16 results on '"Abdelhalim MM"'
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2. Seroprevalence and molecular detection of Brucella infection in livestock in the United Arab Emirates.
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Ameni G, Zewude A, Bayissa B, Alfaki IA, Albizreh AA, Alhosani N, Mohteshamuddin K, Degefa BA, Hamad ME, Alkalbani MS, Abdelhalim MM, Abdelazim AS, Koliyan RA, Kayaf K, Al Nuaimat MM, Barigye R, Willingham AL, Tibbo M, Edo BM, Sori T, and Eltahir YM
- Abstract
Small ruminants and camels are important livestock species in the United Arab Emirates (UAE), although Brucella infection can limit their productivity. This study aimed to investigate the seroprevalence of Brucella infection and its associated risk factors in small ruminants and camels in the Emirate of Abu Dhabi. Additionally, seropositive animals were tested for the DNA of Brucella . Multispecies competitive enzyme-linked immunosorbent assay (c-ELISA) and multispecies indirect (i-ELISA) were used to test 3,086 animals from 2022 to 2023. Brucella cell surface 31 kDa protein (bcsp31) gene-based real-time polymerase chain reaction (q-PCR) was used to detect Brucella DNA. Multivariate logistic regression was used to assess the association between seroprevalence and potential risk factors. The overall seroprevalences of Brucella infection were 1.7% (95% confidence interval [CI], 1.2%-2.2%) and 5.8% (95% CI, 5.0%-6.7%) based on serial and parallel testing, respectively. The DNA of Brucella was detected in 13 of the 51 seropositive animals. The overall seroprevalence of Brucella infection was associated with the region, type of animal holding, species, and age of the animals. In conclusion, this study documented Brucella infection in small ruminants and camels in the Emirate of Abu Dhabi, warranting necessary intervention strategies to eliminate Brucella infections in livestock populations., Competing Interests: No potential conflict of interest was reported by the author(s)., (© 2024 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.)
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- 2024
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3. Molecular Engines, Therapeutic Targets, and Challenges in Pediatric Brain Tumors: A Special Emphasis on Hydrogen Sulfide and RNA-Based Nano-Delivery.
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Fahmy SA, Dawoud A, Zeinelabdeen YA, Kiriacos CJ, Daniel KA, Eltahtawy O, Abdelhalim MM, Braoudaki M, and Youness RA
- Abstract
Pediatric primary brain tumors represent a real challenge in the oncology arena. Besides the psychosocial burden, brain tumors are considered one of the most difficult-to-treat malignancies due to their sophisticated cellular and molecular pathophysiology. Notwithstanding the advances in research and the substantial efforts to develop a suitable therapy, a full understanding of the molecular pathways involved in primary brain tumors is still demanded. On the other hand, the physiological nature of the blood-brain barrier (BBB) limits the efficiency of many available treatments, including molecular therapeutic approaches. Hydrogen Sulfide (H
2 S), as a member of the gasotransmitters family, and its synthesizing machinery have represented promising molecular targets for plentiful cancer types. However, its role in primary brain tumors, generally, and pediatric types, particularly, is barely investigated. In this review, the authors shed the light on the novel role of hydrogen sulfide (H2 S) as a prominent player in pediatric brain tumor pathophysiology and its potential as a therapeutic avenue for brain tumors. In addition, the review also focuses on the challenges and opportunities of several molecular targeting approaches and proposes promising brain-delivery strategies for the sake of achieving better therapeutic results for brain tumor patients.- Published
- 2022
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4. In vitro antibacterial effect of probiotics against Carbapenamase-producing multidrug-resistant Klebsiella pneumoniae clinical isolates, Cairo, Egypt.
