Vol. 37, November, 2011.

ou acheter viagra a montreal 1/37 EFFECT OF CROSS LINKING TIME ON DRUG TARGETING

Hussein A. Sayed, Mamdouh M. Ghorab, Pierre A. Hanna and Shadeed Gad

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt.

Recently, alginates have shown great importance as an efficient tool for targeting drug at specific site of absorption. They were prepared by ionic gelation of sodium alginate polymer with divalent cation like calcium, zinc or magnesium. Calcium-cross linked alginate beads were prepared in this study by dripping the sodium alginate gel droplets into calcium chloride solution as a cross linker for a certain period of time and then dried overnight at room temperature. The finished beads were tested for percentage yield, hardness, percent drug load, encapsulation efficiency, swelling ratios, mucoadhesion and in vitro drug release. It was shown that increasing time of cross linking has lead to an increase in hardness and a decrease in percent drug load, encapsulation efficiency and drug release. It was shown also that an optimum percentage yield, hardness, percent drug load, encapsulation efficiency, swelling ratios and mucoadhesion properties were obtained using a period of 30 min suggesting that effect of cross linking time of alginate drops on finished alginate beads is time limited.

acheter viagra sans ordonnance à montreal 2/37 BIOCHEMICAL MARKERS IN SPONTANEOUS BACTERIAL PERITONITIS

Tarek M. Salman, Mohammed A. Ali*, Gamal A. Omran, Gamil M. Abdalla, and Ahmad M. Salahuddin**

Biochemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

* Hepatology, Gastroenterology and Infectious Diseases Department, Faculty of Medicine, Benha University, Benha, Egypt.

** Biochemistry Department, Faculty of Pharmacy, October University for Modern Sciences and Arts, 6th October, Egypt.

pharmacie en ligne andorre cialis Background: Spontaneous bacterial peritonitis (SBP) is a complication of liver cirrhosis and accounts for significant mortality. The diagnosis of SBP is based on a manual count of ascitic fluid of polymorphonuclear cells (PMN) ≥ 250 cells/mm³. This procedure is operator-dependent and lysis of PMNs during transport to the laboratory may lead to false-negative results. Furthermore, ascitic fluid culture is insensitive and leads to delays in diagnosis. Leukocyte esterase reagent strips (LERS) designed for the testing of urine was used in diagnosis of SBP, the sensitivity and specificity of this test is still controversial. Also, ascitic fluid lactoferrin could serve as a sensitive and specific diagnosis of SBP. levitra 20mg boite de 12 Aims: Conforming the sensitivity and specificity of lactoferrin and LERS for diagnosis of SBP and the assessment the utility of ascitic fluid myeloperoxidase (MPO) and neutrophil gelatinase associated lipocalin (NGAL) for diagnosis of SBP and to identify a cut-off level that can be used for future development of a rapid bedside test. trouve t'on du cialis en pharmacie Methods: These parameters were assayed in ascitic fluid samples aspirated from non-infected cirrhotic patients (n=30, mean age 58 years) and patients with SBP before and after treatment cefotaxime (2 g twice daily for 5 days) (n=21, mean age 56.1 years). combien coute le viagra a la pharmacie Results: The cut-off level of LERS at grade 3 (ca. 500 leukocyte/µL) has sensitivity, specificity, PPV and NPV for diagnosis of SBP at 90.48%, 93.5%, 90.4% and 93.5%. The area under the receiver operating characteristic curve was 0.92. Samples with SBP had a significantly higher concentrations of lactoferrin, MPO and NGAL (mean±SEM, 3435±534 ng/mL, 6329±861 ng/mL, 245±35.9 ng/mL respectively) in compared with sterile samples (mean±SEM, 143±26.2 ng/mL, 108±29 ng/mL, 10.6±4.84 ng/mL respectively) which decline significantly after treatment (mean±SEM, 201±62.3 ng/mL, 1218±402 ng/mL, 50±16.9 ng/mL respectively). The cut-off level of lactoferrin of 255 ng/mL has sensitivity, specificity, PPV and NPV for diagnosis of SBP at 100%, 90.3%, 87.5% and 100%, respectively. The area under the receiver operating characteristic curve was 0.98. The cut-off level of MPO of 1189 ng/mL has sensitivity, specificity, PPV and NPV for diagnosis of SBP at 100%. The area under the receiver operating characteristic curve was 1.00. The cut-off level of NGAL of 25 ng/mL has sensitivity, specificity, PPV and NPV for diagnosis of SBP at 100%, 90.3%, 87.5% and 100%, respectively. The area under the receiver operating characteristic curve was 0.98. médicaments generiques du viagra Conclusions: LERS,lactoferrin, MPO and NGAL can serve as a sensitive and specific test for diagnosis of SBP and a useful index in determining therapeutic response to antibiotic treatment.

est ce que le viagra est en vente libre en suisse 3/37 A NOVEL METHOD FOR SYNTHESIS OF TERTIARY BENZMIDES UTILIZING NBS

Ashraf Hassan Bayoumi

Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.

Synthetic access to tertiary benzamides via oxidation of viagra ultra puissant N,N-disubstituted benzylamine derivatives is presented as effective alternative to the classic acid-amine coupling reactions. The oxidation was accomplished in mild conditions using les indications du viagra N-bromosuccinimide (NBS).

