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   2014| July-December  | Volume 13 | Issue 2  
    Online since December 18, 2014

 
 
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ORIGINAL ARTICLES
Synthesis, antifungal activity, and molecular docking study of some novel highly substituted 3-indolylthiophene derivatives
Heba M Abo-Salem, Eslam R El-Sawy, Ahmed Fathy, Adel H Mandour
July-December 2014, 13(2):71-86
DOI:10.4103/1687-4315.147064  
Background and objectives The currently available antifungal drugs have the limitations of toxicity, potential drug interaction with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with less toxicity is urgently required. The present work aimed to synthesize new 3-indolylthiophene derivatives and evaluate their antifungal activity by studying their molecular docking. Materials and methods New series of thiadiazoles 4a-c , morpholinyl-acetamides 6a-c , 4-methylpiperazinylacetamides 7a-c , thiazolidines 10a-c , azetidines 12a-c - 13a-c , sulfonamides 14a-c - 15a-c , benzamides 16a-c , pyrrolidines 17a-c , succinamic acids 18a-c , acetamides 19a-c , thieno(2,3-c)pyridines 20a-c , thieno(2,3-e)-1,2,4-triazolo(1,5-c)pyrimidines 23a-c , thieno(2,3-d) pyrimidines 24a-c - 26a-c , and thieno(2,3-b)pyridines 27a-c derivatives incorporated into N-substituted 3-indolylthiophenes were prepared by an initial reaction of 2-amino-4-(N-substituted-1H-indol-3-yl)thiophene-3-carbonitriles 1a-c with different reagents. The antifungal activity of the newly synthesized compounds was evaluated against two strains of fungi, namely, Candida albicans (ATCC-10231) and Aspergillus niger (ATCC-10535). However, the mode of action of the most promising antifungal compounds was assessed by docking with cytochrome P450 14 α-sterol demethylase (CYP51) (PDB ID: 1EA1). Results and conclusion Compound 4a showed good inhibitory activity against both C. albicans (ATCC-10231) and A. niger ( ATCC-10535), with minimum inhibitory concentrations values of 9 and 36 μg/disk, respectively, compared with fluconazole, with minimum inhibitory concentrations values of 8 and 34 μg/disk. Docking results showed that compound 4a had the highest docking score, with a binding energy of −30.25 kJ/mol, which is in agreement with the experimental activity value.
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A pharmacognostical study of Vernonia cinerea Less (Asteraceae) and evaluation of anti-inflammatory and antibacterial activities of stem
Anupama Singh, Vikas A Saharan, Indar C Kumawat, Abhishek Khatri, Anil Bhandari
July-December 2014, 13(2):104-112
DOI:10.4103/1687-4315.147069  
Aim This study aimed to establish the pharmacognostical characteristics of leaf, stem and root of Vernonia cinerea, Asteraceae (ash-coloured fleabane), and to verify the anti-inflammatory and antibacterial activities of various extracts of the stem. Background V. cinerea (Asteraceae) is traditionally used to treat inflammation, diarrhoea, cough, smoking cessation, asthma, Parkinson's disease and leprosy. Materials and methods Leaf, stem and root and their powders were examined microscopically, and pharmacognostic standardization parameters were determined according to WHO guidelines. Extracts of different organs of the plant in petroleum ether, chloroform, ethanol, ethanol (50%) and water were prepared and examined by thin-layer chromatography. An antibacterial assay of the stem extracts for Staphylococcus aureus was performed. The anti-inflammatory activity of the same extracts was studied using a carrageenan-induced paw oedema model in Wistar rats. Results and conclusion Microscopic characterization of the different organs of the plant indicated the presence of trichomes, arrangement of vascular bundles (stem: radial, root: scattered), anomocytic and diacytic stomata, and wavy epidermal cells in stomata. The antibacterial assay indicated a zone of inhibition of 20 ± 0 and 19.33 ± 0.33 mm with alcoholic and chloroform extracts of V. cinerea leaf, respectively (extracts of stem showed a zone of inhibition of 21.00 ± 0.57 and 21.00 ± 0.57 mm, respectively). Diclofenac sodium and chloroform extract showed 11.11% inhibition of inflammation, whereas 16.66 and 13.33% inhibition were observed with alcoholic and hydroalcoholic extracts, respectively. Microscopic and pharmacognostic parameters aid in the identification and characterization of different organs of the plant. Traditional claims of antimicrobial and anti-inflammatory activities of the stem have been verified. Various extracts showed significant results for anti-inflammatory and antimicrobial action.