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Abdelhalim MM, Saafan GS, El-Sayed HS, and Ghaith DM
- Abstract
Background: Searching for a non-antibiotic therapeutic option such as probiotics is gaining momentum nowadays. We aimed to evaluate the in vitro antibacterial ability of cell-free supernatant (CFS) of selected Lactobacillus strains (with probiotic properties) against clinical isolates of OXA-48-producing multidrug-resistant (MDR) Klebsiella pneumoniae separately and in combination with cefoperazone antibiotic., Methods: Over a period of 8 months, a cross-sectional experimental study involving 590 Klebsiella pneumoniae isolates was done. Our study took place at The Specialized Pediatric Teaching Hospital of Cairo University. Of the 590 Klebsiella pneumoniae isolates collected from blood cultures, pus, endotracheal aspirates, and pleural fluid, only 50 unrepeated clinical isolates of MDR Klebsiella pneumoniae-producing OXA-48-like detected by CHROMID® OXA-48 (bioMérieux, France) were selected for our study. After determining the minimal inhibitory concentration of CFS of ten Lactobacillus strains and cefoperazone each, the synergistic effect of both was tested., Results: Among ten tested Lactobacillus spp., a significant increase in the mean value of inhibition zone diameter with CFS of L. helveticus (14.32 mm) and L. rhamnosus (13.3 mm) was detected separately. On the contrary, an antagonistic activity against all tested isolates was detected upon combination of Lactobacilli with cefoperazone (512 μg/ml). The mean value of inhibition zone diameter of L. helveticus CFS+ cefoperazone was (11.0 mm) and for L. rhamnosus CFS+ cefoperazone was (10.88 mm) (p value <0.001)., Conclusion: The antimicrobial efficiency of using CFS of Lactobacillus species separately indicates that these therapies may be a substitute treatment strategy against MDR Klebsiella pneumoniae., (© 2022. The Author(s).)
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- 2022
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5. International Nosocomial Infection Control Consortium (INICC) report, data summary of 45 countries for 2013-2018, Adult and Pediatric Units, Device-associated Module.
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Rosenthal VD, Duszynska W, Ider BE, Gurskis V, Al-Ruzzieh MA, Myatra SN, Gupta D, Belkebir S, Upadhyay N, Zand F, Todi SK, Kharbanda M, Nair PK, Mishra S, Chaparro G, Mehta Y, Zala D, Janc J, Aguirre-Avalos G, Aguilar-De-Morós D, Hernandez-Chena BE, Gün E, Oztoprak-Cuvalci N, Yildizdas D, Abdelhalim MM, Ozturk-Deniz SS, Gan CS, Hung NV, Joudi H, Omar AA, Gikas A, El-Kholy AA, Barkat A, Koirala A, Cerero-Gudiño A, Bouziri A, Gomez-Nieto K, Fisher D, Medeiros EA, Salgado-Yepez E, Horhat F, Agha HMM, Vimercati JC, Villanueva V, Jayatilleke K, Nguyet LTT, Raka L, Miranda-Novales MG, Petrov MM, Apisarnthanarak A, Tayyab N, Elahi N, Mejia N, Morfin-Otero R, Al-Khawaja S, Anguseva T, Gupta U, Belskii VA, Mat WRW, Chapeta-Parada EG, Guanche-Garcell H, Barahona-Guzmán N, Mathew A, Raja K, Pattnaik SK, Pandya N, Poojary AA, Chawla R, Mahfouz T, Kanj SS, Mioljevic V, Hlinkova S, Mrazova M, Al-Abdely HM, Guclu E, Ozgultekin A, Baytas V, Tekin R, Yalçın AN, and Erben N
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- Adult, Child, Humans, Infection Control, Intensive Care Units, Prospective Studies, Bacterial Infections epidemiology, Catheter-Related Infections epidemiology, Cross Infection epidemiology, Pneumonia, Ventilator-Associated epidemiology, Urinary Tract Infections epidemiology
- Abstract
Background: We report the results of INICC surveillance study from 2013 to 2018, in 664 intensive care units (ICUs) in 133 cities, of 45 countries, from Latin-America, Europe, Africa, Eastern-Mediterranean, Southeast-Asia, and Western-Pacific., Methods: Prospective data from patients hospitalized in ICUs were collected through INICC Surveillance Online System. CDC-NHSN definitions for device-associated healthcare-associated infection (DA-HAI) were applied., Results: We collected data from 428,847 patients, for an aggregate of 2,815,402 bed-days, 1,468,216 central line (CL)-days, 1,053,330 mechanical ventilator (MV)-days, 1,740,776 urinary catheter (UC)-days. We found 7,785 CL-associated bloodstream infections (CLAB), 12,085 ventilator-associated events (VAE), and 5,509 UC-associated urinary tract infections (CAUTI). Pooled DA-HAI rates were 5.91% and 9.01 DA-HAIs/1,000 bed-days. Pooled CLAB rate was 5.30/1,000 CL-days; VAE rate was 11.47/1,000 MV-days, and CAUTI rate was 3.16/1,000 UC-days. P aeruginosa was non-susceptible (NS) to imipenem in 52.72% of cases; to colistin in 10.38%; to ceftazidime in 50%; to ciprofloxacin in 40.28%; and to amikacin in 34.05%. Klebsiella spp was NS to imipenem in 49.16%; to ceftazidime in 78.01%; to ciprofloxacin in 66.26%; and to amikacin in 42.45%. coagulase-negative Staphylococci and S aureus were NS to oxacillin in 91.44% and 56.03%, respectively. Enterococcus spp was NS to vancomycin in 42.31% of the cases., Conclusions: DA-HAI rates and bacterial resistance are high and continuous efforts are needed to reduce them., (Copyright © 2021. Published by Elsevier Inc.)
