Vol. 33, July, 2010.

acheter tadalafil sans ordonnance 1/33 FORMULATION AND EVALUATION OF METRONIDAZOLE RECTAL SUPPOSITORIES

Shereen A. El-Adawy and Ghada E. Yassin

Pharmaceutical Department, Faculty of Pharmacy (girls), Al-Azhar University, Nasr City, Cairo Egypt.

The objective of the present study is to formulate and evaluate Metronidazole suppositories using different suppository bases and adjuvants. Suppositories (1g) containing 200mg of Metronidazole each were formulated by the moulding method in Witepsol (H15 and E75) and polyethylene glycol (PEG 1500 and 4000) suppository bases, using 5% of (Tween 80, sodium salicylate or methylcellulose) as adjuvants. The weight variation, setting time, solidification point, melting range of the   formulated Metronidazole suppositories disintegration time, crushing strength and drug content were estimated. Suppository base type and the incorporation of different adjuvants on the in vitro release characteristics of Metronidazole from suppositories were investigated. Accelerated stability testing was performed on the formulae of best release after 100 minutes. The results showed that the prepared Metronidazole suppositories complies with pharmacopieal requirements for weight variation, content uniformity, melting point and disintegration time, ease of molding, solidification time and resistance of crushing. The drug release from water-soluble base (polyethylene glycol) was significantly greater than that from lipophilic bases (Witepsol H15 and E75) (P <0.0001). Incorporation of different adjuvants to the formulated Metronidazole suppositiories (Tween 80, sodium salisylate or methylcellulose) at concentrations of 5% were prepared. Tween 80 and sodium salisylate can probably be used to formulate only immediate-release suppositories while methylcellulose can be useful for sustained-release Metronidazole suppositories. When these formulae inspected visually, the water soluble bases (polyethylene glycol) had no sign of instability, while oil soluble bases became too soft which indicate a sign of instabilityof instability.

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antidepresseurs et viagra 2/33 FORMULATION AND CHARACTERIZATION OF KETOTIFEN FUMARATE AS NIOSOMES IN AEROSOL

Esmail Ramadan, Mohamed I. Fetouh*, Thanaa Borg and Mona Arafa*

Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University and *Egyptian Russian University, Egypt

Niosomes, a nano vesicle entrapped with Ketotifen fumarate (KF), and delivered in aerosol has been prepared by Span 60 and cholesterol in molar ratios 3:1, 3:3, 3:5 using chloroform film method with sonication. Particle sizes, morphology of noisome vesicles were characterized using DSC, X-ray diffraction, TEM and SEM. The entrapment efficiency (EE %) and in-vitro release of KF niosomes were evaluated. Metered dose inhaler aerosols were formulated with selected niosomes ratio (3:3 w/w) by suspending niosomes equivalent to 20 mg KF in propellant H11using soya leicithin as suspending agent. The valve is inserted and crimped into place to obtain canisters weight varies from 22.3-23.8 g. Additional propellant H12 is added to obtain the desired pressure using Pamasol packaging line. The valve was subjected to leakage test, total number of puffs per container, weight per puff, delivered dose uniformity. Particle sizes of niosomal drug were estimated using Malvern mastersizer. The results showed that niosomes were exactly spherical in shape with particle size ranging between 2.3-5.7μm. EE is not more than 73% w/w KF. The release of drug from prepared niosomes after 8h was reached 70%w/w, 65%w/w, and 55%w/w for molar ratios 3:1, 3:3, 3:5 respectively. In addition, the leakage test of the prepared aerosols was not exceeding 4mg/ 3 days and the numbers of puffs were up to 200 puffs/can. Moreover the dose delivered per puff was 0.1 mg (20mg drug /can) and particle size ranges from 3.3-4.7μm. These results are offering a novel approach to respiratory delivery of KF by aerosol.

