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Structure and physicochemical properties in relation to drug action
Mohsen M Kamel, Yasmin M Syam
July-December 2013, 12(2):95-108
In this review, classification of drugs, chemical structure, and biological activity, examples of pharmacological activities of some structural moieties, bioisosterism, physicochemical properties in relation to drug action, drug-receptor theory, acid-base chemistry in formulation and biodistribution of the drug, quantitative structure-activity relationship, and molecular docking are briefly presented with examples.
  28,765 5,704 -
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.
  18,324 1,461 2
Synthetic approaches and potential bioactivity of different functionalized quinazoline and quinazolinone scaffolds
Mohsen M Kamel, Wafaa A Zaghary, Reem I Al-Wabli, Manal M Anwar
September-December 2016, 15(3):98-131
Drug discovery and optimization constitutes one of the most important targets in medicinal chemistry. Because of their wide bioactivity spectra, nitrogen-containing heterocycles have received significant attention in many bio(organic) studies. The current review is a simple summary of different environmentally benign synthetic procedures that afford a variety of quinazoline and quinazolinone scaffolds with promising biological potential. The molecular modeling of various classes has also been discussed to elucidate the molecular reasons that led to the observed inhibition profile of different protein kinases, including which amino acids in their active sites would be involved in the anticipated bonding interactions. Furthermore, this article aims to investigate which classes deserve further development to get more specific and more potent quinazoline and quinazolinone candidates in various biological targets.
  5,827 4,552 -
A glance on sweet shrub Stevia rebaudiana Bertoni
Sameer J Nadaf, Heena S Naikwadi
September-December 2015, 14(3):139-147
The sweet shrub Stevia rebaudiana Bertoni has been used throughout the world as a noncaloric biosweetener owing to its two major thermostable phytoconstituents - namely, stevioside and rebaudioside - which have recently been added to the European Union list of permitted sweeteners. A number of countries across the globe, such as Japan, China, Malaysia, Taiwan, Australia, Korea, etc., have approved the use of S. rebaudiana-based sweeteners in foods and beverages. However, several studies on this ancient plant have revealed many of its pharmacological properties, such as anticancer, antihypertensive, antibacterial, etc., and thus S. rebaudiana ought to be called a medicinal plant. As expected, in recent years, researchers have directed the focus toward S. rebaudiana and have been patenting their inventions. A number of review articles have been published on S. rebaudiana in relation to different aspects, but no one has reported on their patents published. Hence, it has become necessary to provide the up-to-date and collective information on studies conducted and patents on S. rebaudiana and its metabolites with respect to their commercial applications. A good number of patents and research articles have been published on S. rebaudiana. These patents and research articles of interest were divided on the basis of their pharmacological activity and pharmaceutical application, described and discussed below in this review article. Furthermore, the yearwise distribution of patents was presented as bar diagram.
  2,457 4,323 -
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
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.
  2,487 4,016 5
Chemical composition and antimicrobial activity of volatile constituents from the roots, leaves, and seeds of Arctium lappa L. (Asteraceae) grown in Egypt
Elsayed A Aboutabl, Mona E El-Tantawy, Manal M Shams
July-December 2013, 12(2):173-176
Background and objective As no literature was traced dealing with the volatile constituents of the leaves or the seeds of Arctium lappa L., it was deemed of interest to carry out a gas chromatography/mass spectrometry (GC/MS) analysis and antimicrobial activity study of the volatile constituents of roots, leaves, and seeds of the plant grown in Egypt. Materials and methods The volatile constituents of the roots, leaves, and seeds were analyzed by GC/MS. The antimicrobial activity was tested using the agar well diffusion technique. Results and conclusion GC/MS of the volatile constituents from the leaves showed 19 identified compounds, the major being caryophyllene oxide (54.2%), followed by β-elemene (6.2%) and β-costol (4.0%). Analysis of the volatile constituents of the roots revealed 14 identified compounds, the major being caryophyllene oxide (51%), followed by aromadendrene (16%) and isoaromadendrene epoxide (6.4%). Analysis of the volatile constituents of the seeds revealed 22 identified compounds, the major being E-citral (28.8%), followed by geraniol (20.3%) and Z-citral (9.5%). The volatile constituents of the leaves and roots exhibited moderate antimicrobial activity against bacteria and significant antifungal activity, in comparison with the standards used, whereas the volatile constituents of the seeds showed moderate antimicrobial activity against bacteria and fungi.
