaminothieno[2,3-b] thiophene-2,5-dicarbo- nitrile; 2-(3-bromo-1-iodoisoquinolin-8-yl) benzonitrile and 3-mercapto-benzo[g]quinolin-4(1H)-one derivatives. The synthesis of the tetrahydrothieno [3, 2-b] quinoline derivatives were explained through the following chemical reactions: Aldol condensation, alkylation, cyclocondensation, dehydration, chlorination, Wolff-Kishner reduction, acylation, Friedlander reaction and intramolecular cyclization.
- Published
- 2022
4. Influence of the Linear Alkylbenzene Sulfonate (LAS) on hematological and biochemical parameters of Nile Tilapia, Oreochromis niloticus
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Ahmed E. Hagras, Mohamed A. Okbah, Asmaa M.R. Gouda, and Maie I. El-Gammal
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Gill ,biology ,Chemistry ,QH301-705.5 ,Linear Alkylbenzene Sulfonate ,Oreochromis niloticus ,Glutathione ,biology.organism_classification ,Acute toxicity ,Superoxide dismutase ,Oreochromis ,Nile tilapia ,chemistry.chemical_compound ,Oxidative Stress ,Catalase ,biology.protein ,Bioassay ,Histopathological Impairments ,Food science ,Biology (General) ,General Agricultural and Biological Sciences ,Reactive Oxygen Species - Abstract
The acute toxicity of household detergent (Ariel) on blood parameters and histology of Oreochromis niloticus was investigated using static bioassay for 96 h. Linear alkylbenzene sulfonate (LAS) is an anionic surfactant widely used in detergents and cleaners, both in industrial and household applications. LAS contaminating aquatic ecosystems as a potential toxic pollutant, was investigated in the present study for acute toxicity. The fish samples were divided into six groups, including 20 fish in each group. Normal feed was given to control group without detergents treatment. Hematological parameters (RBC count, Hb, Ht and platelets) were significantly declined, while WBC count showed a highly significant increase. Compared with the control group, significant elevation of serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) was recorded in fish treated with different concentrations of detergent. Catalase (CAT), Superoxide dismutase (SOD) activities and Reduced Glutathione (GSH) concentration showed a highly significant reduction. Total proteins showed significant decrease, while total lipids, cholesterol and triglycerides significantly increased. The mean lethal concentration (LC50) for 96 h of Ariel was at concentration 10 mg/L. Relative percentage of detergent residues in fish muscles was increased with higher detergent concentrations. In conclusion, exposure to detergents resulted in great alterations in the histological structure of liver and gills.
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- 2022
5. Design, Synthesis and Antitumor Activity of Novel Dispiro[oxindole-cyclohexanone]- pyrrolidines
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Majed Bawzeer, Mohammed Yaseen, Lamees Hegazy, Bahaa El-Dien M. El-Gendy, Mohamed Elagawany, Mohamed Azab, Magy Gouda, and Mostafa E. Rateb
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Pyrrolidines ,Molecular model ,Stereochemistry ,Placenta ,Antineoplastic Agents ,Alkylation ,Structure-Activity Relationship ,chemistry.chemical_compound ,Pregnancy ,Cell Line, Tumor ,Drug Discovery ,medicine ,Humans ,Spiro Compounds ,Oxindole ,Cell Proliferation ,Pharmacology ,Molecular Structure ,Cyclohexanones ,Isatin ,In vitro ,Cycloaddition ,Oxindoles ,chemistry ,Mechanism of action ,Cell culture ,Female ,Drug Screening Assays, Antitumor ,medicine.symptom - Abstract
Background: Spirooxindoles are privileged scaffolds in medicinal chemistry, which were identified through Wang’s pioneering work as inhibitors of MDM2-p53 interactions. Objective: To design and synthesize 2,6-diarylidenecyclohexanones and dispiro[oxindole-cyclohexanone]- pyrrolidines having potential antitumor effect. Method: Dispiro[oxindole-cyclohexanone]-pyrrolidines 6a-h were synthesized in a regioselective manner via 1,3-dipolar cycloaddition reaction of 2,6-diarylidenecyclohexanones 3a-h, isatin, and sarcocine. Compounds 6a-h were alkylated to give (7-10)a,b. All compounds were evaluated in vitro for their antitumor activity and cytotoxic selectivity against breast cancer cell lines (MCF-7 and MDA-MB-231), breast fibrosis cell line (MCF10a), and placental cancer cell line (JEG-3). Molecular modeling inside the MDM2 binding site was performed using AutoDock4.2. Results: Synthesized compounds showed antitumor activity comparable to tamoxifen and compounds 3a,b,f,g and 9a,b showed selective cytotoxicity against tumor cells but reduced toxicity toward MCF-10a cells. Molecular modelling shows that both classes of synthesized compounds are predicted to fit the deep hydrophobic cleft on the surface of MDM2 and mimic the interactions between p53 and MDM2. Conclusion: The synthesized compounds have antitumor activity against MCF-7, MDA-MB-231, and JEG-3. Few compounds showed a selective cytotoxic effect and may have the potential to inhibit MDM2 and stimulate p53. In the future, studies regarding the optimization of medicinal chemistry as well as mechanistic studies will be conducted to enhance the inhibition effect of identified compounds and elucidate their mechanism of action.
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- 2022
6. Development and characterization of silicon dioxide clad silicon carbide optics for terrestrial and space applications
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Arjun Dey, K. V. Sriram, Girish M. Gouda, B. Rudraswamy, and Tayaramma D.P.V. Jalluri
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Materials science ,Scanning electron microscope ,business.industry ,Process Chemistry and Technology ,Polishing ,Substrate (electronics) ,Nanoindentation ,Surfaces, Coatings and Films ,Electronic, Optical and Magnetic Materials ,chemistry.chemical_compound ,chemistry ,visual_art ,Materials Chemistry ,Ceramics and Composites ,Silicon carbide ,visual_art.visual_art_medium ,Optoelectronics ,Texture (crystalline) ,Ceramic ,business ,Layer (electronics) - Abstract
Silicon carbide (SiC), a non-oxide ceramic with superior thermo-mechanical stability, chemical and radiation resistive properties, finds extensive utilization in optical instruments for terrestrial and space applications. However, its inherent porous texture (α-HCP) becomes a deterrent for high-performance optical telescopes, although several techniques of surface alterations over sintered or reaction-bonded SiC are available. In the present work, the physical vapour deposition (PVD) technique is adopted to deposit a thick (∼5 μm) Silicon dioxide (SiO2) clad layer on a sintered and optically polished SiC (SSiC) substrate. SiO2 clad layer coated SSiC (SDO-SSiC) substrate reduces the surface porosity of SSiC which is found to be suitable for optical mirror application. Finally, an Al based reflective and oxides protective coatings are deposited on SiO2 clad layer to achieve reflective behaviour. The surface figure of 75 nm PV (peak-to-valley) and less than 2 nm surface micro-roughness values are achieved which meets the stringent optical telescope specifications for terrestrial and space applications. The structural and nano-mechanical properties of presently developed SiO2 clad layer-based SiC telescopic mirror have been characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive X-Ray Analysis (EDX), atomic force microscopy (AFM), and nanoindentation techniques. The optical properties are investigated by optical profilometry and wavelength based spectrometric (both in visible and infrared ranges) techniques. Finally, space worthiness studies viz., thermo-vacuum, thermal storage, thermal shock and relative humidity tests have been carried out successfully. The process of cleaning, grinding and polishing at each substrate preparation stage and coatings are also reported comprehensively.
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- 2022
7. Preconcentration and separation of Cd(II), Co(II), Cu(II), Ni(II), and Pb(II) in environmental samples on cellulose nitrate membrane filter prior to their flame atomic absorption spectroscopy determinations
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Ahmed Youssef, Ragaa El Sheikh, Hameeda A. Khadrajy, Walaa Gamil, Ayman A. Gouda, and Nancy Gouda
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Trace Amounts ,Chemistry ,Health, Toxicology and Mutagenesis ,010401 analytical chemistry ,Public Health, Environmental and Occupational Health ,Soil Science ,Membrane filter ,010501 environmental sciences ,01 natural sciences ,Pollution ,0104 chemical sciences ,Analytical Chemistry ,Membrane technology ,law.invention ,Ion ,chemistry.chemical_compound ,Nitrate ,law ,Environmental Chemistry ,Cellulose ,Atomic absorption spectroscopy ,Waste Management and Disposal ,0105 earth and related environmental sciences ,Water Science and Technology ,Nuclear chemistry - Abstract
A new and sensitive enrichment membrane filtration method was applied for the preconcentration and separation of trace amounts of Cd(II), Co(II), Cu(II), Ni(II), and Pb(II) ions from environmental ...
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- 2020
8. Pyrimidine-Piperazine Hybrids; Recent Synthesis and Biological Activities
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Mohammed Baashen, V. Lakshmi Ranganatha, Mohammed Al-Ghorbani, and Moustafa A. Gouda
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chemistry.chemical_compound ,Piperazine ,Polymers and Plastics ,Pyrimidine ,Chemistry ,Organic Chemistry ,Materials Chemistry ,Combinatorial chemistry ,Hybrid - Published
- 2021
9. Association between glycemic control and cardiovascular events in older Japanese adults with diabetes mellitus: An analysis of the Japanese medical administrative database
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Ryo Suzuki, Hiroaki Iijima, Maki Gouda, Masaya Inagaki, Akiko Yamazaki, and Koutaro Yokote
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Male ,Databases, Factual ,endocrine system diseases ,Diabetic Cardiomyopathies ,Endocrinology, Diabetes and Metabolism ,Fractures, Bone ,chemistry.chemical_compound ,0302 clinical medicine ,Glycated hemoglobin ,Japan ,030212 general & internal medicine ,Older diabetes patients ,Aged, 80 and over ,Incidence ,Incidence (epidemiology) ,Hazard ratio ,Articles ,General Medicine ,Hospitalization ,Clinical Science and Care ,Quartile ,Cardiovascular Diseases ,Female ,Original Article ,medicine.medical_specialty ,030209 endocrinology & metabolism ,Glycemic Control ,Hypoglycemia ,Diseases of the endocrine glands. Clinical endocrinology ,Cardiovascular events ,03 medical and health sciences ,Diabetes mellitus ,Internal medicine ,Diabetes Mellitus ,Internal Medicine ,medicine ,Humans ,Aged ,Proportional Hazards Models ,Glycemic ,business.industry ,Proportional hazards model ,nutritional and metabolic diseases ,medicine.disease ,RC648-665 ,chemistry ,Heart Disease Risk Factors ,business - Abstract
Aims/Introduction The relationship between glycated hemoglobin (HbA1c) and cardiovascular events in older adults was investigated using a Japanese administrative medical database. Materials and Methods Anonymized medical data on patients with diabetes mellitus aged ≥65 years for the period from January 2010 to December 2019 were extracted from the EBM Provider database. The primary end‐point was a composite of cardiovascular events, whereas the other end‐points included severe hypoglycemia and fracture. The association between cardiovascular events and HbA1c at the index date (i.e., approximately 10 months after initial diabetes mellitus diagnosis) was evaluated using the Cox proportional hazards model. Results Among the 3,186,751 patients in the database, 3,946 older adults with diabetes mellitus were eligible for inclusion and were subsequently grouped according to HbA1c quartiles at the index date. Cardiovascular events occurred in 142 patients. Patients with HbA1c in the highest quartile had significantly higher risk of hospitalization for cardiovascular disease than those with HbA1c in the lowest quartile (hazard ratio 1.948; 95% confidence interval 1.252–3.031, P = 0.003). However, the events risk was similar across subgroups with HbA1c, We investigated the relationship between glycated hemoglobin and cardiovascular events in older adults with diabetes mellitus using administrative medical databases in Japan. Among approximately 4,000 older patients without a history of dementia, cancer or cardiovascular disease, those with glycated hemoglobin in the highest quartile had a significantly higher risk of hospitalization for cardiovascular disease than those with glycated hemoglobin in the lowest quartile. Age, sex, prescription of antihypertensive drugs and comorbidities were also associated with the risk of cardiovascular events.