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qu'est ce que du kamagra 3/33 HISTOLOGICAL AND ULTRASTRUCTURAL STUDIES ON CORPUSCLES OF STANNIUS IN CATFISH (CLARIAS LAZERA)

Nora Ahmed Obaid Al-Kaabi

Department of Biology, Faculty of Science, Dammam University, Saudi Arabia

The present study was carried out on four mature male catfishes ( accoutumance au viagra Clarias lazera) and the specimens were processed for histological and ultrastructure studies. The corpuscles of Stannius in catfish are small oval endocrine glands located in the ventral surface dorsocaudally to the kidneys.The histological results revealed that two type of cells were observed, granulated cells which were PAS-positive and non granulated cells which were PAS-negative. Ultrastructurally there were three types of cells one contain numerous electron dense granules varied in size, with few vacuoles and numerous ribosomes. The second type is characterized by presence of more dark irregular granules, small shrunken nuclei, and strands of rough endoplasmic reticulum (RER). The third type is characterized by having numerous vacuoles which lead to cells to be exhausted in appearance.

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4/33 MOLECULAR DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY OF CERTAIN TRICYCLIC COMPOUNDS BASED ON THIENOPYRIMIDINE SCAFFOLD

Yasmine Mohamad, Mohamed M. Said, *Adel A. El-Gendy and

**Khaled A.M. Abouzid

Organic Chemistry Department, Faculty of Pharmacy, Suez Canal University,

*Organic Chemistry Department, Faculty of Pharmacy, Misr International University,

**Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University.

A series of novel tricyclic compounds based on thienopyrimidine scaffold was designed using drug discovery molecular modeling software. The best scoring compounds were synthesized and their biological evaluation as anticancer agents was performed on human breast cancer cell line (MCF-7). Most of the tested compounds exploited potent anticancer activity with IC50 values in the nanomolar range in particular, compound IVb which displayed the highest activity among the tested compounds with IC50 equal to 17.55 nmol.

 


5/33 MULTIDRUG RESISTANCE OF PSEUDOMONAS SPECIES IMPLICATED IN NOSOCOMIAL INFECTION IN MANSOURA HOSPITALS

Fathi A. Mansour, Mohamed T. Shaaban, *Hosam M. Hassan

and **Mohamed F. Kenawy

Botany Department, Faculty of Science, Mansoura University.

* Botany Department, Faculty of Science, Menoufiya University.

** Microbiology & Immunology Department, Faculty of Medicine, Mansoura University

Pseudomonas aeruginosa can cause a range of infections, from mild urinary tract infections to severe septicemia and bacterial pneumonia with mortality rates that may exceed 50%. The present study was conducted to detect the frequency of P.aeruginosa causing nosocomial infections in Mansoura hospitals with detection of different factors increase the risk of their acquisition. Also detection of strains that produce ESβLase enzyme as a major cause of treatment failure in hospital infected patients. Moreover, special emphasis was laid upon the detection of the presence ESβLase enzyme and to emphasize if the cell wall may be a cause of resistance beside the intracellular enzyme. Clinical samples were collected; regardless the type of infection and the sex of patients, this study was carried out over a period of 8 months from March 2009 to November 2009. Out of 500different clinical specimens collected from patients of different clinical wards, 88(15.1%) P.aeruginosa isolates were recovered. Urine was the commonest type of samples from which P.aeruginosa, followed by burn and wound exudates, and ear discharge specimens.

 

 

6/33 AGRO-INDUSTRIAL BY-PRODUCTS AS A PRODUCTIVE MEDIA FOR MEDICINALLY VALUABLE NATURAL PRODUCTS FROM ENDOPHYTIC FUNGI

Mohamed ashour1, Hany yahia2,3 and Peter Proksch4

1Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University,

2Department of Food Science and Nutrition, Faculty of Home Economics, Helwan University,

3Department of Food Science and Nutrition, College of Food and Agriculture Science, King Saud University

4Institut für Pharmazeutische Biologie und Biotechnologie, Heinrich-Heine-Universität

In this work, we propose the utilization of four different agro-industrial by-products, "sugarcane bagasse, corn-bran, wheat-bran, fenugreek straw" in comparison to the well known solid medium "cooked rice" without any supplemental additions as productive media for fungi-derived natural products. Endophytic fungi, "Alternaria alternate" derived from the Egyptian land-weed "Euphorbia helioscopia" was used as natural source for fungal isolation. alternariol (1), alternariol methyl ether (2) and tenuazonic acid (3) were isolatedand identified using different spectroscopic analysis including Mass spectrometry and one and two dimensional NMR analysis. Cytotoxic activities of (1) and (3) were confirmed through MTT-assay against mouse lymphoma cell, L1578Y. Antimicrobial activities were tested for the isolated compounds.