  5,594 442 3
Fixed dose combination of targeted release paediatric dry syrup containing ofloxacin and ornidazole using natural polymers: formulation and characterization
Bitupan Bhuyan, Ratna J Das, Hemanta K Sharma
September-December 2016, 15(3):132-142
Background Tablets and capsules are difficult to swallow for children. Therefore, liquid formulations are preferred for administration to children. Most of the drugs have bitter taste and children do not support oral administration. Aim The aim of this study was to prepare a palatable paediatric dry syrup with ofloxacin and ornidazole as targeted released formulation using natural polymer and to mask the bitter taste of the drugs with suitable natural polymers. Materials and methods Extraction of the mucilaginous substances was carried out as per the method of extraction of pectin, followed by phytochemical examination, and physicochemical characterization was carried out. Lethal dose, 50% of the extracted natural polymer was determined as per OECD/OCDE guidelines 423. Compatibility study of natural polymer with formulation excipient was carried out. Preparation, characterization and evaluation of microspheres were carried out, including drug-release study in simulated gastric fluid and intestinal fluid, followed by preparation of dry syrup using suitable sweetening and flavouring agents. Results The release study states that the polymers released the drugs at the intestine (site of action) only and not (or little) at the stomach. Drug release from the optimum formulation F5 (Dillenia indica) was 99.97% for ofloxacin and 99.12% for ornidazole after 2.5?h in simulated intestinal fluid as compared with 8.3% for ofloxacin and 8.46% for ornidazole after 8?h in simulated gastric fluid. Microspheres of optimum formulation F5 D. indica were used for preparation of dry syrup. Statistical methods were utilized to analyse the results of different tests performed throughout the investigation. Conclusion Palatable dry syrup containing ofloxacin and ornidazole using natural polysaccharides was successfully prepared without any stability problem. It is expected to be effective/suitable for the paediatric patients with high compliance.
  4,438 1,584 -
Interpenetrating polymer network-based drug delivery systems: emerging applications and recent patents
Gupta Somya, Parvez Nayyar, Bhandari Akanksha, Sharma Pramod Kumar
May-August 2015, 14(2):75-86
Interpenetrating polymer network (IPN) systems use novel polymers that are synthesized by the interlacing of two independent polymers in a cross-linked form. For successful preparation of such IPN systems, at least one of the participating polymers should be synthesized/cross-linked in the immediate presence of the other. The polymers used to fabricate an IPN system are independently cross-linked or cross-linked to each other. They can be prepared by selective combination of the starting polymers to tailor the final product based on the ultimately desired characteristics. The nontoxic nature and biodegradability of natural polymers can thus be combined with the robustness and strength offered by the synthetic polymers by fabricating their IPN systems. The present review aims to summarize the IPN systems in terms of their advantages, disadvantages, and different drug delivery systems based on these polymers and their numerous biomedical applications. This review includes a detailed study of the recent publications and patents describing the use of IPNs in different spheres/formulations.
  4,826 602 2
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.
  4,542 522 -
Safety evaluation of needle-like hydroxyapatite nanoparticles in female rats
Azza I. Hafez, Fatma Hafez, Maaly Khedr, Omayma Ibrahim, Rania Sabry, Mossad A. Abdel-Wahhab
December 2012, 11(2):67-72

The present study was designed to evaluate the safety of synthesized needle-like hydroxyapatite (HAp) nanoparticles ranging from 3 to 7 nm in diameter and from 27 to 46 nm in length when administered in female rats orally or subcutaneously at different concentrations.


Animals in different treatment groups were maintained on their respective diets as follows: group 1, untreated control; group 2, treated orally with HAp (300 mg/kg body weight) for 3 weeks; group 3, treated orally with a low dose of HAp (150 mg/kg body weight) for 3 weeks; and group 4, implanted subcutaneously with HAp (600 mg/kg body weight) once and left for 5 weeks. At the end of the experimentation period, blood samples were collected from all animals for biochemical analysis (alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, uric acid, urea, and creatinine). After sacrifice, histopathological examination of the liver and kidney was carried out.

