17 & 18 February 2021 The1st international ZPSC 2021 The 1st International Scientific Conference of Faculty of Pharmacy, Zagazig University Pharmacy Vision in Egypt Strategy 2030 \"New Trends in Pharmaceutical Research and Drug Development\"
The1st international ZPSC 2021 Under the patronage of Prof. Dr. Othman Shaalan President of Zagazig University Prof. Dr. Mervat Askar Vice president of Zagazig University for post graduate studies and researches Conference Chairman Prof. Dr. Hanan El-Nahas Acting Dean of Faculty of Pharmacy Vice dean of postgraduate studies and researches Conference Coordinator Assistant Prof. Dr. Hend Kothayer Assistant Professor of Medicinal Chemistry
The1st international ZPSC 2021 Acknowledgement for Organizers Prof. Dr. Hanan El-Nahas Acting Dean of Faculty of Pharmacy Vice dean of postgraduate studies and Assistant Prof. Dr. Hend Kothayer researches Dr. Momen Askoura Conference Chairman Dr. Amany Ghanim Assistant Professor of Medicinal Dr. Rania Elrashidy Dr. Noura Eissa Chemistry Dr. Esraa Zakaria Conference Coordinator Dr. Sara Anis Lecturer of Microbiology and Dr. Samar Elbaramawi Immunology Dr. Mona Fekry Lecturer of Organic Chemistry Dr. Ahmed Samy Dr. Naglaa Kabil Lecturer of Biochemistry Asst. Lecturer/ Tarek Metwally Asst. Lecturer/ Nada Rady Lecturer of Pharmaceutics Ph. Ahmed Magdy Ph. Mohamed Wagdy Lecturer of Pharmacology Ph. Mohamed Salah Ph. Mahmoud Emad Lecturer of Pharmaceutical Analytical Chemistry Lecturer of Medicinal Chemistry Lecturer of Pharmacognosy Lecturer of Medicinal Chemistry Lecturer of Pharmaceutical Analytical Chemistry Assistant Lecturer of Pharmaceutics Assistant Lecturer of Pharmacy Practice Demonstrator of Pharmacy Practice Demonstrator of Pharmacy Practice Demonstrator of Pharmaceutics Demonstrator of Pharmacy Practice
The1st international ZPSC 2021 Conference Agenda Wednesday 17/2/2021 9:30 am - 10 am Signing in Opening Session 10 am – 10:15 am • Quran Kareem • Faculty dean and Postgraduate Studies & research affairs vice dean (conference chairman) talk • Vice president Postgraduate Studies & research affairs talk Invited speakers’ Session 10:15 am - 10:45 am • Prof.Dr. Adel Abou-Ali • Prof.Dr. Ahmed Zidan Pharmacology Session Oral Presentation ●PPAR-γ agonist, pioglitazone, reduced oxidative and endoplasmic reticulum stress associated with L- NAME-induced hypertension in rats. Presented by Dr Shereen F. Behairy ●Glycyrrhizic acid and Silymarin alleviate the neurotoxic effects of aluminum in rats challenged with 10:45 am – 11:35 am fructose-induced insulin resistance: possible role of toll-like receptor 4 pathway. Presented by Dr Noura M. Ali Poster Presentation ● Carvedilol protects against hepatic ischemia/reperfusion injury in high-fructose/high-fat diet-fed mice: Role of G protein-coupled receptor kinase 2 and 5. Presented by Dr Samar G. Mohammed Medicinal Chemistry Session Oral Presentation ●Rational design of (1,4-dihydroquinazolin 3(2H)yl)benzamide derivatives as anti-inflammatory, analgesic and COX-1/2 inhibition activities with molecular docking study. 11:35 am – 12:15 pm Presented by Dr Asmaa Sakr Poster Presentation ●Nitrogen: A story behind A6CDQ at h5-HT3A Serotonin Receptors Presented by Dr Ahmed S. Abdelkader ●Synthesis and Antibacterial Evaluation of 2,3-Dihydroquinazolin-4(1H)-ones Presented by Dr Aya M. Emam 12:15 pm – 12:45 pm Break Invited speaker’s Session 12:45 pm: 1:15 pm • Prof.Dr. Salah Ghareib 1:15 pm – 2 pm Biochemistry Session Oral Presentation ●Raspberry Ketone versus Calorie Restriction on Modulating Metabolic Disorders in Obese Rats Presented by Dr Mahmoud E. Zaher Poster Presentation ●Green coffee bean extract in fructose induced Alzheimer’s disease in rats Presented by Dr Nahla N. Younis ●Long-term consumption of Western diet contributes to endothelial dysfunction and aortic remodeling in rats: Implication of Rho-kinase signaling Presented by Dr Rania A. Elrashidy ●Inhibition of Aortic Calcification by Policosanol in Dyslipidemic Rabbits Is Enhanced by Pentoxifylline: Potential Role of PCSK9 Presented by Dr Gehad M. Elnagar
The1st international ZPSC 2021 2 pm – 3 pm Pharmacognosy Session Oral Presentation ●New Cytotoxic Sesquiterpene Oxide-Coumarin From Ferula assafoetida Presented by Dr Mona Fekry ●Micropropagation, Myristicin Production Enhancement, and Comparative GC-MS Analysis of the n- Hexane Extracts of Different Organs of Daucus pumilus (Gouan), Family Apiaceae ** Presented by Dr Asmaa M. Arafa Poster Presentation ●Macro- and micromorphological study of Salix tetrasperma Roxb. cultivated in Egypt. Presented by Dr Eman Fikry Thursday 18/2/2021 9:30 am to 10 am Signing in Invited speakers’ Session 10 am – 11:15 am • Prof.Dr. Ashraf Elshoura • Prof. Dr. Amal A.M Eid • Assistant Professor Dr Hend Kothayer Pharmaceutics session Oral Presentation ● Enhancement The Hypolipidemic Effect of Atorvastatin Calcium Via Floating Microspheres Technique. Presented by Dr Al Zahraa G. Al Ashmawy Poster Presentation 11:15 am – 11:55 am ● Preparation and Characterization of Ivabradine HCl Transfersomes for Enhanced Transdermal Delivery. Presented by Dr Mennatullah M. Faisal ●Transdermal Ethosomal Gel Nanocarriers - A Promising Strategy for Enhancement of Anti- Hypertensive Effect of Carvedilol. Presented by Dr Tarek M. Ibrahim 11:55 am– 12:25 pm Break Pharmacy practice session Oral Presentation ●Efficacy of sofosbuvir plus daclatasvir in treatment of Egyptian patients with chronic HCV infection: A prospective cohort study 12:25 pm – 12:55 pm Presented by Dr. Nada R. Badawy Poster Presentation ● High-Dose Dual Therapy versus Triple Therapy for Treatment of H. Pylori Infection: A Parallel Randomized Study Presented by Dr Aya Ahmed Pharmaceutical Organic Chemisrty session Oral Presentation ● Design, synthesis, antimicrobial, and DNA gyrase inhibitory properties of fluoroquinolone– dichloroacetic acid hybrids. Presented by Dr Israa A. Seliem 12:55 pm – 1:45 pm Poster Presentation ● Efficient Synthesis and Computational Studies of Useful Guanylating Agents: 1H-Benzotriazole-1- Carboximidamides. Presented by Dr Riham M. Bokhtia ●Synthesis of Imidazolidine‐2,4‐Dione and 2‐Thioxoimidazolidin‐4‐one Derivatives as Inhibitors of Virulence Factors Production in Pseudomonas aeruginosa.