- Published
- 2021
10. The Relationship between Serum Procalcitonin and Dialysis Adequacy in Hemodialysis Patients
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Ahmed Yehia Mohamed, Saeed Abdelwahab Saeed, and Khaled Gouda
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Creatinine ,medicine.medical_specialty ,Dialysis adequacy ,business.industry ,Cross-sectional study ,medicine.medical_treatment ,Urea reduction ratio ,bacterial infections and mycoses ,Procalcitonin ,chemistry.chemical_compound ,chemistry ,Internal medicine ,parasitic diseases ,medicine ,Population study ,Medical history ,Hemodialysis ,business ,hormones, hormone substitutes, and hormone antagonists - Abstract
Introduction: In hemodialysis (HD) patients procalcitonin (PCT) considered as an early predictor of acute infection. It represents a new and potential marker of inflammation and may correlate with dialysis adequacy. This makes procalcitonin a potential biomarker for obesity-related low-grade inflammation.Objective: The aim of the work was to assess procalcitonin level in obese prevalent hemodialysis patients and its relation to hemodialysis adequacy. Patients and Methods: A cross sectional study was conducted on 90 patients divided into 3 groups, 40 obese (BMI ≥ 30 Kg/m2) ESRD patients on regular hemodialysis (group A), 40 non obese (BMI < 25 Kg/m2) ESRD patients on regular hemodialysis (group B) attending at Dialysis Unit, El-Sahel Teaching Hospital and 10 healthy individuals with BMI < 25 Kg/m2 as a control group (group C). All patients were subjected to detailed history taking and general examination. All patients were laboratory investigated for CBC, serum urea, creatinine, CRP, urea reduction ratio (URR), equilibrated Kt/v. All controls were subjected to written informed consent, full history, examination and CRP level. Procalcitonin level was done by ELISA technique for all patients and controls.Results: In our study, we found that there was a higher level of procalcitonin (PCT) in obese hemodialysis patient than non-obese. We also found that there was no correlation between PCT and hemodialysis adequacy in our study population.Conclusion: It could be concluded that procalcitonin is a potential biomarker for obesity-related low-grade inflammation, but not related to hemodialysis adequacy.
- Published
- 2021
11. A new carrier element-free coprecipitation method with 3-benzyl-4-p-nitrobenzylidenamino-4,5-dihydro-1,2,4-triazole-5-thiol for separation, preconcentration, and determination of some metal ions in water and food samples
- Author
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Ayman A. Gouda, Hameeda A. Khadrajy, Nancy Gouda, Ragaa El Sheikh, and Wafaa S. Hassan
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chemistry.chemical_classification ,Chemistry ,Coprecipitation ,Health, Toxicology and Mutagenesis ,Metal ions in aqueous solution ,010401 analytical chemistry ,Inorganic chemistry ,Public Health, Environmental and Occupational Health ,Soil Science ,1,2,4-Triazole ,010501 environmental sciences ,01 natural sciences ,Pollution ,0104 chemical sciences ,Analytical Chemistry ,Ion ,chemistry.chemical_compound ,Certified reference materials ,Thiol ,Environmental Chemistry ,Waste Management and Disposal ,0105 earth and related environmental sciences ,Water Science and Technology - Abstract
A new, simple, and accurate carrier element-free coprecipitation method has been developed to separate and preconcentrate of Cd(II), Cu(II), Ni(II), and Pb(II) ions from water and food samples. The...
- Published
- 2020
12. Concomitant Administration of Rosuvastatin and Lefleunamide in Low doses Synergize Against Complete Freunds Adjuvant (CFA)-Induced Rheumatoid Arthritis in Experimental Model
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Gouda Kamel Helal, Abdel-Aziz Saeed, Mohamed El-Shafey, and El-Sayed Akool
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Experimental model ,Thiobarbituric acid ,business.industry ,Arthritis ,Glutathione ,Pharmacology ,medicine.disease ,Malondialdehyde ,chemistry.chemical_compound ,chemistry ,Concomitant ,Rheumatoid arthritis ,medicine ,Rosuvastatin ,business ,medicine.drug - Abstract
Aim: The present work was designed to examine of the potential anti-inflammatory effect of rosuvastatin (ROSV) and/or Lefleunamide (LFLU) against Complete Freunds Adjuvant (CFA)-induced arthritis in rats. Methods: The mRNA level of perxisome proliferator-activated receptor-alpha (PPAR-a) was determined using Real-time PCR. The levels of NF-B, iNOS, IL-6, TNF-a and SOD activity were measured using ELISA. The swollen paws were measured using caliper. The GSH level was measured using colorimetric assay. The level of malondialdehyde (MDA) was determined using thiobarbituric acid reactive substances assay kit. Results: ROSV induced the expression of PPAR-a that suppresses NF-kB as demonstrated by a strong reduction in NF-kB level in animals treated with ROSV. Also, ROSV administration reduced the levels of the inflammatory mediators IL-6 and TNF-a. In addition, iNOS and MDA content as well as expression of MMP-9 and MMP-2 induced by CFA is abrogated in animals treated with ROSV. Also GSH content and SOD activity were highly increased in ROSV-treated animals. Furthermore, the size of right paw induced by CFA was reduced in ROSV-treated rats. Moreover, the histopathological alterations induced by CFA were highly improved in animals treated with ROSV. Similar results were also found in animals treated with LFLU. Importantly, similar effects were obtained in rats treated with both ROSV and LFLU in half doses. Conclusion: This study demonstrates that ROSV as well as LFLU has the ability to inhibit rheumatoid arthritis in experimental model induced by CFA. Importantly, concomitant administration of ROSV and LFLU in half doses synergize against rheumatoid arthritis.
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- 2021
13. Influence of Blastocystis hominis on the small intestine and lactase enzyme activity
- Author
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Gehad A. Basuony, Eman S. El-Wakil, Maha M.A. Basyoni, Mohamed Shemis, Mohamed Sherif Ismail Negm, Enas A. El Saftawy, Eman Ali Mohamed Mostafa, and Abdullah E. Gouda
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medicine.medical_specialty ,Lactose intolerance ,Blastocystis ,Brush border ,Biology ,medicine.disease ,biology.organism_classification ,Small intestine ,chemistry.chemical_compound ,Endocrinology ,medicine.anatomical_structure ,chemistry ,Apoptosis ,Internal medicine ,medicine ,Immunohistochemistry ,Parasitology ,Tumor necrosis factor alpha ,Lactose - Abstract
Blastocystis hominis is a cosmopolitan protozoan that has been associated with several gastrointestinal disturbances involving lactose intolerance. However, the underlying pathogenic factors remain indistinct. 20 Swiss albino mice were utilized and assembled into four groups, each of five mice: group-I: received neither infection nor lactose (healthy control), group-II: received a single dose of 10,000 cysts of Blastocystis and lactose diets in a dose of 12.5 g/day/mouse for 7 consecutive days starting from day 14 p.i., group-III: non-infected mice with oral doses of lactose (12.5 g/day/mouse) for 7 consecutive days (positive control), group-IV: infected mice on lactose free diet (negative control). We investigated the histopathological changes using H&E stain.s Also, lactase enzyme activity was measured using spectrophotometry and the production of TNF-α and apoptotic events were explored via immunohistochemistry and compared in the small intestine of all groups. The active inflammatory changes in the infected animals were moderate in the form of loss of villous architecture, increased ILC (P-value > 0.001) besides scattered forms of the parasite as compared to non-infected mice. There was a reduction in lactase enzyme activity p.i. The TNF-α levels were induced p.i. as compared to non-infected mice (P-value > 0.001). The expression of Bax protein was upgraded, while Bcl-2 expression decreased significantly with a reverse in Bax/Bcl2 ratio in infected animals. Blastocystis infection appears to humble lactase enzyme activity via the induction of apoptosis in the epithelial cells of the small intestinal brush border in a TNF-α associative pathway.
- Published
- 2021
14. Development of effectively costed and performant novel cation exchange ceramic nanocomposite membrane based sulfonated PVA for direct borohydride fuel cells
- Author
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Arafat Toghan, Marwa H. Gouda, and Noha A. Elessawy
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chemistry.chemical_classification ,Materials science ,Nanocomposite ,General Chemical Engineering ,technology, industry, and agriculture ,Proton exchange membrane fuel cell ,02 engineering and technology ,Polymer ,010402 general chemistry ,021001 nanoscience & nanotechnology ,Borohydride ,01 natural sciences ,Polyvinyl alcohol ,0104 chemical sciences ,chemistry.chemical_compound ,Membrane ,Chemical engineering ,chemistry ,Direct borohydride fuel cell ,Polymer blend ,0210 nano-technology - Abstract
A direct borohydride fuel cell (DBFC) is a type of low temperature fuel cell, and to commercialize this type of fuel cell, it requires efficient and inexpensive proton exchange membranes. In this study, a binary polymer blend is formulated from inexpensive and ecofriendly polymers such as iota carrageenan (IC) and polyvinyl alcohol (PVA). Zirconiam phosphate (ZrPO4) was synthesized from a simple impregnation — calcination method and later embedded as a doping agent into the polymeric matrix with percentage (1–7.5) wt.%. The novel nanocomposite membranes were evaluated by TGA, DSC, FTIR, XRD and SEM. The oxidative stability and tensile strength of the obtained membranes were enhanced and achieved results better than those of Nafion117 due to an increase in the number of hydrogen bonds formed between the polymer functional groups and oxygen functional groups of ZrPO4with increasing doping concentration. In addition, the borohydride permeability of the membranes decreased with increasing ZrPO4weight percentage, while the ionic conductivity and power density increased to 25.5 mS cm−1 and 66 mW cm−2, respectively, for membrane with 5 wt.% of ZrPO4. The fabricated membrane with the optimum properties (PVA/IC/ZrPO4− 5) can be efficient as a proton exchange membrane towards the development of green and low cost DBFCs.