  3,925 465 1
Development and evaluation of taste-masked satranidazole granules by the polymer-coating technique
Harshal A Pawar, Pooja R Joshi, Pooja R Gharat, Damayanti Singh
July-December 2014, 13(2):87-94
DOI:10.4103/1687-4315.147065  
Background and objective The objective of the present study was to mask the bitter taste of satranidazole and develop a formulation that is easy to swallow and provides quick relief in amoebiasis. Materials and methods Taste-masked granules were formulated by the wet granulation method and further coated by spraying a coating solution of Eudragit E100. Various batches of granules were prepared by coating with different concentrations of the coating solution. The formulated granules were evaluated for taste masking by in-vivo and in-vitro methods. The granules were tested for their flow property, in-vitro drug release, drug content, granular friability, and size distribution. Scanning electron microscopy of coated and uncoated granules was performed. The optimized batch was subjected to a stability study. The in-vitro release of the drug from granules was compared with that of the marketed tablet formulation. Results and conclusion The formulated granules were found to possess good flow property. Differential scanning calorimetry and Fourier-transform infrared studies confirmed no interaction between the drug and the excipients. The taste-masked granules of the optimized batch showed 99.21% release of the drug within 15 min. The in-vitro release of the drug from granules was found to be better than that of the marketed tablet formulation. The optimized granular formulation was found to be palatable and to provide quick relief in amoebiasis.
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Study of some biological activities of aqueous extract of ginger (Zingiber officinale)
Mohamed MI Helal, Mona Y Osman, Madeha OI Ghobashy, Wafaa A Helmy
July-December 2014, 13(2):144-150
DOI:10.4103/1687-4315.147093  
Purpose This study was designed to evaluate the potential of two aqueous extracts of ginger rhizome under different extraction conditions (cold and hot water). Materials and methods Anticoagulant, fibrinolytic, antimicrobial, prebiotic, and antitumor activities were examined for the two aqueous extracts. The two aqueous extracts were then used for evaluation of yield, total carbohydrates, protein, and monosaccharide contents. The sulfation of crude extracts was carried out by chlorosulfonic acid as a sulfating agent in formamide. Results The results showed that sulfation modification of the two aqueous extracts increased significantly both the anticoagulation and the fibrinolytic activities, but did not affect the antimicrobial, prebiotic, or antitumor activities. However, the two native water extracts showed antibacterial activity against Escherichia coli only, but not for Staphylococcus aureus, and antifungal activity against Candida albicans. Conclusion The chemical modification of the two aqueous extracts of ginger by sulfation will increase significantly its anticoagulation and fibrinolytic activities while not affecting or improving the prebiotic and antimicrobial activities. However, the antitumor activity is high for both the native and the sulfated aqueous extracts of ginger. Thus, this result does not mean that the sulfation modification of the water extracts studied affected the antitumor activity.
  3,257 442 2
Antidiabetic and biochemical effects of new flavonols extracted from Justicia ghiesbreghtiana stem
Reham E Shafek, Nabila H Shafik, Helana N Michael, Emad F Eskander
July-December 2014, 13(2):95-103
DOI:10.4103/1687-4315.147066  
Background and objective The main aim of this study was to examine the biochemical effects of two new natural flavonoid compounds isolated from Justicia ghiesbreghtiana stem extract on diabetes mellitus type II. Materials and methods One kilogram air-dried stems of J. ghiesbreghtiana were exhaustively extracted with 75% aqueous ethanol several times by heat treatment. The resulting extract was fractionated on a Sephadex LH-20 column using water and water/ethanol mixtures as eluents to yield six fractions, from which two new pure natural compounds 1 and 2 were isolated. The antidiabetic effect of compounds 1 and 2 was investigated in this study using 40 adult male rats. Results and conclusion Phytochemical investigation of the ethanolic extract of J. ghiesbreghtiana stem has led to the isolation of nine pure flavonoid compounds of quercetin type; two of them are new and have been identified as quercetin 3-O-α-l-arabinofuranoside-7-O-α-l-rhamnopyranoside-4′-O-β-d-galactopyranoside (1) and quercetin 3-O-α-l-arabinofuranoside-7-O-β-d-glucopyranoside-4′-O-β-d-galactopyranoside (2); in addition, two quercetin diglycosides, four quercetin monoglycosides, and aglycone quercetin were obtained. Their chemical structures have been established by conventional methods of chemical and physical analysis and confirmed by nuclear magnetic resonance spectroscopy. The biochemical study of compounds 1 and 2 on diabetic rats indicated improvement in kidney functions shown by reductions in both urea and creatinine levels. Moreover, glutathione peroxidase and superoxide dismutase concentrations were increased. Also, albumin and total protein levels were reduced, with an increase in liver functions, aspartate aminotransferase, and alanine aminotransferase levels, with a mild decrease in both cholesterol and triglyceride concentrations.
