ORIGINAL_ARTICLE
SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL IODOPHTHALAZINEDIONE DERIVATIVES AS ANTICONVULSANT AGENTS
In view of their expected anticonvulsant activity, some new derivatives of phthalazine (I, II, IIIa-f, IV, V, VIa-f and VIIa-h) were designed and synthesized by condensation of Iodophthalic anhydride with hydrazine hydrate to produce iodophthalazindione I which heating with Alc. KOH to give compound II. The compounds IIIa-f resulted from condensation of compound II with different alkylcholoroacetates. Compound IIb reacted with ammonia, hydrazinehydrate and different alkyl amines resulted compounds IV, V (hydrazide) and VI respectively. Compound V (hydrazide) react with different aromatic aldehydes to produce compounds VIIa-h. the final compounds were structurally elucidated basis of IR , 1HNMR, Ms Carbon, hydrogen and nitrogen analysis. The final compounds were evaluated for anticonvulsant activity using pentylenetetrazole (ptz) to induce convulsion and phenobarbital as reference standard. The compounds I, II, IV, V, VIa, VIb, VIc, VId, VIf, VIIa, VIIb, VIIc and VIIgwere active than Phenobarbital as standard reference the remain compounds less active than Phenobarbital. To under stand the molecular significant of these results we compared the binding modes of these compounds.
Acknalewlgement: Many thanks for Dr. Ahmed Mansour assist. Prof. of pharmacology and Dr. Farg Sherbiny lecturer of organic chemistry
https://ajps.journals.ekb.eg/article_7146_492b48a4d48e96684bcf64c0711b52f5.pdf
2012-03-01
1
13
10.21608/ajps.2012.7146
phthalazine
phthalazinedione and anticonvulsant agent
Rezk
Ayyad
1
Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
COMPARATIVE STUDY ON THERAPEUTIC POTENTIAL OF CAFFEIC ACID AND SILYMARIN IN PARACETAMOL-INDUCED HEPATOTOXICITY: EFFECT ON HO-1, OXIDATIVE STRESS, HEPATIC INFLAMMATION AND NEUTROPHILS INFILTRATION
Paracetamol is a widely used analgesic and antipyretic drug, but at high doses it leads to undesirable side effects, mainly hepatotoxicity. The hepatoprotective effect of caffeic acid has been previously reported, however the mechanism of this protective effect is not fully explored. The current study aimed to investigate the therapeutic potential of caffeic acid vs. silymarin in paracetamol-induced hepatic damage. To better understand the mechanisms by which these phenolic compounds confer their protective effects, parameters of lipid peroxidation, hepatic inflammation and neutrophils infiltration were evaluated. In addition, liver toxicity markers and hepatic antioxidants (enzymatic as well as non-enzymatic) were measured.
Daily administration of paracetamol (700 mg/kg, p.o.) caused hepatic injury that was manifested as increased hepatic levels of malonaldehyde (MDA), tumor necrosis factor-alpha (TNF-α) and heme oxygenase (HO-1) with marked increase in myeloperoxidase (MPO) activity, depletion of liver reduced glutathione, and diminished catalase and super-oxide dismutase (SOD) activities. Furthermore, serum liver enzymes (ALT, AST, GGT) were significantly increased along with hepatocellular degeneration and steatosis. Co-treatment with caffeic acid or silymarin alleviated paracetamol-induced oxidative stress, blunted TNF-α levels and MPO activity, while enhanced HO-1 levels with restoration of antioxidant enzymes activities. This was accompanied by normalization of liver transaminases and improvement of hepatic architecture. Interestingly, the effect of caffeic acid on HO-1, TNF-α, and MPO was more prominent when compared to silymarin.
The present study provide an evidence on the multiple mechanisms by which caffeic acid as well as silymarin grant their hepatoprotective activities mainly through the induction of HO-1 in addition to the reduction of oxidative stress burden in hepatocytes. The powerful anti-oxidant effect was accompanied by a significant anti-inflammatory activity.
https://ajps.journals.ekb.eg/article_7147_e7ff1128c79db5c7e23fb18c64729112.pdf
2012-03-01
14
29
10.21608/ajps.2012.7147
Caffeic acid
Heme oxygenase-1
Hepatotoxicity
Oxidative Stress
Paracetamol
Silymarin
Mona
El-Azab
1
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt
AUTHOR
ORIGINAL_ARTICLE
THERAPEUTIC POTENTIAL OF SILYMARIN IN ACETAMINOPHEN-INDUCED NEPHROTOXICITY IN RATS
Acetaminophen (N-acetyl-p-aminophenol; APAP), a widely used analgesic and antipyretic drug, can cause life-threatening renal dysfunction. Factors which play a role in this toxicity are still ambiguous and no specific treatment was ascertained. The aim of this study was to investigate the potential protective role of silymarin to attenuate the nephrotoxicity induced by a single oral dose (3 g/kg) of APAP in rats. Four groups of Sprague-Dawley rats were used: control, silymarin, APAP and silymarin plus APAP-receiving animals. Interestingly, oral supplementation of silymarin (200 mg/kg/day) for nine days before APAP intoxication dramatically reduced APAP-induced nephrotoxicity as evidenced by measuring serum total protein, serum urea, creatinine clearance (Ccr) and urinary excretions of NAG (N-acetyl-β-D-glucosaminidase). Silymarin administration markedly prevented the generation of thiobarbituric acid reacting substances (TBARS) with substantial improvement in terms of reduced glutathione content (GSH) and activities of antioxidant enzymes in the kidney homogenates. Nitric oxide (NO) levels of urine and renal tissue were significantly inhibited in silymarin pre-treated animals. Furthermore, silymarin administration significantly inhibited the reduction of kidney content of adenosine triphosphate (ATP) parcels associated with this nephropathy. These results suggest that the protective role of silymarin in the prevention of APAP-induced nephrotoxicity in rats was associated with the decrease of oxidative and nitrosative stress in renal tissue as well as its capacity to improve the mitochondrial energy production. Thus, one could conclude that silymarin might be considered for the treatment of APAP-induced nephrotoxicity in rats. However, clinical studies are warranted to investigate such an effect in human subjects.
https://ajps.journals.ekb.eg/article_7148_512f33b486ac7b9fab90f8c3049fb3e3.pdf
2012-03-01
30
41
10.21608/ajps.2012.7148
Acetaminophen, Silymarin
Nephrotoxicity
Nitric oxide, Rat
Mohamed
Abd-Ellah
1
Pharmacology and Toxicology Department, College of Pharmacy, Al-Azhar University, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
SYNTHESES, ANTIMICROBIAL ACTIVITY AND MASS SPECTRAl INVESTIGATION OF SOME NEW THIOHYDANTOIN AND THIAZOLE DERIVATIVES.
5-(p-Tolyl)-2-[(p-tolylethylidene)hydrazino] thiazole (3) and 3-[(p-tolylethylidene )amino]-2-thiohydantoin (6) have been prepared via cyclization of p-methyl acetophenone thiosemicarbazone (2) with p-methylphenacyl bromide and ethyl chloroacetate in presence of fused sodium acetate . Acetylation of 2,3 and 6 with acetic anhydride afforded the corresponding diacetyl derivative(5) and mono acetyl derivatives (4 and 7). Reaction of 2-thiohydantoin (6) with thiophene-2-carboxaldhyde and chloroacetic acid gives 5-(thiophen-2-ylidene)-3-[(p-tolylethylidene)amino] -2-thiohydantoin (8) and 3-[(p- tolylethylidene )amino] -2-thiohydantoin-5-yl acetic acid (10) . The mass spectral fragmentation patterns of some prepared thiazole and 2-thiohydantoin derivatives have been investigated in order to elucidate the structure of the synthesized compounds. The prepared compounds also exhibited antimicrobial activity.
https://ajps.journals.ekb.eg/article_7150_e0f41bef94d6e4a1fd442285a0e791ca.pdf
2012-03-01
42
55
10.21608/ajps.2012.7150
haba
Abd El Hady
1
Chemistry Department, Faculty of Science (For Girls), Al –Azhar University Nasr City, Egypt.