- Published
- 2021
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6. Novel and Affordable Low-Cost Technique for Fixation of Parasymphyseal Fractures in Infants With Unerupted Dentition.
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Abdelhalim MM and El Fahar MH
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- Adult, Bone Plates, Child, Fracture Fixation, Internal, Humans, Infant, Jaw Fixation Techniques, Prospective Studies, Dentition, Mandibular Fractures surgery
- Abstract
Purpose: Pediatric mandibular fractures are immensely challenging compared to adult fractures. The current update management spectrum ranges from the conservative one in the form of soft diet and regular follow-up, or less invasive surgical intervention by closed reduction and nonrigid fixation, to open reduction and internal fixation with plates and screws. In this study, we investigated the use of a straightforward fabricated mold for the parasymphyseal mandibular fracture in infants with an unerupted dentition., Patients and Methods: This prospective study was conducted on 8 infants presenting with parasymphyseal fractures with unerupted dentitions in our specialized trauma center. In the operating room before the induction of anesthesia, the authors used a straightforward plastic airway to create a splint. The curved part was split into 2 transverse halves making 2 U-shaped curved pieces that were utilized as a mold. Intraoperatively, the U-shaped piece was placed over the mandible and stabilized with circummandibular wires. This molded airway is used to stabilize the fracture site for 2-3 weeks. The average period of follow-up was around 6 months., Results: The average time of mandibular fixation was 17.6 ± 2.4 SD (14 to 20) days. The mean of the total operative time was 38.7 ± 3.5 SD minutes, ranging from 35 to 45 minutes. Our infants were observed in the outpatient clinic for 6 months postoperatively during the follow-up period. There were no noticeable complications nor any interference with tooth eruption or mandibular growth., Conclusions: The results of this study suggest that this technique is straightforward to use and affordable. It does not require a long learning period. It also exhibits the advantage of reducing the cost in many developing countries., (Copyright © 2021 American Association of Oral and Maxillofacial Surgeons. Published by Elsevier Inc. All rights reserved.)
- Published
- 2021
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7. Readability of Patient Educational Materials in Pediatric Orthopaedics.