4/37 ROLE OF FLAXSEED ON THE PANCREAS OF ADULT FEMALE ALBINO RATS FED ON HIGH FAT DIET (LIGHT, ELECTRON MICROSCOPIC AND IMMUNOHISTOCHEMICAL STUDIES)

Hekmat A.A. Sorour, Mona A. Salem and Dina A.A. Hassan

Histology Department, Faculty of Medicine for Girls, Al-Azhar University

Introduction:Feeding on high fatdiet )HFD( hasa wellknown aggravating factor in the pathogenesis of manydiseases including; renal diseases,coronary heart disease ,atherosclerosis, elevation of the bloodpressureand ectopic fat depositionsteatosis) in theliver, heart, muscles, and pancreas).Steatosisin pancreas is known also to be related to obesity and/or insulin resistance.A recent animal study reported that lipid deposition inpancreatic islet cells due tohigh fat diet could damage pancreatic beta cells and make them hyperglycemic.However, another study reported that there is no histological evidence of the existence ofsteatosisin the human. Manybiochemicalreports stated thatflaxseed (Linumusitatissimum)cansignificantly reduce levels of total cholesterol and low-density lipoproteins (LDL) andtriglyceridesandit hasanti-inflammatory, antioxidantandantidiabeticeffects .Aim of study: This study aimed to evaluate, histologically, imunohistochemically and ultrastructurally, the effect of high fat diet on the pancreas and the possible protective role of flaxseed on the pancreas when added to the high fat diet. Materials and methods: Thirty adult female albino rats were used in this study. They were divided equally into three groups. Group (I): Control group, that were fed on ordinary balanced diet. Group (II): High fat diet fed animals, that were fed on a HFD formula and Group (III): High fat diet and flaxseed fed animals, that were fed on the HFD formula containing ground or crushed flaxseed. At the end of the experiment which was 12 weeks, blood samples were taken from all animals to estimate total blood cholesterol and fasting blood sugar levels. The animals were sacrificed and specimens from pancreas were processed for light and electron microscopic and immunohistochemical studies. Results: HFD fed’s group revealed marked atrophied pancreatic acini with abnormal wide interlobular septa ,multiple intra-acinar vacuoles, inflammatory cells and thick fibrous connective tissue within pancreatic lobules. Multiple vacuoles were also observed in the islets of Langerhans. Immunohistochemical examination revealed intensive positive immunoreactivity for Fas in most acinar cells and marked reduction in the expression of insulin in β cells in pancreatic islets of Langerhans. Numerous lipid droplets, widening of rough endoplasmic reticulum, many nuclei with irregular outlines were commonly observed in the cytoplasm of serous cells of pancreatic acini under the electron microscope. Interestingly, light and electron microscopic examination and immunohistochemical reaction of group III showed nearly relieving of most of the morphological changes that were observed in group II to be more or less similar to the control group. Conclusion: flaxseed has the ability to ameliorate and protect the pancreas from the dangerous effect of HFD, thus we can advise adult females to use flaxseed in their diet.

5/37 THE ROLE OF IL-18AS AN IMMUNOMODULATOR IN HYPERSENSITIVITY REACTIONS AUTOIMMUNE DISEASES& ANTI-TUMOR IMMUNITY

Mona A. Shalaby, Hanan M. Elsayed, Mai M. Helmy and Enas A. Tantawy

Microbiology& Immunology Department, Faculty of Medicine, Zagazig University

IL-18 is a pleiotropic cytokine that has potent immunomodulatory effects. It is the only cytokine with a unique capacity to induce TH1 or TH2 polarization. It has been implicated in the pathogenesis of several immune mediated processes. The aim of this work was to assess the level of IL-18 in the serum of allergic, autoimmune and cancer patients (before & after treatment) and comparing these findings to the level in the control healthy persons to find a correlation between this finding and those diseases. This study was performed on two groups: Group I (Patient group): 80 patients; 40 hypersensitive patients, 20 patients suffering from autoimmune diseases and 20 cancer patients Group II (Control group): 40 healthy persons. History taking was taken from all members group. Blood sample was taken to measure serum level of IL-18 in patients (before & after treatment) and control groups by ELISA. The following were done for patients; hypersensitive patients (Intradermal skin test, Quantitative detection of serum total IgE by ELISA), autoimmune disease patients (Clinical examination, Autoantibody detection by latex agglutination tests), and for cancer patients (Clinical examination, Biopsy or fine needle aspiration, Tumor marker detection). The results of this study showed that greater percentage of female patients in hypersensitivity (65%) and autoimmune disease (90%) while in cancer group, the percentage of male patients was greater (75%). Statistically high significant increase in total IgE serum levels in hypersensitive patients compared to control group (P<0.001). 76.9% of Rheumatoid arthritis (RA) patients had rheumatoid factor and 71.4% of Systemic lupus erythematosus (S.L.E.) had anti ds- DNA antibodies. Positive tumor markers were detected in the blood of the studied cancer patient group; 60% of lung & 40% of head and neck cancer patients had Carcino Emberionic Antigen (CEA), The 2 patients of liver cancer (100%) had alpha feto-protein (AFP), and all breast cancer patients (100%) had Carbohydrate antigen (CA) 15-3. Highly significant increase in serum IL-18 level in all patient groups before treatment compared to control group (P<0.001). A strong positive correlation between the increase in total serum IgE in hypersensitive patients and serum IL-18 (r =0.47) with P<0.001. Also a positive correlation between serum autoantibodies in autoimmune disease patients and the high levels of IL-18 in their serum (r = 0.68), (P<0.001) but no significant correlation between IL-18 serum level and the presence of tumor markers in cancer patients (P>0.05). A comparison between the serum IL-18 levels in all patient groups before treatment and after treatment showed a statistically highly significant decrease compared to each other (P<0.001)٭٭, however the levels after treatment were still higher than those of the control group. In conclusion, our study showed a strong association between the high level of IL-18 in the study group and their disease conditions, which supports the role of IL-18 as an immunomodulator in these diseases and its determination in serum may find clinical applications in the follow-up of such diseases.

