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   2014| January-June  | Volume 13 | Issue 1  
    Online since June 30, 2014

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Synthesis of certain N-aralkyl-N-(1-((cyclohexylamino)methyl)cyclohexyl)benzenamines and benzamides and their anticonvulsant and analgesic potential
Mohammed N Aboul-Enein, Aida El-Azzouny, Fatma Ragab, Mohammed S Abdel-Maksoud, Yousreya Maklad
January-June 2014, 13(1):1-12
Background and objectives Epilepsy is a central nervous system disorder, affecting about 1% of the world's population, and is mostly prevalent in developing nations. In addition, many geminally disubstituted cyclohexane derivatives have proven to have anticonvulsant and analgesic activities. The aim of this study was to synthesize a new series of N-aralkyl-N-(1-((cyclohexylamino)methyl)cyclohexyl)benzenamines, 6a-h, and N-(1-((cyclohexylamino)methyl)cyclohexyl)-N-phenyl-substituted benzamides, 8a-g, for the purpose of evaluating their anticonvulsant and analgesic potential. In addition, the in-silico properties of the newly synthesized compounds have been discussed. Materials and methods Starting from 1-(N-phenylbenzamido and 4-substituted benzamido)cyclohexane carboxylic acids 3a-g, a new series of N-aralkyl-N-(1-((cyclohexylamino)methyl)cyclohexyl)benzenamines, 6a-h, was synthesized through formation of the corresponding methyl esters 4a-g, which underwent complete reduction of both the ester and the tertiary amidic carbonyl groups to afford the desired amino alcohols, 5a-g. Condensation of the corresponding mesylate esters with cyclohexylamine gave the target diamines 6a-g. Also, the alcohols 7a-g were achieved from 3a-g using NaBH 4 without affecting the amidic group, followed by preparation of the corresponding intermediate mesylate esters, which reacted with cyclohexylamine to yield the benzamidecyclohexyl amines 8a-g. The anticonvulsant and analgesic properties of 6a-h and 8a-h were studied using the pentylenetetrazole screening test and the hot-plate technique, respectively. Results and conclusion The results of the present study revealed that the most active compounds that exhibited remarkable 100% protection in mice were 6b , 6d , 6e , 8a, 8b , 8f and 8h, compared with diphenylhydantoin sodium and valproic acid, which were used as reference drugs. Both N-aralkyl-N-(1-((cyclohexyl amino)methyl)cyclohexyl)benzenamine and N-(1-((cyclohexylamino)methyl)cyclohexyl)-N-phenyl-substituted benzamide series, 6a-h and 8a-h, displayed significant antinociceptive effects. However, the 6a-h series showed higher potential than the 8a-h one. The results of the in-silico studies for the newly synthesized compounds showed that compounds 6c , 6e , 6h , 8e , 8f and 8h exhibit low mutagenic, tumorigenic, reproductive and medium irritant effect, as well as good drug-likeness and drug score.
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Composition of lipoidal matter and evaluation of hepatoprotective, cytotoxic, and antioxidant activities of Khaya grandifoliola C.DC. growing in Egypt
Fatma A Hashem, Elsayed A Aboutabl, Sahar S El-Souda, Amany Selim, Kamel Shaker, Amal A Maamoun
January-June 2014, 13(1):13-20
Background and objectives Liver disease is one of the most common health problems. Schistosoma and hepatic viruses are widespread in Egypt, causing severe liver damage and posing a threat to life, which has motivated researchers to discover and evaluate new hepatoprotective agents, particularly from natural sources. The hepatoprotective effect of the leaf extracts of Khaya grandifoliola C.DC. were investigated, after determination of acute toxicity. The anticancer activity and antioxidant potential of the plant were evaluated, as well as the phytochemical composition of petroleum ether and chloroform extracts. Materials and methods Different extracts of K. grandifoliola C.DC. leaves were prepared and tested for hepatoprotective effect against carbon tetrachloride-induced liver damage in rats using silymarin as the reference drug. Anticancer activity was tested on HEPG2 (liver carcinoma cell line), HCT116 (colon carcinoma cell line), HELA (cervix carcinoma cell line), HEP2 (larynx carcinoma cell line), and MCF7 (breast carcinoma cell line). Its potency was compared with the reference drug Doxorubicin. The antioxidant potential was evaluated using 1,1-diphenyl-2-picrylhydrazyl free radical scavenging assay and ascorbic acid as the reference drug. After saponification of the petroleum ether extract, unsaponifiable matter and fatty acid methyl esters were analyzed by GC/MS. The chloroform extract was subjected to vacuum liquid chromatography. Results and conclusion The ethanolic extract of the leaves showed no toxicity up to 5 g/kg. It exhibited potent cytotoxic activity against HCT116 (colon carcinoma cell line) and MCF7 (breast carcinoma cell line), compared with doxorubicin as the standard. Also the ethanolic extract has significant free radical scavenger (100% inhibition) activity, compared with ascorbic acid. The extracts showed significant hepatoprotective and curative activity. GC/MS analysis of both unsaponifiable matter and fatty acids from petroleum ether extract allowed identification of 94.29% of the total unsaponifiable matter, (hentriacontane represented the major component, 11.98%) and 80.72% of the fatty acid methyl ester content (hexadecanoic acid methyl ester represented the major component, 31.68%). Vacuum liquid chromatography of chloroform extract led to isolation of two sterol glucosides (β-sitosterol-3-O-β-d-glucopyranoside and β-stigmasterol-3-O-β-d-glucopyranoside).