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Ó Doinn T, Broderick JM, Abdelhalim MM, and Quinlan JF
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- Educational Status, Humans, Comprehension, Health Literacy, Internet, Orthopedics, Patient Education as Topic, Pediatrics
- Abstract
Background: Parents are increasingly turning to the internet to seek pediatric health information. Numerous organizations advise that patient educational materials (PEMs) should not surpass the sixth-grade reading level. We aimed to assess the readability of online pediatric orthopaedic PEMs., Methods: The readability of 176 articles pertaining to pediatric orthopaedics from the American Academy of Orthopaedic Surgeons (AAOS), Pediatric Orthopaedic Society of North America (POSNA), and American Academy of Pediatrics (AAP) websites was assessed with the use of 8 readability formulae: the Flesch-Kincaid Reading Grade Level, the Flesch Reading Ease Score, the Raygor Estimate, the SMOG, the Coleman-Liau, the Fry, the FORCAST, and the Gunning Fog. The mean reading grade level (RGL) of each article was compared with the sixth and eighth-grade reading levels. The mean RGL of each website's articles also was compared., Results: The cumulative mean RGL was 10.2 (range, 6.6 to 16.0). No articles (0%) were written at the sixth-grade reading level, and only 7 articles (4.0%) were written at or below the eighth-grade reading level. The mean RGL was significantly higher than the sixth-grade (95% confidence interval [CI] for the difference, 4.0 to 4.4; p < 0.001) and eighth-grade (95% CI, 2.0 to 2.4; p < 0.001) reading levels. The mean RGL of articles on the POSNA website was significantly lower than the mean RGL of the articles on the AAOS (95% CI, -1.8 to -1.0; p < 0.001) and AAP (95% CI, -2.9 to -1.1; p < 0.001) websites., Conclusions: Pediatric orthopaedic PEMs that are produced by the AAOS, the POSNA, and the AAP have readability scores that exceed recommendations. Given the increasing preference of parents and adolescents for online health information, the growing body of online PEMs, and the critical role that health literacy plays in patient outcomes, substantial work is required to address the readability of these materials., Competing Interests: Disclosure: The authors indicated that no external funding was received for any aspect of this work. The Disclosure of Potential Conflicts of Interest forms are provided with the online version of the article (http://links.lww.com/JBJS/G322)., (Copyright © 2021 by The Journal of Bone and Joint Surgery, Incorporated.)
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- 2021
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8. Readability of Patient Educational Materials in Hip and Knee Arthroplasty: Has a Decade Made a Difference?
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Doinn TÓ, Broderick JM, Abdelhalim MM, and Quinlan JF
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- Comprehension, Humans, Internet, Arthroplasty, Replacement, Knee, Health Literacy, Orthopedics
- Abstract
Background: The Internet has become an increasingly popular resource among orthopedic patients for health education. Numerous organisations recommend that patient educational materials (PEMs) should not exceed the 6
th grade reading level. Despite this, studies have repeatedly shown the reading grade level (RGL) of PEMs to be too advanced across a range of surgical specialties. We aimed to determine the readability of online hip and knee arthroplasty PEMs., Methods: The readability of 134 articles pertaining to hip and knee arthroplasty from 5leading worldwide healthcare websites were assessed, using 8 readability formulae; the Flesch-Kincaid Reading Grade Level, the Flesch Reading Ease Score, Raygor Estimate, SMOG, Coleman-Liau, Fry, FORCAST and Gunning Fog. The mean RGL was compared to the 6th and 8th grade reading level. The mean RGL of each website was also compared., Results: The mean cumulative RGL was 12 (range = 7-16.1). No articles (0%) were written at a 6th grade reading level and only 4 articles (3%) were written at or below the 8th grade reading level. The mean RGL was significantly higher than the 6th (95% CI, 5.62-6.30; P < .0001) and 8th grade reading level (95% CI, 3.63-4.30; P < .0001). There was a significant difference between the RGLs of the 5websites (P = .001)., Conclusion: Arthroplasty PEMs produced by leading worldwide healthcare organisations have readability scores that are above the recommended levels. Given the imperative role of health literacy in patient outcomes and satisfaction, and the increasing prevalence of Internet use among orthopedic patients, a substantial amount of work needs to be done to improve the readability of these materials., (Copyright © 2020 Elsevier Inc. All rights reserved.)- Published
- 2020
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9. Synthesis of novel hybrid hetero-steroids: Molecular docking study augmented anti-proliferative properties against cancerous cells.
