Browsing by Author "El-Naa M.M."

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Antioxidant and apoptotic effects of caffeic acid phenethyl ester induced marked inhibition on human breast cancer cell line
(2011) El-Refaei M.F.; El-Naa M.M.; Department of Molecular Biology; Genetic Engineering and Biotechnology Institute; Menoufiya University; Egypt; Department of Pharmacology and Toxicology; Faculty of Pharmacy; October University for Modern Sciences and Arts; Egypt
Cancer is a disease that is marked by high cell proliferation and metastasis which remains incurable even now. The present study aims at investigating the anti-proliferative and apoptotic effects of Caffeic Acid Phenethyl Ester (CAPE) against human carcinogenesis. This fact was established in vitro by our assessment of a ZR-75-1 human breast cancer cell line. Present data showed that 15 ?M CAPE induced a significant inhibition of cell viability after 48 h (nearly 50%). Cell death was characterized by morphology and chromatin condensation changes, of a typical apoptosis. Moreover, there was a scavenging reduction activity in vitro towards both nitric oxide (>47%) and superoxide dismutase reduction (169.3�3.7 ?U L-1). In addition, malondialdehyde was non significantly inhibited compared with untreated tumor cells. The CAPE has significant inhibitory and anti-proliferative effects on tumor cancer cells in vitro. This inhibition may be related to its antioxidant effects and achieved throughout its apoptotic effect. These findings provide the possibility for the future use of CAPE in human clinical trials therapy. � 2011 Academic Journals Inc.
Design, synthesis and structure-activity relationship of novel semi-synthetic flavonoids as antiproliferative agents
(Elsevier Masson SAS, 2014) Ragab F.A.; Yahya T.A.A.; El-Naa M.M.; Arafa R.K.; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; 11562 Cairo; Egypt; Medicinal Chemistry Department; Faculty of Pharmacy; Sana'a University; Sana'a; Yemen; Pharmacology and Toxicology Department; Faculty of Pharmacy; October University for Modern Sciences and Arts; Egypt
Various flavonoid scaffold based derivatives viz furochalcones (3a-e, 6a-d and 9a-d), furoflavones (10a-d, 11a-d, 12a-d, 18a&b), flavones (21a-d), furoaurones (13a,b, 14a-d and 15a-d) and 7-styrylfurochromones (22a-d and 25a-e) were designed and synthesized. The novel compounds were evaluated for their antiproliferative activity against a panel of 60 cancer cell lines comprising 9 types of tumors. Ten compounds belonging to the major subgroups of flavonoids viz furochalcones (3a, 3d, 6b, 9a and 9b), furoflavones (12a and 12c), furoaurones (15d), styrylfurochromones (25b and 25e) showed very promising activity. These active compounds were also evaluated in vitro as kinase inhibitors against CDK2/cyclin E1, CDK4/cyclin D1 and GSK-3? and the best inhibition was displayed against GSK-3? with the allylfurochalcone derivative 9b exhibiting 80% decrease in GSK-3? catalytic activity. On the other hand, the styrylfurochromone 25e interestingly showed a 13% enhancement of GSK-3? catalytic power and a 12% reduction in CDK4/cyclin D1 activity. Finally, the in vivo anti-tumor activity of 25e was evaluated against breast cancer induced in mice. The results showed a profound anti-tumor effect of 25e that accompanies a significant increase and decrease in the levels of GSK-3? and cyclin D1, respectively. � 2014 Elsevier Masson SAS. All rights reserved.
