Al Qanāţir al Khayrīyah, Egypt
Al Qanāţir al Khayrīyah, Egypt

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El-Helby A.-G.A.,Al - Azhar University of Egypt | Ayyad R.R.A.,Al - Azhar University of Egypt | Ayyad R.R.A.,Delta University | El-Adl K.,Al - Azhar University of Egypt | And 4 more authors.
Medicinal Chemistry Research | Year: 2016

A new series of 4-acetyl-1-substituted-3,4-dihydroquinoxalin-2(1H)-ones (2–13) were designed and synthesized in order to evaluate their AMPA-receptor antagonism as a potential mode of anticonvulsant activity. The structure of the synthesized compounds was confirmed by elemental analysis and spectral data (IR, 1HNMR, 13CNMR and Mass). The molecular design was performed for all the synthesized compounds to predict their binding affinity to AMPA-receptor in order to rationalize their anticonvulsant activity in a qualitative way. The data obtained from the molecular modeling was strongly correlated with that obtained from the biological screening which revealed that; compounds 12b, 13, 12a and 7a showed the highest binding affinities toward AMPA-receptor and also showed the highest anticonvulsant activities against pentylenetetrazole -induced seizures in experimental mice. The relative potencies of these compounds were 1.66, 1.66, 1.61 and 0.82 respectively, in comparing to diazepam. © 2016 Springer Science+Business Media New York


Abou-El-Sherbini K.S.,National Research Center of Egypt | Kenawy I.M.M.,Mansoura University | Hafez M.A.H.,Mansoura University | Lotfy H.R.,Delta University | Abdelbary Z.M.E.A.,Mansoura University
Journal of Environmental Chemical Engineering | Year: 2015

The new CO3 2-/Cl- layered double hydroxides (LDHs) (Mg(3-3v)Zn3v)/(Al(1-w)Few) were synthesized and calcined at 450 °C (CLDH), where v and w = 0, 0.1, 0.2, and/or 1, as adsorbents to remove anionic hazards such as Isolan Dark Blue 2SGL-01 (IDB) and CrO4 2- from polluted wastewater. The products were characterized by powder X-ray diffractometry, Fourier transform infra-red spectra, thermogravimetric analysis, elemental analysis, scanning electron microscope, magnetic susceptibility and specific surface area measurements. The effect of composition of LDH's on their uptake capacities (qe) for IDB and chromate ions were studied. CLDH's were more effective in removing anionic hazards than LDH, in particular with IDB and for v and w = 0.1 and/or 0.2. High adsorption capacities were obtained up to 438 and 46.3 mg g-1 (30.1 and 15.7% of the theoretical capacities), for IDB and chromate, respectively. Fe-containing LDHs could be magnetically separated either as-synthesized or loaded. © 2015 Elsevier Ltd.


Khedr N.F.,Tanta University | Khalil R.M.,Delta University
Tumor Biology | Year: 2015

Doxorubicin (DOX) is widely used in cancer therapy of many carcinomas types. Unfortunately, DOX is not sufficiently effective in many cases, and increasing the dosage of it is limited due to its systemic toxicity. A citrus flavonoid hesperidin (HES) is proved to be potent antioxidant and protective agent against many diseases including cancer. In this context, the objective of this study was to examine effect of HES along with DOX on solid Ehrlich carcinoma (SEC) in mice. Forty male mice were divided into four equal groups (n = 10): control SEC, DOX, HES, and DOX + HES. HES (50 mg/kg body weight orally) was given day after day for 16 days along with DOX (4 mg/kg body weight i.p. injection) for 5 cycles every 4 days in ESC-inoculated mice. After 20 days, tumor volume, tumor weight, survival rate, tumor glutathione, nitric oxide content, and serum glutathione were determined. Tumor tissue was examined for histopathological and immunohistochemical study for p53 and VEGF. Tumor resistance for mdr1a gene was assessed in tumor tissue by RT-PCR. HES induced significant increase in tissue and serum glutathione with significant decrease in tumor volume and tumor weight. A possible role of HES to modulate gene expression of mdr1a in tumor tissue was established. In addition, HES alleviated the histopathological changes with significant decrease in p53 and VEGF expression. The use of HES as adjuvant therapy with DOX would enhance the therapeutic efficacy and alleviate the resistance to DOX in treatment of solid tumors. © 2015, International Society of Oncology and BioMarkers (ISOBM).


PubMed | Tanta University and Delta University
Type: Journal Article | Journal: Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine | Year: 2015

Doxorubicin (DOX) is widely used in cancer therapy of many carcinomas types. Unfortunately, DOX is not sufficiently effective in many cases, and increasing the dosage of it is limited due to its systemic toxicity. A citrus flavonoid hesperidin (HES) is proved to be potent antioxidant and protective agent against many diseases including cancer. In this context, the objective of this study was to examine effect of HES along with DOX on solid Ehrlich carcinoma (SEC) in mice. Forty male mice were divided into four equal groups (n=10): control SEC, DOX, HES, and DOX+HES. HES (50 mg/kg body weight orally) was given day after day for 16 days along with DOX (4 mg/kg body weight i.p. injection) for 5 cycles every 4 days in ESC-inoculated mice. After 20 days, tumor volume, tumor weight, survival rate, tumor glutathione, nitric oxide content, and serum glutathione were determined. Tumor tissue was examined for histopathological and immunohistochemical study for p53 and VEGF. Tumor resistance for mdr1a gene was assessed in tumor tissue by RT-PCR. HES induced significant increase in tissue and serum glutathione with significant decrease in tumor volume and tumor weight. A possible role of HES to modulate gene expression of mdr1a in tumor tissue was established. In addition, HES alleviated the histopathological changes with significant decrease in p53 and VEGF expression. The use of HES as adjuvant therapy with DOX would enhance the therapeutic efficacy and alleviate the resistance to DOX in treatment of solid tumors.

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