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Mohamed SA, El-Kady DS, Abd-Rabou AA, Tantawy MA, AbdElhalim MM, Elazabawy SR, Abdallah AEM, and Elmegeed GA
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- A549 Cells, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Proliferation drug effects, Dose-Response Relationship, Drug, Drug Resistance, Neoplasm drug effects, Drug Screening Assays, Antitumor, Hep G2 Cells, Humans, Molecular Structure, Neoplasm Proteins antagonists & inhibitors, Steroids chemical synthesis, Steroids chemistry, Structure-Activity Relationship, Tumor Cells, Cultured, Antineoplastic Agents pharmacology, Molecular Docking Simulation, Steroids pharmacology
- Abstract
Hetero-steroids, hybrid anticancer agents, have received much interest in view of their numerous and promising biological activities. In this study, a novel class of hetero-steroids were synthesized, analytical and spectral data proved the validity of the novel synthesized steroid derivatives. The cytotoxicity of the synthesized compounds 2, 5, 6, 7, 10, 11, 12, 14, 15, 17 were evaluated using human hepatocellular carcinoma cell lines (HepG2 and Huh-7) and non-small cell lung cancer (A549) cell lines. The synthesized compounds reported a remarkable gradual decrease in the cell viability of the three tested cancer cell lines. It was observed that compounds 2 and 12 had the lowest IC
50s and the highest cytotoxic effects against all tested cell lines. As attempt to explain the cytotoxic activity achieved by the tested compounds in the in vitro study, molecular simulation was done to reveal the activity of the tested compounds against four different proteins (CDK2, CYP19, JAK2, and BCL2) which are highly implicated in cancer regulation and progression. We found that compound 2, and 12 were the best docked compounds against all tested receptors, which was indicated by lowest binding energy compared to reference ligand. Interestingly enough, our molecular study was in agreement with the cytotoxic activity. As future prospective, we are recommending further study on compounds 2, and 12 against the four different proteins to prove their mode of action., (Copyright © 2019 Elsevier Inc. All rights reserved.)- Published
- 2020
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10. Synthesis and Evaluation of Novel Cholestanoheterocyclic Steroids as Anticancer Agents.
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El-Kady DS, Abd Rabou AA, Tantawy MA, Abdel-Rahman AA, Abdel-Megeed AA, AbdElhalim MM, and Elmegeed GA
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- Cell Line, Tumor, Heterocyclic Compounds chemistry, Humans, Spectrum Analysis methods, Steroids chemistry, Antineoplastic Agents pharmacology, Cholestanes chemistry, Heterocyclic Compounds chemical synthesis, Heterocyclic Compounds pharmacology, Steroids chemical synthesis, Steroids pharmacology
- Abstract
Modification of steroid molecules by introducing heterocyclic ring into the core structure of steroids has been utilized as an attractive approach for either cancer prognosis or diagnosis. Several new cholestanoheterocyclic steroids were synthesized, and analytical and spectral data proved the validity of the novel synthesized steroid derivatives. The cytotoxicity of synthesized compounds 3, 4, 5, 7, 9, 10, 13, 15b, and 16b was evaluated using human colorectal cancer HCT 116 and Caco-2, cervical cancer HeLa, hepatoma HepG2, and breast cancer MCF7 cell lines. Intriguingly, compound 13 has the highest cytotoxic effect when applied on the majority of cancer cells. In conclusion, compound 13 may be considered as a promising anticancer candidate against all cancer cell lines, because it recorded the lowest IC
50 of the majority of the cancer cell lines used. Furthermore, a molecular docking study was employed to determine the binding modes against aromatase cytochrome P450 (CYP19), cyclin-dependent kinase 2 (CDK2), and B-cell lymphoma (BCL-2) proteins, which are major proteins involved in the pathogenesis of cancer. Molecular docking analyses revealed that compounds 13, 3, and 5 (free energy of binding = - 9.2, - 9.1, and - 9.0 kcal/mol, respectively) were the best docked ligand against aromatase CYP19; compounds 16b, 3, 9, and 10 (free energy of binding = - 9.6, - 9.3, and - 9.2 kcal/mol, respectively) were the best docked ligand against CDK2, while compounds 15b, 16b, and 13 (free energy of binding = - 9.1, - 9.0, and- 8.7 kcal/mol, respectively) were the best docked ligand against BCL2. In conclusion, compounds 3, 13, and 16b were the most promising compounds with the lowest IC50 s against most of the tested cancer cell lines, and they displayed the lowest binding energies, critical hydrogen bonds, and hydrophobic interactions with the three molecular targets compared to other tested compounds.- Published
- 2019
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11. Different Analgesic Routes of Magnesium Sulfate: Intravenous versus Pectoralis II Interfascial Plane Block for Breast Cosmetic Surgeries.