- Published
- 2021
15. Spectrophotometric and conductometric studies of new synthesized azo derived from pyrazole as analytical reagents
- Author
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Farid I. El-Dossoki, F. A. El-Seify, and Mahmoud M. Gouda
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Chromogenic ,General Chemical Engineering ,Metal ions in aqueous solution ,Quinoline ,General Chemistry ,Pyrazole ,Biochemistry ,Industrial and Manufacturing Engineering ,chemistry.chemical_compound ,chemistry ,Stability constants of complexes ,Reagent ,Materials Chemistry ,Titration ,Stoichiometry ,Nuclear chemistry - Abstract
A new pyrazole derivatives azo dye 1-(3-phenyl-5-Pyrazolylazo)-R acid (L1) and 5-(3-phenyl-5-Pyrazolylazo)-8-hydroxy quinoline (L2) was synthesized. The acid–base equilibrium, ionization constants, the effect of pH and some organic solvents on the spectra of ligands, the chromogenic reaction and the stability constant of Co+2, Cu+2,Ni+2 and Zn+2 ion complexes with ligands were studied and determined spectrophotometrically and conductometrically. The optimum pH was determined for the ligands and the complexes. 2:1 and 1:1 (L:M) stoichiometric complexes have been formed in solutions. The stability constants order of the under study complexes was Co+2
- Published
- 2021
16. Celastrol Modulates Multiple Signaling Pathways to Inhibit Proliferation of Pancreatic Cancer via DDIT3 and ATF3 Up-Regulation and RRM2 and MCM4 Down-Regulation
- Author
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Hisham A. Abbas, Mahmoud Youns, Momen Askoura, Wael A H Hegazy, Ahmad J. Almalki, Ahdab N. Khayyat, Gouda H. Attia, Reham M. Goda, and El-Sayed Khafagy
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0301 basic medicine ,Cell growth ,Caspase 3 ,Biology ,medicine.disease ,OncoTargets and Therapy ,03 medical and health sciences ,chemistry.chemical_compound ,030104 developmental biology ,0302 clinical medicine ,Oncology ,Downregulation and upregulation ,chemistry ,Apoptosis ,Celastrol ,030220 oncology & carcinogenesis ,Pancreatic cancer ,medicine ,Cancer research ,Cytotoxic T cell ,Pharmacology (medical) ,Signal transduction - Abstract
Mahmoud Youns, 1, 2 Momen Askoura, 3 Hisham A Abbas, 3 Gouda H Attia, 4, 5 Ahdab N Khayyat, 6 Reham M Goda, 7 Ahmad J Almalki, 6 El-Sayed Khafagy, 8, 9 Wael AH Hegazy 3 1Department of Biochemistry and Molecular Biology, Faculty of Pharmacy, Helwan University, Cairo, Egypt; 2Department of Functional Genome Analysis, German Cancer Research Center (DKFZ), Heidelberg, 69120, Germany; 3Department of Microbiology and Immunology, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt; 4Department of Pharmacognosy, Faculty of Pharmacy, Kafr El-Shiekh University, Kafr El-Shiekh, Egypt; 5Department of Pharmacognosy, College of Pharmacy, Najran University, Najran, Saudi Arabia; 6Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia; 7Department of Microbiology and Biotechnology, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa, Mansoura, Egypt; 8Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj, 11942, Saudi Arabia; 9Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, 41552, EgyptCorrespondence: Mahmoud Youns Tel +0096891742704Email dr.mahmoudyouns@yahoo.comBackground: Pancreatic cancer is one of the most serious and lethal human cancers with a snowballing incidence around the world. The natural product celastrol has also been widely documented as a potent anti-inflammatory, anti-angiogenic, and anti-oxidant.Purpose: To elucidate the antitumor effect of celastrol on pancreatic cancer cells and its modulatory role on whole genome expression.Methods: The antitumor activity of celastrol on a panel of pancreatic cancer cells has been evaluated by Sulforhodamine B assay. Caspase 3/7 and histone-associated DNA fragments assays were done for apoptosis measurement. Additionally, prostaglandin (PGE2) inhibition was evaluated. Moreover, a microarray gene expression profiling was carried out to detect possible key players that modulate the antitumor effects of celastrol on cells of pancreatic cancer.Results: Our findings indicated that celastrol suppresses the cellular growth of pancreatic cancer cells, induces apoptosis, and inhibits PGE2 production. Celastrol modulated many signaling genes and its cytotoxic effect was mainly mediated via over-expression of ATF3 and DDIT3, and down-expression of RRM2 and MCM4.Conclusion: The current study aims to be a starting point to generate a hypothesis on the most significant regulatory genes and for a full dissection of the celastrol possible effects on each single gene to prevent the pancreatic cancer growth.Keywords: celastrol, natural products, pancreatic cancer, RRM2, DDIT3, MCM4
- Published
- 2021
17. Simultaneous preconcentration and determination of zirconium in environmental samples using ultrasound-assisted ionic liquid based dispersive liquid-liquid microextraction combined with spectrophotometry
- Author
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Ayman A. Gouda, Ragaa El Sheikh, Lamees I. Mahfouz, Enas M. El Sheikh, Marwa M. El-Gabry, and Mahmoud S. Khalafalla
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Zirconium ,Materials science ,Chromatography ,medicine.diagnostic_test ,Health, Toxicology and Mutagenesis ,Public Health, Environmental and Occupational Health ,Soil Science ,chemistry.chemical_element ,Ultrasound assisted ,Pollution ,Analytical Chemistry ,Ion ,chemistry.chemical_compound ,chemistry ,Spectrophotometry ,Ionic liquid ,medicine ,Environmental Chemistry ,Liquid liquid ,Waste Management and Disposal ,Water Science and Technology - Abstract
The Green, delicate and rapid ultrasound-assisted ionic liquid-based dispersive liquid-liquid microextraction technique was developed to preconcentrate trace quantities of zirconium Zr(IV) ion in r...
- Published
- 2021
18. Synthesis and reactivity of thieno[2,3‐ b ]quinoline derivatives (Part <scp>II</scp> )
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M. A. Salem, Moustafa A. Gouda, Ahmed A. M. Abdelgawad, and Ameen A. Abu-Hashem
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chemistry.chemical_compound ,chemistry ,Organic Chemistry ,Quinoline ,Reactivity (chemistry) ,Medicinal chemistry - Published
- 2021
19. Impact of Some Novel Synthesized Cationic Surfactants on the Corrosion of Carbon Steel in 1M HCl Solutions
- Author
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M.A. Migahed, Mahmoud M. Gouda, S. A. Abd El-Maksoud, and Farid I. El-Dossoki
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010302 applied physics ,Materials science ,Carbon steel ,Mechanical Engineering ,Langmuir adsorption model ,02 engineering and technology ,engineering.material ,021001 nanoscience & nanotechnology ,01 natural sciences ,Corrosion ,Dielectric spectroscopy ,symbols.namesake ,chemistry.chemical_compound ,Adsorption ,chemistry ,Mechanics of Materials ,Bromide ,0103 physical sciences ,symbols ,engineering ,Gravimetric analysis ,General Materials Science ,Fourier transform infrared spectroscopy ,0210 nano-technology ,Nuclear chemistry - Abstract
The corrosion inhibition of carbon steel in 1 M HCl solutions was studied in the presence of two synthesized cationic surfactants: N, N, N-tributylhexan-1-aminium bromide and N, N, N-tributyldodecan-1-aminium bromide. Gravimetric, electrochemical, and surface analysis techniques were used to describe the corrosion behavior in blank and inhibiting solutions. Weight loss was estimated in the absence and presence of different additives. The studies were achieved at various temperatures (25-45 °C). The thermodynamic parameters were determined. Potentiodynamic polarization (PP) and electrochemical impedance spectroscopy (EIS) were used as electrochemical techniques at 25 °C. The inhibition efficiency increases with the concentration. The two surfactants behave as mixed corrosion inhibitors. It was found that the adsorption process obeys Langmuir isotherm. Adsorption and kinetics parameters were calculated and then explained. The surface morphology of the C-steel and the formed protective film were examined using SEM, AFM, and FTIR spectroscopy. The data obtained from various techniques were in good agreement.
- Published
- 2021
20. Redox-Linked Coordination Chemistry Directs Vitamin B12 Trafficking
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Harsha Gouda, Shubhadra Pillay, and Ruma Banerjee
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Cofactor binding ,biology ,010405 organic chemistry ,General Medicine ,General Chemistry ,010402 general chemistry ,01 natural sciences ,Cobalamin ,Cofactor ,0104 chemical sciences ,chemistry.chemical_compound ,Dimethylbenzimidazole ,Mutase ,chemistry ,Biochemistry ,polycyclic compounds ,biology.protein ,Transferase ,Methionine synthase ,CBLC - Abstract
ConspectusMetals are partners for an estimated one-third of the proteome and vary in complexity from mononuclear centers to organometallic cofactors. Vitamin B12 or cobalamin represents the epitome of this complexity and is the product of an assembly line comprising some 30 enzymes. Unable to biosynthesize cobalamin, mammals rely on dietary provision of this essential cofactor, which is needed by just two enzymes, one each in the cytoplasm (methionine synthase) and the mitochondrion (methylmalonyl-CoA mutase). Brilliant clinical genetics studies on patients with inborn errors of cobalamin metabolism spanning several decades had identified at least seven genetic loci in addition to the two encoding B12 enzymes. While cells are known to house a cadre of chaperones dedicated to metal trafficking pathways that contain metal reactivity and confer targeting specificity, the seemingly supernumerary chaperones in the B12 pathway had raised obvious questions as to the rationale for their existence.With the discovery of the genes underlying cobalamin disorders, our laboratory has been at the forefront of ascribing functions to B12 chaperones and elucidating the intricate redox-linked coordination chemistry and protein-linked cofactor conformational dynamics that orchestrate the processing and translocation of cargo along the trafficking pathway. These studies have uncovered novel chemistry that exploits the innate chemical versatility of alkylcobalamins, i.e., the ability to form and dismantle the cobalt-carbon bond using homolytic or heterolytic chemistry. In addition, they have revealed the practical utility of the dimethylbenzimidazole tail, an appendage unique to cobalamins and absent in the structural cousins, porphyrin, chlorin, and corphin, as an instrument for facilitating cofactor transfer between active sites.In this Account, we navigate the chemistry of the B12 trafficking pathway from its point of entry into cells, through lysosomes, and into the cytoplasm, where incoming cobalamin derivatives with a diversity of upper ligands are denuded by the β-ligand transferase activity of CblC to the common cob(II)alamin intermediate. The broad reaction and lax substrate specificity of CblC also enables conversion of cyanocobalamin (technically, vitamin B12, i.e., the form of the cofactor in one-a-day supplements), to cob(II)alamin. CblD then hitches up with CblC via a unique Co-sulfur bond to cob(II)alamin at a bifurcation point, leading to the cytoplasmic methylcobalamin or mitochondrial 5'-deoxyadenosylcobalamin branch. Mutations at loci upstream of the junction point typically affect both branches, leading to homocystinuria and methylmalonic aciduria, whereas mutations in downstream loci lead to one or the other disease. Elucidation of the biochemical penalties associated with individual mutations is providing molecular insights into the clinical data and, in some instances, identifying which cobalamin derivative(s) might be therapeutically beneficial.Our studies on B12 trafficking are revealing strategies for cofactor sequestration and mobilization from low- to high-affinity and low- to high-coordination-number sites, which in turn are regulated by protein dynamics that constructs ergonomic cofactor binding pockets. While these B12 lessons might be broadly relevant to other metal trafficking pathways, much remains to be learned. This Account concludes by identifying some of the major gaps and challenges that are needed to complete our understanding of B12 trafficking.