  1,911 531 -
Spectrophotometric microdetermination of tranexamic acid in pharmaceutical formulation
Manal S Kamel, Fatma A Bassyouni, Barsoum N Barsoum
July-December 2014, 13(2):151-159
DOI:10.4103/1687-4315.147096  
Background and objectives Tranexamic acid is used to treat various conditions in which there is bleeding or risk of bleeding, such as prostatectomy, dental extraction, menorrhagia, and thrombolytic overdose. Most of the currently available analytical techniques for Tranexamic acid measurement use high-performance liquid chromatography (HPLC) separation or the spectrophotometric method of detection. The aim of the present study was to describe the determination of Tranexamic acid as an active pharmaceutical ingredient in tablets using three accurate and sensitive spectrophotometric methods: the ion-air complex method (method A), the bromination complex method (method B), and the charge transfer complex method (method C). Materials and methods The first method (A) is based on the formation of an ion-pair complex between the basic nitrogen of Tranexamic acid and alizarin red S as an anionic acid dye. The absorbance of the formed complex was measured at λmax equal to 300 nm. The second method (B) is based on the oxidation of Tramexamic acid by N-bromosuccinimide (NBS) and determination of the nonreacted NBS by measurement of the decrease in absorbance of liberated iodine at λmax equal to 520 nm. The third method (C) is based on forming a charge transfer complex with chloranil in absolute ethanol at alkaline pH. The absorbance of the formed charge transfer complex was measured at λmax equal to 330 nm. Linear calibration curves were obtained in the ranges of 2.00-26.00, 2.00-25.00, and 2.00-27.00 μg/ml. The methods showed relative standard deviations of 0.839, 0.952, and 0.984 for methods A, B and C, respectively. Results and conclusion The results showed the suitability, safety, accuracy, and simplicity of these methods for determination of Tranexamic acid as an active pharmaceutical ingredient. The results obtained by the three methods, A, B, and C, is in good agreement with those obtained by the official method. The developed methods were successfully applied to the determination of Tranexamic acid in pharmaceutical preparation (tablets).
  1,885 180 -
Synthesis and antimicrobial activity of some amino acids and sulfamoyl and pyrrole derivatives attached to 4-benzoimidazol-2-yl moiety
Eman A Abd El-Meguid
July-December 2014, 13(2):113-120
DOI:10.4103/1687-4315.147072  
Background and objectives Benzoimidazole moiety is one of the heterocyclic compounds that plays a vital role in biological fields such as antioxidant, antidepressant, anticonvulsant, antimicrobial and anticancer. The aim of this study was to construct new compounds containing 4-(5-benzoyl-benzoimidazol-2) moiety incorporated into different amino acids and sulfamoyl and/or pyrrole analogues and to evaluate their antimicrobial activities. Materials and methods The starting material 4-(5-benzoyl-1H-benzoimidazol-2-yl)-benzonitrile ( 2 ) was prepared through the reaction of (3,4-diamino-phenyl)-phenyl-methanone ( 1 ) with 4-cyanobenzaldehyde in absolute ethanol. Stirring compound 2 with 70% sulfuric acid gave benzoic acid derivative 3 followed by esterification and refluxing with hydrazine hydrate to form the corresponding 4-(5-benzoyl-1H-benzoimidazol-2-yl)-benzoic acid hydrazide ( 5 ). A series of derivatives 6a-d were prepared by coupling of benzoic acid derivative 3 with different amino acids ethyl ester. Reacting ester compound 4 with different amines and sulfa drugs led to the formation of the amides derivatives 7a,b and 8a,b , whereas on reacting the hydrazide compound 5 with different acid anhydrides, cyclohexane-1,4-dione and 5-nitroisatin compounds 9a-c , 10 and 11 were obtained. Results and conclusion Most of the test compounds were found to be significantly effective against Bacillus subtilis and Staphylococcus aureus (gram-positive bacteria), Escherichia coli and Pseudomonas aeuroginosa (gram-negative bacteria) and Candida albicans and Aspergillus niger (fungi) .
