Displaying publications 1 - 20 of 37 in total

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  1. Mohammed, Mohammed Omar Abdalqadir, Arabi, Sami Ahmed Mohammed, Mirghani, Mohamed E. S.
    MyJurnal
    This study was conducted to evaluate the effect of dietary cottonseed oil (CSO) at
    different levels on broiler chickens. Dietary CSO was tested for energy supplementation values in
    poultry at levels 0, 3, 6 and 9% utilizing isonitrogenous (22.5% CP), semi-isocaloric (3100 Kcal/kg)
    rations and run in the experiment. Ninety-six seven-day old unsexed Ross-308 broiler chicks with
    an initial weight of 72.9 g were used for each experiment in a completely randomized design
    (4x4x6). Chicks were fed for 42 days. Supplementation with the oils improved performance
    (p>0.05) but CSO gave significant (p
  2. Mohamed, E., Ibrahim, A.A., Ihab, E.A., Elwany, S., Hassab, M.H., Khamis, H.M.
    MyJurnal
    Introduction: The New Zealand White (NZW) rabbit model is commonly used for the research of
    posterolateral intertransverse lumbar arthrodesis. The standard approach reported by many researchers are a muscle splitting approach through the intermuscular plane between multifidus and longissimus muscles. Methods: In this research the fusion bed was exposed by retracting the three groups of paraspinal muscles (multifidus, longissimus and iliocostalis) medially. Results: This alternative method showed good exposure of the transverse processes and intertransverse membrane with less bleeding from the muscles observed. No death due to surgical complication was observed out of twenty-four rabbits operated. Conclusion: An easy and safe method for performing posterolateral intertransverse lumbar arthrodesis was demonstrated and recommended as an alternative approach for surgery on New Zealand White rabbits.
  3. Anwar S, Madkor HR, Ahmed N, Wagih ME
    Indian J Pharmacol, 2018 9 1;50(3):108-115.
    PMID: 30166747 DOI: 10.4103/ijp.IJP_660_16
    OBJECTIVE: Silymarin, extracted from the seeds of Silybum marianum L. (Milk thistle), is traditionally used for treating various illnesses such as diabetes, cancer, inflammation, hepatitis, liver cirrhosis, and renal problems. Acute cytotoxicity and genotoxicity studies have been reported with ambiguous outcomes; however, its relevant anticlastogenic potential is not yet evaluated. This study was aimed to evaluate in vivo subacute anticlastogenic properties of silymarin to validate its use as a medicinal agent.

    MATERIALS AND METHODS: Silymarin was isolated from seeds of milk thistle. Various genotoxicity bioassays of silymarin were performed using mice. First, the bone marrow cell proliferation was estimated by calculating mitotic index. Second, the chromosomal abnormalities in mice bone marrow cells were studied. Third, micronucleated polychromatic erythrocytes (MPE) test and in vivo activation of sister chromatid exchanges (SCEs) were carried out in mice bone marrow cells. Finally, primary spermatocytes were analyzed to estimate genotoxic effect of silymarin on germ cells.

    RESULTS: We found that silymarin is capable of inducing a significant increase (P ≤ 0.05) in cell proliferation of bone marrow cells. There is no increase in chromosomal aberrations following silymarin treatments. Results clearly showed that it significantly (P ≤ 0.05) decreased the MPE. Likewise, it was found to be a negative inducer of SCEs. It decreased in total abnormal metaphase, SCEs, MPE, and aberrant diakinesis.

    CONCLUSION: The results demonstrated that silymarin has a strong anticlastogenic activity upon mice genome in somatic and germ cells, indicating its safe use as a medicinal substance. Furthermore, it is not only safe but also has protective effect from clastogens.