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- 2021
21. A comparative study to evaluate the effect of Puerarin versus simvastatin as osteoconductive material for Maxillary sinus augmentation: A prospective randomized control clinical trial
- Author
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Mohammed Khashaba, Ghada Abdel Monim, and Ayman Gouda
- Subjects
Sinus Floor Augmentation ,Maxillary sinus ,business.industry ,medicine.medical_treatment ,Dentistry ,Bone grafting ,chemistry.chemical_compound ,Exact test ,medicine.anatomical_structure ,chemistry ,Puerarin ,Medicine ,business ,Bone regeneration ,Dental implant ,Dental alveolus - Abstract
Dental implant is an effective treatment method for oral rehabilitation. Still, it has to be modified because of unfavorable environments such as excessive alveolar bone loss and sinus pneumatization. Maxillary sinus grafting is a standard procedure used to correct such unfavorable conditions in the posterior maxilla. Purpose: to assess and compare changes in height and percentage of Puerarin versus simvastatin as osteoconductive materials following sinus augmentation. Basic procedures: twenty patients with edentulous posterior maxilla were selected and equally grouped into 2 groups. Both groups underwent antral augmentation using either Puerarin on Fisiograft sponge carrier graft (group A) or combination of simvastatin and β-TCP (group B). The amount and percentage of bone graft were evaluated radiographically. Assessment occurred at period intervals 1-week and 6-month postoperatively. Data were presented as mean and standard deviation (SD) values. For non-parametric data, Mann-Whitney U test was used to compare between the two groups. Qualitative data were presented as frequencies and percentages. Fisher’s Exact test was used for comparisons between the groups. The significance level was set at P ≤ 0.05. Main finding: there was decrease in the amount and percentage of bone graft height by 2.5 mm, 19.7% (for Group A) and 3.2 mm, 22.4% (for Group B) at the end of the 6 months period without significant difference in both group (P-value = 0.054, Effect size = 0.919) and (P-value = 0.151, Effect size = 0.678), respectively. Conclusion: Puerarin and Simvastatin are clinically beneficial and safe bone grafting materials in cases of antral augmentation.
- Published
- 2021
22. Association between interleukin 28B polymorphism and sustained virological response to sofosbuvir plus daclatasvir in chronic hepatitis C genotype 4 Egyptian patients
- Author
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El-Sayed M. El-Sayed, Gouda K. Helal, Khalid S. Hassanien, Zakarya M. Zakarya, and Raed S. Ismail
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Adult ,Male ,medicine.medical_specialty ,Pyrrolidines ,Daclatasvir ,Adolescent ,Genotype ,Sustained Virologic Response ,Sofosbuvir ,Hepatitis C virus ,Black People ,medicine.disease_cause ,Antiviral Agents ,Polymorphism, Single Nucleotide ,030226 pharmacology & pharmacy ,Gastroenterology ,Group B ,Young Adult ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Internal medicine ,Ribavirin ,medicine ,Humans ,Pharmacology (medical) ,Prospective Studies ,030212 general & internal medicine ,Aged ,Pharmacology ,business.industry ,Imidazoles ,Valine ,Hepatitis C ,Hepatitis C, Chronic ,Middle Aged ,medicine.disease ,Interleukin 28B ,chemistry ,Drug Therapy, Combination ,Egypt ,Female ,Carbamates ,Interferons ,business ,medicine.drug - Abstract
WHAT IS KNOWN AND OBJECTIVE Sofosbuvir has been approved as the first nonstructural protein 5B polymerase inhibitor with pan-genotypic activity against the hepatitis C (HCV) virus. Daclatasvir is a first-in-class hepatitis C virus nonstructural protein 5A replication complex inhibitor. We aimed to evaluate the usefulness of the reference single nucleotide polymorphism (rs12979860) interleukin 28B (CC genotype) for predicting sustained virological response to sofosbuvir plus daclatasvir in Egyptian patients infected with HCV-4. METHODS Samples were collected at week zero. One hundred and thirty-one patients who reached the end of treatment (at week 12) were divided into three groups, according to their interleukin 28B genotype: Group A included 31 patients (CC genotype), group B included 79 patients (CT genotype) and group C had 21 patients (TT genotype). All patients received treatment for 3 months in the form of sofosbuvir plus daclatasvir with ribavirin (in case of cirrhotic patients) or without ribavirin (in case of non-cirrhotic patients). RESULTS AND DISCUSSION Sustained virological response rate was significantly higher in patients with IL28B (CC genotype) vs. (non-CC genotype) (100 vs.88%) (p
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- 2021
23. Concomitant inhibition of hedgehog signalling and activation of retinoid receptors abolishes bleomycin‐induced lung fibrosis
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Gouda K. Helal, Ahmed Fawzy Eleraky, Raed S. Ismail, and Mohamed F. ElShafie
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0301 basic medicine ,Receptors, Retinoic Acid ,Physiology ,medicine.drug_class ,Pulmonary Fibrosis ,Retinoic acid ,Retinoid receptor ,Retinoid X receptor ,Bleomycin ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Physiology (medical) ,Pulmonary fibrosis ,medicine ,Animals ,Retinoid ,Receptor ,Pharmacology ,Chemistry ,medicine.disease ,Hedgehog signaling pathway ,Rats ,Oxidative Stress ,030104 developmental biology ,030220 oncology & carcinogenesis ,Cancer research ,Signal Transduction - Abstract
Pulmonary fibrosis is a devastating disease with unknown treatment. All-trans retinoic acid (ATRA) attenuates bleomycin-induced lung fibrosis by different mechanistic pathways. However, the role of retinoid receptors in lung fibrosis is still unclear. Forskolin (FSK), a potent inhibitor for the revolutionary hedgehog (Hh) signalling pathway, has a promising antifibrotic effect on other organs such as the liver. This study investigates the interplay between the retinoid receptors modulation and the Hh signalling pathway in bleomycin (BLM)-induced pulmonary fibrosis. Rats were randomised and administrated a single dose of 7.5 mg/kg of BLM alone and with ATRA, FSK and both of them. The effects of FSK and ATRA on lung functions, oxidative stress markers (malondialdehyde [MDA], glutathione [GSH], superoxide dismutase [SOD] and catalase [CAT]), retinoid markers (retinoic acid receptors [RAR] and rexinoid X receptors [RXR]) and Hh signalling markers (patched homolog 1 [Ptch-1], Smoothened [Smo] and glioblastoma-2 [Gli-2]) were assessed. In single therapies, ATRA and FSK ameliorated BLM-induced lung fibrosis. On the contrary, a combination of both drugs synergistically reversed the effect of BLM-induced lung fibrosis, as indicated by the enhancement of lung functions and the decrease of the α-smooth muscle actin (α-SMA) expression and collagen deposition. Additionally, FSK and ATRA ameliorated oxidative stress and inflammation, reduced transforming growth factor β1 (TGF-β1) levels and reversed the effect of BLM on the mRNA expression of Ptch-1, Smo and Gli-2. FSK inhibited the Hh pathway and also activated protein kinase A (PKA) that is, in part, involved in phosphorylation of RAR/RXR heterodimer (a key step in retinoid receptor activation). The present results suggest that a combination of FSK and ATRA has a promising therapeutic value for lung fibrosis management.
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- 2021
24. Novel cytokinin oxidase/dehydrogenase inhibitors for enhancing grain yield in crop plants and potential applications in the biotechnology industry
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Lambodar Behera, Ramakrishna Vadde, Manoj Kumar Gupta, Gayatri Gouda, and Ravindra Donde
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0106 biological sciences ,0301 basic medicine ,Cytokinins ,Physiology ,Chemistry ,Cytokinin oxidase ,Dehydrogenase ,Plant Science ,Plants, Genetically Modified ,01 natural sciences ,Crop ,03 medical and health sciences ,chemistry.chemical_compound ,Horticulture ,030104 developmental biology ,Gene Expression Regulation, Plant ,Cytokinin ,Grain yield ,Edible Grain ,Oxidoreductases ,Biotechnology ,010606 plant biology & botany ,Biotechnology industry - Abstract
This article comments on:Nisler J, Kopečný D, Pěkná Z, Končitíková R, Koprna R, Murvanidze N, Werbrouck SPO, Havlíček L, De Diego N, Wimmer Z, Briozzo P, Moréra S, Zalabák D, Spíchal L, Strnad M. 2021. Diphenylurea-derived cytokinin oxidase/dehydrogenase inhibitors for biotechnology and agriculture. Journal of Experimental Botany 72, 355–370.
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- 2021
25. Effect of nano-potassium fertilization on fruiting of Zaghloul date palm
- Author
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F.M. Gouda, I.F.M. Badawy, A.M. Alsalhy, A.A. Shamroukh, and M.M. Al-Wasfy
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nanotechnology ,potassium ,Potassium ,Vinasse ,food and beverages ,chemistry.chemical_element ,Agriculture ,Ripening ,Biology ,vinasse ,Horticulture ,chemistry.chemical_compound ,Human fertilization ,chemistry ,fertilization ,Anthocyanin ,Orchard ,Palm ,Sugar ,date palm - Abstract
This investigation was conducted during the two successive seasons i.e. 2019 and 2020 on Zaghloul date palm grown at the experimental orchard, Faculty of Agriculture, South Valley University, Qena, Egypt. This work conducted to study the effect of different sources of potassium fertilizers on fruiting of Zaghloul date palm under Qena condition. Potassium fertilization via nano-technology, vinasse and potassin were used. The experiment was arranged in a complete randomized design with three replications. It is evident from the obtained results that using nano-potassium, either soil dressing or foliar spray, as well as foliar spray of vinasse or potassin significantly increased the fruit retention, bunch weight and yield/palm compared to fertilize by potassium sulphate (check treatment). Also, these treatments significantly improved dates quality in terms of increasing fruit weight, flesh percentage, TSS, sugar percentages and anthocyanin contents moreover, decreasing total acidity and total tannins compared to fertilize with the recommended potassium doses via potassium sulphate. From the results, it could be concluded that fertilized Zaghloul date palm with potassium fertilization via foliar spray of either nano-potassium, vinasse or potassium to improve the fertilization efficiency and get high yield with best dates quality. In addition, hasten advance the fruit ripening and overcome potassium fertilization problems.