 

7/33 EFFECT OF RADIOFREQUENCY ABLATION OF CARDIAC ARRHYTHMIAS ON HUMAN PLASMA NERVE GROWTH FACTOR LEVELS

Ola Sayed M. Ali, *Gamal Shaaban, **Randa Ghanoum, ***Doaa Abdel Latef and ****Noha Amer

Biochemistry Department, Faculty of Pharmacy (Girls) Al Azhar University, Electrophysiology Laboratory and Emergency Department of National Heart Institute, Clinical Pathology National Heart Institute

Previous studies support that RF catheter ablation does not increase transcardiac NGF concentrations immediately after the procedure. However, the systemic NGF concentration increased significantly on postoperative days 1 to 3, suggesting that RF ablation resulted in increased NGF expression (Kangavari et al., 2006). The purpose of this study was to test the hypothesis that venous NGF concentrations significantly increase on postoperative day 1 after RF catheter ablation by determining NGF concentrations in peripheral veins before, immediately after and postoperative day 1 after RF ablation in patients and to study the possible applications of determining NGF concentrations after RF catheter ablation. The current study was conducted on a total number of 30 cardiac arrhythmia patients who underwent diagnostic electrophysiologic study and RF ablation with mean age of 39.1 years. The patients were chosen randomly from those attending electrophysiology (EP) laboratory of National Heart Institute, Cairo, Egypt. 10 cardiac arrhythmia patients who underwent routine diagnostic electrophysiologic study without RF ablation matching the same age and socioeconomic status were taken as a control group. Venous blood was sampled from a peripheral vein before, after the procedure and again on postoperative day 1. The plasma samples were used to estimate the following parameters: routine laboratory investigations (which include fasting plasma glucose, kidney function tests (plasma urea & creatinine), total cholesterol, triglycerides, HDL- cholesterol, LDL- cholesterol) and plasma nerve growth factor (NGF). The mean fasting plasma glucose (FBG) level of the arrhythmia patients group was significantly higher than the mean FBG level of the control group at (P < 0.05). The mean plasma levels of total cholesterol and LDL-cholesterol in the arrhythmia patients group were significantly higher than those of the control group at (P < 0.001) .While the mean plasma level of HDL-cholesterol in the arrhythmia patients group was significantly lower than those of the control group at (P < 0.01).There was no significant difference of the mean plasma NGF levels before the operation to immediately after the operation (P > 0.05). However, NGF levels increased significantly from immediately after the operation to 1 day postoperation (P < 0.01).The mean plasma nerve growth factor (NGF) levels in the arrhythmia patients group before the operation and immediately after the operation were significantly higher than those of the control group at P < 0.05. Also, the mean plasma level of NGF in the arrhythmia patients group 1 day postoperation was significantly higher than those of the control group at P < 0.01. RF catheter ablation increases NGF concentrations on postoperative day 1 but not in all cases. Hypercholesterolemia and diabetes mellitus increase the risk of development cardiac arrhythmias.

 


8/33 MOLECULAR GENETIC CHARACTERIZATION OF FAMILIAL MEDITERRANEAN FEVER AMONG SAUDI CITIZEN

Mahmoud El Sayed and *Badr Al Jarallah

Departments of Biochemistry& *Internal Medicine, College of Medicine,

Al Qassim University,

Background: Familial Mediterranean Fever (FMF) which is an autosomal recessive condition that primarily affect population of the Mediterranean basin. If undiagnosed effectively and treated with colchicine for life it may lead to serious consequences in terms of renal amyloidosis and renal failure. Aim of the work:The purpose of this study is to use PCR technique for MEFV gene analysis in order to establish a diagnosis of FMF in symptomatic patients and to perform a preliminary population genetic study in clinically suspected cases among Saudi subjects in Al Qassim region, also as an important step for family counseling and case management.Subjects and Methods:The study is a pilot study to check for the presence of FMF mutations among suspected cases (24 cases) from Saudi subjects in Al Qassim region, The control subjects (7) were selected from healthy volunteers. We examined FMF mutations by PCR technique for MEFV gene analysis in order to establish a diagnosis of FMF by examining two mutations, M694V and E148Q. Results:We found 8.3% (2/24 cases)of cohort are positive for M694V mutation, and all cohort are negative for E148Q mutation . Moreover we found no correlation between clinical severity of the disease phenotype and the nature of the mutation.The normal controls were negative for previous two mutations.Conclusions: Genetic counseling by PCR technique provides a rapid, reliable, cost-effective, noninvasive, and sensitive test for establishing a diagnosis ofFMF in symptomatic patients. The study also provides a rational basis for medical andgenetic counseling of FMF patients and their families.