  2 2,026 242
Hunting for renal protective phytoconstituents in Artemisia judaica L. and Chrysanthemum coronarium L. (Asteraceae)
Howaida I Abd-Alla, Hanan F Aly, Nagwa M. M. Shalaby, Marzougah A Albalawy, Elsayed A Aboutabl
January-June 2014, 13(1):46-57
Aim This study aimed to evaluate the potential renal protective activity of Artemisia judaica L. and Chrysanthemum coronarium L., belonging to family Asteraceae, collected in Mountains of Tabuk, Kingdom of Saudi Arabia. The ameliorative role of petroleum ether, ethyl acetate, and methanol successive extracts thereof on renal hyperlipidemic and hyperglycemic rats was studied. Active compounds isolated from the bioactive ethyl acetate extract of A. judaica were characterized and identified. Material and methods Hyperlipidemia and hyperglycemia were induced in rats. Evaluation of renal protection was carried out through determination of kidney biochemical markers and histopathological examination. Kidney disorder biomarkers (creatinine and total urea) as well as kidney marker enzyme (glyceraldehyde-3-phosphate dehydrogenase) activity were evaluated. Oxidant-antioxidant status in kidney was assessed by determination of glutathione, lipid peroxide, and nitric oxide. The free radical scavenging activity was performed using 1,1-diphenyl-2-picrylhydrazyl. The extract exhibiting the most significant bioactivity was investigated for its phytoconstituents. Results and conclusion Treatment with A. judaica successive extracts, in particular ethyl acetate, effectively ameliorated diabetic renal dysfunction more than those of C. coronarium. The results revealed improvement in all the investigated parameters, which was confirmed by kidney histopathological analysis. Phytochemicals in the most promising extract (ethyl acetate extract of aerial parts of A. judaica) were isolated and characterized through their physical, chemical, chromatographic, and spectral analyses (UV, MS, 1 H NMR, and 13 C NMR). One sesquiterpene lactone, vulgarin ( 1 ); three triterpenes, taraxerol acetate ( 2 ), β-amyrin ( 3 ), and lupeol ( 4 ); a phytosterol, β-sitosterol ( 5 ); and four flavonoids, lutoelin-3’-methyl ether ( 6 ) and its glycoside, luteolin 3’-methyl ether-7-glucoside ( 7 ), luteolin-6,7,4’-trimethyl ether ( 8 ), and artemetin ( 9 ), were identified. All compounds are reported for the first time in the investigated plant except 1 , 6 , and 7 . The bioactivity may be attributed to the terpenoidal and flavonoidal compounds.
