Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
EFFECT OF PIOGLITAZONE ON THE BONE HEALTH OF DIABETIC PATIENTS IN JEDDAH, KSA
1
9
EN
Abdulrahman
Alahdal
Department of Clinical Pharmacy, Faculty of Pharmacy, KAU
10.21608/ajps.2012.7113
<strong>Background: </strong>Osteoporosis is an important health care issue because the resultant bone fractures cause great deal of morbidity and mortality. Among the important risk factors for the development of osteoporosis is diabetes mellitus.
<strong>Objective:</strong> Thiazolidinediones (TZDs), group of antidiabetic drugs used to reduce insulin resistance, have been inconsistently shown to be associated with osteoporotic fractures. The purpose of this study was to find out if the use of pioglitazone, an oral antidiabetic medication belonging to TZDs, has any adverse effects on bone health in patients with type-2 diabetes in Jeddah, KSA.
<strong>Methods: </strong>This case control analysis included 56 subjects, 40 to 65 years old (18 diabetic patients under pioglitazone therapy, 18 diabetic patients under metformin-sulfonylurea therapy, and 20 non-diabetic persons) enrolled in osteoporosis center in Jeddah, KSA. Medication information was taken directly from drug containers during in-person interviews. The main outcome measures were the bone mineral density (BMD) and the serum levels of vitamin D, calcium, and creatinine.
<strong>Results: </strong>No significant BMD and biochemical (serum vitamin D, calcium, and creatinine) changes were be detected in the three groups (Pioglitazone users group; metformin-sulfonylurea users group; and the nondiabetic persons group).
<strong>Conclusion:</strong> Pioglitazone does not cause adverse effect on the BMD and biochemical tests. This is in contrast to other studies that showed decreased BMD and increased risk of fracture in patients on TZDs. Some of this contravention may be explained by factors that are included within bone quality, while some may be related to the other non-skeletal factors. In terms of bone quality, there have been suggestions that there are racial differences in bone strength due to genetic, nutritional, lifestyle, and hormonal factors. The possible other non-skeletal factors include the small number of patients studied in the present work as well as the variation of the dose of the drug, and the duration of therapy. Therefore, large prospective, randomized trials are necessary to evaluate the effect of pioglitazone on the bone health of diabetic patients in KSA.
<strong> </strong>
https://ajps.journals.ekb.eg/article_7113.html
https://ajps.journals.ekb.eg/article_7113_a43c5e92958656870c946a317bbe9ee5.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
BOTANICAL STUDY OF FICUS AURICULATA LOUR.
10
24
EN
Ahlam
El-Fishawy
Dept. of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
10.21608/ajps.2012.7114
The macro- and micromorphological characters of the stem, leaf and fruit of <em>Ficus auriculata</em> Lour. (Family Moraceae) cultivated in Egypt have been studied in order to find out the diagnostic features of these organs which can help in their identification in both entire and powdered forms. This study is considered as a method to check the genuineness of the raw drugs.
Moraceae,Ficus auriculata,Botanical
https://ajps.journals.ekb.eg/article_7114.html
https://ajps.journals.ekb.eg/article_7114_c6d519aaa72087fe83115fe057d0d153.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
SPECTROPHOTOMETRIC DETERMINATION OF FENOTEROL IN PURE FORM AND PHARMACEUTICAL FORMULATION.
25
38
EN
Monir
Amin
Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
10.21608/ajps.2012.7115
Four simple and selective spectrophotometric methods were developed for quantitative determination of Fenoterol in pure forms as well as in its pharmaceutical formulation. <strong>Method [A] </strong>is based on the nitration and subsequent complexation with a nucleophilic reagent forming a yellow colour with λ<sub>max</sub> at 411 nm, Beer's law was obeyed in the concentration range 1-6 μg ml<sup>-1</sup>. LOD and LOQ were found to be 0.024 and 0.08 μg ml<sup>-1</sup> respectively. <strong>Method [B] </strong>is based on the coupling of the drug as a phenolic compound with the diazonium salt of o-nitroaniline forming red azodye with λ<sub>max</sub> at 505 nm. Good linearity obtained in the range of 3-21 μg ml<sup>-1</sup>. LOD & LOQ were found to be 0.12 and 0.41, respectively. <strong>Method [C]</strong> is based on coupling with diazo reagent (method B) and subsequent chelation with copper sulphate and extraction of the resulting chelate into chloroform and measuring the chloroformic layer at 412 nm. Beer’s low was obeyed in the concentration range 3-21 μg ml<sup>-1</sup>. LOQ & LOQ were found to be 0.056 and 0.188 μg ml<sup>-1</sup>. respectively. <strong>Method [D] </strong>involves the reduction of follin ciocalteu's phenol reagent (FCP) by the drug to be a blue colored product which exhibited an absorption maximum at l<sub>max</sub> 655 nm. Regression analysis of Beer's plot showed good correlation in the concentration range of 2-14 μg ml<sup>-1</sup>. LOD & LOQ were found to be 0.011 and 0.038 μg ml<sup>-1</sup>. respectively. The optimization of the reaction conditions was investigated, the methods were successfully applied to the analysis of Fenoterol in its pharmaceutical formulation with good recovery.