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- 2021
26. Impact of in ovo Injection of Certain Vitamins to Improve the Physiological Conditions of Hatching Chicks
- Author
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Mosaad M El-Moniary, Ahmed Gouda, and Samar A Tolba
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Vitamin ,food.ingredient ,Hatching ,Embryogenesis ,Embryo ,Biology ,In ovo ,chemistry.chemical_compound ,Animal science ,Nutrient ,food ,chemistry ,Yolk ,embryonic structures ,Agronomy and Crop Science ,Hatchling - Abstract
BACKGROUND AND OBJECTIVE Exposure of breeder hens to hyperthermia causes disturbances in the breeder's eggs due to insufficient nutrient deposition from heat-stressed hen into the egg. Therefore, this experiment was conducted to test the hypothesis that the adverse effects of heat stress on hatchability, embryonic growth and hatchling health status could be ameliorated by in ovo injection of certain vitamins. MATERIALS AND METHODS A total of 270 fertile eggs from Fayoumi breeders (45 weeks) were randomly assigned to 6 groups (45 eggs/group). During the egg collection period in the summer season, birds were maintained at 9-13°C above the standard thermo-neutral temperature. The experimental groups were: negative control (eggs not injected either with vitamins or Sterile Deionized Water (SDW)), positive control (eggs injected with 0.1 mL of SDW/egg) and four other treatments in which vitamins A, E, D3 and folic acid were injected (1 mg of each vitamin dissolved in 0.1 mL of SDW/egg). The eggs were incubated at 37.7°C and 65% relative humidity in an automatic incubator. RESULTS The residual yolk, embryo length and weight and hatchability% were improved (p
- Published
- 2021
27. Influences of vitamin A, L-carnitine, and folic acid in ovo feeding on embryo and hatchling characteristics and general health status in ducks
- Author
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Ahmed Gouda, Samar A Tolba, and Khalid M. Mahrose
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Vitamin ,animal structures ,Embryogenesis ,Bioengineering ,Embryo ,Biology ,In ovo ,Andrology ,chemistry.chemical_compound ,chemistry ,Folic acid ,embryonic structures ,medicine ,Animal Science and Zoology ,Carnitine ,General health ,Hatchling ,Biotechnology ,medicine.drug - Abstract
The current investigation was conducted to test the potential effects of in ovo feeding of vitamin A, L-carnitine, and folic acid on embryonic growth and post-hatch performance. A total of 450 fert...
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- 2021
28. Tuning the selectivity of biomass oxidation over oxygen evolution on NiO–OH electrodes
- Author
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Laxman Gouda, Pardis Adams, S. David Tilley, Elena Mas-Marzá, Francisco Fabregat-Santiago, Thomas Moehl, and Laurent Sévery
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chemistry.chemical_compound ,Chemical engineering ,Chemistry ,Side reaction ,Oxygen evolution ,Environmental Chemistry ,Electrolyte ,Electrochemistry ,Electrocatalyst ,Pollution ,Alkali hydroxide ,Faraday efficiency ,Catalysis - Abstract
Electrochemical reactions powered by renewable electricity are an important means of reducing the carbon footprint of large-scale chemical processes. Here, we investigate the efficient conversion of biomass-derived 5-hydroxymethylfurfural (HMF) to 2,5-furandicarboxylic acid (FDCA), an important building block in the polymer and pharmaceutical industries, using a cheap and abundant nickel-based electrocatalyst. We elucidate the key factors for tuning the chemical selectivity for HMF oxidation over the competing oxygen evolution reaction (OER) at the catalyst surface. We show that the selectivity for HMF oxidation is enhanced by removing trace impurities of iron species as well as adjusting the composition of the alkali hydroxide electrolyte solution. LiOH solution without iron impurities is more favorable for HMF oxidation, whereas CsOH solution with iron species present is more active for the OER and unfavorable for HMF oxidation. Under optimized conditions, HMF oxidation in 1 M LiOH electrolyte solution without iron (pH 14) achieved 98% faradaic efficiency for the production of FDCA. The principles used in this work can be applied to other electrosynthetic reactions, in particular where the OER is the main competing side reaction.
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- 2021
29. Optical-switchable energy transfer controlled by multiple-responsive turn-on fluorescence via metal–ligand and host–guest interactions in diarylethene-based [2]pseudo-rotaxane polymers
- Author
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Tung Kung Wu, Hong-Cheu Lin, Yaw-Kuen Li, Chong Lun Wei, Kung-Hwa Wei, Feng Cheng Ho, Chinmayananda Gouda, Trang Manh Khang, Chi Chong Xiao, and Ravinder Singh
- Subjects
chemistry.chemical_classification ,Rotaxane ,Supramolecular chemistry ,Photochemistry ,Supramolecular polymers ,chemistry.chemical_compound ,Molecular wire ,Electron transfer ,Förster resonance energy transfer ,chemistry ,Diarylethene ,Cyclen ,Materials Chemistry ,General Materials Science - Abstract
Multi-responsive and optically-active diarylethene-based [2]pseudo-rotaxane polymers Zn2+-TC2/DS(O & C) were synthesized and prepared via metal–ligand and host–guest interactions, where Zn2+ ion was coordinated with two ligands (TC) containing a macrocyclic dibenzo-24-crown-8 (DB24C8) linked to a terpyridyl terminus to form a symmetrical host (Zn2+-TC2) and diarylethene (DAE) bearing two terminal secondary ammonium salts to form a symmetrical guest (DS). Upon irradiation of UV-light (λ = 355 nm), the prominent photo-induced electron transfer (PET) off process to promote optical-switchable Forster resonance energy transfer (FRET) process from the emissive metal-coordination Zn2+-TC2 host to the fluorescent DS(C) guest (in the closed form of emissive DAE unit) was explored for the multiple-responsive turn-on ratiometric fluorescence in supramolecular polymer Zn2+-TC2/DS(C). Remarkably, endowed with the novel features of reversible chemical/chelation-stimuli responsive dis-assembly/re-assembly of non-covalent interactions in response to pH/chelation, the polymer can be used for the sensing of pH and cyclen. Accordingly, the “molecular wire and stimuli-responsive effects” of diarylethene-based [2]pseudo-rotaxane polymer Zn2+-TC2/DS(C) reveal significant supramolecular interactions to elucidate the turn-on fluorescence via the controllable FRET-ON process from Zn2+-TC2 host donor to PET-OFF DS(C) guest acceptor, which pave a promising route to elaborate optical-switchable supramolecular platforms for the future energy transfer applications.
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- 2021
30. Application of stimuli-responsive FRET behavior toward cyanide detection in a photo-switchable [2]pseudorotaxane polymer containing the BODIPY donor and the merocyanine acceptor
- Author
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Hong-Cheu Lin, Venkatesan Srinivasadesikan, Chandrima Maitra, Sarala Chandran, Shu-Pao Wu, Debashis Barik, Ming-Chang Lin, Chinmayananda Gouda, Feng Cheng Ho, and Kai Chieh Liang
- Subjects
Spiropyran ,Quenching (fluorescence) ,Materials science ,Cyanide ,Supramolecular chemistry ,General Chemistry ,Photochemistry ,Acceptor ,chemistry.chemical_compound ,Förster resonance energy transfer ,chemistry ,Materials Chemistry ,Merocyanine ,BODIPY - Abstract
We have developed a supramolecular (close form) [2]pseudorotaxane polymer containing the green-emissive (λem = 523 nm) BODIPY-based pillar[5]arene host and the non-emissive spiropyran (SP)-based cyano guest (close form), which can be converted to a red-emissive (λem = 630 nm) merocyanine (MC)-based guest (open form) upon UV exposure as well as turned into a bi-fluorophoric host–guest polymer with ratiometric PL emission of Forster resonance energy transfer (FRET) behavior in THF/water solution (60% H2O, v/v). The equal host–guest molar ratio and the formation of the [2]pseudorotaxane polymer can be further verified using 1H NMR titration, Job's plot analysis, DOSY and ITC experiments. Hence, the bi-fluorophoric host–guest (with the MC open form) polymer possessed the highest red-emission of the MC acceptor, which was also confirmed using TRPL measurements to possess the shortest lifetime of 0.37 ns and the best FRET efficiency of 83.5%. Since the MC unit could react with CN− to induce a non-emissive quenching process, the mono-fluorophoric guest would show turn-off PL behavior and detect cyanide ions with a corresponding limit of detection (LOD) value of 0.94 μM. In comparison, the optimal LOD value of 0.48 μM toward CN− anion could be achieved by our bi-fluorophoric host–guest polymer via the FRET-OFF process. Therefore, cyanide detection and cell viability tests using the open form of the [2]pseudorotaxane polymer suggest useful bio-imaging applications in living cells.
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- 2021
31. Sensitive spectrophotometric determination of vardenafil HCl in pure and dosage forms
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D.S. Abdel Haleem, M.M. Mabrouk, Ayman A. Gouda, and S.F. El-Malla
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Drug Compounding ,Pharmaceutical Science ,Bromophenol blue ,Sensitivity and Specificity ,030226 pharmacology & pharmacy ,01 natural sciences ,Dosage form ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Vardenafil Dihydrochloride ,Bromothymol blue ,medicine ,Coloring Agents ,Dosage Forms ,Pharmacology ,Detection limit ,Chromatography ,Bromocresol green ,010401 analytical chemistry ,Reproducibility of Results ,Phosphodiesterase 5 Inhibitors ,Reference Standards ,0104 chemical sciences ,Solutions ,chemistry ,Vardenafil ,Standard addition ,Indicators and Reagents ,Spectrophotometry, Ultraviolet ,Bromocresol purple ,Tablets ,medicine.drug - Abstract
Summary Objectives The present work aims to develop and validate a simple, rapid, cost-effective, sensitive and extractive spectrophotometric methods for the determination of phosphodiesterase type 5-inhibitor; vardenafil HCl (VARD) in pure and in dosage forms. Methods The developed methods are based on the formation of ion-pair complexes between vardenafil HCl and dyes, namely, bromocresol green (BCG), bromocresol purple (BCP), bromophenol blue (BPB), bromothymol blue (BTB) and eriochrom black T (EBT) in acidic buffer solutions. Different factors affecting the reactions between VARD and the dyes were studied and optimized. Results The formed complexes were extracted with methylene chloride and measured at 418, 410, 415, 417 and 520 nm using BCG, BCP, BPB, BTB and EBT, respectively. The beer's law was obeyed in the ranges 1.0–10, 1.0–16, 0.5–8.0, 2.0–20 and 1.0–14 μg mL−1 for BCG, BCP, BPB, BTB and EBT, respectively under the optimum conditions. The composition of the ion-pairs was found 1:1. The molar absorptivity's, Sandell's sensitivity, limits of detection and the limits of quantification were calculated. Other method validation parameters, such as accuracy, intra-day and inter-day precision, robustness, ruggedness and selectivity, have been evaluated. Conclusion The proposed methods have been applied successfully for the analysis of vardenafil HCl in pure and dosage forms. The reliability of the methods was further ascertained by performing recovery studies using the standard addition method. Statistical comparison of the results with the reported method was performed by applying student's t- and F-tests and no significant statistical differences were obtained.