Results and conclusion

The biochemical results showed an increase in alanine aminotransferase and aspartate aminotransferase in the groups treated orally and those treated subcutaneously. There was an increase in alkaline phosphatase only in the group receiving the high oral dose; however, animals treated with the low dose or those treated subcutaneously were comparable with the control group. All the rats showed normal kidney function because of normal levels of creatinine, urea, and uric acid. The histopathological results indicated that the liver and kidney of all rats treated with HAp (oral or subcutaneously) had a normal structure. The previous results confirmed the safety of the synthesized nanoneedle HAp when administered orally or subcutaneously at the suggested dose.

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Microspheres based on herbal actives: the less-explored ways of disease treatment
Somya Gupta, Nayyar Parvez, Akanksha Bhandari, Pramod K Sharma
September-December 2015, 14(3):148-157
In recent years, focus has been directed towards the development of drug delivery system using biologically active compounds derived from the natural sources. These formulations based on natural products have been reported to have significant activity and are advantageous over the conventional formulations in terms of solubility, enhanced bioavailability, increased pharmacological activity, stability and fewer side effects. Nowadays, people are switching to the natural products over synthetic compounds, which can be easily obtained from the locally available plants and can help in reducing public health costs. The present review aimed at highlighting the development of microspheres based on herbal actives formulations, in which biologically active compounds are delivered to the targeted site. It also summarizes the method of preparation, therapeutic activity and application of herbal formulations in various biomedical fields.
  3,422 1,471 -
Tropane alkaloids of Atropa belladonna L.: in vitro production and pharmacological profile
Hanan A Al-Ashaal, Mona E Aboutabl, Yousreya A Maklad, Ahmed A El-Beih
July-December 2013, 12(2):130-135
Objective The aim of the present work was to study the production of tropane alkaloids by in vitro cultures of Atropa belladonna L. and to evaluate the anticonvulsant, antinociceptive, motor incoordination, and antioxidant activities of both in vitro and original plant extracts. Background A. belladonna is a very important medicinal plant with multipurpose therapeutic effects. The yield of its alkaloid content is very low, which makes it difficult for industrial application. Materials and methods Murashige and Skoog media were used for callus and plant differentiation induction from leaf explants of A. belladonna L. Qualitative and quantitative analysis of alkaloids was carried out using high-performance liquid chromatography. The anticonvulsant activity was screened by the pentylenetetrazole seizure test. The antinociceptive activity was evaluated by adopting the writhing test, whereas motor incoordination was evaluated using the rotarod test. In addition, antioxidant activity was estimated using the 2,2'-diphenyl-1-picrylhydrazyl radical-scavenging test. Results Callus and differentiated plants were successfully induced in Murashige and Skoog media supplemented with growth regulators. High-performance liquid chromatography analysis revealed the production of higher concentrations of tropane alkaloids in differentiated plants than in the original plant. Anticonvulsant and antinociceptive activities, motor incoordination, and the antioxidant effect of callus extracts were much higher than those of the original plant leaf extract. Conclusion Plant tissue culture could be considered as an efficient and alternative source of continuous supply of tropane alkaloids with potent anticonvulsant, antinociceptive, motor incoordination, and antioxidant activities. It is also a powerful tool for producing A. belladonna strain with a high tropane alkaloid content.
  4,353 456 -
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
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.
  4,261 486 2
Production and partial characterization of collagenase from marine Nocardiopsis dassonvillei NRC2aza using chitin wastes
Azza M Abdel-Fattah
July-December 2013, 12(2):109-114
Background The marine ecosystem has generated considerable interest for the isolation of new microorganisms, especially Streptomyces spp. It is considered a cheaper source of precious enzymes such as collagenase. Objective This study aimed to produce new collagenase enzymes from the locally isolated marine Streptomyces spp. grown on marine wastes for application in industrial fields. Materials and methods The marine isolate was identified as Nocardiopsis dassonvillei NRC2aza by 16S rDNA sequencing. N. dassonvillei NRC2aza was grown on basal medium composed of whole chitin wastes as the sole C and N source for the production of collagenase enzyme. Extraction of the enzyme was performed to study its characteristics. Results and conclusion Maximum collagenase activity (240 U/ml) was obtained after 6 days of incubation in shaken liquid cultures when whole chitin wastes (shrimp and crab wastes) were used as the sole nitrogen and carbon source. A N. dassonvillei NRC2aza isolate was shown to produce significant amounts of collagenase, reaching 1872 U/g, under solid-state fermentation using a mixture of 10 g chitin waste and 2 g of feather. Successive ammonium sulfate fractionation of N. dassonvillei NRC2aza growth extract produced a group of collagenases with different molecular weights. The 80% enzyme fraction was the most active and possessed the highest collagenase activity (1106.66 U/f), reaching about 3.8-fold that of the culture filtrate. The optimum pH and temperature were 8 and 55°C, respectively, and the enzyme was stable at pH range of 6-8. The collagenase exhibited heat stability for 60 min at 50°C. Therefore, collagenases can be applied in food industry as tenderizers of red meat and in fur and hide tanning to ensure uniform dyeing of leather.