https://ajps.journals.ekb.eg/article_7115.html
https://ajps.journals.ekb.eg/article_7115_d64bb3fa5d85b5d000069da7f5b30406.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
SELECTIVE SPECTROPHOTOMETRIC DETERMINATION OF FENOTEROL BY THREE DIFFERENT METHODS.
39
52
EN
Monir
Amin
Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
10.21608/ajps.2012.7116
Three simple and selective spectrophotometric methods were developed for the quantitative determination of Fenoterol in pure forms as well as in its pharmaceutical formulation. <strong>Method [A] </strong>Involves the coupling of the drug as phenolic compound with the diazonium salts of four amines, namely, Benzocaine (BZC), sulphadiazine (SDZ), sulphacetamide (SCM) and sulphanilic acid (SPA) forming red azodyes absorbed at 526, 514, 512 and 513 nm, respectively. Beer's law was obeyed in the concentration ranges of 10-70, 6-42, 4-28 and 3.5-24.5 μg ml<sup>-1</sup> for the four reagents, respectively. <strong>Method [B] </strong>is based on reaction of Fenoterol with cobalt thiocyanate, where by a sparingly soluble blue ion-pair complex is formed. This complex is extracted by toluene and spectrophotometrically measured at 619 nm. Good linearity was obtained in the range of 10-70 μg ml<sup>-1</sup>. <strong>Method [C]</strong> is based on the reduction of iron (III) by Fenoterol in acid medium and subsequent interaction of iron (II) with ferricyanide to form Prussian blue. The product exhibits absorption maximum at 730 nm. Beer's law was obeyed in the concentration range of 1.5–10.5 μg ml<sup>-1</sup>. The reaction conditions for described methods were studied and optimized. The proposed methods were applied to the determination of Fenoterol in pharmaceutical formulation and the results demonstrate that the methods are equally accurate and precise as the reported methods found from the t and F values. The reliability of the methods was established by recovery studies using standard addition technique.
https://ajps.journals.ekb.eg/article_7116.html
https://ajps.journals.ekb.eg/article_7116_d902a3a59f66b38d245cc2eac562ad2f.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
EFFECT OF ASCORBIC ACID, BENZYL ADENINE AND PACLOBUTRAZOL ON GROWTH, YIELD AND SOME METABOLIC CONSTITUENTS OF SUNFLOWER PLANTS
53
63
EN
Emad EL- Dein
Ewais
Botany and Microbiology Department, Faculty of Science, Al-Azhar University, Cairo, Egypt.
10.21608/ajps.2012.7117
A field experiment was conducted to study the effect of foliar spray of ascorbic acid (50 and 100 ppm), benzyl adenine (50 and 100 ppm) and paclobutrazol (25 and 50 ppm) on growth, yield and some physiological parameters of (<em>Helianthus annuus </em>var. Sakha 53). Ascorbic acid was more effective than other treatments in enhancing growth parameters during stage I, while benzyl adenine was most effective during stage II. Paclobutrazol seemed to be less effective regarding growth characteristics. All doses applied tended to increase photosynthetic pigments, total soluble carbohydrates and soluble proteins of sunflower plants. The changes in proteolytic, amylolytic and lipolytic activities were also recorded. This was associated by improving yield quality and the nutritional value of the seeds. The effect of paclobutrazol was superior to that of ascorbic acid, benzyl adenine on increasing yield components. The highest lipid % was recorded by 50 ppm of ascorbic acid, whereas the highest carbohydrates and proteins of the yielded seeds were observed with plants treated with 100 ppm benzyl adenine.
https://ajps.journals.ekb.eg/article_7117.html
https://ajps.journals.ekb.eg/article_7117_4845d7b0dc075e3d4a625ef7d28e3005.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
THE PROTECTIVE ROLE OF VITAMIN C AGAINST PHYSIOLOGICAL AND HISTOLOGICAL CHANGES IN RATS CHRONICALLY EXPOSED FOR DIAZINON AND ALUMINUM PHOSPHIDE INSECTICIDES.