The1st international ZPSC 2021 Presented by Dr Basant Mohamed ● Design, Synthesis, and Biological Evaluation of Novel Nicotinamide Derivatives as Potential Histone Deacetylase-3 Inhibitors. Presented by Dr Mohamed M. S. Hamoud Microbiology and Immunology session Oral Presentation ● Oxidative stress & Pseudomonas aeruginosa: friends or enemies? Presented by Dr Momen Askoura 1:45 pm – 2:25 pm Poster Presentation ● Antibiotic susceptibility of Pseudomonas aeruginosa isolated from different clinical sources Presented by Dr Fatma A. Mohamed ●Antibiotic susceptibility of Staphylococcus aureus isolated from different clinical sources. Presented by Dr Aliaa Abdelghafar Pharmaceutical Analytical Chemisrty session Oral Presentation ● Development and validation of eco-friendly micellar-HPLC and HPTLC-densitometry methods for the simultaneous determination of paritaprevir, ritonavir and ombitasvir in pharmaceutical dosage forms. Presented by Dr Roshdy E. Saraya 2:25 pm – 3:15 pm Poster Presentation ● Spectrophotometric Determination of Etilefrine HCl, Salbutamol Sulphate and Tiemonium Methyl Sulphate Using Surface Plasmon Resonance Band of Gold Nanoparticles. Presented by Dr Naglaa Abdel-Sattar Kabil ● Spectroscopic determination of hydrochlorothiazide and minoxidil in dosage forms and spiked human urine using NBD-Cl . Presented by Dr Omar M.EL-Abassy Closing session 3:15 pm – 3: 25 pm Honorship & Conference recommendations Assistant Professor Dr Hend Kothayer
The1st international ZPSC 2021 Invited speakers Prof.Dr. Ahmed Zidan Division of Product Quality Research, Office of Testing and Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, Food and Drug Administration, MD, USA Identifying the Processing Space of Continuous Granulation of Extended Release Tablets Dr. Adel Abou-Ali Doctorate degree in pharmacy from Massachusetts College of Pharmacy and Health Sciences, a master degree in health management and policy, and a doctorate degree in Epidemiology from University of Massachusetts. He is currently a Global Director of Risk Management and Benefit Risk with pharmaceutical industry, USA. COVID-19 Current Vaccines Prof.Dr. Ashraf Elshora Professor of Chest Disease, Zagazig Faculty of Medicine COVID19 Overview Prof. Dr. Amal A.M Eid Department of Avian and Rabbit Medicine, Faculty of Veterinary Medicine, Zagazig University, Zagazig Efforts for combating Covid-19 Pandemic: Vaccine strategies and challenges
The1st international ZPSC 2021 Dr. Salah A. Ghareib Atteiah Professor of Pharmacology and Toxicology Vitamin D insufficiency and deficiency in COVID-19 severity of infections and mortality Assistant Professor. Dr. Hend Kothayer Assistant Professor of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University Multi-target Drug Design
The 1st international ZPSC 2021 Pharmacology Session -9-
The 1st international ZPSC 2021 Oral Presentation - 10 -
The 1st international ZPSC 2021 PPAR-γ agonist, pioglitazone, reduced oxidative and endoplasmic reticulum stress associated with L-NAME-induced hypertension in rats Eman Soliman a, Shereen F. Behairy a*, Nabila N. Elmaraghy b, Shimaa M. Elshazly a a Department of Pharmacology and Toxicology, Faculty of Pharmacy, Zagazig University b Department of Pharmacology, Toxicology and Biochemistry Future University in Egypt, Egypt Abstract Peroxisome proliferator-activated receptor γ (PPAR-γ) agonist, pioglitazone, is used clinically to improve the glycemic state in patients with type-2 diabetes mellitus. Independent of its blood glucose-lowering properties, pioglitazone ameliorates different cardiovascular disorders. The aim of the present study was to investigate the effect of pioglitazone on cardiovascular complications of N- nitro-L-arginine methyl ester (L-NAME)-induced hypertension and to determine the role of oxidative and endoplasmic reticulum (ER) stress in its activity. Nitric oxide (NO) deficiency induced by chronic L-NAME administration was associated with high blood pressure (BP) and cardiac hypertrophy. L-NAME induced oxidative stress as indicated by reduced glutathione (GSH) levels, superoxide dismutase (SOD) and catalase activities as well as increased malondialdehyde (MDA) levels. Furthermore, L-NAME increased the expression of ER stress markers, activating transcription factor-4 (ATF-4) and C/EPBα- homologous protein-10 (CHOP-10) in both heart and aorta of hypertensive rats. Activation of PPAR-γ by pioglitazone reduced BP, restored the blunted NO levels, increased endothelial NO synthase (eNOS) expression, and restored the antioxidant status of L-NAME-induced hypertensive rats. Moreover, the antihypertensive activity of pioglitazone was associated with a reduction in ER stress and this effect was PPAR-γ dependent. Interestingly, the effect of ER stress inhibitor, 4-phenylbutyric acid (4-PBA) and antioxidant, N-acetylcysteine (NAC), on BP, NO availability, oxidative stress and ER stress mimics the activity of pioglitazone. Taken together, our data suggests that PPAR-γ is a potential target to inhibit vascular complications and cardiac damage associated with NO- deficient HTN and puts more emphasis on the importance of ER stress in regulating PPAR-γ activity. * Oral Presenting author - 11 -
