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  Citation statistics : Table of Contents
   2015| January-April  | Volume 14 | Issue 1  
    Online since April 8, 2015

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Levofloxacin: formulation and in-vitro evaluation of alginate and chitosan nanospheres
Ramadoss Arun Balaji, Sathya Raghunathan, Radhakrishnan Revathy
January-April 2015, 14(1):30-35
Background and objectives Levofloxacin, the active l-isomer of ofloxacin, is a widely used fluoroquinolone, with activity against bacteria that causes respiratory, skin, and genitourinary tract infections, (-)-(S)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido benzoxazine-6-carboxylic acid hemihydrates. It is a new quinolone antimicrobial agent that exhibits broad-spectrum in-vitro bactericidal activities against gram-positive and gram-negative aerobes. The aim of this study was to formulate sodium alginate nanospheres containing levofloxacin and evaluate its physiochemical properties, exploring alternative routes of administration, such as nanoparticle to develop a targeted drug delivery system and to act locally on the organ of infection with enriched therapeutic efficacy. Materials and methods Sodium alginate and calcium chloride solutions were prepared. A constant volume (20 μl) of levofloxacin solution was incorporated into the sodium alginate solution, and then the same method was followed for the preparation of hybrid chitosan-alginate nanoparticles. In-vitro release study was carried out by dialysis membrane for 7 h in the physiological fluid (pH 7.4 phosphate buffer solution). Morphology and structure characterization of nanoparticles were investigated by field emission scanning electron microscope and Fourier transform infrared spectra, zeta potential, X-ray diffraction, particle size analysis, respectively. Results and conclusion This paper reports the possibility to entrap lipophilic levofloxacin within chitosan/alginate (CS/ALG) nanoparticles using a very simple ionotropic pregelation technique; strong electrostatic interactions exist in the nanoparticles. The nanoparticles with a diameter of 25-55 nm were obtained at the optimal mass range of sodium alginate: calcium chloride:chitosan in the meta acid environment. The delivery behavior of levofloxacin from nanoparticles was studied. Levofloxacin released from chitosan-alginate nanoparticles was 71% at pH 7.4 within 7 h. The release profile was characterized by an initial burst effect in phosphate buffer solution, followed by a continuous and controlled release phase. The drug release mechanism from polymer also offers an interesting potential for the delivery of lipophilic compound.
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Production and prebiotic activity of exopolysaccharides derived from some probiotics
Magdel-Din M Hussein, Mohamed F Ghaly, Mona Y Osman, Al Shimaa G Shalaby, Mohamed MI Helal
January-April 2015, 14(1):1-9
Objective The aim of this study was to focus on exopolysaccharides (EPSs) produced by Lactobacillus delbrueckii bulgaricus, Lactobacillus helveticus or Lactobacillus casei and their use as a prebiotic for Lactobacillus reuteri, Lactobacillus rhamnosus, Lactobacillus acidophilus or Bifidobacterium bifidum. Materials and methods Optimization of culture conditions using different carbon and nitrogen sources and different temperature, pH and incubation periods for maximum EPS production was studied. Results and conclusion It was found that the best conditions were as follows: the use of sucrose (20%) instead of glucose in MRS medium, incubation at pH 7.0 and temperature 37°C for 72 h incubation under anaerobic conditions to give the highest EPS yield; a yield of 13.99 g/l was recorded in case of L. helveticus when grown on the aforementioned optimized conditions. It was found that L. delbrueckii bulgaricus EPS has the highest prebiotic indices (I), varying from 7.9 to 10.1. In contrast, L. helveticus and L. casei EPSs have the lowest prebiotic indices (I), varying from 1.4 to 2.4.