6/37 EFFECT OF INHALED BECLOMETHASONE, SALMETEROL AND IPRATROPIUM ON BRONCHIAL HYPERRESPONSIVENESS AND SOME INFLAMMATORY MEDIATORS IN ASTHMATICS

Osama M. Ibrahi, Mohamed Gamal A. El-Kholy*, Hoda A. El- Bahrawy** and Manal A. Selim

Department of Clinical Pharmacy, Faculty of Pharmacy, *Department of Chest Diseases, Faculty of Medicine, and **Department of Biochemistry, Faculty of Pharmacy, Tanta University, Tanta, Egypt.

Bronchial hyperresponsiveness (BHR) has been recognized as a hallmark of chronic asthma. Recently, the mainstay of asthma treatment has been shifted from treating the airflow obstruction to control the inflammatory process. The aim of this study is to evaluate the effects of corticosteroids, long acting β2 agonists (LABAs), and anticholinergics on BHR and some inflammatory mediators in asthmatic patients. Thirty patients were randomly distributed into three groups; each group was treated for four weeks by inhalation of one of the selected drugs. Spirometry and methacholine provocative test were carried out. Plasma histamine, blood serotonin, sputum eosinophil cationic protein (ECP) and nitric oxide (NO) metabolites were also measured. Patients treated with inhaled beclomethasone showed significant improvement in ventilatory functions, BHR and a significant decrease in almost all measured inflammatory mediators. Salmeterol showed improvement in forced expiratory volume in one second (FEV1) and BHR without any significant change in the measured inflammatory mediators. However, ipratropium showed no significant improvement in all measured parameters. The results recommend inhaled steroids as the first control drugs in asthma treatment. The inflammatory process associated with asthma can't be suppressed with LABAs or anticholinergics.

7/37 BIO-GUIDED ISOLATION OF ACETYLCHOLINESTERASE INHIBITORY ALKALOIDS FROM THE BULBS OF CRINUM BULBISPERMUM

Amina H. Abou-Donia, Eman A. Shawky, Mohamed M. Mohy El-Din,

*Hiromitsu Takayama and Ahmed A. Seif El Din

Pharmacognosy Department, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt

*Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, Japan

Inhibition of acetylcholinesterase (AChE), the key enzyme in the breakdown of acetylcholine, is considered as a promising strategy for the treatment of neurological disorders such as Alzheimer’s disease, senile dementia, ataxia and myasthenia gravis. A potential source of AChE inhibitors is certainly provided by the abundance of plants belonging to family Amaryllidaceae. In the present work, an In situ High Performance Thin Layer Chromatography (HPTLC) autobiographic method was employed for preliminary screening of extracts and fractions of the different organs of Crinum bulbispermumMilne-Redhead & Schweick. for compounds with AChE inhibitory effects. Among the tested fractions, the chloroform extract of Crinum bulbispermum bulbs demonstrated a significant inhibition of AChE in the assay. Complete phytochemical investigation of this biologically active extract resulted in the isolation of eight crystalline alkaloids (I-VIII) in addition to the well-known Amaryllidaceae alkaloid, lycorine.The structures of the isolated compounds were characterized by spectral evidence and by comparing the results with the reported physical and spectral data as ismine (I), trisphaeridine (II), latifine (III), 1-O-Acetyllycorine (IV), crinamine (V), powelline (VI), crinine (VII) and 1-epideacetylbowdensine (VIII). It is worth mentioning that this is the first report for the isolation of alkaloids I-IV and VIII from Crinum bulbispermum Milne-Redhead & Schweick.