The 1st international ZPSC 2021 Glycyrrhizic acid and Silymarin alleviate the neurotoxic effects of aluminum in rats challenged with fructose-induced insulin resistance: possible role of toll-like receptor 4 pathway Noura M. Ali*, Amr A. A. Mahmoud , Mona F. Mahmoud and Hassan M. El Fayoumi Department of Pharmacology and Toxicology, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. Abstract Aluminum is implicated in the etiology of different neurodegenerative diseases, diabetes and cancer. The current study was conducted to evaluate the protective effects of glycyrrhizic acid (GAM) and silymarin (SLY) on AlCl3-induced neurotoxicity in insulin resistant rats. Insulin resistance (IR) was induced by fructose (10%) in drinking water for 18 weeks. Rats received AlCl3 (34mg/kg/day) with or without fructose, GAM (40mg/kg/day), or SLY (100mg/kg/day). The administration of GAM or SLY suppressed AlCl3-induced memory deficit, oxidative stress, and neuroinflammation in brain tissue of IR rats. Both agents inhibited AlCl3-induced activation of TLR4 signaling pathway including the downstream activation of NF-jB. The results show that IR can partly exacerbate AlCl3-induced neurotoxicity, particularly memory deficit and neuroinflammation. In addition, GAM and SLY showed promising neuroprotective effect against AlCl3-induced brain damage in IR rats. The neuroprotection induced by these natural products might be mediated through their antioxidant and anti-inflammatory effects. The latter effect seems to be mediated via inhibition of TLR4 signaling pathway providing new insights on the mechanisms implicated in AlCl3-induced neurotoxicity and the neuroprotection afforded by GAM and SLY. * Oral Presenting author - 12 -
The 1st international ZPSC 2021 Poster Presentation - 13 -
The 1st international ZPSC 2021 Carvedilol protects against hepatic ischemia/reperfusion injury in high- fructose/high-fat diet-fed mice: Role of G protein-coupled receptor kinase 2 and 5 Samar G. Mohammed a, b*, Islam A.A.E. Ibrahim a, Mona F. Mahmoud a, Amr A.A. Mohmoud a a Department of Pharmacology and Toxicology, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. b Department of Toxic and Narcotic Drugs, Forensic Medicine, Cairo Laboratory, Medicolegal Organization, Ministry of Justice, Cairo, Egypt; Department of Toxic and Narcotic Drugs, Forensic Medicine, Cairo Laboratory, Medicolegal Organization, Ministry of Justice, Cairo, Egypt. Abstract Hepatic ischemia/reperfusion injury (H-IRI) is associated with irreversible liver damage. The current study aimed to investigate the protective effect of carvedilol against H-IRI in high-fructose high-fat diet (HFrHFD)-fed mice and the role of G protein-coupled receptor kinase 2 and 5 (GRK2 and GRK5). Mice were fed HFrHFD for 16 weeks; then mice were subjected to 30 min of ischemia followed by 1 h of reperfusion at the end of feeding period. Carvedilol (20 mg/kg, i.p.) was administered 30 min before ischemia. To explore the role of GRK2 and GRK5 in mediating carvedilol effects, paroxetine (GRK2 inhibitor, 10 mg/kg, i.p.) and amlexanox (GRK5 inhibitor, 25 mg/kg, i.p.) were administered 30 min before carvedilol administration. Liver function, histopathology and hepatic oxidative stress, as well as inflammatory and apoptotic markers were measured at the end of the experiment. In addition, adrenergic receptor downstream signals were measured in the liver. Results showed increased markers of liver injury (ALT and AST) in mice subjected to H-IRI. Moreover, liver injury was associated with slight collagen deposits as revealed by histopathology and elevated hepatic levels of oxidative stress, inflammatory and apoptotic markers. On the other hand, carvedilol protected mice against H-IRI and improved all associated pathological changes. Furthermore, pre-injection of either GRK2 or GRK5 inhibitor did not change carvedilol effects on serum ALT level and liver collagen deposits, while increased its antioxidant, anti-inflammatory and anti-apoptotic effects. In conclusion, carvedilol protects against H-IRI in HFrHFD-fed mice. GRK2 and GRK5 may not play a potential role in mediating this effect. * Poster Presenting author - 14 -
The 1st international ZPSC 2021 Medicinal Chemistry Session - 15 -
The 1st international ZPSC 2021 Oral Presentation - 16 -
The 1st international ZPSC 2021 Rational design of (1,4-dihydroquinazolin 3(2H)yl)benzamide derivatives as anti-inflammatory, analgesic and COX-1/2 inhibition activities with molecular docking study Asmaa Sakra*, Hend Kothayera*, Mohamed M. Barakaa, Samy M. Ibrahima Samar Rezqb a Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Egypt. b Department of Pharmacology, Faculty of Pharmacy, Zagazig University, Egypt. Abstract The design and synthesis of the new series 1,4-dihydroquinazolin 3(2H)yl)benzamide derivatives as anti-inflammatory, analgesic and COX1/2 inhibitors upon smart new rational study targeting abolish the known side effects for both enzymes. The theory established by the design included; i) incorporation for big central anti-inflammatory ring (Quinazolinone), ii) keep the vicinal shape for two aryl group, iii) The removal of carboxylic acid group which all help in make it difficult to enter COX-1 active site and subsequent prevent COX-1 inhibition. The last modification was removal of substituted sulphonyl group which responsible for high selectivity, that the reason for cardiovascular side effects. The all series of 1,4-dihydroquinazolinbenzamide compounds (4a-o) were synthesized with limited number of reactions along with high purity of yield. The in vivo and in vitro assay exhibited the success of rational with potency and moderate selectivity towards COX-2 also a great success in decreasing the side effects resulted from binding with COX-1 active site such as; ulcer to Zero. The especial focus on the compound 4b as it was the one among the series with the best reasonable results in all the experiments either in vivo or in vitro with docking study that assure the results of the series much more towards COX-2 scores and further far from COX-1 scores; moreover, the predicted in silico studies was magnificent as drug-likeness with future medicinal candidate. * Oral Presenting author - 17 -
The 1st international ZPSC 2021 Poster Presentation - 18 -