AUTHOR
ORIGINAL_ARTICLE
MODULATORY EFFECTS OF L-CARNITINE ON TAMOXIFEN TOXICITY AND ONCOLYTIC ACTIVITY: IN VIVO STUDY
The aim of this study was to investigate the protective effect of L-carnitine (L-CAR) in tamoxifen (TAM)–induced toxicity and antitumor activity.Adult female rats were randomly divided into 4 groups. Group I was served as control, groups II and III were injected with (10mg/kg, P.O) TAM and L-CAR (300 mg /kg, i.p.) respectively while, group IV was treated with both compounds.The treatment continued daily for 28 days. Administration of TAM resulted in significant increase in serum lipid profiles, liver enzymes and bilirubin level. In addition, TAM produced significant increase in lipid peroxides (LPO) level accompanied with significant decrease in superoxide dismutase (SOD) activity of hepatic and uterus tissues and significant decrease in glutathione (GSH) content of uterus tissue. Administration of L-CAR prior to TAM treatment decreased significantly serum lipids and liver enzymes and significantly increased SOD activity in liver and uterus tissues compared to TAM treated group. Furthermore, it restored LPO and GSH levels in uterus tissue. On the other hand, the apoptotic markers of caspases 9 and 3 were not detected in liver of all the treated groups. Histopathologically, alterations in the liver and uterus structures after TAM treatment which was attenuated by L-CAR administration. The antitumor effect and survival of the combined treatment of Ehrlich Ascites Carcinoma (EAC)-bearing mice was less than each one alone. In addition, L-CAR interestingly increased survival rate of EAC-bearing mice more than TAM treated group. In conclusion, L-CAR has beneficial effects regarding TAM toxicity; however, it interferes with its antitumor effect.
https://ajps.journals.ekb.eg/article_7152_8a737349e59aeb2804aeb3c002e95e81.pdf
2012-03-01
56
73
10.21608/ajps.2012.7152
tamoxifen
L-carnitine
organ toxicity
antitumor activity
antioxidants
Amel
Ibrahim
1
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Helwan University, Egypt
AUTHOR
ORIGINAL_ARTICLE
PHARMACOLOGICAL STUDY OF PROTECTIVE EFFECT OF THYMOQUINONE IN A MODEL OF LUNG INJURY
Oxidative stress is caused by the imbalance between the production of reactive oxygen species and the body's ability to detoxify them or repair the resulting damage. Current evidence suggests that acute lung injury can lead to pulmonary fibrosis.Pulmonary fibrosis is a progressive and fatal interstitial pneumonitis with high mortality and limited successful treatment. The present study was designed to assess the protective effect of thymoquinone (TQ) and whether it can attenuate the severity of oxidative stress and inflammatory response during bleomycin (BLM) induced pulmonary fibrosis. Male albino rats were treated with either BLM and/orTQ. BLM significantly increased the levels of Lactate dehydrogenase (LDH), total protein and mucin in bronchoalveolar lavage fluid (BALF) and these effects were significantly ameliorated by TQ treatment. BLM also caused a significant elevation in the levels of lipid peroxides and nitric oxide (NO) accompanied with a significant decrease in the antioxidant enzyme activity of superoxide dismutase (SOD). TQ treatment restored these markers toward normal values. Moreover, histopathological examination confirmed the protective effect of TQ.
https://ajps.journals.ekb.eg/article_7153_6c3be8b1b988a754825e8b66148acf13.pdf
2012-03-01
74
85
10.21608/ajps.2012.7153
Lung injury – thymoquinone – oxidative stress – inflammation
Dalia
El-Khouly
1
Pharmacology & Toxicology Department, Faculty of Pharmacy, Future University, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
IMPROVEMENT OF THE BIOAVAILABILITY OF BUSPIRONE HCL USING INTRANASAL DELIVERY SYSTEMS
The purpose of the present study was to improve the bioavailability of buspirone hydrochloride using oil-in-water microemulsion, which was suggested to be suitable for intranasal delivery. Different pseudo-ternary phase diagrams were constructed to determine the microemulsion existing zone. The optimized microemulsion system was chosen. Different formulations were thus prepared and they were subsequently characterized for their polarized light microscopy, % transmittance, droplet size, and pH. An optimal microemulsion formulation consisting of 5% isopropyl myristate, 50% water, and 45% (w/w) surfactant/cosurfactant [Tween 80 30%, propylene glycol 15 % at 2: 1 weight ratio] was transparent with % transmittance 99.52 ± 0.43%, mean globule size 35.1 ± 0.5nm, and pH 6.4 ± 0.03, was thus selected for preparation of buspirone microemulsion formulation. Drug release was carried out using modified Franz diffusion cell. Various pharmacokinetic parameters including Cmax, tmax and AUC0-t were determined using Wister albino rats as the animal model. The absolute bioavailability (0–6 h) was 15.85% compared to the intravenous administration in rats, whereas the oral bioavailability of buspirone hydrochloride was 4%. The results confirmed that the suggested intranasal buspirone microemulsion formulations improved to a much promising extent its bioavailability.
https://ajps.journals.ekb.eg/article_7154_77740f480035dc809ee2460b2617c701.pdf
2012-03-01
86
102
10.21608/ajps.2012.7154
Intranasal delivery (IN)
Microemulsion (ME)
Buspirone Hydrochloride (BH)
bioavailability (BAV)
Hamza
Bshara
1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazamet El Wehda El Afrikia St., El Abbassia, Cairo, Egypt.
AUTHOR
ORIGINAL_ARTICLE
PREPARATION AND CHARACTERIZATION OF EUDRAGIT RS 100 MICROSPHERES CONTAINING CIPROFLOXACIN HYDROCHLORIDE
Controlled drug delivery systems have received considerable attention in the last years as they provide a more controlled drug concentration at site of action leading to an improvement in the therapeutic outcomes. In this study, ciprofloxacin hydrochloride (Cip. HCl) microspheres were prepared using Eudragit RS 100 polymer applying the emulsion solvent evaporation method. The drug polymer ratios were selected to be 1:2 and 1:3. Scanning electron microscopy (SEM), X-ray diffractometry (XRD) and differential scanning calorimetry (DSC) analysis were used to characterize the obtained microspheres as well as the yield percent (%) and drug content. The in-vitro release patterns and the antibacterial activity of the formulated microspheres were also investigated. It was found that drug release was retarded by increasing the amount of the polymer and X ray diffractometry verified that there was no interaction between the drug and polymer. The antibacterial activity of the drug was improved as indicated by the increase in the inhibition zone diameter of the microsphere formulation.
https://ajps.journals.ekb.eg/article_7155_e89db61301c0fb581f261b41e6629cf4.pdf
2012-03-01
103
112
10.21608/ajps.2012.7155
Khaled
Saleh
1
Department of Pharmaceutics and Industrial Pharmacy, Al Azhar University, Assiut
AUTHOR
ORIGINAL_ARTICLE
ISOLATION AND PARTIAL CHARACTERIZATION OF SALMONELLA PHAGE FROM MAROJARM PLANTS
Themarjoram plant is recorded as medicinal one, traditionally recommended as stimulant / tonic , and help to reduce the severity of asthma, indigestion, headache, rheumatism and toothache.
Results of this study showed high total count of contaminating bacteria in marjoram plants in non-packed samples collected from eight Egyptian governorates as compared with the pre-packed ones from two local companies. The presence of Bacillus sp. and E. coli, butnot Salmonella sp. are note-worthy.