64
89
EN
El Yamany
El Zawahry
Zoology Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, Egypt.
10.21608/ajps.2012.7118
<strong>Background: </strong>Insecticides occupy a rather unique position among many chemicals that man encounters daily, in that they are deliberately added to the environment for the purpose of killing or injuring some form of life. Vitamin C consider as antioxidant substance which has a protective role against deleterious effects of Diazinon and Aluminium phosphide. <strong>The aim</strong> is to evaluate effects of Diazinon, Aluminum phosphide and vitamin C on liver, kidney and brain of albino rats. <strong>Results:</strong> data shows a significant increase in liver enzymes AST, ALT in addition to GGT and ALP by the action of the used pesticides Diazinon and Aluminum phosphide also this pesticides cause a significant increase in serum urea, uric acid and creatinine while the histological study showed that the chronic treatment with doses of the insecticides induced different deleterious histopathological lesions in the brain of treated rats. The treatment using vitamin C cause amelioration in liver functions tests and kidney functions tests, although, all these tests did not show any significant decrease. <strong>Conclusion:</strong> Vitamin C can ameliorate the deleterious effects of Diazinon and Aluminum phosphide on liver and kidney.
https://ajps.journals.ekb.eg/article_7118.html
https://ajps.journals.ekb.eg/article_7118_5c6d8845f7da3e3caefe839cdfe5f34f.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
THE USE OF KETOPROFEN NIOSOMES FOR FORMULATION OF SUSTAINED RELEASE TABLET DOSAGE FORM
90
99
EN
Mohamed
Raslan
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo
10.21608/ajps.2012.7119
The objective of this study was to formulate sustained release tablet dosage form (100 mg) using Ketoprofen Niosomes. Ketoprofen Niosomes were prepared by lipid hydration method and then dried and compressed into sustained release tablets (100 mg). The tablet excipients employed include: Avicel PH 101, Avicel PH 102, and Mannitol as diluents, Cab-O-Sil (colloidal silica) as a glidant, Starch as a disintegrant and Magnesium Stearate as lubricating agent. The tablets were tested for weight variation, hardness, friability, thickness, disintegration, drug content and release ratio. Finally the release kinetics of Ketoprofen tablets were calculated.
Ketoprofen,Niosomes,lipid hydration method,sustained release tablets, direct compression
https://ajps.journals.ekb.eg/article_7119.html
https://ajps.journals.ekb.eg/article_7119_0cabbb27675ee6ce9ede6ca170524ac2.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
LOSS OF RETINOID RECEPTORS RAR-A AND RXR-A DURING MONOCROTALIN/LIPOPOLYSACCHARIDE-INDUCED RENAL TOXICITY IS TISSUE FACTOR DEPENDENT
100
114
EN
Mohamed
Abdel-Bakky
Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt
10.21608/ajps.2012.7139
Retinoic acid receptors (RARs) are ligand-controlled transcription factors that function as heterodimers with retinoid X receptors (RXRs) to regulate cell growth, differentiation, survival and death. Due to their regulatory potential, these nuclear receptors (NRs) are major drug targets for a variety of pathologies, including cancer and metabolic diseases. We reported earlier the involvement of tissue factor (TF) in the release of retinoid receptors RAR-α and RXR-α as accumulated lipid droplet during monocrotaline/lipopolysaccharide (MCT/LPS)-liver injury in mice. In the kidney, little is known about the localization and the functional significance of RXR-a and RAR- a. In this study, we were able to find RXR-a receptor in distal, proximal tubules as well as glomeruli of mice kidney. In addition, RAR-a expression is restricted to the glomeruli and endothelial cells of the blood vessels. Furthermore, following MCT/LPS co-treatment, we found the translocation of RXR-a from basolateral into the apical site in the distal tubules and collecting duct along with downregulation of glomerular RAR-a. This study reports the involvement of TF in the tubular translocation of retinoid receptor RXR-α and the glomerular downregulation of RAR-a during MCT/LPS-renal injury. The fact that TF antisense oligonucleotides (TF-AS ODN) treatment not only down-regulated TF but also obliterated the tubular translocation of RXR-a and glomerular RAR-a downregulation points towards TF being an important regulatory molecule for renal RAR-α and RXR-α.