  4. Aburigal, Yasmin A. A., Elmogtaba, Elfadl Y., Sirible, Awatif M., Hamza, Nada B., Hussein, Ismail H., Mirghani, Mohamed E. S.
    MyJurnal
    Sweet basil (Ocimum basilicum L.) is a very important food additive as well as for its therapeutic and cosmetic potential. The composition of essential oils in plants is affected by genetics and environmental conditions, which is determined by growth region and harvesting time in terms of ontogenetical variability. This study was carried out to assess the effect of plant ontogeny (pre-flowering, at flowering, fruiting) on essential oil content and chemical constituents for four sweet basil cultivated under irrigation conditions in the experimental farm of the National Oilseed Processing Research Institute (NOPRI), University of Gezira, Sudan. The essential oils were hydro-distilled from the leaves using Clevenger apparatus and the chemical constituents were determined by GC-MS. The results reveal that the essential oil yield content ranged from 0.1% to 0.2% at pre-flowering stage, whereas the oil content obtained at post-flowering stage was 0.1% for the investigated accessions. The highest essential oil content was recorded at flowering stage (0.2-0.5%), where the two Sudanese accessions had the maximum content (0.5%). The major chemical constituents, linalool, citral, methyleugenol, and eucalyptol reported at different developmental stages, punctuated between 5.73% and 32.93% in the four investigated accessions.
  5. Saifullah B, El Zowalaty ME, Arulselvan P, Fakurazi S, Webster TJ, Geilich BM, et al.
    Drug Des Devel Ther, 2014;8:1029-36.
    PMID: 25114509 DOI: 10.2147/DDDT.S63753
    The treatment of tuberculosis by chemotherapy is complicated due to multiple drug prescriptions, long treatment duration, and adverse side effects. We report here for the first time an in vitro therapeutic effect of nanocomposites based on para-aminosalicylic acid with zinc layered hydroxide (PAS-ZLH) and zinc-aluminum layered double hydroxides (PAS-Zn/Al LDH), against mycobacteria, Gram-positive bacteria, and Gram-negative bacteria. The nanocomposites demonstrated good antimycobacterial activity and were found to be effective in killing Gram-positive and Gram-negative bacteria. A biocompatibility study revealed good biocompatibility of the PAS-ZLH nanocomposites against normal human MRC-5 lung cells. The para-aminosalicylic acid loading was quantified with high-performance liquid chromatography analysis. In summary, the present preliminary in vitro studies are highly encouraging for further in vivo studies of PAS-ZLH and PAS-Zn/Al LDH nanocomposites to treat tuberculosis.
  6. Husain IA, Alkhatib MF, Jammi MS, Mirghani ME, Bin Zainudin Z, Hoda A
    J Oleo Sci, 2014;63(8):747-52.
    PMID: 25007744
    Presence of fat, oil, and grease (FOG) in wastewater is an ever-growing concern to municipalities and solid-waste facility operators. FOG enters the sewer system from restaurants, residences, and industrial food facilities. Its release into the sewer system results in a continuous build-up that causes eventual blockage of sewer pipes. Several researchers have investigated FOG deposition based on the local conditions of sewers and lifestyle. This paper attempts to review the physical and chemical characteristics of FOG, sources of FOG, and potential chemical and biological reactions of FOG. The effect of the aforementioned factors on the FOG-deposition mechanism is also discussed. Moreover, insight into the current control and treatment methods and potential reuse of FOG is highlighted. It is expected that this review would provide scientists and the concerned authorities a holistic view of the recent researches on FOG control, treatment, and reuse.
  7. Hayyan M, Hashim MA, Al-Saadi MA, Hayyan A, AlNashef IM, Mirghani ME
    Chemosphere, 2013 Sep;93(2):455-9.
    PMID: 23820537 DOI: 10.1016/j.chemosphere.2013.05.013
    In this work, the cytotoxicity and toxicity of phosphonium-based deep eutectic solvents (DESs) with three hydrogen bond donors, namely glycerine, ethylene glycol, and triethylene glycol were investigated. The cytotoxicity effect was tested using brine shrimp (Artemia salina). The toxicity was investigated using the two Gram positive bacteria Bacillus subtilis and Staphylococcus aureus, and two Gram negative bacteria Escherichia coli and Pseudomonas aeruginosa. The cytotoxicity of tested DESs was much higher than that of their individual components, indicating their toxicological behavior was different. It was also found that there was toxic effect on the studied bacteria, indicating their potential application as anti-bacterial agents. To the best of our knowledge, this is the first time the cytotoxicity and toxicity of phosphonium-based DESs were studied.
  8. Kabbashi NA, Atieh MA, Al-Mamun A, Mirghami ME, Alam MD, Yahya N
    J Environ Sci (China), 2009;21(4):539-44.
    PMID: 19634432