One phage successfully infected Salmonella typhimurium was isolated using plaque assay which produced circular turbid plaques .The electron micrograph of negatively stained preparation indicated that the phage particles have hexagonal head (~80 nm) with short tail (~20 nm), which is classified to family Podoviridae. The biological characterization of the phage isolate is found to be : inactivation point at 62°C for 10 min., longevity in vitro for 72 hrs, dilution end point of 10-3 and stability for 1.5 hrs at pH 7.2.
https://ajps.journals.ekb.eg/article_7156_d11ea83d11b85480dde48f059ecfd066.pdf
2012-03-01
113
120
10.21608/ajps.2012.7156
Marjoram plants
microbial contamination
Salmonella phages
Eman
Marie
1
Virology Lab, Department of Agriculture Microbiology, Faculty of Agriculture, Ain Shams University, Shoubra El-Kheima, Cairo, Egypt.
AUTHOR
ORIGINAL_ARTICLE
EFFECT OF ALUMINUM, CADMIUM AND LEAD ON RAT LUNG: PROTECTIVE ROLE OF SELENIUM.
Adult male and female albino rats were treated orally with either sublethal doses of aluminum chloride, cadmium chloride or lead acetate alone or in combination with sublethal dose of sodium selenite. The rats were treated on alternate day for eight weeks and divided into eight groups of 5 rats each: control, (aluminum chloride 30 mg/kg bw, cadmium chloride 10 mg/kg bw and lead acetate 25 mg/kg bw) alone or in-combination with 0.4 mg/kg bw sodium selenite for each group. All animals were decapitated and lung tissues were dissected out, from each animal. Tissue samples were processed for light microscopical examination. Results showed that treatment with metals alone reduced rat body weight gain, and few rats died. There were many histopathological changes in the lung tissue of rats treated with metals alone such as, general impairment of the normal architectural organization of lung lobes and shredding of the bronchiolar epithelium cell with debris within its lumen and thickening of the interalveolar septa due to the inflammatory cells infiltrated of the alveolar walls. In some examined sections interalveolar septa ruptured forming large alveolar sacs as well as, hemorrhage and thick walled congested blood vessels. Many extrinsic allergic aveolitis were also seen in different areas of the pulmonary tissue. In some slides a lung abscess was seen and represented with a necrotic area and many pus cells. Administration of selenium concurrently with these metals ameliorated all the above adverse effects. In conclusion, Se has beneficial effects and could be able to antagonize Al, Cd and Pb toxicity on lung; effects that might be attributed to its antioxidant activity leading to scavenging free radicals.
https://ajps.journals.ekb.eg/article_7157_cfe70e43f8a65e6a26479e173f8be283.pdf
2012-03-01
121
136
10.21608/ajps.2012.7157
Heavy metals
Cadmium chloride, Lead acetate, and Aluminum chloride, Antioxidants
Sodium selenite, lung rats
El-Bamby
albambi
1
Environment and Bio-Agriculture, Department, Faculty of Agriculture Al-Azhar University, Cairo, Egypt.
AUTHOR
ORIGINAL_ARTICLE
IN VITRO AND IN VIVO EFFICIENCY OF EUPHORBIA ANTIQUORUM AS ANTIOXIDANT AND HEPATOPROTECTIVE AGAINST CCL4 – HEPATIC HAZARDS IN RATS.
The aqueous extract of the aerial parts of Euphorbia antiquorum (EA) Linn was evaluated for its in vitro antioxidant efficiency as well as in vivo hepatoprotective and antioxidant activity to validate its use in traditional therapeutic medications. The activity of different doses of EA extract ( at 20 ug ,40 ug, 60 ug, 80 ug and 100 ug/ml) exerted in vitro significant antioxidant activity as it caused reducing power, hydroxyl and superoxide anion radical scavenging activities and inhibition properties. The in vivo study was performed on 50 male and female albino rats from the animal house of National Organization for Drug Control and Research (NODCAR) weighing 150 - 250 grams. Normal animals were employed simultaneously with experimental groups. Rats were divided equally into five groups (G1 ) rats received saline as a normal for 4 weeks , (G 2) rats received orally CCl4 and were served as intoxicated control for 4 weeks,(G3) rats received both CCl4 and silymarin as a reference agent for 4 weeks ,(G4) rats received both CCl4 and EA (125 mg/kg b.w) for 4 weeks and (G5) received both CCl4 and EA (250 mg/kg b.w) for 4 weeks. It may be pointed out in the current study that antioxidant efficacy was reinforced by a significant hepatoprotection of EA (at 125 mg and 250 mg/kg b.w) displayed by decreasing the serum levels of alanine Transferase ( ALT), aspartate transferase (AST), alkaline phosphatase (ALP) , as well as bilirubin (total, conjugated and unconjugated) ,cholesterol, triglycerides (T.G), Total proteins (T.P), albumin ( Alb) and carbonyl protein (PC) after treated with carbon tetrachloride (CCl4), the two extracts also significantly increased lipid peroxidation (malondialdhyde MAD) levels of tissue in a dose dependant manner and increased superoxide anion radical (SOD), glutathione (GSH), glutathione peroxide (GPX), glutathione transferase (GST) levels. The antioxidant and hepatoprotective activities of the two test extracts where assessed in vivo and in vitro where either of the two test extracts or silymarin exhibited marked hepatoprotection against the toxic dose of CCL4. The results obtained pointed out that EA could be a potential source of natural antioxidant and hepatoprotection.
https://ajps.journals.ekb.eg/article_7158_714a3ca34e0f1b3a6f447a40d7559617.pdf
2012-03-01
137
154
10.21608/ajps.2012.7158
Mansour
Gait
1
Manger of Applied Research of Medicinal Plants (ARCMP) and Head of antibiotic Department National Organization for Drug Control and Research (NODCAR)
AUTHOR
ORIGINAL_ARTICLE
EFFICIENCY AND CHARACTERIZATION OF AN ANTIBACTERIAL SECONDARY METABOLITE FROM ZINGBER OFFICINALE AGAINST AEROMONAS HYDROPHILA CAUSING AEROMONAS SEPTICEMIA IN TILAPIA NILOTICA ( OREOCHROMIS NILOTICUS
This study was conducted to isolate and identify Aeromonas hydrophila which is the causative agent of motile Aeromonas septicemia MAS in freshwater fish (Oreochromis niloticus) and to study the efficacy and characterization of an antibacterial agent from Zingber officinaleagainst Aeromonas hydrophila in vitro which is causative agent of MAS.
This study was carried out using 100 O. niloticus weighting 80 ± 5 g Oreochromis niloticus were suffering from lose of appetite, lethargic, swim near the water surface, hemorrhage at the fins bases ulcer behind the head , roughness of scales (bristle out), slight distended abdomen and redness of anal opening. Internally the fish exhibited congestion of gills, liver, spleen, kidney and hemorrhage in peritoneal cavity, distended gall bladder, enlarged kidney and accumulation of serious fluid in abdominal cavity.
The bacteriological examination of the samples taken from clinically affected fish revealed the isolation of Aeromonas hydrophila . The incidence of infection in O. niloticus reach 58% .
The experimental infection with the isolated Aeromonas hydrophila intraperitoneally resulted in 90% mortality in O. niloticus . The antibiogram sensitivity test revealed that ciprofloxacin in a dose of 5mg was highly effective in control of Aeromonas hydrophila. The separation of the active ingredient and its purification was performed using both thin layer (TLC) and column chromatography techniques. The physico-chemical characteristics of the purified antibacterial agent viz. color, melting point, solubility, elemental analysis, spectroscopic characteristics and assay of total phenolics have been investigated.
An imperical formula ofZingber officinale a suggested empirical formula of C11 H19 O8N which was evaluated as an antibacterial agent against A. hydrophila organism.
https://ajps.journals.ekb.eg/article_7237_17436ad450fa92228500df5e4224b917.pdf
2012-03-01
155
168
10.21608/ajps.2012.7237
Bakry
Haroun
1
Botany and Microbiology Dep t.– Al Azhar University (Boys) Cairo. Chief Researcher of fish Health.