  1,740 252 1
Effect of five plant extracts on adhesion of Candida albicans onto human buccal epithelial cells: an in-vitro study
Jain Amrath Pavithra, G Srinikethan, C Shubhada, K Pradeep, Mugeraya Gopala, Raghavendra Kulkarni, KR Praveenchandra
July-December 2014, 13(2):137-143
DOI:10.4103/1687-4315.147089  
Background There is increased prevalence of both fluconazole-resistant Candida albicans and non-albicans Candida spp. isolated from oral candidiasis (OC) lesions. OC is the most common oral lesion, encountered in HIV infection. On the basis of this, the antiadherence approach to treat or prevent oropharyngeal candidiasis was studied using plant extracts. Aim The present study aimed to perform preliminary screening of five plant extracts, namely, aloe vera, Singapore cherries, tea tree, neem, and lemon grass, for their effect on adhesion of C. albicans to human buccal epithelial cells (HBEC) in an in-vitro condition. Materials and methods A set of 5 and 10 g of plant material, leading to a final concentration of 10 and 20%, respectively, was used. Both aqueous and ethanol extracts were tested. Both C. albicans and HBEC were treated with plant extracts under different in-vitro conditions. An adhesion assay was carried out under an in-vitro condition. C. albicans, RL-24 and RL-112, isolated from OC lesions in HIV-seropositive individuals were analyzed for adhesion. The adhesion pattern of C. albicans to HBEC under test conditions was compared with the adhesion pattern observed under the control condition. The variation in adhesion was recorded. Statistical analysis Statistical analysis was carried out by two-way analysis of variance using IBM SPSS-version 20. Results Both aqueous and ethanol extracts of neem. followed by lemon grass were found to consistently inhibit adhesion, which was statistically significant. Conclusion This preliminary work has shown a trend that different plant extracts could efficiently inhibit the adherence of C. albicans to HBEC and can be explored for an antiadherence therapeutic approach. Development of antiadherent agents using plant extracts seems to be a promising approach in the treatment of OC.
  1,733 254 -
β-Glucosidase production by mixed culture using crude hemicellulose from rice straw black liquor and peat moss as an inert support
Hoda M. A. Shata, Azza M Noor El-Deen, Galal A Nawwar, Mohamed A Farid
July-December 2014, 13(2):121-129
DOI:10.4103/1687-4315.147074  
Background and objectives Rice straw black liquor (RSBL) has no commercial significance and causes environmental pollution because of its poor disposal, although it holds promise as a cheap substrate for the production of β-glucosidase. The objective of the present work was to improve and optimize the cultural conditions of mixed cultures of Trichoderma reesei NRRL 6165 and Aspergillus niger NRC 9A under solid-state fermentation (SSF) for the production of β-glucosidase using crude hemicellulose (CHC) prepared from RSBL and peat moss as an inert support. Materials and methods Mixed cultures of the mycelial fungi T. reesei NRRL 11236 and T. reesei NRRL 6165 and A. niger strains (NRC 5A, NRC 7A, and NRC 9A) were evaluated for their ability to produce β-glucosidase using CHC prepared from RSBL and peat moss as an inert support under SSF. Optimization of initial pH (4-8), supplementation with different concentrations of corn steep liquor and ammonium sulfate, the initial moisture content (63.6-87.4% v/w), inoculum size and ratio of microorganisms, CHC/peat moss ratio, and incubation time (0-14 day) were studied. The extracted enzyme was assayed using p-nitrophenyl-β-d-glucopyranoside as a substrate. Data analysis was performed by one-way analysis of variance using computer software Minitab 16. Results and conclusion Mixed cultures of the mycelial fungi T. reesei NRRL 11236 and T. reesei NRRL 6165 and A. niger strains (NRC 5A, NRC 7A, and NRC 9A) were evaluated for their ability to produce β-glucosidase using CHC prepared from RSBL and peat moss as an inert support under SSF. The most potent coculture composed of A. niger NRC 9A (192.39 ± 7.37 U/g CHC) and T. reesei NRRL 6165 (12.56 ± 0.42 U/g CHC) was used in a mixed culture to enhance β-glucosidase production by coculturing under SSF. In mixed culture, β-glucosidase of the coculture (265.32 ± 0.25 U/g CHC) was nearly 1.3-fold and 10.6-fold than that of monocultures of A. niger NRC 9A and T. reesei NRRL 6165, respectively. Optimization of the environmental and culture parameters, different solid supports, concentration of nitrogen sources (ammonium sulfate and corn steep liquor), initial pH value, CHC/peat moss ratio, inoculum size and ratios of the two strains, moisture content, and incubation time exhibited a significant increase (466 ± 5.42 U/g CHC) in β-glucosidase production compared with before optimization. The study demonstrated that a substrate that does not find any commercial significance and causes environmental pollution because of its poor disposal holds promise as a cheap substrate for the production of β-glucosidase.