Tissue Factor,retinoic acid receptor alpha,retinoid X receptor alpha,tissue factor antisense oligodeoxynucleotides
https://ajps.journals.ekb.eg/article_7139.html
https://ajps.journals.ekb.eg/article_7139_11a4c381954c92dab5f8e92738b0f32e.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
COMPARITIVE STUDY BTWEEN PANTOPRAZOLE AND RANITIDINE ON SOME CARDIOVASCULAR PREPARATIONS
115
137
EN
Maryam
Hammoda
Pharmacology Dept., Faculty of Medicine for Girls Al-Azhar University
10.21608/ajps.2012.7140
Because of the abundant use of proton pump inhibitors (PPIs) and histamine H<sub>2- </sub>receptors antagonists ( H<sub>2</sub>RAs) and considering the hazards of high intravenous (IV) dosing especially in critically ill intensive care unit ( ICU) patients and in view of controversy about the cardiac effects of these drugs. So it was of interest in the present work to investigate and compare the effects of either pantoprazole or ranitidine on some cardiovascular aspects using both isolated and intact experimental animal preparations.
The effect of different increasing doses of pantoprazole or ranitidine on the amplitude of myocardial contraction of isolated perfused rabbit heart and on NE-induced contraction of aortic spiral strips of rabbits were studied. Their effects on the mean arterial blood pressure (MABP), heart rate (HR) and electrocardiogram (ECG) of anaesthetized cats were also investigated.
This stady showed that, pantoprazole caused a significant dose-dependent reduction in the amplitude of myocardial contraction with mean percentage reductions ranged from 2.5 ± 0.55 to 58.4 ± 3.82, while ranitidine had no effect. The cardioinhibitory effect of pantoprazole was proven to be due to a calcium channel blocking effect. On NE-induced contraction of aortic spiral strips, both pantoprazole and ranitidine produced a significant dose dependent reduction. The mean percentage reductions ranged from 3.9 ± 0.59 to 40.3 ± 2.13, and8.3 ± 2.45 to 45.4 ± 5.82 for pantoprazole and ranitidine respectively. Intravenous bolus injection of both drugs produced a significant dose-dependent reduction in MABP. The mean percentage reductions ranged from 0.6 ± 0.23 to 16.1 ± 3.15 and 0.7 ± 0.19 to 42.6 ± 3.21 for pantoprazole and ranitidine respectively and were found to be statistically significant. On the other hand, continuous intravenous infusion of pantoprazole 1.5 mg/kg or ranitidine 2 mg/kg which is equivalent to the human therapeutic dose (HTD), for 2 hours did not produce any change in the MABP, ECG pattern and heart rate of an anaesthetized cat all over the time of infusion.
In conclusion, ranitidine had no cardioinhibitory effect compared to pantoprazole. So, it could be prefered to pantoprazole especially in cardiac patients. On the other hand, the possibility of negative inotropic effect with pantoprazole should be considered carefully especially in patients with myocardial contractility dysfunction.
In the setting where intermittent IV bolus administration of either pantoprazole or ranitidine is needed, pantoprazole seems to be more favourable of the two drugs evident by its less hypotensive effect plus insignificant effect on heart rate and no changes in ECG record even at high doses.
The continuous IV infusion route may be safer and better chosen rather than IV bolus intermittent dosing to avoid any possible cardiovascular side effects of either pantoprazole or ranitidine.
https://ajps.journals.ekb.eg/article_7140.html
https://ajps.journals.ekb.eg/article_7140_5959fb18d4e636af3c3bf0d9666a1fac.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
FEEDING PATTERN, HORMONAL OXIDATIVE BALANCE AND LIVER EXPECTANCY
138
148
EN
Ali
Ahmed
Special Food and Nutrition Dept. Food Technology Research Institute, ARC. *Fac. Specific Edu. Alex. Univ.