8/37 ANALYSIS OF THE MECHANISMS OF RESISTANCE OF PSEUDOMONAS AERUGINOSA TO FLUOROQUINOLONES

Yousra I. Nagy, Abdel-Gawad M. Hashem, Yasser M. Ragab and Magdy Amin

Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, Cairo, Egypt

            The study was designed to investigate the mechanisms of resistance to fluoroquinolones in Pseudomonas aeruginosa clinical isolates and whether it is mainly attributed to alteration in target sites (gyrase and topoisomerase IV) or to other mechanisms. Accordingly a total of 103 isolates of Pseudomonas aeruginosa were recovered from sputum samples from four different hospitals located in Cairo. The MIC and resistance pattern of Pseudomonas aeruginosa isolates towards fluoroquinolones (ciprofloxacin, levofloxacin and gatifloxacin) was determined. Ciprofloxacin uptake by fluoroquinolone resistant Pseudomonas aeruginosa isolates was determined spectrophotometrically using the quinolone accumulation assay. Changes in QRDRs (Quinolone Resistance Determining Regions) of gyrA and parC genes were determined by PCR and DNA sequencing.The antibiotic susceptibility pattern of Pseudomonas aeruginosaisolates showed a significant cross-resistance to fluoroquinolones. The number of isolates that showed marked resistance to gatifloxacin was lower than those showing resistance against ciprofloxacin. Meanwhile, the magnitude of resistance towards ciprofloxacin was much lower than that towards gatifloxacin. The MIC results of the tested fluoroquinolones in the presence of efflux pump inhibitors (omeprazole and piperine) showed no clear effect. Interestingly, an increase in the MIC of ciprofloxacin, levofloxacin and gatifloxacin upon the use of sub-inhibitory concentrations of tetracycline and chloramphenicol was observed. On the other hand, there was a decrease in MIC of such fluoroquinolones upon the use of gentamicin. Mutations recorded in QRDRs cause alteration in the amino acid sequence of gyrA gene: Thr at position 83 to Ile, while the most predominant substitution in parC gene occurred at position 87 in which Ser is substituted by Leu. These results suggest that different elements and resistance mechanisms have a role in the overall resistance pattern of Pseudomonas aeruginosa to fluoroquinolones.

9/37 BACTERIOLOGICAL AND MOLECULAR STUDY ON ENTEROCOCCI CLINICALLY ISOLATED FROM ZAGAZIG UNIVERSITY HOSPITALS

Ahmed A. Shaheen, Lobna A.E. Mohammed, Mai M. Helmy and

Maher M. Elshafei

Microbiology and Immunology Department, Faculty of Medicine, Zagazig University

Many of the recent years reports have focused on the increasing interest in enterococci. Members of the genus Enterococcus beside their ability to cause serious infections like endocarditis, bacteremia, and intraabdominal infections, they also exhibited an increasing resistance to many antimicrobial agents. Hence the aim of this study was to determine the incidence; the antimicrobial susceptibility patterns of enterococcal isolates from patients at Zagazig University Hospitals, and study the vancomycin- resistance genotypes of the isolated enterococci. The present work included 900 patients suffering from various types of nosocomial infections scattered among the departments at Zagazig University Hospitals. Clinical data for all patients were documented. From these patients, 1101 clinical specimens were collected (urine, wound, blood, sputum specimens as well as tracheal aspirate and ear swabs). Specimens were cultivated on Enterococcus selective differential (ESD) medium where the growing colonies were identified for enterococci using classical tests (colonial morphology, Gram’s stain, catalase test, Sodium chloride test and API 20 Strep system). The susceptibility of isolated enterococci to antimicrobial agents was examined using disc diffusion method. The minimum inhibitory concentration (MIC) for vancomycin & teicoplanin was determined by E-test, and genotypic confirmation of vancomycin resistant enterococci (VRE) by PCR. The result of this study showed that: 58(5.3 %) out of 1101 samples were enterococci, of which 41(70.7 %) identified as E.faecalis &17 (29.3 %) as E.faecium. Out of the 58, 11 (19 %) Enterococcus isolates were VRE while the rest (81 %) were sensitive.VRE were significantly more sensitive to impenem (90.9%) &ampicillin +sulbactum (81.8%), while significantly more resistant to ciprofloxacin (90.9%). Previous antibiotic therapy (86.2 %) & prolonged hospitalization of more than 20 days (51.7%) were the most important risk factors associated with VRE in our study. Ten isolates of VRE were of vanA type (90.9%) by both E-test and PCR while one (9.1%) was negative by PCR for vanA and positive for vanB by E-test. In addition two vancomycin sensitive enterococci by E-test were VRE of vanA geneotype by PCR. The sensitivity, specificity, positive and negative predictive values of E-test in relation to vanA PCR were 83.3%, 97.8%, 90.9% and 95.7%; respectively. In conclusion; the molecular methods are significant tools superior to bacteriological ones in detecting the genotypes of vancomycin resistance.

10/37 EFFECTS OF EXERCISE ON CENTRAL AND PERIPHERAL CANNABINOID RECEPTOR -1 (CB-1) IN TYPE 2 DIABETIC RATS

Azza Saad Abdou and Maha Mostafa Attia

Department of Physiology, Medical Research Institute, Alexandria University, Alexandria, Egypt.

The endocannabinoid system modulates metabolic pathways through the actions of CB-1 receptors. However, its role in type 2 diabetes mellitus remains unclear. This study aimed to investigate central and peripheral CB -1 receptors in type 2 Diabetes mellitus rats and whether their modulation through moderate exercise could affect the associated cardiometabolic risk factors.Sixty adult albino male rats were divided into: control, obese and diabetic groups, each was subdivided into non exercised and exercised groups.Diabetes was induced by high fat diet and a single I.P dose of Streptozotocin (35mg/kg b.wt), exercise was performed by swimming 1 hour/day 5 days/ week for 4 weeks. Serum cardiometabolic risk factors (glucose, lipid profile, C –reactive protein (CRP), insulin and adiponectin) levels were determined. CB-1 receptor levels were assayed in Brain, liver and adipose tissues.Exercise demonstrated a significant decrease in all cardiometabolic risk factors. A significant increase was detected in brain CB-1 receptor while, a significant decrease was obtained in both liver and adipose tissue receptor levels in exercised as compared to non exercised groups.In both diabetic groups, a significant positive correlation was detected between liver, adipose tissue CB-1 receptors and all cardiometabolic risk factors. Furthermore, a negative correlations was noticed with HDL-C and adiponectin. Brain CB-1 receptors were also negatively associated with both liver and adipose tissue receptors.Data of the present work indicate the role of CB-1 receptors in the pathophysiology of diabetes mellitus and suggest that targeting peripheral tissue receptors could be a new therapeutic approach to counteract diabetes and the associated cardiometabolic risk.