Flexible nano-sized lipid vesicles for the transdermal delivery of colchicine; in vitro/in vivo investigation
(Editions de Sante, 2019) El-Feky G.S.; El-Naa M.M.; Mahmoud A.A.; Department of Pharmaceutical Technology; Pharmaceutical and Drug Industries Research Division; National Research Center; Dokki; Cairo; Egypt; October University for Modern Sciences and Arts; Egypt; Department of Pharmacology and Toxicology; Faculty of Pharmacy; Fayoum University; Egypt; Department of Pharmaceutics and Pharmaceutical Technology; Faculty of Pharmaceutical Sciences and Pharmaceutical Industries; Future University; Cairo; Egypt
Colchicine (CL) is the most effective treatment of acute gout, however, it is associated with side effects in 80% of the patients at therapeutic doses, in addition, it's a water-soluble strong base (pKa ?12.8) which ionizes at physiological gastrointestinal pH resulting in low oral bioavailability of 44%. This work employed enhancing the bioavailability and reducing the side effects of CL through combining the benefits of the transdermal route together with those of elastic lipid nano-vesicles. Transfersomes (TRs) have been studied as vehicles for transdermal drug delivery, however, poor encapsulation of drugs and drug leaking of the vesicles required complexation of CL with ?-cyclodextrin (?-CD) before formulation. The composition of the designed CL-?-CD-TR was studied to balance the flexibility of the vesicles to their entrapment ability. CL-?-CD-TR were characterized for their shape, size, entrapment efficiency, elasticity, release profile, ex vivo skin permeation, pharmacological efficacy, and histopathological effect. Encapsulation efficiency of CL-?-CD complex in the vesicular formulations ranged from 42.3% to 93.8%. Particle size ranged from 70.6 nm to 138.5 nm and zeta potential ranged from 16.1 mV to 23.4 mV. The in vitro release of CL from the selected CL-?-CD-TR formulation (F3) showed a controlled, biphasic profile. Ex vivo study reported the great potential of F3 (CL-?-CD-TR) for skin permeation. In vivo experiment demonstrated that F3 (CL-?-CD-TR) possessed high biological efficacy with reduced skin irritation. � 2018 Elsevier B.V.
In-vivo antioxidant and anti-inflammatory activity of rosiglitazone, a peroxisome proliferator-activated receptor-gamma (PPAR-γ) agonists in animal model of bronchial asthma.
(Blackwell Publishing Ltd, 2015) El-Naa M.M.; El-Refaei M.F.; Nasif W.A.; Abduljawad S.H.; El-Brairy A.I.; El-Readi M.Z.; Department of Pharmacology and Toxicology; Faculty of Pharmacy; October University for Modern Sciences and Arts; 6 October City; Egypt; Molecular Biology Department; Institute of Genetic Engineering and Biotechnology; Sadat City University; Sadat City; Egypt; Department of Biochemistry; Faculty of Pharmacy; Al-Azhar University; Assiut; Egypt; Department of Biochemistry; Faculty of Medicine; Umm Al-Qura University; Makkah; Saudi Arabia; Department of Food Sciences; Faculty of Family Science; Taibah University; Al Madinah Al-Munawarah; Saudi Arabia; Department of Clinical Biochemistry; Faculty of Medicine; Umm Al-Qura University; P.O. Box 13174; Abdia; Makkah; 21955; Saudi Arabia
Objectives Peroxisome proliferator activated receptor-gamma (PPAR-?) has been shown to play an important role in the control of immunological and inflammatory responses. This study aims at investigating the potential role of rosiglitazone, a strong PPAR-? agonist in a murine model of bronchial asthma. Methods Adult male Guinea pigs were administered ovalbumin 100 mg/kg subcutaneous (SC) and 100 mg/kg intraperitoneal (IP). Treatment with rosiglitazone [5 mg/kg/day, per oral (PO)] was assessed for 21 days. On day 21, the animals were challenged with the same dose of ovalbumin. The forced expiratory volume in 1 s (FEV1) to forced vital capacity (FVC), FEV1/FVC, was measured using a spirometer to diagnosis lung obstruction. Serum levels of interleukin-5 (IL-5) and immunoglobulin E (IgE) were assessed. The activity of superoxide dismutase (SOD) and catalase and the level of reduced glutathione (GSH) were determined in lung tissue homogenates. Key findings Our results demonstrated that treatment with rosiglitazone resulted in a statistically significant improvement in lung function and histopathological features. Significant decrease in the serum levels of IL-5 and IgE were observed. The activity of SOD and catalase as well as the GSH level were significantly increased in the lung tissues of treated animals compared with untreated asthmatic animals. Serum IgE concentrations and IL-5 levels were directly correlated to each other and inversely correlated to the SOD, GSH and catalase levels in the all studied Guinea pigs. Conclusions Our results provide evidence that the PPAR-? agonist rosiglitazone may have potential in the development of therapies for bronchial asthma. 2015 Royal Pharmaceutical Society.