    The capability of carbon nanotubes (CNTs) to adsorb lead (Pb) in aqueous solution was investigated. Batch mode adsorption experiment was conducted to determine the effects of pH, agitation speed, CNTs dosage and contact time. The removal of Pb(II) reached maximum value 85% or 83% at pH 5 or 40 mg/L of CNTs, respectively. Higher correlation coefficients from Langmuir isotherm model indicates the strong adsorptions of Pb(II) on the surface of CNTs (adsorption capacity Xm = 102.04 mg/g). The results indicates that the highest percentage removal of Pb (96.03%) can be achieved at pH 5, 40 mg/L of CNTs, contact time 80 min, and agitation speed 50 r/min.
  9. Lum LC, Abdel-Latif ME, de Bruyne JA, Nathan AM, Gan CS
    Pediatr Crit Care Med, 2011 Jan;12(1):e7-13.
    PMID: 20190672 DOI: 10.1097/PCC.0b013e3181d505f4
    To determine the factors that predict outcome of noninvasive ventilation (NIV) in critically ill children.
  10. Hayyan M, Hashim MA, Hayyan A, Al-Saadi MA, AlNashef IM, Mirghani ME, et al.
    Chemosphere, 2013 Feb;90(7):2193-5.
    PMID: 23200570 DOI: 10.1016/j.chemosphere.2012.11.004
    In continuation of investigation for environmentally benign protocol for new solvents termed deep eutectic solvents (DESs), it is herein reported results concerning the toxicity and cytotoxicity of choline chloride (ChCl) based DESs with four hydrogen bond donors including glycerine, ethylene glycol, triethylene glycol and urea. The toxicity was investigated using two Gram positive bacteria Bacillus subtilis and Staphylococcus aureus, and two Gram negative bacteria Escherichia coli and Pseudomonas aeruginosa. The cytotoxicity effect was tested using the Artemia salina leach. It was found that there was no toxic effect for the tested DESs on all of the studied bacteria confirming their benign effects on these bacteria. Nevertheless, it was found that the cytotoxicity of DESs was much higher than their individual components (e.g. glycerine, ChCl) indicating that their toxicological behavior is different. For our best knowledge this is the first time that toxicity and cytotoxicity of DESs were studied. The toxicity and cytotoxicity of DESs varied depending on the structure of components. Careful usage of the terms non-toxicity and biodegradability must be considered. More investigation on this matter is required.
  11. Badawy MEI, El-Nouby MAM, Kimani PK, Lim LW, Rabea EI
    Anal Sci, 2022 Dec;38(12):1457-1487.
    PMID: 36198988 DOI: 10.1007/s44211-022-00190-8
    Analytical processes involving sample preparation, separation, and quantifying analytes in complex mixtures are indispensable in modern-day analysis. Each step is crucial to enriching correct and informative results. Therefore, sample preparation is the critical factor that determines both the accuracy and the time consumption of a sample analysis process. Recently, several promising sample preparation approaches have been made available with environmentally friendly technologies with high performance. As a result of its many advantages, solid-phase extraction (SPE) is practiced in many different fields in addition to the traditional methods. The SPE is an alternative method to liquid-liquid extraction (LLE), which eliminates several disadvantages, including many organic solvents, a lengthy operation time and numerous steps, potential sources of error, and high costs. SPE advanced sorbent technology reorients with various functions depending on the structure of extraction sorbents, including reversed-phase, normal-phase, cation exchange, anion exchange, and mixed-mode. In addition, the commercial SPE systems are disposable. Still, with the continual developments, the restricted access materials (RAM) and molecular imprinted polymers (MIP) are fabricated to be active reusable extraction cartridges. This review will discuss all the theoretical and practical principles of the SPE techniques, focusing on packing materials, different forms, and performing factors in recent and future advances. The information about novel methodological and instrumental solutions in relation to different variants of SPE techniques, solid-phase microextraction (SPME), in-tube solid-phase microextraction (IT-SPME), and magnetic solid-phase extraction (MSPE) is presented. The integration of SPE with analytical chromatographic techniques such as LC and GC is also indicated. Furthermore, the applications of these techniques are discussed in detail along with their advantages in analyzing pharmaceuticals, biological samples, natural compounds, pesticides, and environmental pollutants, as well as foods and beverages.
  12. Abdullah A, Haron N, Mohamed E, Yusof MIM, Shahril MR
    Med J Malaysia, 2024 Mar;79(Suppl 1):158-167.
    PMID: 38555901
    INTRODUCTION: Obesity can be considered a major public health concern throughout the world. Various studies have been conducted to combat the rising number of cases of this health problem. Therefore, identifying the roots of the disease is critical in developing the desperately needed treatment approaches. However, in order to fully understand the origin of this disease, figuring out the metabolites present, and the alterations that occurred in a particular metabolism are crucial, and the information regarding the metabolites involved is limited. The aim of this study is to analyse the literature relevant to the metabolites involved in obesity conditions through a scoping review.