11/37 FORMULATION AND EVALUATION OF TOPICAL FORMULATIONS OF NYSTATIN

Maha A. Marzouk, Amal A. Ammar, Manal K. Darwish, Heba A. El-Sayed

Department of Pharmaceutic and Industrial Pharmacy, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt

Nystatin is a polyene antifungal that is of particular interest because it exhibits remarkable action against a wide range of pathogenic and non-pathogenic yeast and fungi. Different topical gel formulations were prepared to improve the antifungal activity of nystatin with objectives of prolonging its action. Bases used were sodium carboxy methylcellulose (NaCMC), hydroxypropylmethylcellulose (HPMC), methyl cellulose (MC), carbopol 934 (cp) and poloxamer 407(polox). Characterization of nystatin and its gel bases, including solubility, partition coefficient, pH, rheolgical behavior and drug content was done. The drug shows a lipoid solubility, with a moderate aqueous solubility, suggesting it as a good candidate for topical application. The rhelogical properties measurements demonstrate thixotropic behaviors of the chosen gel formulations. In vitro release study was evaluated to investigate the ideal concentration of gel bases for best release, using an adaptation of the FDA paddle method (USP apparatus 2) as the base was held in position in the dissolution vessel by sandwiching it between a watch glass and an aluminium wire screen. The dissolution profile of the tested bases was determined over a 6-h period, and kinetic estimation was done. The optimal formulae were those containing carbopol gel bases, cp1% (100.2%), HPMC 3% (94.92%), NaCMC5% (91.78%), MC3% (61.27%) and poloxamer 407 gel bases that showed 100 % nystatin release after 1 hour. Finally it was concluded that nystatin could be used successfully as topical delivery system.

12/37 FORMULATION AND EVALUATION OF CHITOSAN BASED MUCOADHESIVE PROLONGED RELEASE GELS OF MITRONIDAZOLE FOR THE TREATMENT OF CHRONIC PERIODONTITIS.

Amal A. Ammar and   Fatma M. Rayan*2

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy (girls), Al Azhar University, Cairo, Egypt.

* Department of Diagnosis & Radiology, Al Azhar University, Cairo, Egypt.

The aim of this study was to design a mucoadhesive gel formulations containing chitosan for prolonged local delivery of metronidazol (MZ) at the injection site and thereby increasing its therapeutic efficacy to treat periodontitis. To prolong the gel retention time within the periodontal pocket, It was developed six binary polymeric formulations of chitosan with a thermosensitive in situ gelling as poloxamer 407(PL407), gelling agent as hydroxypropylmethylcellulose (HPMC), and the mucoadhesive polyacrylic acid polymer carbopol 934P (CB934P). The formulated gels were evaluated for clarity, drug content, surface pH, viscosity, antimicrobial susceptibility and in vitro drug release studies. An in vivo evaluation was performed to monitor the bacterial count and metronidazole concentrations in the gingival crevicular fluid (GCF) samples collected from periodontal pockets of patients treated with the different gel formulations. In vitro evaluation obviates that F7 containing 15% PL407 has encountered the advantages of having lowest viscosity value (91.6 cp) which could be beneficial of having higher syringeability, spreadability and significant release retardant effect with t1/2 (6.72days). In vivo evaluation of the different gel formulations showed a correlation coefficient of -0.86 between the viable bacterial count and the amount of drug retained in the GCF after 7 days of drug administration.

13/37 SYNTHESIS OF SOME NEW THIOPYRIMIDINE DERIVATIVES AS ANTICANCER AGENTS

Omar A. Fathalla,Ali S. El-Sayed and *Emad S.I. Hassan

Department of Therapeutic Chemistry, Pharmaceutical and Drug Industries Division, National Research Centre, Giza, Egypt.

*Department of Organic Chemistry,Faculty of Science, Al-Azhar University, Cairo, Egypt.

A series of some new Thiopyrimidine derivatives was synthesized via the reaction of ethyl cyanoacetate with thiourea and the appropriate aldehydes namely, 3-methoxy-benzaldehyde, 2,5-dimethoxy-benzaldehyde and 3,5-dimethoxy-benzaldehyde to give The pyridine thiones 1a-c. Compounds 1a-c were chlorinated to give the chloro compounds 2a-c, then condensation of 2a-c via different reagents gave compounds 3-10. Also condensation of compounds 1a-c with monochloroacetic acid, different aldehydes to give 11-14. All structures of the new compounds were elucidated by their correct elemental analysis and spectral data. The anticancer activity of some of these compounds were studied.

14/37 ANTI-MICROBIAL ACTIVITIES OF MATRICARIA CHAMOMILLA L. FLOWER

Naglaa H.M. Hassanen and Gehad F.A. Fath El-bab*

Special Food and Nutrition Department, Food Technology Research Institute, Agricultural Researches Center, Giza, Egypt.