9/33 CHITOSAN-ALGINATE NANOPARTICLES AS A DRUG DELIVERY CARRIER FOR SULINDAC-CYCLODEXTRIN COMPLEXES

Hussein O. Ammar, *Soheir A. El-Nahhas, **Mamdouh M. Ghorab, Alaa H.Salama

Pharmaceutical Technology Department, National Research Center

*Pharmaceutics Department, Faculty of Pharmacy, October 6 University

**Pharmaceutics Department, Faculty of Pharmacy, Suez-Canal University

One of the most attractive areas of research in drug delivery today is the design of nanosystems that are able to deliver drugs to the right place, at appropriate times and at the right dosage. Chitosan (CS) has gained interest for nanoparticulate oral delivery systems due to its ability to reduce the transepithelial electrical resistance and transiety opening tight conjunctions between epithelial cells. Alginates (ALG) exhibit an easy gelling property induced by calcium ions. Chitosan has been used to combine with the alginate to prepare nanoparticles. The addition of chitosan, not only endows nanoparticles positive surface charge, but also prolong the time that the active ingredients contact with the epithelium and enhance absorption through the tight conjunctions. Cyclodextrin complexation has been thoroughly investigated for improving the unfavourable biopharmaceutical properties of drugs, such as poor solubility and/or stability. In the present study, two types of cyclodextrins, namely, β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were used to enhance the solubility of sulindac. Sulindac-CD complexes were entrapped in CS/ALG nanoparticles. The morphology of the prepared nanoparticles was elucidated via both transmission and scanning electron microscopy and particle size analysis was performed by photon correlation spectroscopy. Encapsulation efficiency, loading capacity, yield as well as the release properties of the prepared formulations were also assessed. The results revealed that the encapsulation efficiency increases with increasing cyclodextrin concentration. All formulations showed a significant drug burst release which amounts up to 64 and 81% for nanoparticles containing β-CD and HP-β-CD complexes, respectively. The anti-inflammatory effect of the prepared formulations were assessed in Wistar rats and compared with that of one of the marketed sulindac tablet products. Localized inflammation was induced by subplantar injection of 0.1 ml of 2% (v/v) formaldehyde solution into the left footpad of the rat’s hind paw. The initial paw size was then determined using a plethysmometer and the oedema volume was afterwards assessed at different time intervals. The pharmacodynamic parameters taken into consideration were tmax and area under percentage increase in oedema versus time curve. These parameters were computed using WinNonLin®software. The statistical analysis of the results revealed evident higher biological efficiency of the prepared nanoparticles compared to that of the market tablet product.

 

 

10/33 ENHANCING AVAILABILITY AND REDUCING ULCEROGENIC EFFECTS OF IBUPROFEN USING CYCLODEXTRIN AFTER ORAL AND RECTAL ADMINISTRATION

Fathy Ibrahim Abd-Allah

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy,

Al-Azhar University, Nasr City, Cairo, Egypt.

Improving solubility and consequently bioavailability of ibuprofen a poorly water soluble non steroidal anti-inflammatory drug using cyclodextrin derivatives are a good objective. The formulation of such mixture in an oral route and in a suppository form to decrease the ulcerogenic activity of drug was of interest. Ibuprofen with β-cyclodextrin and HP-β-cyclodextrin were prepared by physical mixture and kneading method then characterized and evaluated to study solubility, dissolution and complexation. The incorporation of such drug polymer in Witepsol H15 and E75 enhance drug availability and decrease ulcerogenic activity comparable to oral route using rabbits were investigated. Results showed that remarkable improvement was observed in in-vitro drug profiles in water with drug binary mixture. Drug also showed improvement in in-vivo activity when administrated orally and rectally to rabbits as compared with ibuprofen alone. Moreover the gastric mucosa were not affected upon administration of drug-cyclodextrin suppositories, while minor gastric pitting accompanied with hyper plassia were observed with oral administration comparable to plain drug.