    MATERIALS AND METHODS: This review utilises three databases (SCOPUS, Science Direct, and PubMed). The search phrases used are (Metabolomic* OR Metabolite*) for metabolomic study, (3T3-L1 OR Adipocyte OR "Adipose Tissue") for experimental design, and (Obesity) for obesity condition. Each of the search keywords was separated by an "AND" term in the databases. Other terms related to obesity, such as insulin resistance, heart disease, type 2 diabetes, muscular disorders, respiratory problems, and psychological problems were omitted because they did not contribute to the total number of studies discovered.

    RESULTS: A total of 27 research publications were included in this scoping review. Most of the study focuses on metabolomics in obesity. Metabolites detected were found in various metabolic pathways including amino acids, carbohydrates, lipids as well as other metabolisms. Most of these metabolites discovered in obese conditions showed an alteration when compared to the level of the metabolite in normal conditions.

    CONCLUSION: Unfortunately, these studies had some limitations in which the metabolites detected varied between the articles and the information concerning the relationship between the technique or instrument utilised and the metabolites detected in the samples were not well described. Therefore, using the findings obtained in this study, it can help to determine the direction of the study in the future.

  13. Hussein-Al-Ali SH, El Zowalaty ME, Kura AU, Geilich B, Fakurazi S, Webster TJ, et al.
    Biomed Res Int, 2014;2014:651831.
    PMID: 24900976 DOI: 10.1155/2014/651831
    Nystatin is a tetraene diene polyene antibiotic showing a broad spectrum of antifungal activity. In the present study, we prepared a nystatin nanocomposite (Nyst-CS-MNP) by loading nystatin (Nyst) on chitosan (CS) coated magnetic nanoparticles (MNPs). The magnetic nanocomposites were characterized by X-ray powder diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), thermogravimetry analysis (TGA), vibrating sample magnetometer (VSM), and scanning electron microscopy (SEM). The XRD results showed that the MNPs and nanocomposite are pure magnetite. The FTIR analysis confirmed the binding of CS on the surface of the MNPs and also the loading of Nyst in the nanocomposite. The Nyst drug loading was estimated using UV-Vis instrumentation and showing a 14.9% loading in the nanocomposite. The TEM size image of the MNPs, CS-MNP, and Nyst-CS-MNP was 13, 11, and 8 nm, respectively. The release profile of the Nyst drug from the nanocomposite followed a pseudo-second-order kinetic model. The antimicrobial activity of the as-synthesized Nyst and Nyst-CS-MNP nanocomposite was evaluated using an agar diffusion method and showed enhanced antifungal activity against Candida albicans. In this manner, this study introduces a novel nanocomposite that can decrease fungus activity on-demand for numerous medical applications.
  14. Hayyan A, Alam MZ, Mirghani ME, Kabbashi NA, Hakimi NI, Siran YM, et al.
    Bioresour Technol, 2010 Oct;101(20):7804-11.
    PMID: 20541401 DOI: 10.1016/j.biortech.2010.05.045
    In this study, biodiesel was produced from sludge palm oil (SPO) using tolune-4-sulfonic monohydrate acid (PTSA) as an acid catalyst in different dosages in the presence of methanol to convert free fatty acid (FFA) to fatty acid methyl ester (FAME), followed by a transesterification process using an alkaline catalyst. In the first step, acid catalyzed esterification reduced the high FFA content of SPO to less than 2% with the different dosages of PTSA. The optimum conditions for pretreatment process by esterification were 0.75% (w/w) dosage of PTSA to SPO, 10:1 M ratio, 60 °C temperature, 60 min reaction time and 400 rpm stirrer speed. The highest yield of biodiesel after transesterification and purification processes was 76.62% with 0.07% FFA and 96% ester content. The biodiesel produced was favorable as compared to EN 14214 and ASTM 6751 standard. This study shows a potential exploitation of SPO as a new feedstock for the production of biodiesel.