  10 4,716 686
Estimation of total phenolic, tannins, and flavonoid contents and antioxidant activity of Cedrus deodara heart wood extracts
Sourabh Jain, Aakanchha Jain, Sanjay Jain, Neelesh Malviya, Vikas Jain, Dharmendar Kumar
January-April 2015, 14(1):10-14
Purpose The present study was investigated to determine in-vitro antioxidant activity and total phenolic, total flavonoids, and total tannins contents of extracts of Cedrus deodara heart wood. Materials and methods Antioxidant activity of aqueous and alcoholic extract of C. deodara heart wood was evaluated against 2,2-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 1,1-diphenyl-2-picryl hydrazyl (DPPH), and hydroxyl radical-scavenging activity models. Total flavonoids, tannins, and phenolic content of C. deodara were also determined. Results and conclusion Among both extracts, aqueous extract showed the highest total phenolic contents (23.97 μg/g of gallic acid equivalent/g of extract). In DPPH, superoxide anion, and ABTS scavenging test, the IC 50 (μg/ml) value of aqueous and alcoholic extract was 61.89, 75.79, 87.76, 121.55, 115.29, and 122.42, respectively. Hence, the above evidences suggest that C. deodara heart wood is a potential source of natural antioxidant and can be used to prevent diseases associated with free radicals.
  4 6,421 721
Isolation and microbiological identification of bacterial contaminants in food and household surfaces: How to deal safely
Amal S Othman
January-April 2015, 14(1):50-55
Objective This study investigates and reveals the relationship between pathogenic bacteria in some types of food and that present in different household sites (kitchens) and determines an effective disinfecting method to eliminate bacteria from common kitchen locations, some of which could be harmful or pathogenic. Materials and methods A total of 90 samples were collected; 85 samples were taken from different sites from five home kitchens and five samples were collected from different types of food. Samples were obtained (before and after disinfection) from kitchen towels, cooking gas stove knobs, refrigerator handles, water taps, and kitchen sponges used for washing utensils by using sterile cotton swabs. Bacteria were identified according to the conventional biochemical methods. DNA fragmentation was done to show the effect of disinfectants on the most common bacteria. Results and conclusion Escherichia coli , Klebsiella spp., and Staphylococcus aureus were the most abundant bacteria in the isolates. After disinfection using disinfectants containing sodium perborate and sodium silicate (detergent), sodium hypochlorite (Clorox), 5% amphoteric surfactant and chlorine (dishwashing powder), and Dettol, the samples were free of bacterial contamination. There was also a correlation between food contamination and bacteria isolated from the kitchens. As E. coli was the most highly abundant pathogen in the kitchen and was removed by the tested disinfectants, it was chosen for DNA fragmentation assay to examine the effect of the disinfectants on the bacterial DNA. Kitchen towels, cooking gas stove knobs, refrigerator handles, water taps, and kitchen sponges are the most common sites in kitchens that transmit pathogenic bacteria. They must be disinfected routinely after preparing food.
  4 36,911 2,080
The composition of the lipoidal matter of the seeds of Pleiogynium timorense (DC.) Leenh
Ataa A Said, Elsayed A Aboutabl, Ahmed A Hussein, Gehan F Abdel Raoof
January-April 2015, 14(1):65-68
Background and objectives Nothing dealing with the chemistry of the seeds of Pleiogynium timorense (DC.) Leenh. could be traced in the available literature. The objective of the present work was to investigate the lipoidal matter from P. timorense seeds and to isolate and identify the major sterols and triterpenes in the petroleum ether extract. Materials and methods The petroleum ether extract of P. timorense seeds was prepared. The extract was subjected to column chromatography using silica gel (type 60-230 mesh) as an adsorbent. The unsaponifiable matter and fatty acid methyl esters were analyzed by GC/MS. Results and conclusion GC/MS analysis of the unsaponifiable matter from the petroleum ether extract of P. timorense seeds revealed the identification of 70.04% of unoxygenated compounds and 23.34% oxygenated compounds. Hydroxylated compounds, ketones, and steroidal compounds represent 23.24, 0.20, and 3.19%, respectively. 1-Heptene (66.47%) was the major compound in the USM, followed by butylated hydroxy toluene (21.07%). GC/MS analysis of fatty acid methyl esters showed that nine fatty acid methyl ester derivatives could be identified, representing 95.84% of the total composition. The major fatty acid was 9,12-octadecadienoic acid (linoleic acid) (33.8%). Saturated fatty acids represent 36.93% of the total fatty acid content, whereas monounsaturated and diunsaturated fatty acids represent 25.11 and 33.8% of the total fatty acid content, respectively. Column chromatography of the petroleum ether extract led to the isolation of two compounds [α-amyrin and 5,24(28)-cholestadien-24-methylen-3β-ol].