Inhibitory effect of caffeic acid phenethyl ester on mice bearing tumor involving angiostatic and apoptotic activities
(2010) El-Refaei M.F.; El-Naa M.M.; Molecular Biology Department; Genetic Engineering and Biotechnology Institute; Menoufiya University; Egypt; Department of Pharmacology and Toxicology; Faculty of Pharmacy; October University for Modern Sciences and Arts; Egypt
This study aims at investigating the anti-tumor effect of caffeic acid phenethyl ester (CAPE) against animal carcinogenesis. In order to substantiate this fact implanted tumor Ehrlich carcinoma cells were assessed in vivo to Swiss mice strain. We found that administrating of CAPE (15. mg/kg S.C.) showed that the tumor volume decreased significantly by 51%. As a result, it improved animal chances of survival and they became healthier. An anti-angiogenic effect of CAPE in vivo was observed, as determined by a significant serum matrix metalloproteinase (MMP-9) reduction (142.1. ng/ml), activation of endostatin serum level (1.9. ng/ml), as well as DNA fragmentation in tumor treated mice when compared with untreated ones. Conclusion: CAPE has a significant inhibitory effect on tumor in vivo. This inhibition may be related to its angiostatic and apoptotic effects. It also reduced angiogenic factors which may shift the equilibrium to the angiostatic effect of CAPE. These findings provide the possibility for the future use of CAPE as tumor therapy in human clinical trials. � 2010 Elsevier Ireland Ltd.
Profile of bioactive compounds in Nymphaea alba L. leaves growing in Egypt: Hepatoprotective, antioxidant and anti-inflammatory activity
(BioMed Central Ltd., 2017) Bakr R.O.; El-Naa M.M.; Zaghloul S.S.; Omar M.M.; October University for Modern Sciences and Arts (MSA); Pharmacognosy Department; Faculty of Pharmacy; Giza; Egypt; October University for Modern Sciences and Arts (MSA); Pharmacology Department; Faculty of Pharmacy; Giza; Egypt; October University for Modern Sciences and Arts (MSA); Pharmaceutics Department; Faculty of Pharmacy; Giza; Egypt; Universite Laval; Axe of Regenerative Medicine; Faculty of Medicine; Quebec City; Canada
Background: Nymphaea alba L. represents an interesting field of study. Flowers have antioxidant and hepatoprotective effects, rhizomes constituents showed cytotoxic activity against liver cell carcinoma, while several Nymphaea species have been reported for their hepatoprotective effects. Leaves of N. alba have not been studied before. Therefore, in this study, in-depth characterization of the leaf phytoconstituents as well as its antioxidant and hepatoprotective activities have been performed where N. alba leaf extract was evaluated as a possible therapeutic alternative in hepatic disorders. Methods: The aqueous ethanolic extract (AEE, 70%) was investigated for its polyphenolic content identified by high-resolution electrospray ionisation mass spectrometry (HRESI-MS/MS), while the petroleum ether fraction was saponified, and the lipid profile was analysed using gas liquid chromatography (GLC) analysis and compared with reference standards. The hepatoprotective activity of two doses of the extract (100 and 200 mg/kg; P.O.) for 5 days was evaluated against CCl4-induced hepatotoxicity in male Wistar albino rats, in comparison with silymarin. Liver function tests; aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), gamma glutamyl transpeptidase (GGT) and total bilirubin were performed. Oxidative stress parameters; malondialdehyde (MDA), reduced glutathione (GSH), catalase (CAT), superoxide dismutase (SOD), total antioxidant capacity (TAC) as well as inflammatory mediator tumour necrosis factor (TNF)-? were detected in the liver homogenate. Histopathological examination of the liver and immunohistochemical staining of caspase-3 were performed Results: Fifty-three compounds were tentatively identified for the first time in N.alba leaf extract, where ellagitannins represent the main identified constituents. Nine hydrocarbons, two sterols and eleven fatty acids were identified in the petroleum ether extract where, palmitic acid and linolenic acids represented the major saturated and unsaturated fatty acid respectively. N.alba AEE significantly improved the liver function, oxidative stress parameters as well as TNF-? in addition to the amelioration of histopathological features of the liver and a profound decrease in caspase-3 expression. Conclusion: These results shed light on the hepatoprotective effect of N. alba that is comparable with that of silymarin. The antioxidant activities of N. alba extract in addition to the inhibition of crucial inflammatory mediator, as TNF-?, might be the possible hepatoprotective mechanisms. � 2017 The Author(s).