 

 


11/33 RADIOTHERAPY OF   PELVIC CANCER AND ITS EFFECT ON HEMOGLOBIN   STRUCTURE

.Aisha A. Saad-EL-Din-, Laila M. Anis* - Zinab H. Eltanahy**, Sozan N.El-Sayed** Samir A. Nouh. *** and. Hoda A. Froah *

Biophysics Dept. NCRRT, *Health Rad. Res. Dept., NCRRT., **Al-Azhar University (Girls) Physics Dept., and***Ain Shams University Physics Dept., National Centre for Radiation Research & Technology (NCRRT), Atomic Energy Authority, Nasr City, Cairo, Egypt.

Local g-irradiation of pelvic cancer patient caused different structure changes in hemoglobin (Hb). Hb X-ray diffraction (XRD) for patients has decreases in intensities value than -ve control (healthy), on radiotherapy at accumulated doses (45-50Gy) 5 fractions/ week for 5 weeks. This indicates a decrease in crystalline phase. TheFourier Transform Infrared Spectroscopy (FTIR) Hb. spectra showed that cancer patients suffer from some destruction in all amide groups, indicated by decreases in absorbance. On local pelvic g-irradiation at the accumulative doses (24, 20&18 Gy), there were more destructive effect in all amide groups. At the end of radiotherapy, there was more increase in absorbance which indicates some sort of repair. All patients hemoglobin viscosity have been increased compared to healthy. So, we can conclude that on radiotherapy hemoglobin viscosity has been more increased compared to both healthy and patients. Also, the numbers of free radicals of Hb in patients have been increased as a result of radiotherapy. Furthermore, UV-Visible spectra measurements indicated that globin-heme bond has been stretched in patients. Interestingly, at the end of radiotherapy there was some sort of repair.

12/33 FORMULATION AND EVALUATION OF AMLODIPINE BESYLATE FAST DISSOLVING TABLETS

Ahmed Abdel Bary*, Omneya M. Khowessah* and Mugahed M. Al-Gamrah

*Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El Aini street, Egypt.

Amlodipine besylate is an antihypertensive drug of dihydropyridine calcium channel blocker class, administered orally as a long acting antihypertensive agent that is used in the treatment of acute and chronic hypertension and as prophylactic treatment of angina pectoris. Fast-dissolving tablets (FDTs) of amlodipine besylate were prepared bydirect-compression method. Nine formulaehaving three subliming agents at three different concentration levels were prepared to assess the most efficient and critical concentration level. Twelve formulaehavingthree subliming agents at the predetermined level and two superdisintegrants at two different concentration levels were prepared to assess the efficiency of superdisintegrants and their critical concentration level. Six formulaehavingthree subliming agents at the most efficient level and coprocessed superdisintegrant at different concentrations levels were prepared to assess the efficiency of coprocessed superdisintegrants and its critical concentration level. The prepared tablets were evaluated with respect to their shape, size, organoleptic properties, drug content uniformity, weight variation, mechanical strength, water absorption ratio, wetting time, dissolution behavior and disintegration time. All the prepared powder blends showed passable to excellent flowability. The prepared tablets were of acceptable drug content and weight variation according to USP specifications. Tablets containing Camphor (15%) and Ac- Di- Sol (8%) showed superior organoleptic properties, mechanical properties, water absorption ratio, wetting time, along with excellent in-vivo disintegration time and drug release, as compared to other formulae.

 

 

13/33 TANNIN AND FLAVONOID COMPOUNDS FROM CASSIA BREWSTERI GROWING IN EGYPT

Mohamed A. Selim, Abdel-Rhman O. El Shabrawy, *Sameh F.S. Abou Zeid

and *Asmaa I.I. Owis

FROM

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

*Pharmacognosy Department, Faculty of Pharmacy, Beni-Seuf University,

Beni-Seuf, Egypt.