  2 1,887 165
Synthesis, cytotoxic, proapoptotic evaluation, and molecular docking study of some new N-substituted sulfonyl-3-indolyl heterocycles
Eslam R El-Sawy, Heba M Abo-Salem, Shaymaa M Yahya, Manal S Ebaid, Adel H Mandour
January-April 2015, 14(1):15-29
Background and objectives Apoptosis, also called programmed cell death, is a fundamental biological phenomenon that plays a crucial role in processes such as immune regulation, embryogenesis, and general tissue homeostasis. B-cell lymphocyte/leukemia-2 (BCL-2) family members are key regulators of apoptosis. The ability of the indole derivative to disrupt microtubule assembly and induce G2/M arrest, polyploidy, and apoptosis through mitochondrial pathways in COLO 205 cell has been reported; in addition, it reduced the levels of procaspase-3, procaspase-9, BCL-xL, and BCL-2 gene. The aim of this study is to describe the synthesis of some new N-substituted sulfonyl-3-indolyl heterocycles and to study their cytotoxic and proapoptotic effects. In addition, a molecular docking study of the most biologically active compounds against the BCL-2 protein is discussed. Materials and methods A new series of triazolopyridines 3a-c , diaminopyridines 4a-c , acetamides 5a-c , triazolo[1,5-a]pyridines 6a-c-8a-c , pyrido[1,2-b][1,2,4]triazines 9a-c , 10a-c , pyrazoles 11a-c, 12a-c , and pyrimidine derivatives 13a-c-15a-c were prepared by an initial reaction of 2-((N-substituted sulfonyl-1H-indol-3-yl)methylene) malononitriles 2a-c with different reagents. The newly synthesized compounds were tested for their cytotoxic activity against the HepG2 cell line. The compounds that showed promising IC 50 values were chosen for the study of their proapoptotic effect on the BCL-2 gene, which is an antiapoptotic factor, and they significantly inhibited the expression levels of the BCL-2 gene. The binding mode of the most promising proapoptotic compounds was assessed by docking studies with the CHIMAERIC BCL2-XL protein (PDB ID: 2W3L). Results and conclusion From the data obtained, the most active compounds against the HepG2 cancer cell line were in the descending order of 10b>4c>10a>10c , whereas compounds 3c , 6c , 9c , 4b , and 5c showed moderate to slight growth inhibition. Compounds 4c , 5c , 9c , 10a , 10b , and 10c significantly inhibited the expression levels of the BCL-2 gene. Docking results showed that compounds 5c and 9c showed good fitting within the pocket site of the protein molecular surface and had a minimum binding energy of −20.29 and −18.98 kJ/mol, respectively, in comparison with the co-crystallized ligand, which is in agreement with the experimental result of a proapoptotic effect.
  2 2,487 358
Phytoconstituents from Curcuma longa L. aqueous ethanol extract and its immunomodulatory effect on diabetic infected rats
Manal H Shabana, Eman M Shahy, Mona M Taha, Gehan M Mahdy, Maha H Mahmoud
January-April 2015, 14(1):36-43
Background and objectives Curcuma longa L. (C. longa) has been shown to possess a wide variety of pharmacological properties against malignant proliferation, inflammation, and parasitosis. Further, C. longa has been reported to possess antioxidant and hypoglycemic activities. The aim of this study was to isolate and elucidate the structure of the phytoconstituents of turmeric and test the hypoglycemic, antioxidant, antibacterial, and anti-inflammatory properties of the alcohol extract of C. longa on diabetic rats infected with Staphylococcus aureus. Materials and methods The extraction and isolation of the constituents of C. longa were performed according to the standard methods of column, paper, and thin-layer chromatography. The chemical structure of the isolated compounds was established by R f , by characterization of acid hydrolysates, by ultraviolet spectral analysis, and by 1 H-NMR spectroscopy. Serum glucose, immunoglobulin E (IgE), nitric oxide, cytokine levels (IL-6, TNF-α, and IL-1β), and blood cell counts (total and differential) were determined. Results and conclusion Three compounds were isolated from the alcohol extract of C. longa. These compounds were identified as apigenin 7-O-rhamnoside 4′-O-glucoside, a new compound isolated for the first time from nature, and 7-methoxyapigenin-6-C-glucoside and N-(3-methoxyphenyl) acetamide, two known compounds isolated from C. longa for the first time. Also, the alcohol extract of C. longa ameliorated the serum glucose, IgE, nitric oxide, and cytokine levels in diabetic infected rats with S. aureus.