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- 2021
32. Variability in Rhizoctonia solani causing sheath blight of rice and its chemical management
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Neelam Maurya, Dharmendra Kumar, and Amaresh Gouda S
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biology ,Carbendazim ,food and beverages ,Fungus ,biology.organism_classification ,Rhizoctonia solani ,Fungicide ,Propiconazole ,chemistry.chemical_compound ,Horticulture ,Sheath blight ,chemistry ,Hexaconazole ,Tebuconazole - Abstract
Rhizoctonia solani is infamous fungus for its highly destructive pathogenic effect that can result in extensive damage of rice crop. To know the variability among the Indian isolates of R. solani inciting sheath blight in rice, four isolates were isolated from diseased samples of Uttar Pradesh, Uttrakhand, Gujarat and Karnataka states of India. Variability in isolates was observed with respect to the cultural, morphological and pathogenic level. Evaluation of toxicity of various fungicides against R. solani under in vitro condition showed the maximum sensitivity of R. solani by carbendazim even at 1 ppm concentration followed by Tebuconazole + trifoxystrobin and Hexaconazole. R. solani showed good tolerance to Kresoxim methyl even at 100 mg kg-1 concentration. All tested fungicides namely Propiconazole, Hexaconazole, Kresoxim-methyl, Tebuconazole 50% + Trifloxystrobin 25%, Tricyclazole and Carbendazim caused complete inhibition of colony growth of R.solani at 1000 ppm. Foliar spray of Carbendazim @ 0.1% was found highly effective for the management of sheath blight in field condition with highest per cent reduction in disease (86.29%) followed by Tebuconazole + Trifloxystrobin (83.30%), Hexaconazole (74.20%) and Propiconazole (45.28%). Plots treated with Tricyclazole and Kresoxim Methyl had only 29.15 and 12.24 per cent reduction over control, respectively.
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- 2021
33. Recent progress on the chemistry of thieno[3,2‐ b ]quinoline derivatives (part <scp>III</scp> )
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Ameen A. Abu-Hashem, Moustafa A. Gouda, and Ahmed A. M. Abdelgawad
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chemistry.chemical_classification ,Part iii ,chemistry.chemical_compound ,Ketone ,chemistry ,Organic Chemistry ,Quinoline ,Organic chemistry ,Reactivity (chemistry) - Published
- 2020
34. Development and experimental evaluation of titanium diboride particulate reinforcements on the Al6061 alloy composites properties
- Author
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P. S. Shivakumar Gouda, Mandadi Surya Vamsi, Tammila Subash, K. Naresh, U Srinivas Kumar Chowdary, G.B. Veeresh Kumar, and R. Pramod
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0209 industrial biotechnology ,Materials science ,Alloy ,02 engineering and technology ,engineering.material ,Particulates ,021001 nanoscience & nanotechnology ,Industrial and Manufacturing Engineering ,chemistry.chemical_compound ,020901 industrial engineering & automation ,chemistry ,Mechanics of Materials ,Ultimate tensile strength ,engineering ,General Materials Science ,Composite material ,0210 nano-technology ,Reinforcement ,Titanium diboride - Abstract
In recent times, industries are focusing to develop newer materials with superior properties compared to the materials available at present. In this regard, the present investigation is aimed at th...
- Published
- 2020
35. Functional Low Fat Fruit Yoghurt
- Author
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Mervat Hamed, Khoulod Blassy, and Magdy Osman Amin Gouda
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chemistry.chemical_classification ,Antioxidant ,Chemistry ,Pulp (paper) ,medicine.medical_treatment ,Flavonoid ,Flavour ,food and beverages ,engineering.material ,Total dissolved solids ,Low fat yoghurt ,Lactic acid ,Extended storage ,chemistry.chemical_compound ,engineering ,medicine ,Food science - Abstract
Low fat set yoghurt (0.7%) fortified with different fruit pulps (persimmon, mango and guava) and ratios (5, 10 and 15%, w/w) were prepared and stored at 5±1oC for 14 days. Chemical, rheological, total viable lactic acid bacteria and sensory properties were measured when fresh and at 7 and 14 days of storage period. There were significant (p≤0.05) differences between plain yoghurt (control) and functional low fat fruit yoghurt in the total solids (T.S %), antioxidant scavenging activity (ASA%), total phenolic compounds (TPC) and total flavonoid compounds (TFC), they were increased with the increase of the fruit pulp ratios added. While, the pH value and fat% were decreased with the increase of the fruit pulps percentage. The results showed that pH value decreased with extended storage period. Highest values of ASA, TFC and TPC were belonged to yoghurt fortified with guava, mango and persimmon, respectively at 15 % ratio and at 7 days then decreased. The yoghurt containing guava pulp had the highest total viable lactic acid bacteria count compared with plain yoghurt and other fruits yoghurt. The highest (p≤0.05) apparent viscosity was recorded in yoghurt fortified mango, guava and persimmon pulps, respectively. Yoghurt treatments containing 10% mango, 10% persimmon and 5% guava recorded highest sensory scores in low fat yoghurt compared with plain yoghurt and other ratios. The results of current study demonstrated that addition of fruits to the yoghurt significantly improved the rheological properties, body & texture and flavour and support production of low fat yoghurt with more bioactive compounds.
- Published
- 2020
36. Functional Properties of Yoghurt Fortified with Fruits Pulp
- Author
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Khoulod Blassy Magdy Osman, Amin Gouda, and Mervat Hamed
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chemistry.chemical_classification ,Free Radical Scavenging Activity ,Control treatment ,Chemistry ,Pulp (paper) ,Flavour ,Food fortification ,Flavonoid ,food and beverages ,engineering.material ,Total dissolved solids ,Lactic acid ,chemistry.chemical_compound ,engineering ,Food science - Abstract
The world interested in food fortification with fruits (e.g. persimmon, mango and guava) that have nutritive and healthy benefits. Therefore, the present study is focused to study the antioxidants properties of yoghurt fortified with fruit pulps. Full fat set yoghurt fortified with different fruit pulps at ratios (5, 10 and 15%, w/w) were prepared and stored at 5±1°C for 14 days. Chemical, rheological, total viable lactic acid bacteria and sensory properties were measured when fresh and after 7 and 14 days of storage period. The results indicated that, there were significant differences between plain yoghurt and fruit yoghurt in the total solids (T.S%), free radical scavenging activity (RSA%), total phenolic compounds (TPC) and total flavonoid compounds (TFC), which increased with the increase of the fruit pulp ratios. While, pH value was decreased with the increase of the fruit pulps percentage added and with extended storage period. The yoghurt containing guava pulp had the highest total viable lactic acid bacteria count compared with plain yoghurt and other fruit yoghurt. Sensory evaluation results showed that there were significant (p < 0.05) differences among the yoghurt treatments. The yoghurt containing 10% mango, 10% persimmon and 5% guava were recorded highest scores in full fat yoghurt compared with plain yoghurt and other ratios. The highest apparent viscosity was recorded in yoghurt containing persimmon, mango and guava pulps, respectively. The results of current study demonstrated that addition of fruits to the yoghurt significantly improved the rheological properties, body & texture and flavour compared with control treatment and support set yoghurt with more bioactive compounds.
- Published
- 2020
37. Design and In vitro Investigation of Grafted Chitosan as Chitosan Nanoparticles Containing Deflazacort Drug Coated by Calcium Starch Glycolate
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Mona E. Ibrahim, Ammar N. Harmal, Moustafa A. Gouda, and Elsayed M. Abdel Bary
- Subjects
chemistry.chemical_classification ,Materials science ,Polymers and Plastics ,General Chemical Engineering ,chemistry.chemical_element ,Cyclohexanone ,02 engineering and technology ,General Chemistry ,Polymer ,Mannich base ,Calcium ,010402 general chemistry ,021001 nanoscience & nanotechnology ,01 natural sciences ,In vitro ,0104 chemical sciences ,Chitosan ,Deflazacort ,chemistry.chemical_compound ,chemistry ,medicine ,0210 nano-technology ,Acetamide ,medicine.drug ,Nuclear chemistry - Abstract
Novel chitosan nanoparticles (SCN) were synthesized via reaction of chitosan with different concentration of 2-chloro-N-(3-methylisoxazol-5-yl) acetamide (5 %, 10 % and 15 %) at 70–80 °C for 7 h to give the grafted polymer, which condensed with cyclohexanone Mannich base 45 °C for 7 h to afford the corresponding (SCN). These were stirred with Deflazacort drug to achieve the Deflazacort loading (SCN), which, compressed with calcium starch glycolate (CaSgly) to give the corresponding tablets. The pH 2. 1 and concentration of SCN-10 %/CaSgly (1:4) was found to be important parameters in controlling the release profiles.
- Published
- 2020
38. Docking studies of sesquiterpene lactones isolated from Ambrosia maritima L. reveals their potential anti-inflammatory and cytotoxic activities
- Author
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Sameh AbouZid, Amira Mohamed, Ahmed M. Gouda, Dalia El Amir, and Marwa H.A. Hassan
- Subjects
010405 organic chemistry ,medicine.drug_class ,Stereochemistry ,Organic Chemistry ,Plant Science ,Sesquiterpene ,01 natural sciences ,Biochemistry ,Anti-inflammatory ,0104 chemical sciences ,Analytical Chemistry ,010404 medicinal & biomolecular chemistry ,chemistry.chemical_compound ,chemistry ,Docking (molecular) ,Cell culture ,medicine ,Cytotoxic T cell ,Ambrosia ,IC50 - Abstract
Five sesquiterpene lactones were isolated and identified from Ambrosia maritima L. Hymenin showed highest cytotoxic activity against HCT-116, A-549, and MCF-7 cell lines (IC50= 3.83 ± 0.2, 5.48 ± 0...
- Published
- 2020
39. Design of a novel optical sensor for determination of trace amounts of tin in food and in environmental samples
- Author
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Alaa S. Amin and Ayman A. Gouda
- Subjects
Trace Amounts ,Health, Toxicology and Mutagenesis ,010401 analytical chemistry ,Inorganic chemistry ,Public Health, Environmental and Occupational Health ,Soil Science ,chemistry.chemical_element ,010501 environmental sciences ,equipment and supplies ,01 natural sciences ,Pollution ,Colorimetry (chemical method) ,0104 chemical sciences ,Analytical Chemistry ,Ion ,chemistry.chemical_compound ,chemistry ,Sodium tetraphenylborate ,Environmental Chemistry ,Tin ,Waste Management and Disposal ,0105 earth and related environmental sciences ,Water Science and Technology - Abstract
A novel sensitive, selective, and reversible tin(IV) ion optical sensor was prepared depends on the incorporation of amino-4-(3-nitrophenylazo)pyridine-3-ol, (ANPAP) and sodium tetraphenylborate (N...