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Abo-Zeid MA, Ghareeb S, and Abdelhalim MM
- Abstract
Purpose: The purpose of the study is to evaluate the most effective analgesic route of magnesium sulfate (MgSO
4 ) either intravenous (i.v.) or pectoralis interfascial plane block., Patients and Methods: Fifty adult female patients were divided into two equal groups: i.v. MgSO4 and Pecs II block MgSO4 (Pecs MgSO4 ) group. After general anesthesia, in i.v. MgSO4 group, the local anesthetic (LA) for Pecs II block was prepared by adding 3 mL saline to 57 mL bupivacaine 0.25% divided equally for each side. A bolus i.v. solution of MgSO4 10% 0.5 mL.kg-1 diluted in saline in a total volume of 100 mL was given over 15 minutes. Then, the solution for continuous i.v. infusion; 30 mL MgSO4 10% and 70 mL saline was infused at the rate of 0.5 mL.kg-1 .h-1 intraoperatively. For PecsMgSO4 group, LA formed of 3 mL MgSO4 10% added to 57 mL bupivacaine 0.25%. Whereas, 100 mL saline was given as bolus i.v. followed by continuous infusion of 100 mL normal saline at the rate of 0.5 mL.kg-1 .h-1 ., Results: In the group received MgSO4 -bupivacaine Pecs II block, there was a nonsignificant decrease in postoperative morphine consumption compared to i.v. administration of MgSO4 . The two groups were comparable in the intensity of pain and sedation scores., Conclusion: The use of bupivacaine Pecs II block enhanced with addition of MgSO4 to pectoralis interfascial plane block or intravenously in patients underwent breast cosmetic surgeries under general anesthesia was associated with comparable results of the postoperative morphine requirements, intensity of postoperative pain, and extension of the duration of postoperative analgesia. The intraoperative hemodynamic effects i.v. MgSO4 were superior to the pectoralis interfascial plane route of administration., Competing Interests: There are no conflicts of interest., (Copyright: © 2019 Anesthesia: Essays and Researches.)- Published
- 2019
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12. One-pot three-component synthesis of novel heterocyclic steroids as a central antioxidant and anti-inflammatory agents.
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Mohamed NR, Abdelhalim MM, Khadrawy YA, Elmegeed GA, and Abdel-Salam OM
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- Animals, Anti-Inflammatory Agents chemistry, Antioxidants chemistry, Brain cytology, Brain drug effects, Chemistry Techniques, Synthetic, Neurons drug effects, Neurons metabolism, Oxidative Stress drug effects, Rats, Steroids chemistry, Anti-Inflammatory Agents chemical synthesis, Anti-Inflammatory Agents pharmacology, Antioxidants chemical synthesis, Antioxidants pharmacology, Heterocyclic Compounds chemistry, Steroids chemical synthesis, Steroids pharmacology
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Oxidative stress and inflammation have been implicated in several neurodegenerative and developmental brain disorders. The present work was devoted to the design and synthesis of novel steroid derivatives bearing promising heterocyclic moiety that would act to reduce neuro-inflammation and oxidative stress in brain. The novel heterocyclic steroids were synthesized and their chemical structures were confirmed by studying their analytical and spectral data. The tested compounds were assayed in the model of neuro-inflammation produced in rats by cerebral lipopolysaccharide injection. The intracerebral administration of bacterial endotoxin resulted in cerebral inflammatory state evidenced by increased malondialdehyde (MDA), decreased reduced glutathione (GSH) level, increased nitric oxide as well as increased acetylcholinesterase (AChE) activity in the brain. Compounds 6, 10, 8b and 13a markedly increased reduced glutathione. Malondialadehyde and nitric oxide levels were reduced to normal values after treatment with all tested compounds. AChE activity was normalized by compound 8b and reduced to below normal values by compounds 10 and 14a. These results are exciting in that these agents might be useful candidates in treatment of cerebral inflammation., (Copyright © 2012 Elsevier Inc. All rights reserved.)
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- 2012
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13. Synthesis and biological evaluation of some nitrogen containing steroidal heterocycles.