  15. Radwan EM, Abdullah R, Al-Qubaisi MS, El Zowalaty ME, Naadja SE, Alitheen NB, et al.
    Mol Med Rep, 2016 May;13(5):3945-52.
    PMID: 26987078 DOI: 10.3892/mmr.2016.4989
    Patients with cancer often exhibit signs of anemia as the result of the disease. Thus, cancer chemotherapies often include erythropoietin (EPO) in the regime to improve the survival rate of these patients. The aim of the present study was to determine the effect of EPO on doxorubicin-treated breast cancer cells. The cytotoxicity of doxorubicin alone or in combination with EPO against the MCF-7 and MDA-MB‑231 human breast cancer cells were determined using an MTT cell viability assay, neutral red (NR) uptake assay and lactate dehydrogenase (LDH) assay. The estimated half maximal inhibitory concentration values for doxorubicin and the combination of doxorubicin with EPO were between 0.140 and 0.260 µg/ml for all cells treated for 72 h. Treatment with doxorubicin in combination with EPO led to no notable difference in cytotoxicity, compared with treatment with doxorubicin alone. The antiproliferative effect of doxorubicin at a concentration of 1 µg/ml on the MDA‑MB‑231 cells was demonstrated by the decrease in viable cells from 3.6x10(5) at 24 h to 2.1x10(5) at 72 h of treatment. In order to confirm apoptosis in the doxorubicin-treated cells, the activities of caspases-3/7 and ‑9 were determined using a TBE assay. The results indicated that the activities of caspases-3/7 and ‑9 were significantly elevated in the doxorubicin-treated MDA-MB-231 cells by 571 and 645%, respectively, and in the MCF 7 cells by 471 and 345%, respectively, compared with the control cells. EPO did not modify the effect of doxorubicin on these cell lines. The results of the present study suggested that EPO was safe for use in combination with doxorubicin in the treatment of patients with breast cancer and concurrent anemia.
  16. Saifullah B, Arulselvan P, El Zowalaty ME, Tan WS, Fakurazi S, Webster TJ, et al.
    Int J Nanomedicine, 2021;16:7035-7050.
    PMID: 34703226 DOI: 10.2147/IJN.S297040
    Introduction: Mycobacterium tuberculosis infections are associated with severe local inflammatory reactions, which may be life-threatening and lead to tuberculosis pathogenesis and associated complications. Inorganic nanolayers have been vastly exploited for biomedical applications (especially in drug delivery) because of their biocompatible and biodegradable nature with the ability to release a drug in a sustained manner. Herein, we report a new nanodelivery system of inorganic nanolayers based on magnesium layered hydroxides (MgLH) and a successfully intercalated anti-tuberculosis drug para-aminosalicylic acid (PAS).

    Methods: The designed anti-tuberculosis nanodelivery composite, MgLH-PAS, was prepared by a novel co-precipitation method using MgNO3 as well MgO as starting materials.

    Results: The designed nano-formulation, PAS-MgLH, showed good antimycobacterial and antimicrobial activities with significant synergistic anti-inflammatory effects on the suppression of lipopolysaccharide (LPS) stimulated inflammatory mediators in RAW 264.7 macrophages. The designed nano-formulation was also found to be biocompatible with human normal lung cells (MRC-5) and 3T3 fibroblast cells. Furthermore, the in vitro release of PAS from PAS-MgLH was found to be sustained in human body simulated phosphate buffer saline (PBS) solutions of pH 7.4 and pH 4.8.

    Discussion: The results of the present study are highly encouraging for further in vivo studies. This new nanodelivery system, MgLH, can be exploited in the delivery of other drugs and in numerous other biomedical applications as well.

  17. Elsayed MEG, El-Abasiri RA, Marzo RR, Dardeer KT, Kamal MA, Abdelaziz H, et al.
    PLoS One, 2023;18(2):e0282264.
    PMID: 36848375 DOI: 10.1371/journal.pone.0282264
    BACKGROUND: Coronavirus disease-19 emerged in December 2019. Healthcare workers were exposed to this highly infectious virus during the pandemic and suffered several social and psychological consequences, such as anxiety, psychological distress, and burnout.