10.21608/ajps.2012.7141
One of the most clinical assignments affecting human being in the present time is liver defect. Therefore, several factors that known to positively or negatively dealt with this organ were investigated in the present study. A 60 rats have been divided into four groups (3x6, 2x6, 3x6 and 2x6) of ten specific subgroups as follows: The control groups fed on basal diet (G1); G2 is a high fat diet HFD containing 20% animal fat or same with 5 % of doum waste powder (HFD+DW) as G3; G4 is tetra cholro carbon (TCC) and G5 is alike received grape laves extract. In G6 animal received TPN solution, while G7 treated the same pluse lasix as duritic synthetic druge and G8 replcinng this drug with natural one. In G9 diet was contamented with afflatoxin, meanwhile, G10 was similar but a rich protein antioxidant was subleminted. It seems that the liver homeorhestic function, i.e., cortisone to insulin is governed by its homeostatic control of organ, or vice versa, hence dismutase SOD, catalase, were sharply reduced and each of GOT, GPT or AP enzymes increased with food contaminated or artificial drug administration concurantly to a sort of hormonal imbalanc. Significat repairment were noticed for feeding systemes used. These findings have been approved by organ microscopically tests. The
DW, for instance, successfully decreases the influances of HFD. There were also evidence of the hepatotoxicity of TCC and of the hepatoprotective effect of the extract of grape leave juces. The minimal or maximal disruptions of the hepatocyte structure are complemented the liver enzyme data of GOT, GPT and ALP activities and other biological parameters. In case of TPN histopathology, liver of rat treated with TPN of mixed natural extract minamized the effect of TPN alone. Likewise, the microscopical examination of liver of rat with diet contaminated of micotoxin, a highly protection for a high protein-antioxidant (HPAO) formula arises. Seemingly, feeding pattern affects hormonal oxidative balanc to perform better liver expectancy. In general conclusion, feeding pattern should be developed to help in protecting human liver, especially in poor areas allover the world. Very simple foods or even food wastes is considered hepatoprotective agents. The hormonal oxidative balance has to be further investigated in order to produce such important food that may protect liver worldwide.
https://ajps.journals.ekb.eg/article_7141.html
https://ajps.journals.ekb.eg/article_7141_2e482ec5b89e68b725b91871a142f081.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
PHYTOCONSTITUENTS FROM DELONIX REGIA RAF ROOTS AND THEIR BIOLOGICAL ACTIVITIES
149
160
EN
Mohammed
Hosny
Pharmacognosy Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
10.21608/ajps.2012.7142
Phytochemical investigation of the roots of <em>Delonix regia</em> yielded six compounds. They were identified as, aliphatic alcohol; heptadecanol [1], two phenolic acids; vanillic acid [2] and <em>p</em>-hydroxy benzoic acid [3], a mixture of the ester isomers of the <em>trans</em>- and <em>cis</em>-ferulate glucopyranoside [4], one flavonol glycoside; Kampferol-3-<em>O</em>-<em>α</em>-L-arabinopyranoside [5] and one megastigmanes; (6<em>R</em>, 9<em>S</em>)-3-oxo-<em>α</em>-dihydro-ionyl-9-<em>β</em>-D-glucopyranoside (Blumenol C-<em>O</em>-<em>β</em>-D-glucopyranoside) [6]. Identification of these compounds was based on ESI-MS, 1D and 2D-NMR analysis. All six compounds are new to the constituents of genus <em>Delonix</em>. The isolated compounds (1-5) were evaluated for their cytotoxic activities against human promyelocytic leukemia HL-60 cells and human monocytic leukemia U937 cells. The antioxidant activities were also evaluated using 1, 1-diphenyl-2-picrylhydrazyl free radical (DPPH), assay method.
https://ajps.journals.ekb.eg/article_7142.html
https://ajps.journals.ekb.eg/article_7142_a6720e256bf1229996ea6a79d505c391.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
ONE-POT SYNTHESIS AND ANTIMICROBIAL SCREENING OF NEW [1,5] –BENZODIAZEPINE DERIVATIVES CATALYZED BY TBAB
161
168
EN
Kamal
El-Gaml
Organic Chemistry Department, Al-Azher University, Nasr City , Cairo,11884, Egypt
10.21608/ajps.2012.7143
A new [1,5]-benzodiazepines <strong>(VI)</strong> were synthesized by the reaction of <em>o</em>-phenylenediamine with 2-chloro-3-acetylquinoline in the presence of tetrabutyl ammonium bromide (TBAB) in short reaction time with excellent yield.