The 1st international ZPSC 2021 Nitrogen: A story behind A6CDQ at h5-HT3A Serotonin Receptors Ahmed S. Abdelkhalek,*1, 2, Małgorzata Dukat2 1Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt 2Department of Medicinal Chemistry, School of Pharmacy, VCU, Richmond, VA, USA Abstract 2-amino-6-chloro-3,4-dihydroquinazoline (A6CDQ), binds at human 5-HT3 receptors and displayed antidepressant-like activity in a pre-clinical assay, the mouse tail suspension test (TST). Our goal is to study the structure-affinity relationships (SAFiR) of A6CDQ at h5-HT3A receptors. Quinazoline deconstructed and N-substituted analogs were synthesized and biologically evaluated using radioligand binding assay. The obtained results showed that A6CDQ binds with higher affinity than its deconstructed analogs and N- substituted analogs. The N1 nitrogen atom appears to be crucial for binding affinity. The N2 and N3 nitrogen atoms contribute to but are not crucial for binding at h5-HT3A receptors. Substituents at the terminal nitrogen (even a single methyl group) are not tolerated by h5-HT3A receptors; a primary amine seems optimal for binding affinity at h5-HT3A receptors. 3D molecular modeling studies revealed that hydrogen bond features are important for the binding of A6CDQ at 5-HT3A receptors and the results are consistent with the binding affinity data. * Poster Presenting author - 19 -
The 1st international ZPSC 2021 Synthesis and Antibacterial Evaluation of 2,3-Dihydroquinazolin-4(1H)-ones Aya M. Emam*1, Hend Kothayer1, Samy M. Ibrahim1, Mohamed Elsadek1 1Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Egypt Abstract Antibacterial agents structurally based on quinazolin-4-one pharmacophore, have been designed and synthesized. Where the targeted compounds 5a, c and 6a-c were in vitro screened against three gram positive and three gram negative bacteria strains compared to ciprofloxacin as reference drug. Most of compounds had moderate antibacterial activity while compound 5c showed the most significant activity and could be considered as a new lead compound for antibacterial drug design. * Poster Presenting author - 20 -
The 1st international ZPSC 2021 Biochemistry Session - 21 -
The 1st international ZPSC 2021 Oral Presentation - 22 -
The 1st international ZPSC 2021 Raspberry Ketone versus Calorie Restriction on Modulating Metabolic Disorders in Obese Rats Asker ME a, Ali SI a, Younis NN a, Shaheen MA b, Zaher ME a* a Department of Biochemistry, Faculty of Pharmacy, Zagazig University, 44519, Egypt b Department Medical Histology and Cell Biology, Faculty of Medicine, Zagazig University, 44519, Egypt Abstract Obesity management regimens suffer from discomfort, undesirable side effects and/or unsuccessful outcomes. This study compared normal diet (ND) regimen with raspberry ketone (RK) supplementation and calorie restriction (CR). 40- MaleWistar rats received high fat diet (HFD) for 16 weeks. Obese control group was maintained on HFD for another 6 weeks (n=10). Other obese groups (n=10 each) received ND, CR diet or ND with RK oral supplement (44 mg/kg) for 6 weeks. HFD increased body and visceral white adipose tissue (WAT) weights, serum glucose, total cholesterol, TG, LDL-C, inflammatory markers (MCP-1, IL-6 and TNF-α) in WAT, while decreased serum HDL-C and WAT adiponectin. Like CR diet, ND with RK supplementation restored the changes attained by HFD. Conclusion RK supplement with ND regimen effectively attenuated obesity-related changes. Such approach could be an alternative to CR in the management of obesity, thereby overcome the side effects of applying CR for long time. * Oral Presenting author - 23 -
The 1st international ZPSC 2021 Poster Presentation - 24 -
The 1st international ZPSC 2021 Green coffee bean extract in fructose induced Alzheimer’s disease in rats Nahla N. Younis*a, Hoda E. Mohameda, Mervat E. Askera, Mohamed A. Shaheen b, Rana G. Eissaa a Department of Biochemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519, Egypt b Department of Histology and Cell Biology, Faculty of Medicine, Zagazig University, Zagazig, 44519, Egypt Abstract Increased fructose consumption is one of the bad nutritional habits that contributes to the increased incidence of neurodegenerative diseases including Alzheimer's disease (AD). In this study we proposed that coffee, the most popular beverage consumed by adults worldwide, may protect against the development of AD. We therefore aimed to investigate the protective potential of green coffee bean extract (GCBE) either alone or combined with pioglitazone (PIO) in fructose-induced AD. Twenty four rats [12 untreated and 12 pre-treated (4 weeks) with GCBE] were allowed to consume 10 % fructose in drinking water for 18 weeks. Twelve of these rats (6 GCBE-untreated and 6 GCBE-pre- treated) were treated with PIO during the last 6 weeks of fructose consumption. Oxidative stress, cholinergic activity, amyloid beta (Aβ) extracellular plaques formation and learning/memory ability were examined. GCBE attenuated oxidative damage and retarded the activation of acetylcholine esterase (AChE), hence increased acetylcholine (ACh) level in the cortex of fructose-induced AD. It also impeded the up-regulation of beta-secretase 1(BACE1) and the accumulation of Aβ plaques that were induced by fructose drinking. Our results suggest that the consumption of GCBE may protect against the development of AD and may delay the progression of AD when given with pioglitazone. * Poster Presenting author - 25 -