  3,079 1,570 2
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.
  4,008 542 2
Novel keratinase from marine Nocardiopsis dassonvillei NRC2aza exhibiting remarkable hide dehairing
Azza M Abdel-Fattah
July-December 2013, 12(2):142-147
Background The isolation of the locally marine Nocardiopsis dassonvillei NRC2aza was characterized by the exceptional dehairing properties of its subtilisin-like keratinase. Objectives The aim of this work was to extract keratinase enzyme from the marine Nocardiopsis dassonvillei NRC2aza to be an alternative to sodium sulphide, which is the major pollutant from tanneries. Its unique nonactivity on collagen enhances its industrial potential. Material and methods Fermentation of the marine isolate Nocardiopsis dassonvillei NRC2aza on whole-feather medium was performed for keratrinase enzyme production. Extraction of the enzyme was carried out by solid-state fermentation (SSF). Results and conclusion Nocardiopsis dassonvillei NRC2aza have excellent characteristics of crude keratinase, producing 1680 U/ml in a shaking submerged culture (SmF) and 19 760 U/g using SSF after 4 days at pH 7. The effect of inoculum concentration on SSF was studied, whereby higher concentrations (150-200%) lowered the activity. Fractional precipitation of the enzyme by ammonium sulphate produced four fractions, of which 70% was the most active and produced remarkable hide dehairing. A new locally isolated Streptomyces spp. from marine ecosystem produced a highly active keratinase enzyme that exhibits remarkable hide dehairing.
  4,084 333 4
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
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.
  2,503 1,722 -
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.
  3,600 623 7
Medicinal mushrooms as a new source of natural therapeutic bioactive compounds
Waill A Elkhateeb, Ghoson M Daba, Paul W Thomas, Ting-Chi Wen
April-June 2019, 18(2):88-101
In the ancient books of traditional medicines, medicinal mushrooms were occupying the headlines, and the main topics were confirming to their miraculous therapeutic powers. The presence of various phenolic compounds, polysaccharides, and terpenoids and other compounds, is the reason for their potent biological activities as anticancer, antioxidant, antimicrobial, antiaging, hepatic protective, hypoglycemic, hypocholesterolemic, and much more biological activities are discovered every day. Many mushroom genera are famous for their promising therapeutic capabilities. One of the mushrooms genera attracting attention is Cordyceps which has long been used in Asian countries for maintaining long and healthy life. Numerous studies on different metabolic activities of Cordyceps have been performed both in vitro and in vivo. This review describes the importance of medicinal mushrooms with focus on Cordyceps as an example of globally commercialized mushrooms.
  3,603 468 -
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
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.
  3,470 461 2
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.
  3,333 578 7
Characterization of heavy metal and antibiotic-resistant bacteria isolated from polluted localities in Egypt
Saad A Moghannem, Bahgat M Refaat, Gamal M El-Sherbiny, Mohamed H El-Sayed, Islam A Elsehemy, Mohamed H Kalaba
September-December 2015, 14(3):158-165
Objective The aim of this study was to isolate and identify heavy metal-resistant and antibiotics-resistant bacteria from contaminated samples (wastewater and soil) collected from different industrial areas in Egypt and determine their role in heavy metal removing. Materials and methods Samples were collected from Helwan and 10th of Ramadan city areas and enriched in culture broth containing 200, 100, and 10 ppm of arsenic (As), lead (Pb), and cadmium (Cd) as AsHNa 2 O 4·H 2 O, Pb(NO 3 ) 2 , and CdSO 4 , respectively. The highly resistant isolate (ST6) was selected and identified biochemically and also subjected to 16S rDNA sequencing. The growth parameters were optimized and the maximum tolerable concentration of the respective metals as well as the antibiotic resistance was determined. Result and conclusion After enrichment culture we isolated and purified 20 bacterial isolates resistant to the respective heavy metals As, Pb, and Cd. The morphological, biochemical, and phylogenetical characteristics of the most resistant bacterial isolates (ST6) were studied. The results showed that this isolate belongs to the species Pseudomonas stutzeri. The optimum temperature was 35°C, whereas the optimum pH was in the range of 6-7. Maximum tolerable concentration values for As, Pb, and Cd were 3500, 1750, and 50 ppm, respectively. Also, the isolate ST6 showed resistance against different antibiotics. The metal removal ability was 42.5, 57.1, and 52.9% of As, Pb, and Cd, respectively. It was concluded that the ST6 isolate was resistant and removed high concentrations of As, Pb, and Cd. Hence, this isolate may play a role in bioremediation processes of heavy metal in polluted areas.