AUTHOR
ORIGINAL_ARTICLE
BACTERIAL INFECTION PROFILES AND TUMOR BIOMARKERS IN EGYPTIAN LUNG CANCER PATIENTS
A substantial number of bacterial pathogens have been putatively linked to cancer. In patients with lung cancer, pneumonia is the most important complication and has a high mortality. However, the common pathogens causing pneumonia are not clear. Also there is a need for identification of circulating tumor biomarkers by highly specific and accurate blood tests that can be performed at any medical facility. For these reasons the aim of the present study is identifying the major bacterial species present in sputum of lung cancer patients complaining from pneumonia and to measure the serum level of tumor markers with the assessment of their clinical significance. Methods: 60 patients diagnosed for lung cancer; 44 non small cell lung cancers (NSCLC) & 16 small cell lung cancers (SCLC); as well as 10 control normal healthy adults were included. The sputum of the patients & control were cultured on different culture media for identification of bacteria. Minimum Inhibitory Concentration (MIC) was determined by Microscan. The serums of the same candidates were analyzed for angiopoietin-2 (Ang-2), survivin, Carcinoembryonic antigen (CEA) and Neuron – specific enolase (NSE). Results: E. coli was isolated from 15 sputum samples, α or non hemolytic Streptococci were isolated from 43, Staphylococcus aureus was isolated from 3, K. pneumonia was isolated from 14, P. aeruginosa in 2, other bacteria in 9, Proteus mirabilis in 1, Acintobacter sp. in 2, Enterobacter cloacae in 2, Morganella morganii in 2, Serratia sp. in 1 and Candida in 3. The isolated bacteria showed multidrug resistance to the tested antibiotics.
Serum Ang-2 was significantly higher in SCLC and NSCLC groups as compared to normal group. Mean value of serum survivin was significantly higher in SCLC group as compared to normal and NSCLC groups. While there was no significant increase of serum survivin level in NSCLC group as compared to normal group. Mean value of serum NSE was significantly higher in SCLC group and NSCLC as compared to normal group. Serum NSE was higher in SCLC than in NSCLC group but the difference was not statistically significant. Mean value of serum CEA was significantly higher in SCLC group and NSCLC as compared to normal group. Also the mean value of serum CEA in NSCLC was significantly higher than the mean value of SCLC group. Conclusion: The spectrum of pulmonary infection in patients with lung cancer is wide and depends on the underlying neoplasm and the immunologic deficit or deficits related to it, and to various treatment modalities. The development of drug resistance among common respiratory pathogens is of great concern and underscores the need for the appropriate use of antimicrobial agents and the importance of infection control.
Serum survivin may be a useful marker in diagnosis of SCLC and also for differentiation between SCLC and NSCLC. Serum Ang-2 may be a good marker for lung cancer.
https://ajps.journals.ekb.eg/article_7238_d13cd21df255ce575e9aed4806f5f927.pdf
2012-03-01
169
180
10.21608/ajps.2012.7238
Omnia
Ismail
1
Biochemistry Dept., Faculty of Pharmacy, Egyptian Russian University
AUTHOR
ORIGINAL_ARTICLE
EFFECT OF SOME VITAMINS ON THE IONIC BALANCE AND PROTEIN PROFILES OF SALT- STRESSED FLAX SEEDLINGS
Theadverse effects of salinity on some physiological and biochemical responses of flax (Linum usitatissimum) seedlings grown at 100, 200, and 300 mM NaCl were studied. Salinity induced marked decreases percentage of germination, reduction in nucleic acids, as well as membrane stability index (MSI) of salinized flax seedlings. Data also revealed that salinized flax seedlings accumulated high levels of Na, Cl, P and Mgwhile Kand Caions were significantly decreased. Application of some vitamins (folic acid, ascorbic acid and cobalamin) counteracted the adverse effects of salinity. The mechanism of these vitamins on alleviating salt stress hazards might be mediated by stimulating the de novo synthesis of new set of low molecular weight proteins, reduction in some ions (Na and Cl) coupled with increases in the accumulation of others (K, Ca, P and Mg), consequently vitamins maintain high percentage of MSI throughout the experiment, thereby enhanced the capacity for germination under salt stress conditions
https://ajps.journals.ekb.eg/article_7239_77b6a35ad861a614fb6ea25e9e86d6b0.pdf
2012-03-01
181
197
10.21608/ajps.2012.7239
Flax
salinity
vitamins
Protein profile
membrane stability index
Manal
Emam
1
Botany Department, Faculty of Science, Ain Shams Univeristy, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
OPTIMIZATION OF NUTRIENT COMPOSITION MEDIUM AND CULTURE CONDITION FOR MANNANASE PRODUCTION BY BACILLUS VELEZENSIS NRC-1 USING TAGUCHI METHOD
The effect of different nutrient composition media on the production of mannanase by Bacillus velezensis NRC-1 was investigated. Medium 1 (composed of (g/L), peptone, 2.0; (NH4)2SO4, 1.5; MgSO4·7H2O, 0.5; K2HPO4, 10.0; locust bean gum, 10.0, urea and 0.3, pH 5.3) was found to be the most favorable medium for mannanase production which recorded, 2.19 U/mL, after 7 days of incubation at 30 ºC. Taguchi orthogonal array method was used for optimization of nutrient composition medium and culture condition for mannanase production. Eight nutrient factors were studied including peptone, ammonium sulphate, urea, magnesium sulphate, dihydrogen potassium phosphate, locust bean gum, pH and fermentation volume with three levels. Analysis of variance (ANOVA) revealed that peptone concentration, locust bean gum and pH of the medium were the most influencing factors with percent participation 19.25, 13.46 and 57.89%, respectively. An increase in mannanase production to 8.7 U/mL could be achived after the optimization process.
https://ajps.journals.ekb.eg/article_7240_19f1e126a006f17c952aee7a5be9ef3d.pdf
2012-03-01
198
207
10.21608/ajps.2012.7240
Bacillus velezensis
Taguchi Method
Mannanase
Tarek
Mazeed
1
Chemistry of Natural and Microbial Products Department, National Research Centre, Dokki, Giza 12622, Egypt.
AUTHOR
ORIGINAL_ARTICLE
PHYTOCHEMICL AND ANTIPROLIFERATIVE INVESTIGATIONS OF STRYCHNOS NUX-VOMICA LEAVES
There are no uses for the strychnine tree (Strychnos nux-vomica L.) in modern medicine although it was widely used in medicine before World War II. The properties of Nux Vomica are those of the alkaloid strychnine. Herein we investigated phytochemically the aqueous methanolic extract of the S. Nux vomica and isolated five phenolic compounds; Kaempferol-7 Glucoside 1, 7 hydroxy Coumarin 2, Quercetin-3-Rhamnoside 3, Kaempferol 3-rutinoside 4, and Rutin 5. At the same time, the cytotoxic activity of the extract was evaluated against different cancer cell lines. The extract showed potential cytotoxic activity against human epidermoid larynx carcinoma cells, with IC50 value 17.8 μg/mL. It also exhibited promising cytotoxic activity against breast carcinoma cell line (MCF-7) with IC50 36.3 μg/mL. Colon carcinoma cells were the least one affected by the extract as its IC50 was 41.2 μg/mL.
https://ajps.journals.ekb.eg/article_7241_4986f2e445fc925e8dcad46928c36cc2.pdf
2012-03-01
236
243
10.21608/ajps.2012.7241
Omayma
Eldahshan
1
Pharmacognosy Department, Faculty of Pharmacy, Ain shams University, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
THE PROGNOSTIC VALUE OF ANTI CITRULLINATED PROTEIN ANTIBODY TEST IN RHEUMATOID ARTHRITIS
Background: Rheumatoid arthritis (RA) is a chronic, systemic inflammatory disorder that may affect many tissues and organs, but principally attacks synovial joints. About 1% of the world's population is afflicted by rheumatoid arthritis, women three times more often than men. Onset is most frequent between the ages of 40 and 50, but any age group can be affected.