  2 3,386 345
Study of soil mycobiota diversity in some new reclaimed areas, Egypt
Abdel-Nasser A Zohri, Waill A Elkhateeb, Mohamed B Mazen, Mohamed Hashem, Ghoson M Daba
January-June 2014, 13(1):58-63
The objective of this survey was to study the diversity of soil fungi, as they play an important role in knowing the soil quality and increase plant productivity. In this work, the chemical composition of soil samples in newly reclaimed localities at Assiut Governorate was studied; mycobiota of those areas were studied reporting some medically important substances produced by three fungal species, namely Aspergillus terreus, Emericella nidulans, and Penicillium chrysogenum, which recorded the highest occurrence all over the year in different studied areas. Soil samples were collected monthly for a whole year from the four selected reclaimed regions at Assiut Governorate, namely Protectorate of Assiut (PR), El-Ghorayeb (GH), El-Wady El-Assiuty (WA), and Petroleum's Farm (PF), and samples were identified using the morphological and microscopic features according to many references and confirmed by Assiut University Mycological Center (AUMC) followed by physiochemical analysis of soil, including measuring total soluble salts and determining the organic matter content, maximum and minimum temperatures, relative humidity, and soil texture. The highest numbers of fungal genera and species were recorded in PR followed by WA and PF, whereas the lowest numbers were recorded in GH. E. nidulans var. acristata and Penicillium funiculosum were isolated with moderate frequency from GH; Aspergillus aegyptiacus and Aspergillus ustus were isolated with moderate frequency from WA; A. aegyptiacus, Eurotium amstelodami, and Fusarium solani were isolated with moderate frequency from PF; Eurotium repens was isolated only from GH; Arthrinium sacchari, Cochliobolus sativus, and Fusarium xylarioides were isolated only from WA; Aspergillus deflectus, Penicillium expansum, and Rhizopus arrhizus were isolated only from PF; Aspergillus niger, Fusarilla indica, Fusarium semitectum, and Trimmatostroma eriodictyonis were isolated only from PR. There are no adequate mycological studies carried out to describe the fungal flora of these areas. Hence, any information on the endemic mycobiota is of great significance.
  1 2,089 175
Synthesis of nonapeptide (B 22 -B 30 ) of insulin B-chain using modified solid-phase methods with and without microwave energy
Mohamed Aly Zewail, Somaia Abdel Rahman, Ahmed M Naglah
January-June 2014, 13(1):21-26
Background and objectives This work embraced a systematic search for potentiated methodology for peptide synthesis through an approach for convenient synthesis of the nonapeptide B 22 -B 30 of human insulin B chain. The modified solid-phase method with and without microwave technique was used for synthesis of this active part. Materials and methods Nonapeptide Arg-Gly-Phe-Phe-Tyr-Thr-Pro-Lys-Thr-OH corresponding to B 22 -B 30 of human insulin B chain was synthesized using modified solid-phase peptide synthesis. Time consumption, yields, and purity of all products using the different methods were compared with each other. Results and conclusion We can interpret that these results provide a bird's eye view of the benefits of microwave energy with solid phase peptide synthesis (SPPS) in the enhancement of coupling and deprotection reactions in peptide synthesis. In addition, the application of microwave energy with SPPS provides an efficient tool for peptide synthesis, as microwave energy can effectively disrupt intermolecular aggregation and prevent β-sheet formation. Microwave technique proved to be the better approach used for this purpose in the present work. In addition, the advantages of microwave energy include reduced side reactions that result in racemization, cyclization, or premature peptide formation. Microwave energy produces peptides with yields and purity better than the conventional method. It can accelerate the rate of coupling and deprotection reactions, reducing the reaction time from hours to minutes.
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Biologically active fungi recorded for the first time from new reclaimed soil, Egypt
Abdel-Nasser A Zohri, Waill A Elkhateeb, Mohamed B Mazen, Mohamed Hashem, Ghoson M Daba
January-June 2014, 13(1):27-32
Objective This work was designed to record fungal isolates of known biological activities isolated for the first time from new reclaimed soil in El-Wady El-Assiuty and Assiut Petroleum farm in Assiut, Egypt. Materials and methods Soil, phyllosphere, and phylloplane samples were collected from El-Wady El-Assiuty and Petroleum farm, which represent the largest distinctive regions of newly reclaimed soil at Assiut Governorate. Identification of the isolated fungi during our investigation was carried out on the basis of many reported morphological and microscopic features, which was confirmed by Assiut University Mycology Center. Results and conclusion Three fungal species, in addition to one unidentified ascomycete, were isolated for the first time from new reclaimed soil in El-Wady El-Assiuty and Assiut Petroleum farm in Assiut, Egypt. They were identified and recorded by the Mycological Laboratories at Assiut University. They were identified as Arthrinium sacchari (Speg.) M.B. Ellis, which was isolated from the phylloplane of Guava, Beltrania querna Harkn., which was isolated from the soil from Petroleum farm, and Papulaspora immersa Hotson, which was isolated from the phyllosphere of Wheat plants; the newly unidentified ascomyceteous fungal species was obtained from the phyllosphere of pomegranate. The endemic mycobiota of these areas is of great significance, as there are no adequate mycological studies that have been performed to describe the fungal flora of these areas.