  2 3,432 339
Evaluation of bronchodilatory properties of fruits of Opuntia elatior Mill
Sanjay P Chauhan, Navin R Sheth, BN Suhagia
January-April 2015, 14(1):44-49
Background Traditionally, fruits of Opuntia elatior Mill. were used for their immunomodulatory and antiasthmatic action. The presence of potentially active nutrients and their multifunctional properties make prickly pear a perfect candidate for the production of phytopharmaceutical products. Objective The objective of the present study was to evaluate the bronchodilatory properties of fruits of O. elatior Mill. Materials and methods The bronchodilatory properties were evaluated using bronchospasm induced by acetylcholine and histamine, anticholinergic action on isolated rat ileum, and antihistaminic action on isolated guinea pig ileum. Result and discussion Bronchodilating effect of fruit juice was dose dependent against spasm induced by acetylcholine and histamine. O. elatior Mill. fruits possess a significant inhibitory effect on rat and guinea pig ileum contraction through antihistaminic and antimuscarinic action. Conclusion This study suggested that fruits of O. elatior Mill. possess a significant inhibitory effect on rat and guinea pig ileum, and betacyanin, an active principle compound in prickly pear, may be responsible for the action.
  - 2,193 175
Preliminary clinical trials of karela, Momordica charantia, on non-insulin-dependent diabetes mellitus patients
Mouchira Abdel Salam, Souad E El-Gengaihi, Emad N Zikry
January-April 2015, 14(1):69-74
Background Traditional methods of treatment for diabetes was recommended by WHO in 1985. On in-vivo trials in animal models, one of the authors revealed the potentiality of karela in the treatment of diabetes. Aim The aim of the study was to evaluate the effects of Momordica charantia as a hypoglycemic in type 2 diabetic patients. Formulated tablets from M. charantia (karela) juice of the unripe fruits were used. Materials and methods Juice from immature fruits was filtrated through specific membranes to separate active polypeptide mimic insulin. The powder obtained after spray drying was formulated as a 20 mg tablet of polypeptide. Eighteen of 60 patients continued the treatment. All patients had type 2 diabetes. They were followed up for 1-8 weeks and examined clinically and investigated for different parameters. Results As this trial is a case analysis, the result of each case was presented and the overall trial results were discussed. Conclusion M. charantia can be used as an effective oral adjunct hypoglycemic, with no reportable clinical side effects. The treatment must be continued for 4 weeks.
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Formulation and evaluation of fast-dissolving films of lisinopril
Prabhakara Prabhu, Akhilesh Dubey, Karthik Kamath
January-April 2015, 14(1):56-64
Objective The aim of this study was to formulate and evaluate the oral fast-dissolving film of lisinopril for the effective management of hypertension and cardiac diseases. Materials and methods Fast-dissolving films were prepared by the solvent-casting method using a combination of different polymers, HPMC E5 LV, HPMC E 3 and HPMC 4KM, along with PEG as a plasticizer. The Fourier-transform infrared study for the drug-polymer interaction was carried out. Evaluation of physical parameters such as physical appearance, surface texture, uniformity of weight, uniformity of strip thickness, surface pH, folding endurance, uniformity of drug content and percentage of moisture absorption were performed. Kinetic data analysis for the release study and the stability study were also performed. Result and conclusion Results of uniformity of weight, thickness, folding endurance, surface pH, tensile strength, percentage drug content, swelling index, tensile strength and percentage elongation of all the films were found to be satisfactory with respect to variation of these parameters between films of same formulation. The Fourier-transform infrared study indicated that there was no interaction between the drug and the polymers. The in-vitro drug release study showed that a better rate of drug release was achieved by formulations FA3, FB1, FB4 FC8 and FD10 compared with other formulations. The stability study did not show any significant difference in the external appearance, the drug content and the in-vitro drug release. The ex-vivo study indicated that the drug has a better ability to cross the sublingual barrier at a faster rate, and hence the delivery system was found to be promising as it has the potential of overcoming the drawbacks associated with tablet formulations available in the market presently.
  - 12,111 659