- Published
- 2020
40. Landscape of Lipid Management Following an Acute Coronary Syndrome Event: Survey of Canadian Specialists
- Author
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Milan Gupta, Robert C. Welsh, Michelle Padarath, Robert A. Hegele, Pishoy Gouda, and Jean Grégoire
- Subjects
lcsh:Diseases of the circulatory (Cardiovascular) system ,Acute coronary syndrome ,medicine.medical_specialty ,education.field_of_study ,Lipid management ,Statin ,medicine.drug_class ,Cholesterol ,business.industry ,Population ,Familial hypercholesterolemia ,medicine.disease ,Clinical trial ,chemistry.chemical_compound ,chemistry ,lcsh:RC666-701 ,Internal medicine ,medicine ,Original Article ,lipids (amino acids, peptides, and proteins) ,Cardiology and Cardiovascular Medicine ,education ,business ,Lipoprotein - Abstract
Background: Following the occurrence of an acute coronary syndrome (ACS), patients are at high risk for subsequent cardiovascular events. Therapies to lower the level of low-density lipoprotein (LDL) cholesterol remain a pillar in secondary prevention approaches following ACS. Significant variability remains in the application of therapies to lower cholesterol level in clinical practice. Methods: A cross-sectional, online survey was conducted of 200 cardiovascular and lipid specialists across Canada who routinely care for patients following the occurrence of ACSs. The survey consisted of 50 multiple-choice questions with opportunities for free-text entry exploring knowledge of lipid guidelines and recent clinical trials, and in-hospital and outpatient management of lipids and familial hypercholesterolemia. Results: A total of 67.5% (n = 135) of participants stated that a lipid panel would routinely be obtained during the first 24 hours of an admission for an ACS, and 68.5% (n = 137) stated that their hospitals had standing orders for statin initiation at ACS presentation. In high-risk patients, the majority (75.5%; n = 151) of participants indicated that they target an LDL cholesterol level of 70% of their ACS patients were at or below guideline-recommended LDL cholesterol levels. Respondents generally underappreciated the prevalence of familial hypercholesterolemia in both the general population and ACS patients. Conclusions: There is significant variation in practice patterns involving therapies to lower LDL cholesterol level in the post–ACS onset period. To improve management of lipids in this high-risk population, changes to institutional policies, shared responsibility of lipid management across multiple disciplines, and physician education are required. Résumé: Contexte: Après un syndrome coronarien aigu (SCA), le risque qu’un autre événement cardiovasculaire survienne est élevé. Les traitements visant à réduire le taux de cholestérol des lipoprotéines de basse densité (C-LDL) demeurent l’un des piliers de la prévention secondaire après un SCA. Dans la pratique clinique, l’utilisation de ces traitements varie considérablement d’un praticien à l’autre. Méthodologie: Nous avons mené une enquête transversale en ligne auprès de 200 spécialistes de la santé cardiovasculaire et des lipides de partout au Canada, qui traitent régulièrement des patients ayant subi un SCA. L’enquête comprenait 50 questions à choix multiples; les participants pouvaient aussi donner des réponses détaillées permettant d’évaluer leurs connaissances des lignes directrices en matière de maîtrise des lipides et des essais cliniques récents, ainsi que de la prise en charge de la lipidémie et de l’hypercholestérolémie familiale en contexte hospitalier et ambulatoire. Résultats: Au total, 67,5 % (n = 135) des participants ont déclaré demander systématiquement un bilan lipidique complet dans les 24 heures suivant l’admission d’un patient en raison d’un SCA, et 68,5 % (n = 137) des participants ont dit que la norme dans leur hôpital était d’instaurer un traitement par statine chez tous les patients ayant subi un SCA. Dans le cas des patients présentant un risque élevé, la majorité des participants (75,5 %, n = 151) ont indiqué qu’ils ciblaient un taux de C-LDL de moins de 1,8 mmol/l. Une partie de ces répondants (22 %; n = 4) ont dit cibler un taux de C-LDL encore plus bas, soit de 0,5 à 1,7 mmol/l. Seulement 32,0 % (n = 64) des répondants ont déclaré que plus de 70 % de leurs patients ayant subi un SCA avaient un taux de C-LDL à la limite ou en deçà du taux recommandé dans les lignes directrices. Les répondants ont en général sous-estimé la prévalence de l’hypercholestérolémie familiale dans la population générale et chez les patients ayant subi un SCA. Conclusions: Les pratiques varient considérablement d’un praticien à l’autre en ce qui concerne les traitements visant à diminuer le taux de C-LDL après la survenue d’un SCA. Afin d’améliorer la prise en charge de la lipidémie dans cette population exposée à un risque élevé, il conviendrait de revoir les politiques des établissements, de répartir la responsabilité de la prise en charge de la lipidémie entre les intervenants de différentes disciplines et de mieux informer les médecins.
- Published
- 2020
41. Potentiometric Study of a New Schiff Base and its Metal Ion Complexes: Preparation, Characterization and Biological Activity
- Author
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O. A. Farghaly, Hamed Al-Saidi, and Gamal A. Gouda
- Subjects
Metal ,chemistry.chemical_compound ,Schiff base ,Chemistry ,visual_art ,Potentiometric titration ,Electrochemistry ,visual_art.visual_art_medium ,Biological activity ,Nuclear chemistry ,Characterization (materials science) - Published
- 2020
42. Pharmacophore-based virtual screening, synthesis, biological evaluation, and molecular docking study of novel pyrrolizines bearing urea/thiourea moieties with potential cytotoxicity and CDK inhibitory activities
- Author
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Ahmed M. Gouda, Ahmed M. Shawky, Ashraf N. Abdalla, Nashwa A. Ibrahim, and Mohammed A.S. Abourehab
- Subjects
urea derivatives ,Drug Evaluation, Preclinical ,Antineoplastic Agents ,RM1-950 ,01 natural sciences ,Structure-Activity Relationship ,chemistry.chemical_compound ,Cyclin-dependent kinase ,Cell Line, Tumor ,Drug Discovery ,Humans ,Urea ,Pyrroles ,pyrrolizine ,Cytotoxicity ,Protein Kinase Inhibitors ,Cell Proliferation ,Biological evaluation ,Pharmacology ,Virtual screening ,Dose-Response Relationship, Drug ,Molecular Structure ,biology ,010405 organic chemistry ,Cyclin-Dependent Kinase 2 ,apoptosis ,General Medicine ,Combinatorial chemistry ,0104 chemical sciences ,Molecular Docking Simulation ,010404 medicinal & biomolecular chemistry ,Thiourea ,chemistry ,cdk-2 ,biology.protein ,cytotoxicity ,cell cycle ,Therapeutics. Pharmacology ,Urea derivatives ,Drug Screening Assays, Antitumor ,Pharmacophore ,Research Article ,Research Paper - Abstract
In the current study, virtual screening of a small library of 1302 pyrrolizines bearing urea/thiourea moieties was performed. The top-scoring hits were synthesised and evaluated for their cytotoxicity against three cancer (MCF-7, A2780, and HT29) and one normal (MRC-5) cell lines. The results of the MTT assay revealed potent cytotoxic activities for most of the new compounds (IC50 = 0.16–34.13 μM). The drug-likeness study revealed that all the new compounds conform to Lipinski’s rule. Mechanistic studies of compounds 18 b, 19a, and 20a revealed the induction of apoptosis and cell cycle arrest at the G1 phase in MCF-7 cells. The three compounds also displayed potent inhibitory activity against CDK-2 (IC50 = 25.53–115.30 nM). Moreover, the docking study revealed a nice fitting of compound 19a into the active sites of CDK-2/6/9. These preliminary results suggested that compound 19a could serve as a promising scaffold in the discovery of new potent anticancer agents., Graphical Abstract Highlights Virtual screening of 1302 pyrrolizines was done using the pharmacophore model of the multi-CDKI 3. The top-scoring hits were synthesised and evaluated for their cytotoxic activities. Compound 19a showed potent in vitro cytotoxic activity against CDK-2. Compound 19a induced apoptosis and cell cycle arrest at the G1 phase in MCF-7 cells. The docking study revealed nice fitting of compound 19a into CDK-2/6/9 with high binding affinities.
- Published
- 2020
43. Ultrasound-Assisted Ionic Liquid Microextraction for Preconcentration of Cadmium in Water, Vegetables and Hair Samples Prior to FAAS Determination
- Author
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Ragaa El Sheikh, Ali Sayqal, Ayman A. Gouda, Eman M. Hafez, and Najla AlMasoud
- Subjects
Cadmium ,chemistry.chemical_compound ,Chromatography ,010405 organic chemistry ,Chemistry ,010401 analytical chemistry ,Ionic liquid ,chemistry.chemical_element ,Ultrasound assisted ,01 natural sciences ,0104 chemical sciences ,Analytical Chemistry - Abstract
Background:: Cadmium (Cd2+) is considered to be one of the most important hazardous heavy metals due to its toxicity for living organisms at low concentration levels. Therefore, the estimation of trace Cd2+ in different types of various samples is a very important objective for chemists using effective methods. In the present work, a novel, green, easy and fast ultrasoundassisted ionic liquid-dispersive liquid phase microextraction technique (UA-IL-DLPME) was developed to preconcentrate and determine trace quantities of cadmium (Cd2+) ions from real samples, prior to detection by FAAS. Methods: The proposed technique is based on utilization of ionic liquid (IL) (1-hexyl-3- methylimidazolium tris(pentafluoroethyl)trifluorophosphate [HMIM][FAP]) as an extraction solvent for Cd2+ ions after complexation with 2-(6-methylbenzothiazolylazo)-6-nitrophenol (MBTANP) at pH 7.0. The impact of different analytical parameters on the microextraction efficiency was investigated. The validation of the proposed procedure was verified by the test of two certified reference materials (TMDA-51.3 fortified water, SRM spinach leaves 1570A) applying the standard addition method. Results: In the range of 2.0-200 μg L−1, the calibration graph was linear. Limit of detection, preconcentration factor and the relative standard deviation (RSD %, 100 μg L-1, n=5) as precision was 0.1 μg L-1, 100 and 3.1%, respectively. Conclusion: Green UA-IL-DLPME method was developed and applied to preconcentrate and determine trace quantities of Cd2+ in real water, vegetables and hair samples with satisfactory results.