  1,584 176 -
Improved mannanase production from Penicillium humicola and application for hydrolysis property
Mona A El-refai, Om Kalthoum H Khattab, Siham A Ismail, Amal M Hashem, Amany A Abo-Elnasr, Shaimaa A Nour
July-December 2014, 13(2):160-167
DOI:10.4103/1687-4315.147102  
Objectives The aim of this research is to produce β-mannanases from a new microbial source using wastes in their nutrition medium. The enzyme produced can be used for the production of galactomanno-oligosaccharides, which are very useful in the health and medical fields. Materials and methods Seven fungal strains and five bacterial strains were tested for the production of β-mannanases. Enzyme activity, protein content, and biomass production were determined in all the cultures produced using standard methods. Optimization studies to maximize enzyme production from the most potent microorganisms, including culture conditions and medium compositions, were also carried out. Preliminary studies for the production of galactomanno-oligosaccharides from locust bean gum using partially purified enzymes were also carried out and followed by thin-layer chromatography techniques and Somogyi methods. Results and conclusion The highest mannanase activities were produced by Penicillium humicola (8.8 U/ml) and Penicillium spp. v (7.75 U/ml) in shaking cultures after 10 days using gum locust bean as a carbon source. Among 13 carbon sources examined, coffee residue and ceratonia seeds were the best carbon sources (10.3 and 8.9 U/ml, respectively) for P. humicola, whereas the best nitrogen source was a mixture of peptone, urea, and ammonium sulfate for the same microorganism. The optimum temperature and pH for enzyme reaction was 55 and 5.5°C, respectively. The enzyme was thermostable and retained 80% of its activity after 1 h at 50°C. The highest reducing sugar of 8900 μg/ml was obtained from locust bean gum hydrolytes after 28 h.
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Synthesis and antimicrobial evaluation of some novel benzoimidazole Schiff's bases and their C-nucleoside derivatives
Eman A Abd El-Meguid, Nayera AM Abdelwahed
July-December 2014, 13(2):130-136
DOI:10.4103/1687-4315.147082  
Background and objectives The discovery of C-nucleosides and continuous study of their biological activities led us to construct new compounds containing 4-(5-benzoyl-benzoimidazol-2)-benzoic acid hydrazide Schiff's bases incorporated into different aldoses, thiazolidinones, and/or their C-nucleoside analogues. The aim of this study is to describe the synthesis of some new heterocycles derived from 4-(5-benzoyl-benzoimidazol-2)-benzoic acid hydrazide and to evaluate their antimicrobial activities. Materials and methods The starting material 4-(5-benzoyl-1H-benzoimidazol-2-yl)-benzonitrile ( 2 ) was prepared through the reaction of (3,4-diamino-phenyl)-phenyl-methanone ( 1 ) with 4-cyanobenzaldehyde in absolute ethanol. Stirring compound 2 with 70% sulfuric acid yielded benzoic acid derivative 3 , followed by esterification and refluxing with hydrazine hydrate to yield the corresponding 4-(5-benzoyl-1H-benzoimidazol-2-yl)-benzoic acid hydrazide ( 5 ). A series of Schiff's bases derivatives 6a-c and 8a-e were prepared by condensation of hydrazide 5 with different monosaccharides and/or with arenaldehydes. Treatment of 6a-c with thioglycolic acid led to the formation of the C-nucleosides ( 7a-c ), whereas treatment of 8a-e with thioglycolic acid yielded the corresponding 2-arylthiazolidin-4-one ( 9a-e ). Results and conclusion Compound 6b showed the highest antimicrobial activity against Bacillus subtilis, Staphylococcus aureus (gram-positive bacteria), Escherichia coli, and Pseudomonas aeuroginosa (gram-negative bacteria), and Candida albicans and Aspergillus niger (fungi) .
  1,364 144 -
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