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Abdelhalim MM, Kamel EM, Rabie ST, and Mohamed NR
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- Antineoplastic Agents chemistry, Cell Line, Tumor, Cell Proliferation drug effects, Dose-Response Relationship, Drug, Doxorubicin chemistry, Doxorubicin pharmacology, Drug Screening Assays, Antitumor, Humans, Liver Neoplasms pathology, Molecular Structure, Stereoisomerism, Steroids, Heterocyclic chemistry, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Hydrazones chemistry, Liver Neoplasms drug therapy, Steroids, Heterocyclic chemical synthesis, Steroids, Heterocyclic pharmacology
- Abstract
epi-Androsterone 1 was converted into its hydrazone derivative through the reaction with hydrazine hydrate 80%. Hydrazonoandrostane derivative 2b reacted with hydrazonoyl halides in the presence of K(2)CO(3) forming the corresponding hydrazopyridazinoandrostane derivatives 6a-d. The 3β-acetyl-17-hydrazonoandrostane derivative 2b reacted with a halogen reagent, benzoyl chloride, to form the non-cyclic 16-benzoylated hydrazone 9. On the other hand, compound 2b produced the corresponding pyridazinoandrostane derivatives 11 and 12 via its reaction with phenacyl bromide and chloroacetone respectively. Reaction of the hydrazono derivative 2b with benzaldehyde in the presence of acetic acid drops led to the formation of the benzylidenehydrazonoandrostane derivative 13. The product 14, phosphinom-ethylenehydrazonoandrostane was obtained by the reaction of the derivative 13 with trisdimethylaminophosphine in the presence of dry benzene. The reaction of compound 2b with phenyl isothiocyanate followed by boiling in chloroacetic acid or thioglycolic acid produced the pyrazoloandrostane derivatives 17 and 18 respectively. The biological activity of compounds 6a, 6d, 11, 12, and 15 was evaluated as inhibitor of growth in a human liver carcinoma cell line and doxorubicine was used for comparison. Compounds 15 and 12 showed a higher potency than the other tested compounds., (Copyright © 2010 Elsevier Inc. All rights reserved.)
- Published
- 2011
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14. Synthesis and antidepressant evaluation of five novel heterocyclic tryptophan-hybrid derivatives.
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Elmegeed GA, Baiuomy AR, Abdelhalim MM, and Hana HY
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- Animals, Antidepressive Agents administration & dosage, Antidepressive Agents chemistry, Dose-Response Relationship, Drug, Drug Evaluation, Preclinical methods, Female, Heterocyclic Compounds administration & dosage, Heterocyclic Compounds chemistry, Hypnotics and Sedatives administration & dosage, Hypnotics and Sedatives chemistry, Mice, Molecular Structure, Motor Activity drug effects, Structure-Activity Relationship, Swimming, Tryptophan administration & dosage, Tryptophan chemistry, Antidepressive Agents chemical synthesis, Heterocyclic Compounds chemical synthesis, Hypnotics and Sedatives chemical synthesis, Tryptophan analogs & derivatives
- Abstract
This study aimed at evaluating the reactivity of L-Tryptophan (TRP) 1 towards various chemical reagents to produce new bi- and tri-heterocyclic systems providing basic pharmacological activities. Indol-3-yl hydroxyoxazol-2-yl acetonitrile derivatives 5 and 6, indol-3-yl-hydroxyoxazol-2-yl-1,2,4-triazine derivatives 8 and 9, indol-3-yl-hydroxyoxazol-2-yl-aminopyrazole derivatives 11a, b, and indol-3-yl-hydroxyoxazol-2-yl-aminoisoxazole derivative 12 were synthesized via straightforward and efficient methods. The structures were characterized by spectral data (IR, (1)H-NMR, (13)C-NMR, and MS) and the purity was ascertained by microanalysis. Also, this work was extended to study the potential role of the novel synthesized TRP derivatives 5, 6, 9, 11a, and 12 as antidepressant and sedative agents in comparison with TRP. All compounds showed significant antidepressant activity in the forced-swimming test at two doses (50 or 100 mg/kg). Also, all tested compounds (at 50 or 100 mg/kg) produced a significant decrease in locomotor activity of mice during a 30 min observation period. The most potent antidepressant and sedative effect was produced by the tri-heterocyclic compounds 9 and 12, followed by 11a and TRP.