Aim of Work : To study the value of Anti cyclic citrullinated protein (Anti-CCP) test as a predictor of disease course, disability, prognosis and response to treatment in Rheumatoid arthritis patients of a specific age group with regard to history, clinical and radiological findings. The results for Anti-CCP will be compared to Rheumatoid factor test. Patients: 80 female cases were collected from rheumatology outpatient clinics, with disease duration of 3- 5 years and age range from 35 to 40 years Methods: All cases underwent thorough history taking, clinical examination, radiological and laboratory assessment as well as disability and health assessment scoring. Each patient will undergo a quantitative test of Anti cyclic citrullinated protein (Anti-CCP) and Rheumatoid factor. Results : Our study showed that there was high significant relation between positive and negative RF and Anti-CCP titres. (p=0.0000) for the patients in the studied group. There was a high significant correlation between Anti-CCP and RF titres (r=0.81, p<0.05)
Also there was a significant correlation between Anti-CCP and ACR disability class. In addition, there was a positive but not significant correlation between Anti-CCP and STLW score. (Clinical findings score- Swelling, Tenderness, limitation of movement, Warmth) and with VAS (Visual analogue scale) Conclusion: Our study found that Anti-CCP has a reasonably good prognostic value, especially as regards disability and functional status prediction. It also showed that Anti-CCP is very comparable to Rheumatoid factor when comparing prognostic values. It is only slightly more indicative in terms of clinical, radiological and health assesment.
https://ajps.journals.ekb.eg/article_7242_716e42f9b2d23201b49be41688935080.pdf
2012-03-01
253
264
10.21608/ajps.2012.7242
Rheumatoid Arthritis
anti-CCP
ACPA
Rheumatoid factor
prognosis
radiographic damage
Disability
functional status
Safwat
Araby
1
Al-Azhar University, Faculty of Medicine, Rheumatology, Physical Medicine and Rehabilitation department.
AUTHOR
ORIGINAL_ARTICLE
OPTIMIZATION OF AGITATION AND INCUBATION PERIOD ON PRODUCTION OF MANNANASE BY BACILLUS VELEZENSIS NRC-1 USING BENCH-SCALE BIOREACTOR
The effect of agitation speed and incubation period on the production of mannanase enzyme by Bacillus velezensis NRC-1 using bench-scale bioreactor at 45ºC was investigated. Results revealed that the increase in agitation speed from 200 to 800 rpm resulted in a significant increase in mannanase production to 21.04 U/mL. The increase in agitation speed affected dissolved oxygen (DO) concentration which in turn affected cell growth and mannanase production. The maximum mannanase production in the bioreactor was attained after 72 h of incubation at 45 ºC. Mannanase activity in the bioreactor (21.04 U/mL) while much higher than that obtained from the shake flask fermentation (15.6 U/mL) also the incubation period decreased from 7 days in shake flask fermentation to 3 days in bioreactor.
https://ajps.journals.ekb.eg/article_7243_0063cff6f4a8bc89093dc0e1d1cd6562.pdf
2012-03-01
265
273
10.21608/ajps.2012.7243
Bacillus velezensis
Mannanase
shaking
Bioreactor
Tarek
Mazeed
1
Chemistry of Natural and Microbial Products Department, National Research Centre, Dokki, Giza 12622, Egypt.
AUTHOR
ORIGINAL_ARTICLE
SYNTHESIS AND ANTICANCER ACTIVITY OF IMIDAZOLE DERIVATIVES INCORPORATING CHROMENE MOIETY
The oxo-chromene-6-carbaldehyde derivative 1 was used as a starting material for the synthesis of some novel pyrano[3,2-b] xanthene-4,7-dione 2 and chromen-oxazol-5-(4H)-one derivatives 4,5. Furthermore, the oxazolone derivative 4 was used as key intermediates to synthesize some novel imidazol derivatives 6-14. The structures of target compounds were confirmed by elemental analyses and spectral data. All the target compounds were subjected to in-vitro antitumor activity against breast and colon human tumor cell lines (MCF7 and HCT). Most of the screened compounds showed interesting cytotoxic activities compared to a reference drug.
https://ajps.journals.ekb.eg/article_7244_8e836ff1529fcd4ee820e117e192d5bd.pdf
2012-03-01
312
322
10.21608/ajps.2012.7244
Chromene
oxazolone
imidazole
antitumor activity
Nashwa
Saleh
1
Department of Chemistry, Faculty of Science (Girl’s), Al-Azhar University, Nasr City, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
DETECTION OF CIRCULATING HEPATITIS C VIRUS NON-STRUCTURAL PROTEIN IN CHRONIC HEPATITIS C VIRUS AND IN HAEMODIALYSIS PATIENTS
Infection with hepatitis C virus (HCV) is a major cause of chronic liver disease. On the other hand, Nosocomial transmission of HCV is a concern in haemodialysis (HD) units worldwide. In these patients, blood transfusions and long term dialysis are risk factors for transmission of HCV. Diagnosis of HCV infection is currently based on the detection of anti HCV antibodies by ELISA, and is confirmed by HCV RNA. The aim of the present study was to identify and detect the circulating non structural protein by using ELISA ,SDS-PAGE and Western blot techniques and to evaluate the usefulness of the detection of HCV antigen using ELISA for therapeutic follow-up (at 0 times, 12, 24 and 48 weeks) in selected 10 positive HCV-RNA patients at 0 times . Serum samples of 75 chronic hepatitis C (CHC) patients, serum samples of 75 haemodialysis patients and 25 healthy individual's sera as a negative control were included in this study. HCV antigen was detected in these samples using ELISA and Western blotting techniques. Western blot analysis showing a single immune reactive band in serum of CHC and haemodialysis patients infected with HCV at 27-KDa. ELISA technique was applied to detect the 27-KDa antigen. The cutoff level of ELISA above or below which the tested sera were considered positive or negative was calculated and was found to be 0.28 Based on this cut off the HCV antigen was detected in 80 % of CHC patients and in 36 % of haemodialysis patients. While, it was found that all healthy individuals used as a control were 100 % negative for HCV antigen. Furthermore, detection of HCV-RNA using nested PCR and HCV-NS4 antigen using ELISA for pre-therapeutic and therapeutic (combined interferon (IFN) and ribavirin therapy) at 0 time, 12, 24 and 48 weeks in 10 HCV-infected persons undergoing treatment was studied. The detection of HCV-NS4 antigen for these 10 positive HCV-RNA samples at (12 weeks and 24 weeks) showed that (60 %) were responsive for treatment and it was found that (40 %) did not respond.
https://ajps.journals.ekb.eg/article_7245_cb15cf15805ddb50fde516a9f5f91d46.pdf
2012-03-01
323
337
10.21608/ajps.2012.7245
HCV
Diagnosis
non-structural protein
detection
haemodialysis
Ahmed
Barakat
1
Microbiology department, Faculty of Science, Ain shams University, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
SYNTHESIS REACTIONS AND ANTIOXIDANT ACTIVITY OF SOME NEW HETEROCYCLES DERIVED FROM 2-ACETYLNAPHTHALENE
2-Methyl-4-(1-(naphthalen-2-yl)ethylidene)oxazol-5(4H)-one 2 was used as precursor for the preparation of some novel (1-(4-substituted)-2-methyl-4-(1-naphthalen-2-yl)ethylidene)-1H-imidazol-5(4H)-one derivatives 4a, b and other derivatives 3a,b, 5-12. Furthermore, the preparation of thieno[2,3-d]pyrimidin-4(3H)-one derivative 16,17 and 4-iminothieno[2,3-d] pyrimidin-3-ylamine derivative 18, 19 is described starting from 2-aminothiophen-3-carbonitrile derivative 15a. Some of the prepared products revealed a promising antioxidant activity by using 1,1-diphenyl-2,2-picryl hydrazyl free radical (DPPH) method.