The 1st international ZPSC 2021 Long-term consumption of Western diet contributes to endothelial dysfunction and aortic remodeling in rats: Implication of Rho-kinase signaling Rania A. Elrashidy a,b*, Jing Zhang c, and Guiming Liu a a Department of Surgery, MetroHealth Medical Center, Case Western Reserve University, Cleveland, OH, USA b Department of Biochemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt c Department of Hyperbaric Oxygen, Capital Medical University Beijing Chao-Yang Hospital, Beijing, China Abstract Western diet (WD), rich in saturated fat and sugars, has become a risk factor for obesity and metabolic syndrome, however, its effect on endothelial function and vascular remodeling is not fully elucidated. Recent evidence suggests cross-talk between Rho kinase (ROCK) pathway and cardiovascular system. We aimed to investigate the effect of WD on aortic remodeling, and the contribution of ROCK signaling. Eight week old male Sprague-Dawley rats were fed either standard chow diet (SD) or high fructose/high fat diet, typically as in WD. After 42 weeks, WD-fed rats showed hyperglycemia, dyslipidemia and hypertension without marked weight gain, compared to SD-fed rats. Significant up-regulation of ROCK-1 and -2, along with a decline in eNOS expression were found in aortic tissue of WD-fed rats. Additionally, WD-fed rats displayed oxidative stress and fibrosis in their aortic tissues versus controls. Our findings suggest that long-term feeding of WD contributes to endothelial dysfunction and aortic remodeling in adult male rats. ROCK activation seems to be involved in WD-related vascular disorders, and may represent a promising therapeutic target. * Poster Presenting author - 26 -
The 1st international ZPSC 2021 Inhibition of Aortic Calcification by Policosanol in Dyslipidemic Rabbits Is Enhanced by Pentoxifylline: Potential Role of PCSK9 Mohamed M. Elseweidy, PhD1 , Hoda E. Mohamed, PhD1, Rania A. Elrashidy, PhD1, Hebatallah H. Atteia, PhD1, and Gehad M. Elnagar*, Msc1 1 Department of Biochemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt Abstract Policosanol (POL) is a hypocholesterolemic drug of natural origin and has been shown to reduce circulating levels of proprotein convertase subtilisin/kexin type 9 (PCSK9) in healthy participants. Recently, we have reported that POL can attenuate aortic calcification in diabetic dyslipidemic rats; however, the underlying mechanism is not fully elucidated. We aimed to investigate the effect of POL on aortic calcification and whether PCSK9 has a contributory role and also to examine whether the combination of POL with pentoxifylline (PTX) as anti–tumor necrosis factor α would offer additional benefits. Thirty adult male New Zealand rabbits weighing 1.5 to 2 kg were randomly assigned to 5 groups. One group received standard chow diet and served as normal control group (NC). The other 4 groups received 0.5% wt/wt cholesterol-rich diet for 12 weeks and concurrently treated with placebo, POL, PTX, or a combination of POL and PTX. Sera samples and aortic tissue were collected for biochemical measurements and histological assessment. Rabbits fed a cholesterol-rich diet demonstrated dyslipidemia, increased inflammatory state, and elevated serum levels of PCSK9, compared to the NC group. Aortic calcification was evident in dyslipidemic rabbits, represented by increased calcium deposition and osteopontin expression in aortic tissue, along with elevated serum levels of alkaline phosphatase and osteocalcin. Dyslipidemic rabbits showed a significant upregulation of wingless- type MMTV integration site family 3A and bone morphogenetic protein 2 genes in their aortic tissue. Policosanol significantly reduced circulating PCSK9 levels, suppressed calcification markers, and attenuated aortic calcification. Combination of POL with PTX alleviated aortic calcification to a greater extent than either monotherapy, which may be attributed to further suppression of PCSK9 and calcification markers. These findings suggested that POL exerted anticalcifying effect partly via inhibition of PCSK9. Combination of POL and PTX offered additional benefits and might represent a promising therapeutic option for aortic calcification. * Poster Presenting author - 27 -
The 1st international ZPSC 2021 Pharmacognosy Session - 28 -
The 1st international ZPSC 2021 Oral Presentation - 29 -
The 1st international ZPSC 2021 New Cytotoxic Sesquiterpene Oxide-Coumarin From Ferula assafoetida Mahmoud M. Abdel-Aal, Azza M. El-Shafae, Abd El-monem M. Ateya, Gamal Dora, Mona Fekry* and Maged M. Abou-Hashem Pharmacognosy Department, Faculty of Pharmacy, University of Zagazig, 44519, Zagazig, Egypt Abstract Bioguided fractionation of Ferula assafoetida L. (Apiaceae) oleogum resin using petroleum ether, methylene chloride and ethylacetate leads to the isolation of the new sesquiterpene oxide-coumarin, (+) farnesiferol C (1) together with five known compounds, (-) farnesiferol C (2), umbelliprenin (3), colladonin (4), ethyl ferulate (5) and ferulic acid (6). The structures of these compound were established using different spectroscopic methods including IR, mass, 1H-NMR, 13C-NMR, DEPT, COSY, HMBC and HSQC. (+) Farnesiferol C showed a potent cytotoxic activity against Human hepatocarcinoma cell line (Hep-G2) with IC50=1.3 µg/ml compared to doxorubicin (IC50 1.2 µg/ml). * Oral Presenting author - 30 -
The 1st international ZPSC 2021 Micropropagation, Myristicin Production Enhancement, and Comparative GC-MS Analysis of the n-Hexane Extracts of Different Organs of Daucus pumilus (Gouan), Family Apiaceae ** Asmaa M. Arafa*, Afaf E. Abdel-Ghani, Samih I. El-Dahmy, Sahar Abdelaziz Pharmacognosy Department, Faculty of Pharmacy, Zagazig University, 44519 Zagazig, Egypt Abstract Aim: This work aimed to study the somatic embryogenesis and organogenesis of endangered Daucus pumilus (Gouan) for the conservation of this plant and improving the production of secondary metabolites of medicinal value. Materials and Methods: The callus formation and in vitro propagation of D. pumilus (Gouan) by using a different combination of naphthalene acetic acid and benzylaminopurine were established. Various embryogenic stages were tracked using scanning electron microscopy and light microscopy. The volatile constituents of the n-hexane extracts of D. pumilus (Gouan) that extracted by ultrasonic-assisted technique were analyzed by gas chromatography–mass spectrometry. Results and