  - 2,351 209
Valsartan augments the beneficial effect of rosuvastatin with respect to lipid profile, oxidative stress, and the nitric oxide pathway in high-fat diet-induced hypercholesterolemic rats
Omnia E Baheg, Yousreya A Maklad, Amina Gamal El Din, Manal A Badawy, Sanaa A Kenawy
January-June 2014, 13(1):33-45
Background The renin-angiotensin system contributes considerably to a variety of cardiovascular diseases and is the target of angiotensin receptor blockers (ARBs). Recent studies have reported that in experimental models, as well as some human studies, ARBs had shown the ability to affect lipid metabolism in a modest but significant way. In addition to their primary mode of action, statins and ARBs have common additional properties such as restoration of endothelial activity and antioxidant properties. These properties may potentially aid the improvement treatment of cardiovascular disease. Objective The present study was designed to evaluate the possible beneficial effects of both therapies valsartan (ARB) and rosuvastatin (3-hydroxy-methylglutaryl coenzyme reductase inhibitor) beyond their blood pressure-lowering and cholesterol-lowering effects, and the possibility that valsartan may enhance the beneficial effects of rosuvastatin in high-fat diet-induced hypercholesterolemic (HC) rats with respect to lipid profile, oxidative stress, and the nitric oxide pathway. Materials and methods HC was induced in male albino Wistar rats by a daily gavage of a cocktail containing 1 l peanut oil, 100 g cholesterol, and 100 g cholic acid over a period of 21 days. These animals were assigned randomly to the following groups: HC, HC/rosuvastatin, HC/valsartan, and HC/rosuvastatin+valsartan. Results Daily gavage of the cocktail for 3 weeks induced a significant increase in plasma total cholesterol (TC), triglyceride (TG), and low-density lipoprotein and a significant reduction in high-density lipoprotein (HDL), but did not induce any significant changes in arterial blood pressure and heart rate. Meanwhile, the plasma nitric oxide level was reduced to 17.49% of its normal level and the plasma malondialdehyde level was significantly increased by 32.53%. Coadministration of valsartan with rosuvastatin normalized plasma HDL, significantly decreased plasma TC and low-density lipoprotein to a greater extent than monotherapy with each drug as well as ameliorated the effect of HC diet on the plasma TG level in HC rats. Moreover, the combined treatment induced a significant increase in the plasma nitrate+nitrite level compared with the corresponding HC value and normalized the plasma malondialdehyde level with respect to the effect of rosuvastatin or valsartan alone. In addition, histopathological and morphometric studies of the aorta and liver showed marked improvement after combined treatment with rosuvastatin and valsartan when compared with the HC group. Conclusion Conclusively, coadministration of rosuvastatin and valsartan in high-fat diet-induced HC rats conferred a greater degree of protection as it ameliorated the increase in the plasma TC and TG and restored HDL to its normal value, improved the endothelial function, and reduced oxidative stress, together with improvement in the histopathological features in rats that had previously received a high-fat diet.
  - 2,603 274
Survey of all mycobiota associated with rhizosphere and rhizoplane of different cultivated plants in new reclaimed soil, upper Egypt, and examination of the most common fungal isolates to produce mycotoxins
Abdel-Nasser A Zohri, Waill A Elkhateeb, Mohamed B Mazen, Mohamed Hashem, Ghoson M Daba
January-June 2014, 13(1):64-70
This survey was designed to study the diversity and occurrence of rhizosphere and rhizoplane fungi in the protectorate of Assiut in Egypt, followed by testing the ability of the most common isolated fungal strains to produce mycotoxins. Not many mycological studies have been carried out to describe the fungal flora of this area, which will be of great significance for the endemic mycobiota. Rhizosphere and rhizoplane samples were collected from the protectorate of Assiut, which represents one of the largest distinctive regions of newly reclaimed soil at the Assiut Governorate. The identification of the isolated fungi during our investigation was carried out using the morphological and microscopic features according to many references and confirmed by the Assiut University Mycology Center (AUMC). The most common four fungal species were examined for their capability to produce mycotoxins; in addition, chemical confirmatory tests for mycotoxins were examined.
  - 1,811 199