    OBJECTIVES: To assess the psychological distress, anxiety, depression, coping strategies, risk perception, and attitude toward interprofessional teamwork among Egyptian healthcare workers during the COVID-19 pandemic.

    METHODS: We conducted a cross-sectional online survey which consisted of five sections. The primary outcomes were anxiety (GAD-7), depression (PHQ-9), risk perception towards COVID-19, interprofessional teamwork attitude, and coping strategies during the Coronavirus disease-19 pandemic. The web-based questionnaire was distributed to Egyptian healthcare workers from the 20th of April 2020 to the 20th of May 2020. A snowball sampling method was used. Regression analysis was conducted to test the relationship between the socioeconomic characteristics and the previously mentioned outcomes.

    RESULTS: A total of 403 participants responded to the online questionnaire. The majority were females (70.5%) and within the age group of 26-40 years (77.7%), with 2-5 years of work experience (43.2%). Most participants were pharmacists (33%) and physicians (22.1%). Eighty-two participants (21%) reported moderate to severe anxiety, and 79 participants reported (19.4%) moderate to severe depressive symptoms. In the univariate model, the marital status was associated with depression (OR 0.47, 95% CI 0.28-0.78), anxiety (OR 0.52, 95% CI 0.32-0.85), and an attitude toward interprofessional teamwork (β = -1.96 95% CI -2.72 to -1.2). Providing direct care to the patients was associated with lower anxiety symptoms (AOR 0.256, 95% CI 0.094-0.697). More severe anxiety and depressive symptoms were associated with difficulties in everyday life and the professional work environment (AOR 4.246 and 3.3, P = 0.003 and 0.01, respectively). Availability of mental health facilities at the workplace was associated with a lower risk perception towards COVID-19 (β = -0.79, 95% CI -1.24 to -0.34) and a more positive attitude towards teamwork (β = 2.77 95% CI 1.38-4.15).

    CONCLUSIONS: According to our results, the COVID-19 pandemic was associated with mild anxiety and depression among healthcare workers in Egypt, especially pharmacists and physicians. We recommend more research targeting the mental health of healthcare workers in Egypt. If proven cost-effective and needed, wide-scale mental health screening and public health campaigns can facilitate effective prevention and treatment strategies. In addition, the availability of mental health facilities at the workplace could alleviate some of the risk perception associated with health emergencies and improve interprofessional teamwork.

  18. Firouzamandi M, Moeini H, Hosseini SD, Bejo MH, Omar AR, Mehrbod P, et al.
    Int J Nanomedicine, 2016;11:259-67.
    PMID: 26834470 DOI: 10.2147/IJN.S92225
    Plasmid DNA (pDNA)-based vaccines have emerged as effective subunit vaccines against viral and bacterial pathogens. In this study, a DNA vaccine, namely plasmid internal ribosome entry site-HN/F, was applied in ovo against Newcastle disease (ND). Vaccination was carried out using the DNA vaccine alone or as a mixture of the pDNA and dextran-spermine (D-SPM), a nanoparticle used for pDNA delivery. The results showed that in ovo vaccination with 40 μg pDNA/egg alone induced high levels of antibody titer (P<0.05) in specific pathogen-free (SPF) chickens at 3 and 4 weeks postvaccination compared to 2 weeks postvaccination. Hemagglutination inhibition (HI) titer was not significantly different between groups injected with 40 μg pDNA + 64 μg D-SPM and 40 μg pDNA at 4 weeks postvaccination (P>0.05). Higher antibody titer was observed in the group immunized with 40 μg pDNA/egg at 4 weeks postvaccination. The findings also showed that vaccination with 40 μg pDNA/egg alone was able to confer protection against Newcastle disease virus strain NDIBS002 in two out of seven SPF chickens. Although the chickens produced antibody titers 3 weeks after in ovo vaccination, it was not sufficient to provide complete protection to the chickens from lethal viral challenge. In addition, vaccination with pDNA/D-SPM complex did not induce high antibody titer when compared with naked pDNA. Therefore, it was concluded that DNA vaccination with plasmid internal ribosome entry site-HN/F can be suitable for in ovo application against ND, whereas D-SPM is not recommended for in ovo gene delivery.
  19. Saeed MEM, Boulos JC, Elhaboub G, Rigano D, Saab A, Loizzo MR, et al.
    Phytomedicine, 2019 Sep;62:152945.
    PMID: 31132750 DOI: 10.1016/j.phymed.2019.152945
    BACKGROUND: Cucurbitacin E (CuE) is an oxygenated tetracyclic triterpenoid isolated from the fruits of Citrullus colocynthis (L.) Schrad.