tetrabutyl ammonium bromide,[1,5]- Benzodiazepine,2-chloro-3-acetylquinoline derivatives,o-phenelendiamine
https://ajps.journals.ekb.eg/article_7143.html
https://ajps.journals.ekb.eg/article_7143_1913f9076eadf79773b180f6d3494ab3.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
BIOLOGICAL ACTIVITES AND FUNDAMENTAL VARIATIONS BETWEEN FUNGAL ISOLATES BELONG TO ASCOMYCETES
169
184
EN
Amal
Mekawey
The Regional Center of Mycology and Biotechnology, Al-Azhar University, Cairo, Egypt
10.21608/ajps.2012.7144
Sexuality in fungi has long been a matter of concern and debates that always necessitated extensive analysis of the relationship between organisms assumed to represent different developmental forms of the same organism. Random amplification of polymorphic DNA (RAPD), amino acids, fatty acids and secondary metabolites profiles were performed for four isolatesbelong to ascomycetes fungi; <em>Aspergillus nidulans </em>and <em>Aspergillus chevalieri</em> and their teleomorph <em>Emercilla nidulans </em>and <em>Eurotium chevalieri</em>. Comparison of their activities as antibacterial and antifungal potency against many of Gram positive, Gram negative bacterial and several fungal species including yeast were determinate. Changes in fatty acid, secondary metabolite and RAPD profiles of sexual and their corresponding asexual isolates were observed. Oleic acid was of lower concentrations in <em>A.nidulans </em>and <em>A. chevalieri</em> than in <em>E. nidulans </em>and <em>E. chevalieri</em> while the opposite was observed for linoleic and linolenic acids. RAPD bands of molecular weights of 559 and 790 bp were the only different ones between <em>A. chevalieri </em>and <em>E. chevalieri </em>using primer 5 while those of molecular weights of 1239 and 1757 bp using primer 3 as well as that of 1209 bp using primer 5 represented the only different bands between <em>A. nidulans </em>and <em>E. nidulans</em>. Some intra- and extracellular secondary metabolites were undetected in the imperfect isolates while were detected in the corresponding perfect ones as contract with amino acids percentage detection where exhibited in imperfect isolates much more than perfect one. Deep relationship among cleistothecia formation, amino acids, fatty acid and secondary metabolite biosynthesis has been shown. Study of biological potency of four ascomycetes fungi exhibited great activities of <em>Emercilla nidulans </em>and <em>Eurotium chevalieri</em> (cleistothecia producing isolates) against Gram negative bacterial growth and yeast like fungi on contrast <em>Aspergillus nidulans </em>and <em>Aspergillus chevalieri</em> (two non-cleistothecia producing ones) show high inhibition of growth of Gram positive bacterial and filamentous fungi isolates.
Sexuality in fungi,Teleomorph,Cleistothecium Formation,Aspergillus,Ascomycetes,Amino acids,fatty acids,secondary metabolites,RAPD-PCR
https://ajps.journals.ekb.eg/article_7144.html
https://ajps.journals.ekb.eg/article_7144_78ec83334ba8d323c15b3cb402e16fc5.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
46
2
2012
09
01
DESIGN, SYNTHESIS, MOLECULAR DOCKING AND BIOLOGICAL EVALUATION OF SOME NOVEL QUINAZOLIN-4(3H)-ONE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS
185
203
EN
Mohamed
Ibrahim
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
10.21608/ajps.2012.7145
In view of their expected anti-inflammatory activity, novel series of 6-iodo-2-phenyl-quinazolin-4(3<em>H</em>)-one (4-12<sub>a-d</sub>) were designed and synthesized in order to evaluate their anti-inflammatory activity using carrageenan-induced rat paw edema assay. Most of the novel quinazolinone derivatives showed considerable potent anti-inflammatory activities of superior G.I.T. safety profile in experimental rats in comparing to indomethacin as a reference drug. The molecular docking was performed for all synthesized compounds to assess their binding affinity to COX-2 enzyme in order to rationalize their anti-inflammatory activity in a qualitative way. The obtained data from the molecular modeling was strongly correlated with that obtained from the biological screening. The highest binding affinities were noticed for compounds <strong>8<sub>a</sub></strong>, <strong>12<sub>b</sub></strong> and <strong>10<sub>b</sub></strong> which showed the highest anti-inflammatory activities of this series. Compounds <strong>12<sub>b</sub></strong>, <strong>9<sub>c</sub></strong> and <strong>8<sub>a</sub></strong> exhibited the least ulcerogenic effect in all of the experimental animals.
6-Iodoquinazolin-4(3H)-ones,Molecular docking,COX-2,Anti-inflammatory
https://ajps.journals.ekb.eg/article_7145.html
https://ajps.journals.ekb.eg/article_7145_1c24d035c0362074666b4f03b44a9832.pdf