Discussion: Somatic embryogenesis and organogenesis of endangered D. pumilus (Gouan) were established for the first time. Myristicin and elemicin were successfully increased during micropropagation to 70.89% and 2.19%, respectively. Furthermore, the induction of compounds such as 6-methoxymellein, eugenin, methyl behenate, and 1,6- dimethylnaphthalene was also detected. Conclusion: Commercially, this protocol decreases the dependence on wild medicinal plants, enhances the manufacturing of valuable phytochemicals to meet the great demands of the pharmaceutical industries, and acts as a mean for genetic transformation of this plant. **Arafa, A.M., Abdel-Ghani, A.E., El-Dahmy, S.I. and Abdelaziz, S., 2020. Micropropagation, myristicin production enhancement, and comparative GC-MS analysis of the n-hexane extracts of different organs of Daucus pumilus (Gouan), family Apiaceae. Journal of Pharmacy & Bioallied Sciences 12(3), 324-334. * Oral Presenting author - 31 -
The 1st international ZPSC 2021 Poster Presentation - 32 -
The 1st international ZPSC 2021 Macro- and micromorphological study of Salix tetrasperma Roxb. cultivated in Egypt Afaf El-Sayed, Assem El-Shazly, and Eman Fikry* Pharmacognosy Department, Faculty of Pharmacy, Zagazig University, 44519 Zagazig, Egypt Abstract In a previous study, the phytochemical investigation of Salix tetrasperma Roxb. (Salicaceae) resulted in the isolation of β-sitosterol acetate, friedelin, 3 β- friedelinol, β-amyrin, β-sitosterol, β-sitosterol-O- glucoside in addition to palmitic acid from the light petroleum fraction of the stem bark. From the dichloromethane fraction of the leaves, catechol and tremulacin were isolated. In addition, salicin and its derivatives tremuloidin and 2'-O-p-(E)- coumaroyl salicin were isolated from the ethyl acetate fraction of the leaves. Moreover, the total methanolic extract was evaluated for several biological activities since it revealed significant anti-inflammatory, antioxidant (DPPH free radical scavenging) and analgesic activities. The literature review showed no report concerning the macro- and micromorphology of the plant. Therefore, the present work covers the macro- and micromorphological investigation of Salix tetrasperma Roxb. With the aim of facilitating the identification of the characteristic features of the stem, leaves and flowers of the plant in both entire and powdered forms. * Poster Presenting author - 33 -
The 1st international ZPSC 2021 Pharmaceutics and Industrial Pharmacy Session - 34 -
The 1st international ZPSC 2021 Oral Presentation - 35 -
The 1st international ZPSC 2021 Enhancement The Hypolipidemic Effect of Atorvastatin Calcium Via Floating Microspheres Technique Marwa H. Abdallah1, 2, Al Zahraa G. Al Ashmawy1*, Hanan M. El Nahas1 1 Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt 2 Department of Pharmaceutics, College of Pharmacy, University of Hail, Hail 81442, Saudi Arabia Email: [email protected]. Abstract The purpose of this study was to investigate the influence of hypolipidemic atorvastatin calcium (ATC) floating microspheres on the LDL and HDL level in rabbit blood. Floating microspheres-loaded ATC were prepared by emulsion solvent evaporation method using Eudragit S100. The effect of certain factors including drug: polymer ratio, stirring rate, emulsifier concentration and internal: external phase volume ratio on the floating microspheres formulae were performed. Evaluation of floating microspheres was done using particle size analysis, percentage yield, in-vitro buoyancy, entrapment efficiency determination, optical microscopy, in-vitro drug release studies, Thermal analysis and Fourier transform infrared spectroscopy. The best formula prepared was (F5) which revealed the highest drug release % (66% up to 8 h) and significantly decrease the blood LDL and increase HDL than the market drug (ATOR ®) and it succeeded in lowering the rabbit's blood total cholesterol level by 74.42%. Key words: Atorvastatin calcium, Eudragit S100, floating microspheres, HDL, LDL and total lipid. * Oral Presenting author - 36 -
The 1st international ZPSC 2021 Poster Presentation - 37 -
The 1st international ZPSC 2021 Preparation and Characterization of Ivabradine HCl Transfersomes for Enhanced Transdermal Delivery Gehan F. Balata, Mennatullah M. Faisal*, Hanaa A. Elghamry, Shereen A. Sabry Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University Abstract Ivabradine HCl (IVB) is used in treatment of stable angina pectoris. The aim of the work was to prepare a once daily transdermal film of transfersomes loaded IVB. Transfersomes were prepared by modified ethanol injection method using three formulation factors namely: surfactant type, drug: phospholipid ratio and surfactant: phospholipid ratio. The transfersomes were characterized for entrapment efficiency, particle size, zeta potential, in vitro drug release, optical and transmission electron microscopy imaging, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The best transfersomes showed optimal properties as well as pure drug were further formulated in transdermal film and characterized for content uniformity, folding endurance, weight and thickness, moisture content, moisture uptake, tensile strength and permeation through excised ear rabbit skin. Pharmacokinetic parameters of transfersomes incorporated film were compared with oral solution of the same drug dose. A maximum of about 82.03% entrapment efficiency, size of 206.7 nm, zeta potential of -88.3 Mv and 66.7% of drug release after24h were obtained from sodium lauryl sulphate based transfersomes at drug : phospholipid and surfactant : phospholipid ratio of 1:20 and75:25 w/w, respectively. Films contained IVB transfersomes exhibited improved permeability and skin retention when compared with pure drug as well as enhanced pharmacokinetic parameters. * Poster Presenting author - 38 -