    PURPOSE: This study outlines CuE's cytotoxic activity against drug-resistant tumor cell lines. Three members of ABC transporters superfamily, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and ABCB5 were investigated, whose overexpression in tumors is tightly linked to multidrug resistance. Further factors of drug resistance studied were the tumor suppressor TP53 and the epidermal growth factor receptor (EGFR).

    METHODS: Cytotoxicity assays (resazurin assays) were used to investigate the activity of Citrullus colocynthis and CuE towards multidrug resistant cancer cells. Molecular docking (In silico) has been carried out to explore the CuE's mode of binding to ABC transporters (P-gp, BCRP and ABCB5). The visualization of doxorubicin uptake was done by a Spinning Disc Confocal Microscope. The assessment of proteins expression was done by western blotting analysis. COMPARE and hierarchical cluster analyses were applied to identify, which genes correlate with sensitivity or resistance to cucurbitacins (CuA, CuB, CuE, CuD, CuI, and CuK).

    RESULTS: Multidrug-resistant cells overexpressing P-gp or BCRP were cross-resistant to CuE. By contrast, TP53 knock-out cells were sensitive to CuE. Remarkably, resistant cells transfected with oncogenic ΔEGFR or ABCB5 were hypersensitive (collateral sensitive) to CuE. In silico analyses demonstrated that CuE is a substrate for P-gp and BCRP. Immunoblot analyses highlighted that CuE targeted EGFR and silenced its downstream signaling cascades. The most striking result that emerged from the doxorubicin uptake by ABCB5 overexpressing cells is that CuE is an effective inhibitor for ABCB5 transporter when compared with verapamil. The COMPARE analyses of transcriptome-wide expression profiles of tumor cell lines of the NCI identified common genes involved in cell cycle regulation, cellular adhesion and intracellular communication for different cucurbitacins.

    CONCLUSION: CuE represents a potential therapeutic candidate for the treatment of certain types of refractory tumors. To best of our knowledge, this is the first time to identify CuE and verapamil as inhibitors for ABCB5 transporter.

  20. Al-Sanea MM, Ali Khan MS, Abdelazem AZ, Lee SH, Mok PL, Gamal M, et al.
    Molecules, 2018 Jan 31;23(2).
    PMID: 29385071 DOI: 10.3390/molecules23020297
    A new series of 1-phenyl-3-(4-(pyridin-3-yl)phenyl)urea derivatives were synthesized and subjected to in vitro antiproliferative screening against National Cancer Institute (NCI)-60 human cancer cell lines of nine different cancer types. Fourteen compounds 5a-n were synthesized with three different solvent exposure moieties (4-hydroxylmethylpiperidinyl and trimethoxyphenyloxy and 4-hydroxyethylpiperazine) attached to the core structure. Substituents with different π and σ values were added on the terminal phenyl group. Compounds 5a-e with a 4-hydroxymethylpiperidine moiety showed broad-spectrum antiproliferative activity with higher mean percentage inhibition values over the 60-cell line panel at 10 µM concentration. Compound 5a elicited lethal rather than inhibition effects on SK-MEL-5 melanoma cell line, 786-0, A498, RXF 393 renal cancer cell lines, and MDA-MB-468 breast cancer cell line. Two compounds, 5a and 5d showed promising mean growth inhibitions and thus were further tested at five-dose mode to determine median inhibitory concentration (IC50) values. The data revealed that urea compounds 5a and 5d are the most active derivatives, with significant efficacies and superior potencies than paclitaxel in 21 different cancer cell lines belonging particularly to renal cancer and melanoma cell lines. Moreover, 5a and 5d had superior potencies than gefitinib in 38 and 34 cancer cell lines, respectively, particularly colon cancer, breast cancer and melanoma cell lines.
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