*Food Hygiene Department, Animal Health Research Institute, Dokki, Giza.

In an attempt for utilization of some common spices, Matricaria chamomilla is popular implementations because of their flavoring and antimicrobial activity which mainly comes from polyphenols. The aim of the study was to investigate the effect of spices or their essential oils compared with drug (gentamicin antibiotic) on the serum of induced Staphylococcus aureus rats by measuring the extent of infection damage as well as the status of the antimicrobial substaces defense system.A total number of ninety six young male Albino rats, average weight of 150±5 g were divided into sixteen groups and subjected to infection with Staphylococcus aureus micro-organism then treated with gentamicin antibiotic and Matricaria chamomilla essential oil as antimicrobial substances. The chemical components of Matricaria chamomilla essential oil fractionated and identified by GC/Mass technique. The antimicrobial effects of Matricaria chamomilla essential oil at concentrations of 0.1, 0.3, 0.6, 1, 10, 50 and 100% were determined in comparison with phenol, at concentration of 1.0 and 10%, against eleven bacterial strains and two yeast strains. The diameters of the inhibition zones (mm) were taken as a criterion for measuring the antimicrobial activity, in vitro of Matricaria chamomilla essential oil. Organoleptic evaluation of Matricaria chamomilla represented the mean scores and their statistical analysis indication for color, aroma, taste, texture and overall acceptability for biscuit treatments mixed with different concentrations of Matricaria chamomilla powders or their essential oils. The results indicated that there are no significant differences in the quality attributes. Gentamicin residues were appeared in both kidney and serum. The haematological data of staph infected rats and treated with Matricaria chamomilla essential oil and gentamicin were recorded. Administration of staph produced significant adverse effects on the liver functions and kidney functions of the rats, which is evidenced by a significant increase in the activities of ALT, AST, ALP and LDH enzymes and kidney functions (urea and creatinine) as compared with gentamicin infected rats. The histopathological effect due to addition of Matricaria chamomilla and injection of gentamicin were detected in liver, kidney and muscle tissues.

15/37 OMENTIN-1 LEVELS IN EGYPTIAN TYPE 2 DIABETES MELLITUS WITH AND WITHOUT CORONARY ARTERY DISEASE AND ITS RELATION TO ADIPONECTIN

Hanan Abdelmawgood and Fawkia Eissa *

Biochemistry Department, Faculty of Pharmacy (girls) and *Internal Medicine Department, Faculty of Medicine (girls), Al-Azhar University.

Recently, Omentin is a newly identified secretory protein that belong to the adipokine family, highly expressed in visceral adipose tissue relative to subcutaneous adipose tissue. In vitro studies have shown that omentin increases insulin signal transduction and enhancing insulin-stimulated glucose transport in isolated human adipocytes. Thus, omentin may play a paracrine or endocrine role in modulating insulin sensitivity. It has recently been characterized as a potent insulin-sensitizing adipokine and seem to be related to metabolic risk factors. There are few studies about obesity, diabetes mellitus, atherosclerosis and omentin-1 so, this study was designed to investigate whether the levels of omentin-1 and adiponectin are altered in Egyptian type 2 diabetes mellitus patients with and without coronary artery disease (CAD) and to evaluate the relationship of omentin-1 with adiponectin, IL-6, obesity, insulin resistance as well as other metabolic and anthropometric variables. After an overnight fasting,a single blood sample was obtained. The levels of omentin-1, adiponectin, IL-6 and insulin were measured in patients with type 2 diabetes mellitus with and without coronary artery disease together with matched healthy control subjects by enzyme-linked immunosorbent assay (ELISA), whereas glucose and lipid profile were measured using colorimetric enzymatic methods. Obesity was measured using waist circumference (WC) and body mass index (BMI). Insulin resistance was measured using Homeostasis Model Assessment-Insulin Resistance (HOMA-IR). Serum levels of omentin-1 and adiponectin were found to be significantly decreased in patients with type 2 diabetes mellitus (19.51 ± 2.44 ng/ml, 7.85 ± 0.5µg/ml respectively) and further decreased in type 2 diabetic patients with CAD (14.8 ± 2.88 ng/ml, 5.07 ± 0.4 µg/ml respectively) compared with healthy control subjects (23.68 ± 3.41 ng/ml, 10.8 ± 0.7 µg/ml respectively) at P < 0.0001. In addition, omentin-1 levels were found to be significantly correlated with BMI, insulin resistance and lipid profile. In conclusion, omentin-1 and adiponectin levels were significantly decreased in diabetic patients and further decreased in diabetic patients with coronary artery disease compared with healthy control subjects. Omentin-1 was negatively related to BMI, IL-6 and insulin resistance but was positively related toadiponectin in type 2 diabetic group. In the diabetic group with CAD there was a significant negative correlation between omentin-1 and LDL-c and T-Cholesterol but there was a significant positive correlation between omentin-1 and adiponectin and HDL-c. Finally, omentin-1 and adiponectin levels were significantly higher in female than male. The data may point toward a role of omentin-1 and adiponectin in insulin resistance and type 2 diabetes mellitus. The low levels of omentin-1 and adiponectin are closely linked with the presence of coronary artery disease and that omentin-1 and adiponectin serves as a novel biomarker for coronary artery disease.