The 1st international ZPSC 2021 Transdermal Ethosomal Gel Nanocarriers - A Promising Strategy for Enhancement of Anti-Hypertensive Effect of Carvedilol Tarek M. Ibrahim1*, Marwa H. Abdallah1,2, Nagia A. El-Megrab1, Hanan M. El-Nahas1 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Egypt 2Department of Pharmaceutics, College of Pharmacy, Hail University, Hail, Kingdom of Saudi Arabia *Corresponding author e-mail address: [email protected] Abstract The current study was conducted to develop vesicular ethosomal gel (ethogel) systems for upgrading the transdermal delivery of the anti-hypertensive carvedilol. Ethosomes were prepared by thin-film hydration method with sonication. Carvedilol-loaded ethosomes were characterized by microscopic examinations followed by other in-vitro assessments. Selected ethosomal formulation (E10) was incorporated into different gelling agents to prepare the ethogel formulations followed by physicochemical characterization and in-vitro, ex-vivo and in-vivo release studies. The smooth ethosomes demonstrated vesicular size of 201.55–398.55 nm, entrapment efficiency of 30.00–90.66% with zeta potential range of -30.30 to -44.90 mV. The homogeneous ethogels exhibited appropriate results of pH (5.44–5.81) and drug content (96.80–99.77%) measurements. Spread ability was observed as a function of viscosity as the latter increased, the former decreased. In comparison to pure carvedilol gel, tested formulations (E10 and G2) developed high in-vitro drug release, ex-vivo permeation and drug retention through skin layers. The in-vivo study of G2 formulation revealed a significant gradual decline (p<0.01) in the mean arterial pressure of rats at the second hour of experiment (146.11mmHg) with continuous significant decrease (p<0.001) after 6 h (98.88mmHg). In conclusion, ethogels as promising lipid carriers proved their potential to enhance skin permeation with extended anti-hypertensive action of carvedilol. * Poster Presenting author - 39 -
The 1st international ZPSC 2021 Pharmacy Practice Session - 40 -
The 1st international ZPSC 2021 Oral Presentation - 41 -
The 1st international ZPSC 2021 Efficacy of sofosbuvir plus daclatasvir in treatment of Egyptian patients with chronic HCV infection: A prospective cohort study Nada R. Badawy1*, Hanaa A. El-Ghamry2, Nahla E. El-Gammal3 1Pharmacy Practice Department, Faculty of Pharmacy, Zagazig University, Egypt 2 Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Egypt 3Tropical Medicine Department, Faculty of Medicine, Zagazig University, Egypt Abstract Back ground and aims of the study: Chronic hepatitis C virus infection is a major health challenge in Egypt with high prevalence rate within the Egyptian population of different age groups. New DAAs in the past few years have proven to be highly effective in the treatment of HCV infection. This study aimed at evaluating the efficacy of a sofosbuvir-based treatment protocol composed of sofosbuvir plus daclatasvir with or without ribavirin in Egyptian patients with genotype 4 infection in Sharkia governorate. Patients and methods: One hundred patients were included in the study and divided into 3 groups; group I: 48 treatment-naïve patients without cirrhosis who received dual therapy (sofosbuvir+daclatasvir) for 12 weeks, group II: 32 treatment-naïve patients with cirrhosis who received triple therapy (sofosbuvir+daclatasvir+ribavirin) for 12 weeks, and groupIII: 20 chronic HCV patients, not receiving antiviral therapy as a control group. Patients were followed up thoroughly by clinical and laboratory evaluation monthly throughout the course of treatment and for 3 months after the end of treatment (EOT). In addition, the virological response for each patient was reported. Results: There was no statistically significant difference between the two groups that received treatment regarding virological response, since 100% of patients in both groups achieved SVR12 rates. Conclusion: The combination of sofosbuvir plus daclatasvir with or without ribavirin for a duration of 12 weeks is highly effective in the treatment of cirrhotic and non-cirrhotic naïve Egyptian patients with chronic HCV genotype 4 infection in Sharkia governorate. *Oral Presenting Author - 42 -
The 1st international ZPSC 2021 Poster Presentation - 43 -
The 1st international ZPSC 2021 High-Dose Dual Therapy versus Triple Therapy for Treatment of H. Pylori Infection: A Parallel Randomized Study Aya Ahmed1*, Gehan F. Balata1, Hany M. Elsadek2, Mohamed Nour EL-Din3, Ahmed Amin4 1Department of Pharmacy Practice, Faculty of Pharmacy Zagazig University, Zagazig, Egypt. 2Internal Medicine department, Faculty of Medicine Zagazig University, Zagazig, Egypt. 3Gastroenterology and tropical medicine department, Abu-Hammad Central Hospital, Abu- Hammad, Egypt. 4Department of Clinical Pharmacy, Faculty of Pharmacy Kafr El-Sheikh University, Kafr El- Sheikh, Egypt. Abstract Background & Aims: The prevalence of antibiotic resistance has considerably increased and as a result, the eradication rates for Helicobacter pylori (H. pylori) infection have decreased significantly to an unacceptable level. High dose dual therapy (HDDT) has been suggested as an alternative to standard triple therapy (TT) for the first-line treatment of H. pylori infection. The aim of the present study was to compare the effectiveness and tolerability of HDDT with standard TT, for treatment of H. pylori infection. Methods: This randomized parallel interventional study was carried out on 130 treatment naïve H. pylori infected patients, selected from outpatient clinic of Hepatology and Gastroenterology department of Zagazig University Hospitals, during the period between November 2017 and December 2018. All patients were H. pylori positive as was evidenced by stool antigen test. Patients were divided into two groups; group A (n=65) received a 14-day HDDT (esomeprazole 40 mg twice daily and amoxicillin 1 g three times daily) whereas group B (n=65) received a 14-day TT (esomeprazole 20 mg, amoxicillin 1 g and clarithromycin 500 mg, each administered twice daily). Eradication rates, drug compliance, and adverse events were compared among the two groups. Results: There was no significant difference in the eradication rate between the two regimens. The eradication rates were 80% for TT and 72.3% for HDDT (P= 0.3). There were no significant differences between both groups regarding the adverse events or patient adherence. Conclusion: HDDT is as effective and safe as TT as empiric first-line therapy for H. pylori infection. * Poster Presenting author - 44 -