https://ajps.journals.ekb.eg/article_7246_f8cce1eff8083f6cb8d07e59b3973797.pdf
2012-03-01
338
351
10.21608/ajps.2012.7246
Imidazoles
thienopyrimidines
Antioxidant activity
Nadia
Taha
1
Department of Chemistry, Faculty of Science (Girls), Al-Azhar University, Nasr City, Cairo, Egypt ABSTRACT :
AUTHOR
ORIGINAL_ARTICLE
SYNTHESIS, REACTIONS AND ANTITUMOR EVALUATION OF SOME POLYCONDENSED THIAZOLOPYRIMIDINE DERIVATIVES
Some novel thiazolo[3,2-a]pyrimidines, pyrimidino[1',2':3,2]thiazolo[4,5-b] pyridines,pyrimidino[1'',2'':3',2']thiazolo[4',5':2,3]pyrido-[2,3-d]pyrimidines, pyrimidino [1',2':3,2]thiazolo[4,5-d]pyrimidines, pyrimidino[1',2':3,2]thiazolo[4,5-d][1,2,4] triazolo[3,4-b]pyrimidines (2-10) were prepared starting with 2-(arylmethylene) trimethylthiazolo [3,2-a]pyrimidin-3-one(2). Also, some, S-alkylated thiazolo[4,5-d] pyrimidine derivatives were synthesized via reaction of 4-substited-7,7,9-trimethyl-1,3,4-trihydropyrimidino[1',2':3,2]thiazolo[4,5-d]pyrimidin-2-thione (6b) with different reagents. Furthermore, some of the prepared products were selected and tested for activity against HCT116 and MCF-7 (human colon carcinoma and human breast carcinoma).
https://ajps.journals.ekb.eg/article_7247_5d7b72697ce6127bb2fcf1af8d869097.pdf
2012-03-01
352
364
10.21608/ajps.2012.7247
Antitumor evaluation
thiazolopyrimidines
Triazolopyrimidines
Nermin
El-Seadawy
1
Department of Chemistry, Faculty of Science (Girls), Al-Azhar University, Nasr City, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
PROTECTIVE ROLE OF TELMISARTAN, CANDESARTAN AND OLMESARTAN ON COLD RESTRAINT STRESS -INDUCED GASTRIC ULCER IN RATS: INFLUENCE OF PPAR Γ MRNA
Certain angiotensin receptor blockers (ARBs) possess peroxisome proliferators activator receptor gamma (PPAR-γ) activating potency that correlates with their degree of lipophilicity. So, the present study was conducted to evaluate the gastro-protective effect of telmisartan; the well-established ARB with the highest lipophilicity; on cold-restraint stress (CRS) -induced gastric ulcer models in rats, in comparison with other ARBs (candesartan and olmesartan), to justify the possible role of PPAR-γ agonistic activity of ARBs in gastro-protection. Rats were assigned to sham control, cold-restraint stress, telmisartan, candesartan and olmesartan pre-treated groups (10 mg/kg each for 15 days). Pre-treatment with telmisartan, candesartan or olmesartan for 15 days induced elevation in PPAR-γ mRNA associated with an increase in the defensive factors by virtue of its ulcer score, antioxidant enzyme activities as well as the prostaglandin E2 (PGE2) level and a decreased in the aggressive factors like malondialdehyde (MDA), free acidity, pepsin, myeloperoxidase (MPO) activity and TNF-α level. Moreover, telmisartan provided superior gastroprotection to candesartan and olmesartan. In conclusion, telmisartan, candesartan and olmesartan could protect rats' gastric mucosa from CRS –induced ulcerations most possibly through its anti-oxidant activity, anti-secretory actions and enhanced mucosal protection. Activation of PPAR-γ might be one potential AT1-independent mechanism of action that explains the superiority of telmisartan in gastroprotection than candesartan and olmesartan.
https://ajps.journals.ekb.eg/article_7248_6509b515f82a7053cb665678d0d8a3ed.pdf
2012-03-01
365
382
10.21608/ajps.2012.7248
Cold-restraint stress
Telmisartan
Candesartan
Olmesartan
oxidative stress
TNF-α
Prostaglandin E2
Mona
Tawfik
1
Department of Pharmacology, Faculty of Medicine, Suez Canal University, Ismailia, Egypt
AUTHOR
ORIGINAL_ARTICLE
DESIGN AND OPTIMIZATION OF TOLMETIN SODIUM MICROSPHERES PREPARED BY EMULSIFICATION-INTERNAL GELATION USING RESPONSE SURFACE METHODOLOGY
In a trial to delay the release rate of tolmetin sodium from alginate coated microspheres, the use of a copolymer was suggested. Mixtures of polymers can have a significant property than that of individual polymer to achieve controlled release microspheres. A 32 factorial design was employed to produce controlled release microspheres of tolmetin sodium in sodium alginate and ethyl cellulose copolymers by emulsification internal gelation methodology. The effect of critical formulation variables namely, drug to polymer ratio(D:P ratio) and speed of rotation on drug loading efficiency (LE), drug release at the end of 2 hours (Rel2) and drug release at the end of 8 hours (Rel8) were analyzed using response surface methodology. The parameters were evaluated using the F test and mathematical models containing only the significant terms were generated for each parameter using multiple linear regression analysis and analysis of variance.The produced microspheres were spherical in shape with large pores at D:P ratio 1:2 and small pores at drug to polymer ratio 1:4. Differential scanning calorimetry confirmed the stable character of tolmetin sodium in the drug loaded microspheres and revealed crystalinity form. Both formulation variables studied exerted a significant influence (p < 0.05) on the drug release whereas the speed emerged as a lone factor significantly influencing the drug loading efficiency. Increasing the D: P ratio decreases the release of the drug after two and eight hours. The increase of speed results in an increase of drug release after two and eight hours. The drug release from the microspheres followed zero order kinetics.
https://ajps.journals.ekb.eg/article_7249_686186c79d65b987c20912c186eb5a96.pdf
2012-03-01
383
398
10.21608/ajps.2012.7249
Mahmoud
Elsayed
1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Assiut branch, Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
ISOLATION AND IDENTIFICATION OF NATIVE EGYPTIAN CURDLAN PRODUCING AGROBACTERIUM ISOLATE
One hundred and eighty bacterial isolates were isolated from different soil samples and different crown galls from some plants (grape, apple, peach) grown in Egyptian soil in different area. Gram stains were applied on all isolates and the results showed that 120 isolates were Gram negative and 60 strains were Gram positive. The Gram negative isolates were selected for pathogenicity tests and were used to infect some hosts (grape, tomato and kalanchoe). The results showed that about 60 isolates cause infections of the above mentioned plants, these isolates were subjected to grow on some selective media as aniline blue medium and Congo red medium to detect curdlan producer isolates. The results obtained indicated that seven isolates give positive reaction toward curdlan production, three isolates were selected for production of curdlan after some chemical analysis and the most potent isolate was selected for optimization and identification. The potent isolate have been identified by morphological, biochemical and phylogenetic analyses.
https://ajps.journals.ekb.eg/article_7250_031ecd3ffffa18000a34eb44b23d871b.pdf
2012-03-01
399
412
10.21608/ajps.2012.7250
isolation
Screening
identification
Agrobacterium and curdlan
Islam
El-Sehemy
1
Chemistry of Natural and Microbial product Dept., Pharmaceutical industry Dev., National Research Centre Dokki, Cairo, Egypt.
AUTHOR
ORIGINAL_ARTICLE
STATISTICAL OPTIMIZATION OF CURDLAN PRODUCTION BY LOCAL EGYPTIAN AGROBACTERIUM ISOLATES
Curdlan is a linear D-glucans, belongs to the class known as beta (1, 3) - D -glucan macromolecules, Curdlan gum is a neutral polysaccharide was discovered by Dr. Harada in 1964, Curdlan gum is insoluble in water but soluble in most organic solvents. Curdlan is one of the FDA approved biopolymer used in food industries such as jelly, noodles, and edible fibers manufacturing process approved in 1996, Curdlan gum produced by many Agrobacterium species under nitrogen-limiting conditions, has many useful benefits in food, agriculture, pharmaceutical, and medicine industry.