16/37 SIDE EFFECT OF CARBAMAZEPINE (TEGRETOL) DRUG ON THE DEVELOPMENT OF OVARY OF THE ALBINO RAT.

Fawzyah Abdullah Al-Ghamdi, Badria Fathy Abd-Elmagid and Ahlam Harasani

Department of Zoology (embryology), Girls College of Education in Jeddah, King Abdul-Aziz University

This study concerned with the effect of Carbamazepine on the morphogenesis and histogenesis of the ovary of postnatal albino rat at (60) days old. In this study (30) mature albino rats were used, (20) female and (10) male. After mating, the pregnant mothers were divided equally to (4) groups: control group and (3) treated groups.tow acute groups, one single and the other repeated, also one chronic repeated group. The morphological studies include malformation effects, differences of weight and height were recorded. The ovaries was removed to be examined by histological studies. The results showed swelling of the abdominal part in most of the treated groups, differences of weight and height. The most affected group was that treated by two acute doses. The ovaries were small in size and also showed delayed of development. The graffian follicles were reduced, follicular cells were degenerated and, the apoptotic follicular cell were seen. We concluded that the effect was proportionality with repetition and also with the time of dose, the dose either before or during the sensitively period of the development of the ovary.

17/37 PHYTOCHEMICAL AND BIOLOGICAL STUDY OF RIPE FRUITS OF ZILLA SPINOZA PRANTL. FAMILY BRASSICACEAE

Mohamed Abdelghaffar Ashour

Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.

New sinnapic acid derivative, [p-(5-O-xylonyl-2-sulphate-1,4-lactone)-3,5-dimethoxycinnamoyl] glucoside (1), and four known phenolic compounds: sinapine (2), Quercetin 3-O- rutinoside (3), isorhamnetin 3-O- rutinoside (4) and Kaempferol 3-O- rutinoside (5), in addition to 1,2,3,4-Tetrahydro-β-carboline-3-carboxylic acid (6), were isolated for the first time from the fruits of Zilla spinoza Prantl. The structures of the compounds were elucidated using 1D and 2D NMR spectroscopy, IR, MS spectrometry. The antioxidant activity and total flavonoid contents have been determined for the fruits (siliques) of Zilla spinosa growing in Egypt. The EC50 of ripe fruits as antioxidant is 156 + 17 mg (dry weight). The total flavonoid content of the fruits [26 microgram quercetin equivalent/ gram powdered sample (µQE /g) ] is much lower than that of the total herb [83.2 µQE /g]. The LC50 of the total extract, methanolic and dichloromethane fractions as cytotoxic on brine shrimps were 3.5, 4.1 and 6.7 mg, respectively, while LC50 of compounds 3, 4 and 5 were 1.0, 1.05 and 1.14 mg, respectively.


18/37 COLORIMETRIC METHODS FOR THE QUANTITATIVE ESTIMATION OF LOMEFLOXACIN

Sawsan A. Abdel Razeq, Manal M. Fouad, Noha Yehya and Ahmed Ashour *

Analytical Chemistry Dept, Faculty of Pharmacy, Al-Azhar and Misr-International* Universities, Cairo, Egypt.

Four simple and sensitive spectrophotometric methods have been developedfor the determination of lomefloxacin in pure form and pharmaceutical formulations. The first method was based on the chelation of the drug with Fe(II) giving a yellowish chelate measured at 360 nm. The second involved the reaction of lomefloxacin with 3-methyl-2-benzothiazolinone in presence of Ce (IV) via an oxidative coupling mechanism to yield an orange- red colored product picked at 469 nm. The third one depend on coupling of the studied drug with 2,6-dichloro-quinone-4-chlorimide in presence of weak alkaline medium of sodium acetate through its electrophilic substitution yielding a purple colored product having a maximum at 517 nm. In the last method, the drug reacted with 1,2-naphthoquinone-4-sulphonate in presence of K2HPO4 yielding an orange red colored product measured at 460 nm. Moreover, the first method was proved to be a stability- indicating that could determine the intact drug in presence of up to about 36 % of its decarboxylated degradate. Variables affecting the reactions were carefully investigated and the conditions were optimized. Linear relationships were obtained over concentration ranges of 20-140, 20-120, 40-200 and 20-150 µg mL-1 for the four methods, respectively. The methods have been successfully applied to determine lomefloxacin in pharmaceutical formulations with mean recoveries of 99.13-102.98±1.07-1.15%. Results of analysis were validated, as per ICH and showed excellent agreement.

19/37 SYNTHESIS AND ANTICONVULSANT EVALUATION OF SOME NEW QUINOXALINONE DERIVATIVES

Ashraf Bayoumi, Adel Ghiaty, Ahmed El-Morsy, Hamada Abul-Khair and

Salwa Elmeligie*

Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

*Organic Chemistry Department, Faculty of Pharmacy, Cairo University.

This study involves the synthesis 1-ethyl-3-hydrazinylquinoxaline-2-(1H)-one (8), several novel thiosemicarbazides (9-10), Semicarbazide (11), and (1,2,4) triazolo(4,3-a)quinoxalin-4(5H)-ones 12-17 were synthesized. The structure of the synthesized compounds was confirmed by elemental analyses and spectral data (IR, 1H NMR, 13C NMR and Mass). All of the synthesized compounds were evaluated as anticonvulsant and the results were compared with Phenobarbitone sodium as a standard anticonvulsant. Compounds 14-17 showed moderate activity as anticonvulsants.