Three known tannin compounds were isolated for the first time from the acetone (70% in water) extract of the seeds of Cassia brewsteri (F. Muell.) Benth., Family Fabaceae and were identified by chemical and spectroscopic examination as; epiafzelechin-(4β→8, 2β→O→7)- afzelechin (geranin A) 1, (-)- epiafzelechin 2 and guibourtinidol-(4β→8)- epiafzelechin 3. Tannin content of the seeds, leaves and stems extracts were found to be the highest in seeds (8.75g%) followed by leaves (6.25g %) and stems (3.75g%) when determined gravimetrically.Four known flavonoid compounds were isolated for the first time from the ethyl acetate extract of the leaves and were identified by chemical and spectroscopic examination as; quercetin 4, kaempferol-3-O-β-D-glucoside (astragalin) 5, quercetin-3-O-α-L-rhamnosy(l→6)β-D-glucoside (rutin) 6, kaempferol-3-O-rutinoside 7. Flavonoid content in the seeds, leaves and stems were found to be highest in leaves (1.013g%), followed by stems (0.226 g%), and seeds (0.155 g%).

14/33 RADIOPROTECTIVE EFFECTS OF GARLIC AND MELATONIN ON ANTIOXIDANT BIOMARKERS AND BLOOD VISCOSITY IN RATS

Aisha A. Saad-El-Din and Laila M. Anis*

Radiation Physics Department and *Health Radiation Research Department, National Center for Radiation Research and Technology (NCRRT), Cairo, Egypt

The development of radioprotective agents has been the subject of intense research in view of their potential for use within a radiation environment, such as space exploration, radiotherapy and even nuclear war. However, no ideal, safe synthetic radioprotectors are available to date, so the search for alternative natural sources has been on going for several decades. For this purpose, male albino rats of 6-8 weeks age were examined by orally giving them garlic extract (500 mg/Kg body weight/day), or melatonin (20 mg/Kg body weight/day)for 5 consecutive days. Thereafter the rats wereirradiated by 4 grays, 2 hours after the final feeding. Animals were sacrificed 1st, 3rd, 7th and 10th days post-irradiation. The data revealed significant decreases of reduced glutathione (GSH), glutathione peroxidase (GSH-Px) and superoxide dismutase (SOD) activities along with significant increase of malondialdehyde (MDA) levels in blood at different times after irradiation. Moreover, both garlic and melatonin administrations ameliorated the changes in these parameters in addition to reducing blood viscosity. Garlic decreased plasma Na+ and K+ concentration significantly, while melatonin caused significant decrease in K+ only. Na+/ K+ ratio was significantly increased by administration of both garlic and melatonin. Both garlic and melatonin administrations ameliorated the changes in these parameters. Whole body γ-irradiation of rats (4Gy) caused significant decrease in blood viscosity at different shear rate (100-350 sec-1) after (1, 3,7and 10 days); also the calculated plastic viscosity was decreased. Na+ concentration significantly increased at all time post irradiation, while K+ concentration decreased at the 1st and 3rd days and increased at the 7th day. Therefore, administration of garlic before γ-irradiation exerted a good protection in the 1st and 10th days for blood viscosity and the 1st and 7th days for both Na+ and K+ concentration.Meanwhile melatonin ameliorated the radiation effects at the 1st, 3rd and 7th day for blood viscosity and at the all time post treatments for plasma Na+ and K+ concentration. Na+/ K+ ratio was ameliorated for both garlic and melatonin. It is thus concluded that garlic and melatonin administered prior to irradiation may protect against the damage produced by radiation by the up-regulation of antioxidant enzymes and by scavenging free radicals generated by ionizing radiation.

 

 

15/33 SYNTHESIS AND ANTIMICROBIAL EVALUATION OF CERTAIN PYRIDIN-2-ONE, THIOPHENE AND THIAZOLINE-2-THIONE DERIVATIVES

Hend M. El-Sehrawi

Pharmaceutical Chemistry Department, Faculty of Pharmacy (Girls),

Al-Azhar University, Cairo, Egypt.

Cyano-acetic acid hydrazide was employed for preparation of novel heterocyclic compounds with potential antimicrobial activity such as coumarine, pyridin-2-ones, thiophenes and thiazoline-2-thione. In-vitro antimicrobial screenings of the synthesized compounds were measured. 5-Acetylthiophen,VIc showed promising broad-spectrum antimicrobial agent (MIC=64.5-500 ug/ml).