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- 2010
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15. Synthesis and in vivo anti-mutagenic activity of novel melatonin derivatives.
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Elmegeed GA, Khalil WK, Raouf AA, and Abdelhalim MM
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- Animals, Antimutagenic Agents chemistry, Antineoplastic Agents, Alkylating pharmacology, Bone Marrow Cells metabolism, Cholinesterases metabolism, Cyclophosphamide pharmacology, DNA genetics, DNA metabolism, Erythrocytes metabolism, Male, Melatonin chemistry, Mice, Micronucleus Tests, Peroxidase metabolism, Proteins metabolism, RNA genetics, RNA metabolism, Antimutagenic Agents chemical synthesis, Antimutagenic Agents pharmacology, Bone Marrow Cells drug effects, DNA Damage drug effects, Erythrocytes drug effects, Melatonin chemical synthesis, Melatonin pharmacology
- Abstract
Extensive literature suggests that melatonin play a role against the degenerative effect of central neurotoxins by its acting as free radical scavenger. This study aimed at evaluation of the anti-mutagenic activity of novel synthesized indole derivatives 2, 4a, and 8 in albino male mice in comparison with the parent melatonin. Efficacy of melatonin and its derivatives to influence cyclophosphamide (CP)-induced genotoxicity was tested using micronuclei (MN) formation in the bone marrow cells and determination of DNA, RNA and protein levels as well as cholinesterase and peroxidase activities in several organs of male mice. Following intragastrical injection of melatonin or one of its derivatives daily for 1 week, CP was given intraperitoneally, i.p., as a single dose of 25mg/kg BW. Pyridazin-4-yl thiadiazoloindole derivative 8, diaminothiophen-5-yl thiadiazoloindole derivative 4a and melatonin were significantly able to reduce the number of micronucleated polychromatic erythrocytes (MnPCEs) in the bone marrow cells induced by CP (P<0.0001, P<0.001, P<0.01, respectively). However, reduction of MN formation in the bone marrow cells was not significant when thiadiazoloindole derivative 2 was administered (P=0.14). Examination of the protective effect of melatonin and its derivatives on the levels of DNA, RNA and protein as well as enzyme activities showed that compound 8 had the ability to inhibit the clastogenic effect of CP in several organs of male mice. These findings suggest that compounds 4a, 8 and melatonin were able to reduce the mutagenicity effect of CP in male mice. The ability of compounds 4a, 8 and melatonin to reduce CP-related genotoxicity is possibly attributed to their antioxidant activity.
- Published
- 2008
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16. Synthesis of novel steroidal heterocyclic derivatives as antibacterial agents.
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Abdelhalim MM, el-Saidi MM, Rabie ST, and Elmegeed GA
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- Anti-Bacterial Agents chemistry, Anti-Bacterial Agents pharmacology, Gram-Negative Bacteria growth & development, Gram-Positive Bacteria growth & development, Microbial Sensitivity Tests, Steroids, Heterocyclic chemistry, Steroids, Heterocyclic pharmacology, Anti-Bacterial Agents chemical synthesis, Steroids, Heterocyclic chemical synthesis
- Abstract
This study aimed at the synthesis of novel structurally promising steroidal heterocycles and to elucidate the potential role of these compounds as antibacterial agents. Epi-androsterone 1 reacted with CS2 and sodium hydride in dimethylsulfoxide to yield alpha-oxoketene dithiodisodium salt 2. The non-isolable salt 2 reacted with acetyl chloride, benzoyl chloride, phenacyl bromide and iodomethane to afford the corresponding alpha-oxodithioacetal derivatives 4a,b, 6 and 7, respectively. Interaction of 2 with the alkyl halide reagents 8a-d yielded the corresponding thiophene derivatives 10a-d. Alpha-oxoketene dithioacetal 7 reacted with urea and thiourea to furnish the pyrimidinoandrostane derivatives 12a,b. Compound 7 also reacted with ortho-phenylene diamine and ortho-aminophenol 13a,b to produce the dinucleophilic adducts 15a,b. The in vitro antibacterial evaluation of some newly prepared compounds showed that all compounds have high significant antibacterial activity against the used strains of gram positive and gram negative bacteria.
- Published
- 2007
- Full Text
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