20/37 ISOLATION, BIOLOGICAL EVALUATION AND IDENTIFICATION OF BIOACTIVE METABOLITES FROM ASPERGILLUS FUMIGATUS

Mahmoud M. Elaasser, Marwa M. Abdel-Azi* and Sahar M. Radwan*

The Regional Center for Mycology & Biotechnology, Al-Azhar University

*Microbiology Department, Faculty of Pharmacy (for Girls), Al-Azhar University

The purpose of this study, part of our ongoing search for bioactive compounds from fungi, is to evaluate the antimicrobial, antiviral and antitumor activities of certain compound isolated from Aspergillus fumigatus. Eight liters of yeast extract sucrose broth medium were used for the biosynthesis of extracellular Aspergillus fumigatus secondary metabolites. The concentrated crude fungal extract was evaluated for its antimicrobial activity by using agar well diffusion method and exhibited an antibacterial activity against 91 % the tested bacteria (highly relevant bacterial clinical pathogens). Bacillis subtilis, Streptococcus pyogenes and Escherichia coli were the most sensitive while Micrococcus lutea and Pseudomonas aeruginosawere the lowest. Aspergillus niger, Candida albicans and Geotrichum candidum were the susceptible fungi. The filtrate was extracted either with ethyl acetate and chloroform: methanol (2:1, v/v) and then subjected to bioguided separation using column chromatography with reevaluation of each fraction till we find the active principle(s). This Aspergillus fumigatus extract was found to be a mixture of three main active components. The active ingredients were purified to three compounds and identified using FTIR, 1HNMR and EI-MS analyses. The first two were a yellow powder (Compound 1) and a white crystals present in minor proportion in this extract (Compound 2) obtained from chloroform/methanol fractionation. The third active compound (Compound 3) was purified as colorless oil through ethyl acetate bioguided fractionation. The purified compounds were then reevaluated for the antibacterial activity by determination of the minimal inhibitory concentrations (MICs) using the microdilution broth method.The antibacterial activities of the compound I exhibited good MIC values ranged from 12.5 to 50 µg/ml. Compound II and III showed high MIC values more than 100 µg/ml against all the tested bacterial isolates under this screening condition. Cell toxicity was monitored on vero cells. Weak cytotoxic effects were observed for compounds II & III toward vero cells with CC50 values more than 250 µg/ml, while compound I resulted in almost no CPE in vero cells. The antitumor activity was evaluated on four carcinoma cell lines namely; MCF-7, HCT, HeLa and HepG2 cells. Compound I significantly had potent antitumor activity against HepG2, HCT, MCF-7 and HeLa tumor cells, with IC50 of 12.4, 19.2, 8.6 and 24.1 µg/ml, respectively. Weak inhibitory activity to the carcinoma cell lines tested was detected for compound II and compound III. The antiviral activity was determined by cytopathic effect (CPE) inhibition assay. Compound 3 observed moderate antiviral activities against HSV-1 & HSV-2, while compound 1 exhibited weak antiviral activity against HSV-1 & HSV-2.


21/37 NEWAPPROACHFORTHETREATMENTOFHYPERTENSIONAND HYPERLIPIDEMIAUSINGOLEAEUROPAEAEXTRACT

HebaAliAbdel-AziMahmoud El-Ramly, *Mohamed E.A. Abdelrahim, **Khaled Mohamed Hosny, NadaFarag ElNaidany, ***SherifEl-Degwi

Clinical PharmacyDept., October University for Modern Sciences and Arts (MSA)

*Clinical Pharmacy Dept., Faculty of Pharmacy, Beni Suef University, Beni Suef, Egypt

**Pharmaceutics Dept., Faculty of Pharmacy, Beni Suef University, Beni Suef, Egypt

***Cardiovasculer Dept., Faculty of Medicine, Cairo University, Cairo, Egypt

Cardiovascular disorders(CVDs) as hyperlipidemia and hypertensionandthereby atherosclerosisarethenumberonecauseof deathgloballyAccordingtothe WorldHealthOrganization(WHO).Thepresentstudy aimedto explorethe effects ofoleuropeinonmetabolic syndromesas hyperlipidemiaand hypertension and subsequently atherosclerosistopave theway foritsuseasa safeandeffective antihyperlipidemic andantihypertensivedrug. Twentyeligiblemild hypertensive and\ormild hyperlipidimicpatientswere subjected. Threeblood sampleswerecollectedfromeach patient, before oleuropein administration (control group), after administration of oleuropein (500 mg twice daily) for 4 weeks and for 6 weeks. Theobtaineddatarevealedthatthereweresignificant decreases inserum TC,LDL,andTGsbutno significantchangeinserum HDL. Also, therewasamarkeddecreaseinboth systolic and diastolic blood pressure (SBPandDBP respectively).Inaddition, oleuropein treatmentresultedina markeddecreaseinserum malondialdehyde (MDA)but markedly increased the activity of superoxide dismutase (SOD) enzyme. Moreover, there wasnoalterationinthe tested liver enzymes. It could be concluded that Oleuropein can act as an antihyperlipidemicdrug and possesses anti-hypertensive activity.These effects may be mediated, at least in part, by its antioxidant and free radical scavenging abilities.

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