Sequential optimization strategy, based on statistical experimental designs, was employed to enhance the production of curdlan by local Agrobacterium sp isolate, which include (Plackett–Burman design and Box–Behnken design)
https://ajps.journals.ekb.eg/article_7251_5e54bbcb7e74f04f2718a695a66cd3cc.pdf
2012-03-01
413
424
10.21608/ajps.2012.7251
islam
El-Sehemy
1
Chemistry of Natural and Microbial product Dept., Pharmaceutical industry Dev., National Research Centre Dokki, Cairo, Egypt.
AUTHOR
ORIGINAL_ARTICLE
ACYLATED (+)-CATECHIN GLYCOSIDES FROM ULMUS PUMILA L. GROWING IN EGYPT
Extensive isolation work on the n-BuOH-soluble fraction obtained from the stem and root barks of Ulmus pumila L. afforded five compounds. Four were identified as (+)-catechin 1, (+)-catechin 7-O-gallate 2, (+)-catechin-5-O-b-D-apiofuranoside 3, and (+)-catechin-7-O-b-D-apiofuranoside 4. The structures of the remaining new compound was elucidated to be, (+)-catechin-7-O-gallate-5-O-(5``-trans-caffeoyl)-b-D-apiofuranoside-3-O-b-D-apiofuranosyl-(1®2)-glucopyranoside 5, by chemical and spectroscopic analysis. The ethanolic and n-butanol extracts and the isolated compounds (1-5) were tested for their antioxidant activity using DPPH radical scavenging assay, xanthine oxidase-induced generation of superoxide radical and lipid peroxidation assay by thiobarbituric acid-reactive substances (TBARS) method using rat tissue homogenates.
https://ajps.journals.ekb.eg/article_7252_0a9d6952f8ad1d7c52a423cef9de62c1.pdf
2012-03-01
425
436
10.21608/ajps.2012.7252
Ulmus pumila L
Ulmuaceae
acylated (+)-catechin glycosides, DPPH , Xanthine oxidase, Lipid peroxidation
Said
Esmail
1
Department of Pharmacognosy, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
AUTHOR
ORIGINAL_ARTICLE
HPLC AND SPECTROPHOTOMETRIC STABILITY – INDICATING STUDY OF RALOXIFENE IN PURE FORM AND TABLETS
Five simple, sensitive, accurate and precise methods were developed for determination of raloxifene (RLX) in pure form as well as in its pharmaceutical preparation. Method [A] is HPLC stability–indicatingmethod, where the intact drug (RLX), the internal standard (methocarbamol) and RLX degradation products were separated using a YMC-pack ODS-AQ C18 column (150 mm X 4.6 mm ID, 3µm particle size ) using acetonitrile–0.05 M KH2PO4 adjusted to pH 2.5 using H3PO4 (50 : 50 v/v ) as a mobile phase at a flow rate 1 ml/min. and UV detection at 280 nm, where a good linearity was obtained in the range of 0.5 – 8 µgml-1.The LOD was 0.077 µg ml-1 and the LOQ was 0.258 µgml-1. Method [B] depended on measurement of the difference absorbance (ΔA) of the drug in the presence of its degradate between solutions in methanolic 0.1 M HCl and 0.1 M NaOH at 285 nm. Beer’s low was obeyed in the range of 3 – 27 µgml-1. LOD and LOQ were found to be 0.233 and 0.778 µg ml-1,respectively. Method [C] is stability – indicating First-Derivative (1D) for the determination of intact RLX in presence of its degradation product at 268 nm in the range of 3 – 18 µg ml-1 with LOD of 0.254 µg ml- and LOQ of 0.849 µg ml-1. Method [D] depended on ion pairing of RLX with eosin-Y dye at pH 3.5 to produce red coloured complex measured at 545 nm. Beer’s low was obeyed in the range of 2 – 20 µgml-1. LOD and LOQ were found to be 0.276 and 0.920 µg ml-1,respectively. Method [E] depended on ion pairing of RLX with bromothymol blue (BTB) dye at pH 2.6 to form a chloroform-soluble coloured ion association complex. The formed complex could be extracted and measured at 420 nm. Good agreement with Beer’s low was found in the range of 4 – 28 µgml-1. LOD and LOQ were found to be 0.633 and 2.110 µg ml-1,respectively. The percent recoveries ± RSD% of these methods were 100.83±0.920, 100.24±0.724, 100.15±0.586, 100.26±0.383 and 99.98±0.261, respectively. The obtained results were compared with those of the reported method and no significant difference was observed regarding accuracy and precision.
https://ajps.journals.ekb.eg/article_7253_a049a24d7bcca8b570a4de91ac534aa2.pdf
2012-03-01
437
454
10.21608/ajps.2012.7253
Khalid
Attia
1
Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
AUTHOR
ORIGINAL_ARTICLE
PHYTOCHEMICAL AND BIOLOGICAL INVESTIGATION OF RUSSELIA EQUISTIFORMIS (SCROPHELARIACEAE) CULTIVATED IN EGYPT
From the methanol extract of Russelia equisetiformis (Scrophelariaceae) cultivated in Egypt ten phenolic compounds were isolated and identified as gallic acid, methylgallate, vicenin II, chrysoeriol-7-O-ß-D-4C1 glucopyranoside, luteolin 7-O-glucoside, luteolin-7-O-ß-D-4C1-arabinoside, quercetrin, apigenin, luteolin and acetoside. The structures of the isolated compounds were elucidated on the basis chromatographic and spectroscopic data (UV, IR and NMR) where all compounds were isolated for the first time except acetoside. The biological investigation antidepressant and hepatoprotective effect of different extracts of Russelia equisetiformis was carried out, concerning the antidepressant property the n-butanol was the most active, followed by aqueous and crude phenylethanoids extract respectively and Fluoxetine as reference standard, while the hydro-alcohol extract exhibited significant hepatoprotective effect against carbon tetrachloride injured liver cells
https://ajps.journals.ekb.eg/article_7254_718597e8fa2e21cf2dff6f0c9b436543.pdf
2012-03-01
455
474
10.21608/ajps.2012.7254
Russelia equisetiformis
Phenolic compounds
Antidepressant
fluoxetine
Hepatoprotective
Carbon tetrachloride
Atef
El Hela
1
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University "Boys", Cairo.
AUTHOR
ORIGINAL_ARTICLE
FORMULATION, CHARACTERIZATION, STABILITY, INVITRO EVALUATION AND OPTIMIZATION OF DIACEREIN NIOSOMES
Niosomes or non-ionic surfactants vesicles are microscopic lamellar structures formed on the admixture of a non-ionic surfactant, cholesterol and stearylamine with subsequent hydration in aqueous media. The delivery of drugs by “vesicular drug delivery system” such as niosomes provides several important advantages over conventional drug therapy. Diacerein is an Interleukin-1 inhibitor and it is highly effective in relieving the symptoms of osteoarthritis. Diacerein, in contrast to NSAIDs, are potent inhibitor of IL-1 beta induced nitric oxide production by chondrocytes and cartilage, without reducing prostaglandin E2 production.
The main objective of this study was to design suitable niosome-encapsulated drug delivery for anti-inflammatory drugs like Diacerein and evaluate the vesicle size, entrapment efficiency, in vitro release and physical stability of the system. Non-ionic surfactants used were Tween (40&60), cholesterol and stearylamine in molar ratio 1:1:0.1. The niosomes were prepared by thin film hydration method. The higher entrapment efficiency was observed with niosome (F11) prepared from tween 60, cholesterol and 2.5 min sonication. The release pattern shown by these formulations were first order & Higuchi diffusion controlled mechanism. The physical stability study show that niosomal preparation stored at refrigerated temperature for 60 days show maximum drug retained compare to room temperature and elevated temperature conditions. Finding of all this investigation conclusively demonstrate prolongation of drug release at a constant and controlled rate after niosomal encapsulation of Diacerein.
https://ajps.journals.ekb.eg/article_7255_0184e017203e53d394718fb17ae358cf.pdf
2012-03-01
475
484
10.21608/ajps.2012.7255
formulation
stability
Niosome
Cholesterol
diacerein
Tween
Stearylamine
Abdelsaboor
Hassan
1
Pharmaceutics and Industrial Pharmacy Dept., Faculty of Pharmacy (Boys), Al-Azhar University.