The 1st international ZPSC 2021 Pharmaceutical Organic Chemistry Session - 45 -
The 1st international ZPSC 2021 Oral Presentation - 46 -
The 1st international ZPSC 2021 Design, synthesis, antimicrobial, and DNA gyrase inhibitory properties of fluoroquinolone–dichloroacetic acid hybrids Israa A. Seliem1,2*, Siva S. Panda1, Tarek S. Ibrahim2, Amany M. M. Al‐ Mahmoudy2, Zakaria K. M. Abdel‐samii2 1 Department of Chemistry and Physics, Augusta University, Augusta, GA, USA 2 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt Abstract A series of new fluoroquinolone conjugates 8a–g and 9a–f were synthesized via Benzotriazole‐mediated synthetic approach with good yield and purity. Some of the synthesized analogs exhibited significant antibacterial properties against Escherichia coli and Staphylococcus aureus with potency higher than that of the parent drugs through in vitro standard bioassay procedure (conjugates 8c and 8d reveal antimicrobial properties with potency 1.9, 61.9, 20.7 and 2.4, 37.1, 8.3 folds relative to the parent antibiotic 6 against E. coli, S. aureus, and Enterococcus faecalis, respectively). The observed experimental data were supported by enzymatic DNA gyrase inhibitory property. Developed BMLR‐ QSAR model validates the observed experimental data and recognizes the parameters responsible for the enhanced antibacterial properties. Published paper: Chem Biol Drug Des. 2020;95:248-259. doi:10.1111/cbdd.1363 * Oral Presenting author - 47 -
The 1st international ZPSC 2021 Poster Presentation - 48 -
The 1st international ZPSC 2021 Efficient Synthesis and Computational Studies of Useful Guanylating Agents: 1H-Benzotriazole-1-Carboximidamides. Riham M. Bokhtia,[a,b]* Siva S. Panda,[a] Adel S. Girgis,[c] Girinath G. Pillai,[d] Tarek S. Ibrahim,[b,e] ElSayed M. Shalaby,[f] Lara Gigli,[g] Eatedal H. Abdel-Aal,[b] and Amany M. M. Al-Mahmoudy[b] [a] Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, USA [b] Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt [c] Department of Pesticide Chemistry, National Research Centre, Dokki, Giza 12622, Egypt [d] Discovery Chemistry, Nyro Research, Kochi, Kerala 682021, India [e] Department of Pharmaceutical Chemistry, King Abdulaziz University, Jeddah 21589, Saudi Arabia [f] X-Ray Crystallography Lab., Physics Division, National Research Centre, Dokki, Giza 12622, Egypt [g] Elettra-Sincrotrone, Basovizza, Trieste 34149, Italy. Abstract A new synthetic protocol for the synthesis of 1H-benzotriazole1- carboximidamides starting from aryl amines in presence of acylbenzotriazole has been reported. The versatile guanylating agents could be an efficient synthetic tool for the synthesis of various guanidines. The present approach enables all possible variations of the substituents at different positions of the products. Single crystal of compound 4e was obtained by recrystallization from suitable solvent systems for X-ray and DFT studies. The reaction goes faster and yields more product with higher purity when Cbz protected aminoacyl benzotriazole used instead of aryl benzotriazole for the synthesis of the 1H-benzotriazole-1-carboximidamides. Computational studies were carried out to elucidate the energy profile and transition states to support the experimental data. Short reaction time, simple workup, high yields, and mild conditions are the key advantages of this protocol. Published paper: Med Chem (Los Angeles). 2020;16:1-14. doi:10.2174/1573406415666190904143852 * Poster Presenting author - 49 -
The 1st international ZPSC 2021 Synthesis of Imidazolidine‐2,4‐Dione and 2‐Thioxoimidazolidin‐4‐one Derivatives as Inhibitors of Virulence Factors Production in Pseudomonas aeruginosa Basant Mohamed1*, Zakaria K. Abdel‐Samii1, Eatedal H. Abdel‐Aal1, Hisham A. Abbas2, Moataz A. Shaldam3, Amany M. Ghanim1. 1Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University. 2Department of Microbiology and Immunology,Faculty of Pharmacy, Zagazig University 3Department of Pharmaceutical Chemistry,Faculty of Pharmacy, Kafrelsheikh University. Abstract In an attempt to counteract bacterial pathogenicity, a set of novel imidazolidine‐ 2,4‐dione and 2‐thioxoimidazolidin‐4‐one derivatives was synthesized and evaluated as inhibitors of bacterial virulence. The new compounds were characterized and screened for their effects on the expression of virulence factors of Pseudomonas aeruginosa, including protease, hemolysin, and pyocyanin. Imidazolidine‐2,4‐diones 4c, 4j showed complete inhibition of the protease enzyme, and they almost completely inhibited the production of hemolysin at 1/4 MIC (1/4 minimum inhibitory concentration; 1, 0.5 mg/ml, respectively). 2‐Thioxoimidazolidin‐4‐one derivative 7a exhibited the best inhibitory activity (96.4%) against pyocyanin production at 1 mg/ml (1/4 MIC). A docking study was preformed to explore the potential binding interactions with quorum‐sensing receptors (LasR and RhlR), which are responsible for the expression of virulence genes. Published paper: Arch Pharm (Weinheim). 2020;353(5):1-12. doi:10.1002/ardp.201900352 * Poster Presenting author - 50 -
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