 

16/33 IMMUNOLOGICAL RECOVERY AFTER ALLOGENEIC BONE MARROW TRANSPLANTATION AND INTERFERON ALPHA TREATMENT IN IRRADIATED RATS.

Maha G. Soliman*, Omaima M. Ashry**, Elham M. Hussein**

and Yasmine H. Abd El-Naby

*Zoology Department, Faculty of Science, Al-Azhar University for Girls **Radiation Biology Department, National Center for Radiation Research and Technology.

This work was conducted to point out the influence of the biological response modifiers namely interferon alpha (IFN-α) and bone marrow transplantation (BMT) on boosting the immunological response and protection from oxidative stress in irradiated rats. Bone marrow cells were given to male rats, 3 hours post gamma irradiation at the dose level 5Gy. Those were injected subcutaneously with 10 units of IFN-α weekly for 5 weeks. The results revealed that total body irradiation (TBI) caused a significant decrease in all the investigated blood parameters, GSH as well as bone marrow lymphocyte count and viability. Related to immunological data, tumor necrosis factor alpha (TNF-α) and interleukin 2 (IL-2) also recorded a significant depression while lipid peroxidation was conversely elevated. Most of the investigated parameters, WBCs, RBCs, Hb, Hct, lymphocytes and GSH in irradiated animals receiving BMT and IFN-α, were significantly elevated, while MDA was significantly depressed as compared with the irradiated group. Bone marrow lymphocytic count and viability percentage were significantly increased while IL-2 and TNF-α were normalized. The curative action of IFN-α enforcing significant innate response could trigger and augment adaptive immune response by bone marrow transplantation. Such therapies boosting both components of immunity would be considered a potential strategy for irradiation treatment.

 

17/33 SYNTHESIS AND ANXIOLYTIC ACTIVITY OF CERTAIN   5-OXO-1, 4-OXAZEPINE DERIVATIVES

Bothina A. Mosa, *Maha M. A. Khalifa, *Hend M. El Sehrawi, *Eman A. H. Fayed, **Ashraf H. Bayomi and *Makarim Saeid

Organic Chemistry Departement, Faculty of Pharmacy, Cairo University.

*Pharmaceutical Chemistry Departement and ** Organic Chemistry Departement, Faculty of Pharmacy (Girls and Boys), Al-Azhar University, Cairo, Egypt.

A novel synthetic procedure for a series of 4-Aryl-3-phenyl-6,7,8,9-tetrahydro- benzothieno[3,2-f][1,4]oxazepin-5(4H)-one 8a-s derivatives had been described. Six compounds 8a,b,h,j,m,s were selected and submitted to pharmacological evaluation for anxiolytic activity in the open field test. All the test compounds except 8b significantly reduced the exploratory activity and the emotionality of the rats in the open-field. These inhibitory results are in agreement with the effect of reference standard chlorpromazine as a tranquillizer and anxiolytic in the same conditions.

 

 

18/33 SYNTHESIS, ANXIOLYTIC ACTIVITY AND ANTIMICROBIAL SCREENING OF SOME NOVEL 5-OXO-1,4-OXAZEPINE DERIVATIVES

Bothiana A. Abdel Fattah, *Hend El-Sehrawi, *Maha M.A. Khalifa, *Eman Fayed, **Ashraf Bayoumi and Makarem Said

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

*Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University (Girls), 11754, Cairo, Egypt.

**Department of Organic Chemistry, Faculty of Pharmacy, Al-Azhar University (boys), Cairo, Egypt.

A novel series of   4-aryl-3-phenyl-7,8-dihydro-6H-cyclopenta[4,5]thieno[3,2-f] [1,4]oxazepin-5(4H)ones have been synthesized and their structures were established by means of spectral data in addition to elemental analysis. Six compounds VI 1,2,8,10,13,19 were selected and submitted to pharmacological evaluation for anxiolytic activity in the open field test. Unfortunately, all test compounds were inactive. In addition, twelve compounds VI 1,5,7,9,10,13-19 were submitted to antibacterial and antifungal testing, among which compound VI 5 was found to be the most potent against the bacterial strains as well as a fungus used exerting its activity with the least MIC concentration, thus it could be a candidate for further investigation as a possible antimicrobial agent.

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