AUTHOR
ORIGINAL_ARTICLE
EVALUATION OF THE MODULATORY EFFECTS OF CURCUMIN AGAINIST DOXORUBICIN-INDUCED CARDIO- AND NEPHROTOXICITIES IN RATS
The current study was designed to evaluate the modulatory effects of curcumin treatment on doxorubicin-induced nephrosis and cardiomyopathy in sprague-dawley rats. Intravenous administration of a single doxorubicin dose (7.5 mg/kg) induced apparent sings of nephrotoxicity and cardiomyopathy as manifested by marked deteriorations in both renal and cardiac parameters in association with significant changes in the histological structures of these tissues. Curcumin administration was remarkably able to mitigate the induced cardiac and kidney injuries. Moreover, it exhibited marked protective effects against such alterations. These data suggest that curcumin may have a profound therapeutic potential against such toxic effects.
https://ajps.journals.ekb.eg/article_7260_36c5773bfdbc3f1a50104a1112945e44.pdf
2012-03-01
485
498
10.21608/ajps.2012.7260
Bakheet
Elsadek
1
Department of Biochemistry, College of Pharmacy, Al-Azhar University, Assiut Branch, P.O. Box 71524 Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
IMPROVEMENT THE RELEASE AND AVAIALBILITY OF CELECOXIB CO-ADSORBATE FROM FLOATING CAPSULES
Celecoxib is a selective COX-2 inhibitor non-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis. Celecoxib is practically inslouble in GIT pH. Consequently, it suffers from low and variable bioavailability following oral administration of solutions (64-88%) and capsules (20-40%)
In the present study, gastroretentive controlled release single-unit floating capsules of Celecoxib were designed and evaluated. Various grades of low and high viscosity polymers of HPMC 4000 and 15.000 cps and NaCMC were used for formulation of Celecoxib capsules.
For the purpose of enhancing the poor dissolution rate of Celecoxib, co-adsorption with Tween 80 onto surface of Florite® was investigated in this study. Thus, controlled release limited by drug solubility was percluded and delivery of active material was controlled by the formulation. In the present study conventional capsules containing Celecoxib using HPMC and NaCMC were developed and evaluated. Floating capsules containing Celecoxib, co-adsorption with Tween 80 onto surface of Florite and Aerosil 200 in different ratios were also formulated and investigated for the release of the drug from these capsules. The results obtained of this study showed that Celecoxib capsules containing HPMC 15000cps as a swelling matrix has a good floating behaviour and retarding effect on the drug release. Also, different concentrations of sodium bicarbonate confirmed and maintained the floating properties of the prepared formulations without affecting the drug release. From DSC and X-ray diffraction studies it was found that crystalline Celecoxib was converted into the amorphous form in the presence of Florite® at (1:5 w/w drug: carrier ratio) in the adsorbate and co-adsorbate with Tween 80. The loaded and ground mixtures of Celecoxib with either Florite® or Aerosil 200 increased the dissolution rate of the drug. Furthermore, co-adsorbate of the drug with Florite® and Tween 80 at these ratios of (1:5:3 and 1:5:5) gave the highest percentage released of Celecoxib (reached about 100% at 30 and 45 min., respectively).
https://ajps.journals.ekb.eg/article_7261_a3f23519c8f4b166e1eed5d75b92fe4d.pdf
2012-03-01
499
523
10.21608/ajps.2012.7261
Sherif
Abu-elyazid
1
Pharmaceutics and Industrial Pharmacy Deptartment, Faculty of Pharmacy-(Boys) - Al-Azhar University, Cairo, Egypt
AUTHOR
ORIGINAL_ARTICLE
COMPARSION BETWEEN RENOPROTECTIVE EFFECTS OF CARVEDILOL AND LISINOPRIL IN L-NAME-TREATED RATS
Aim The present study compared the renoprotective effects of curative and prophylactic doses of carvedilol and lisinopril in L-NAME treated rats.
Material and methods Rats were divided into seven groups: the first and second (normal control and hypertensive control) groups received distilled water and L-NAME (L-nitro argentine methyl ester, 50 mg/kg per day), respectively, for eight weeks. The third and fourth groups received L–NAME (50mg/kg per day) in combination with a prophylactic dose of carvedilol (15mg/kg per day) or lisinopril (20mg/kg per day), respectively, for eight weeks. The fifth, sixth and seventh groups received L-NAME (50mg/kg per day) for eight weeks, followed by curative doses of carvedilol (30mg/kg per day), lisinopril (40mg/kg per day) or carvedilol (15mg/kg per day) in combination with lisinopril (20mg/kg per day), respectively, for five weeks. The drugs were administered by gastric gavage.
Results During prophylactic therapy, carvedilol and lisinopril decreased L-NAME induced rise in systolic blood pressure (SBP) and serum creatinine levels. Furthermore, both drugs improved microalbuminuria and renal histopathological changes and increased serum nitric oxide (sNO). During curative therapy, carvedilol improved microalbuminuria and renal histopathological changes. lisinopril or the combination of carvedilol and lisinopril improved all L-NAME induced changes. The combination improved renal histopathological changes more significantly than each individual drug.
Conclusion carvedilol and lisinopril have prophylactic and curative renoprotective effects in L-NAME treated rats. Carvedilol has similar effectiveness as the converting enzyme inhibitor, lisinopril, in reducing the hypertension, proteinuria and glomerulosclerosis associated with L-NAME induced chronic hypertensive renal failure in rats making chronic renal disease as a therapeutic target for this drug. Moreover, a combination of both drugs at half the therapeutic doses significantly ameliorated hypertension-induced renal damage and improved renal functions, indicating the role of this low-dose combination as an effective therapeutic option if a multi-anti-hypertensive regimen is desirable.
https://ajps.journals.ekb.eg/article_7262_e812b2ee7103a3e70727c1da8d0875d5.pdf
2012-03-01
524
534
10.21608/ajps.2012.7262
Carvedilol
lisinopril
L-NAME
Nitric oxide
Amany
Ibrahim
1
Department of pharmacology, 2Department of histology, Faculty of Medicine, Benha University, Egypt.
AUTHOR
ORIGINAL_ARTICLE
STABILITY INDICATING HPLC METHOD FOR THE DETERMINATION OF AGOMELATINE INPLASMA AND TABLET FORMULATION
A stability indicating HPLC method was developed and validated for quantitative determination of agomelatine in plasma and tablet formulation in the presence of degradation products generated from forced degradation studies. An HPLC method was developed to separate the drug from the degradation products using Waters spherisorb Cyano C18 column (250 x4.6mm, 5μm) and a mobile phase constituted of trifluoroacetic acid buffer and methanol (50:50 % v/v). The wave length of the detection is 230 nm at a flow rate 1mL/min. The validation data showed that the assay is accurate, precise, sensitive, specific and reproducible for the determination of agomelatine in plasma as well as in tablet formulation in the presence of its degradants. The method is linear from 12.5-37.5 μgmL-1 and accuracy of the method was found to be 100.5 -100.9 % for tablets and 97.84 – 101.24% for plasma. The proposed method was found to be suitable for quantitative determination and the stability study of the drug in plasma and tablet formulation.
https://ajps.journals.ekb.eg/article_7263_988e65e6b4edaa7958239e2575e1be58.pdf
2012-03-01
535
548
10.21608/ajps.2012.7263
Agomelatine
stability indicating HPLC method
plasma and tablet formulation
Hamed
Abuseada
1
Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
AUTHOR