- Published
- 2020
44. Correlation of VEGF and MMP-2 levels in oral lichen planus: An in vivo immunohistochemical study
- Author
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Ossama M. Gouda, Hala H. Hazzaa, Nora Abdelgawad, Naglaa M. Kamal, and Marwa A. M. El Shiekh
- Subjects
Pathology ,medicine.medical_specialty ,business.industry ,Review Article ,030206 dentistry ,Matrix metalloproteinase ,medicine.disease ,Malignant transformation ,Vascular endothelial growth factor ,Pathogenesis ,stomatognathic diseases ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,stomatognathic system ,Otorhinolaryngology ,chemistry ,In vivo ,030220 oncology & carcinogenesis ,Reticular connective tissue ,Medicine ,Immunohistochemistry ,Oral lichen planus ,business ,General Dentistry - Abstract
BACKGROUND: This study aimed to investigate the relation between vascular endothelial growth factors (VEGF) and matrix metalloproteinase-2 (MMP-2) in different oral lichen planus (OLP) forms compared to control patients. METHODS: Biopsies from 60 patients were selected and equally distributed as follows: reticular/popular OLP (R/PLP), atrophic/erosive OLP (A/ELP) patients, healthy subjects (Control). All biopsies were immune-histochemical stained and statistically analyzed for VEGF and MMP-2 expression. RESULTS: Immune-expression of VEGF was significant between OLP and control (P-value
- Published
- 2020
45. The Effect of Low Dose Doxycycline Combined with Nonsurgical Periodontal Therapy on The Level of Nitric Oxide in Gingival Crevicular Fluid of Patients with Stage I Periodontitis. A randomized clinical trial
- Author
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Osama Mohamed Gouda and Marwa Mohamed Tawfiq
- Subjects
Doxycycline ,Periodontitis ,0303 health sciences ,medicine.medical_specialty ,business.industry ,Combined use ,Low dose ,Healthy subjects ,030206 dentistry ,medicine.disease ,Gastroenterology ,law.invention ,Nitric oxide ,Crevicular fluid ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Randomized controlled trial ,chemistry ,law ,Internal medicine ,Medicine ,business ,030304 developmental biology ,medicine.drug - Abstract
The aim of this study was recording, the effect of conventional periodontal therapy (SRP) combined low dose doxycycline on nitric oxide level (NO) in gingival crevicular fluid (GCF) of patients with stage I periodontitis. Materials and methods: 40 patients had stage I Periodontitis were grouped into two groups: (group 1): 20 patients will receive SRP at three sessions + doxycycline 20 mg systemically twice daily (for 2 weeks). (Group 2): 20 patients will receive only SRP at three sessions for 2weeks. With 20 healthy subjects acting as control group (group 3). Clinical evaluation and GCF sample was collected from two groups (1& 2) at base line, 15 and 30 days intervals and from healthy group at base line only. Results: All the clinical indices and NO levels were found significantly higher in stage I Periodontitis groups compared to the control group at base line where (p < 0.001) with no statistically significant differences between (Group 1) and (Group 2) where (p < 0.05). When comparing the 2 studied patients groups and the healthy control group, founded improvement in clinical indices and NO levels at 15 and 30 days respectively with non-significant differences in all groups. Conclusion: The current results provided that combined use SRP with low dose doxycycline had a reducing effect than SRP only for NO levels in GCF of patients with stage I periodontitis.
- Published
- 2020
46. <scp>3D</scp> ‐pharmacophore study molecular docking and synthesis of pyrido[2,3‐ d ]pyrimidine‐4( <scp> 1 H </scp> ) dione derivatives with in vitro potential anticancer and antioxidant activities
- Author
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Mounir A. I. Salem, Mustafa A. S. Gouda, and Naglaa F. H. Mahmoud
- Subjects
chemistry.chemical_compound ,Antioxidant ,Pyrimidine ,chemistry ,Stereochemistry ,medicine.medical_treatment ,Organic Chemistry ,medicine ,Pharmacophore ,In vitro - Published
- 2020
47. Recent progress on coumarin<scp>scaffold‐based</scp>anti‐microbial agents (Part<scp>III</scp>)
- Author
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Mohammed Al-Ghorbani, Mohamed H. Helal, Wafaa S. Hamama, Ameen A. Abu-Hashem, M. A. Salem, and Moustafa A. Gouda
- Subjects
Part iii ,chemistry.chemical_compound ,Scaffold ,Chemistry ,Organic Chemistry ,Anti-Microbial Agents ,Coumarin ,Combinatorial chemistry - Published
- 2020
48. Comparison of Effectiveness of 70%-isopropanol, 65%-ethanol and 1%-chlorhexidine for Stethoscope Decontamination
- Author
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G. Naveen, Jeevika Mattoo, Swapna Kotian, Sheetal Gouda, and F. Sneha Kukanur
- Subjects
stethoscope ,Stethoscope ,Applied Microbiology and Biotechnology ,Microbiology ,law.invention ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,law ,medicine ,030212 general & internal medicine ,disinfection ,0303 health sciences ,Ethanol ,Chromatography ,isopropyl alcohol ,030306 microbiology ,business.industry ,chlorhexidine ,Chlorhexidine ,Human decontamination ,QR1-502 ,ethyl alcohol ,chemistry ,business ,hospital acquired infection ,Biotechnology ,medicine.drug - Abstract
Stethoscopes are potential vector for health care associated infections worldwide. Ethyl alcohol (EA), isopropyl alcohol (IPA) and chlorhexidine (CH) are widely used for disinfecting stethoscope, however, comparative analysis of these disinfectants are scarce. Hence this paper aims to compare the reduction in bioburden with respect to stethoscope decontamination. A randomized, double-blind study was undertaken from various categories of health care workers (HCW) working in various departments. Each participant was asked to fill a questionnaire and diaphragms of their stethoscopes were imprinted on blood agar and sabourauds dextrose agar before and after disinfection with either 65%-EA, 70%-IPA or 1%-CH. The culture plates were incubated aerobically and the growth was further identified. 384 HCW participated in the study. 168 participants never cleaned their stethoscope, out of which 147 respondents (91.6%) comprised of students. EA (47%) and IPA (23%) were the two major types of alcohols used as disinfecting agents. 280 samples showed growth among which 51.8% were potent pathogens. Before disinfection, Staphylococcus aureus (27%) was the predominant pathogen, followed by Klebsiella (6.8%), Enterococcus and Candida respectively. Among the disinfectants used, maximum antimicrobial activity was exhibited by IPA (92.5%) compared to EA (82.5%) and CH (77.8%). Huge lacunae regarding knowledge, attitude and practice of stethoscope maintenance was found among student community. The microbial growth varies at various department. Disinfecting stethoscope with 70%-IPA for just 30 seconds is equally efficient compared to 1 minute and IPA was superior to EA and CH for decontaminating stethoscope. Stethoscopes are potential vector for health care associated infections worldwide. Ethyl alcohol (EA), isopropyl alcohol (IPA) and chlorhexidine (CH) are widely used for disinfecting stethoscope, however, comparative analysis of these disinfectants are scarce. Hence this paper aims to compare the reduction in bioburden with respect to stethoscope decontamination. A randomized, double-blind study was undertaken from various categories of health care workers (HCW) working in various departments. Each participant was asked to fill a questionnaire and diaphragms of their stethoscopes were imprinted on blood agar and sabourauds dextrose agar before and after disinfection with either 65%-EA, 70%-IPA or 1%-CH. The culture plates were incubated aerobically and the growth was further identified. 384 HCW participated in the study. 168 participants never cleaned their stethoscope, out of which 147 respondents (91.6%) comprised of students. EA (47%) and IPA (23%) were the two major types of alcohols used as disinfecting agents. 280 samples showed growth among which 51.8% were potent pathogens. Before disinfection, Staphylococcus aureus (27%) was the predominant pathogen, followed by Klebsiella (6.8%), Enterococcus and Candida respectively. Among the disinfectants used, maximum antimicrobial activity was exhibited by IPA (92.5%) compared to EA (82.5%) and CH (77.8%). Huge lacunae regarding knowledge, attitude and practice of stethoscope maintenance was found among student community. The microbial growth varies at various department. Disinfecting stethoscope with 70%-IPA for just 30 seconds is equally efficient compared to 1 minute and IPA was superior to EA and CH for decontaminating stethoscope.
- Published
- 2020
49. Synthesis and cytotoxic activity of some new heterocycles incorporating cyclohepta[b]thiophene‐3‐carboxamide derivatives
- Author
-
Moustafa A. Gouda, Mohammed Al-Ghorbani, and Nabil Al-Zaqri
- Subjects
chemistry.chemical_compound ,medicine.drug_class ,Chemistry ,Organic Chemistry ,medicine ,Thiophene ,Cytotoxic T cell ,Carboxamide ,Combinatorial chemistry - Published
- 2020
50. EFFECT OF FEEDING BUFFALOES ON DIETS CONTAINING VEGETABLE OILS RICH IN UNSATURATED FATTY ACIDS ON ITS PRODUCTIVE PERFORMANCE AND MILK QUALITY
- Author
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G.A. Gouda, A. M. Kholif, A. F. Sayed, Hoda Alzahar, and M. Abd El Aziz
- Subjects
food.ingredient ,Cholesterol ,food and beverages ,Total dissolved solids ,Soybean oil ,chemistry.chemical_compound ,Animal science ,food ,Blood serum ,chemistry ,Latin square ,Urea ,lipids (amino acids, peptides, and proteins) ,Dry matter ,Lactose - Abstract
Four lactating buffalos with an average weight of 515 kg were randomly assigned to four experimental groups in a 4 × 4 Latin Square design experiment with repeated measures in time for 16 weeks (4 treatments and four experimental periods).Each group received one of the following four dietary treatments:1- Control ration(fed a basal diet of berseem clover and concentrates (60:40 DM basis), 2- flax group (fed the control diet +2% flaxseed oil), 3- soya group (fed the control diet +2% soybean oil) and 4- flax & soya group (fed the control diet +2% soybean oil plus flaxseed oil (1:1 v/v)). The results showed that the supplementation of buffaloes’ diets with soybean, flaxseed oils or mix-oils had no negative effects on total dry matter intake. Concerning blood serum parameters, flax group had highest values of serum TP, albumin, glucose, triglycerides, cholesterol (HDL, LDL), creatinine, and GOT, while soybean oil treated group recorded the highest values of serum cholesterol, AG ratio, (GPT) and urea-N followed by flax group then flax+soya group. The flax group recorded the highest values of daily milk yield (8.55 kg/h/d), F C M yield (12.71 kg/h/d) and fat content (7.24%), while soya oil treatment recorded the highest values of total solids (19.10%), solids not fat (12.04%), protein (4.91%), lactose (6.16%) and ash content (1%). Control group revealed the lowest values of total solids (17.73%), fat content (6.64%), solids not fat (11.09%), lactose (5.71%). Flaxseed group recorded the highest values of all milk constituents yield except total protein yield followed by soya group, then flax + soya group, while control group recorded the lowest values. Fatty acids in milk showed that C16:0 was higher in control diet than treated diets. Stearic acid (C18:0), C18:4, C20:0 and C20:1 revealed higher values with treated diets than control. At the same time, treatment with soya or mixture of soya and flax oil showed higher values for C18:2 than control or flax treated animals. It could be concluded that adding vegetable oils to buffaloes diet enhanced milk yield and fat content and C18:0, C18:4, C20:0 and C20:1, however, treatment with soya or mixture of soya and flax oil showed higher values for C18:2 than control or flax treated animals.
- Published
- 2020
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