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Schistosomiasis ( chemoprophylaxis and treatments)
Magdy I El-Zahar, Somaia El-Karim
June 2012, 11(1):1-15

Schistosomiasis is a chronic parasitic disease affecting about 207 million individuals worldwide. It is still a major health problem in many tropical and subtropical countries, as well as for travelers from developed countries. The treatment strategies of schistosomiasis can be divided into two main routes: (a) chemotherapy treatment including trivalent antimony compounds, hycanthone mesylate, niridazole, metrifonate, oxamniquine, oltipraz, artemisinins, albendazole, amoscanate mirazid, and praziquantel; (b) vaccines that may play an important role in the control of schistosomiasis in the future.

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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.
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Optimization and characterization of l-asparaginase production by a novel isolated streptomyces spp. strain
Abeer A El-Hadi, Hanan Mostafa Ahmed, Rania A Hamzawy
April-June 2019, 18(2):111-122
Introduction and purpose Microbial l-asparaginase (l-asparagine amino hydrolase, E.C. has been applied as the most important chemotherapeutic agent in the treatment of certain human cancers, especially in acute lymphoblastic leukemia. Actinomycetes are recognized as a comparatively less explored source for l-asparaginase and therefore act as candidates for the production of l-asparaginase. The possibility of using novel actinomycete as a source of production of some industrially important microbial l-asparaginase was investigated in this study. Materials and methods Genomic DNA of the actinomycetes isolate from soil samples was extracted using the Gene JET Genomic DNA purification kit (Thermo scientific #k0721). The actinomycete isolate was identified by 16S rDNA. The identified actinomycete isolate was inoculated on starch casein agar slants and incubated for 7–10 days at 28°C, and then it was maintained at 4°C until further use. Inoculum was prepared from a 7-day old culture of the strain. Production of l-asparaginase was initially tested in four different media. The actinomycete strain was used further for the optimization of cultural conditions, namely, l-asparagine substrate concentrations, pH, temperature, and incubation conditions. The pH of the medium was varied from pH 3.0 to pH 9.0; the incubation temperature was varied from 30 to 50°C. The effect of carbon source and nitrogen source on l-asparaginase production was studied. Modified Czapex Dox broth was supplemented with different carbon and nitrogen sources such as starch, mannitol, mannose, sucrose, cellulose, and fructose at a concentration of 1% (w/v) and ammonium sulfate, beef extract, yeast extract, and peptone at a concentration of 0.2% (w/v), respectively, keeping other components constant. The properties of Streptomyces spp. l-asparaginase were also studied such as pH, assay temperature, and thermal stability. Results and discussion Genotypic characterization of the most promising unknown actinomycete isolate showing the maximum production was identified by 16S rDNA. PCR amplified the 16 s rDNA region using primers. Genotypic characterization of the most promising unknown actinomycete isolate showing the maximum production was identified by16S rDNA. The 16 s rDNA region was amplified by PCR (about 1000 bp) using primers. According to sequencing similarities and multiple alignments, the isolate was found to be closely related to Streptomyces griseoplanus strain NRRL-ISP 5009 16 s ribosomal RNA gene with 85% identity. Higher enzyme activity was observed in modified Czapex Dox broth as compared with other media used. Modified Czapex Dox broth was supplemented with different concentrations of l-asparagine; the enzyme production was maximum at 1.5% l-asparagine (126.20 U/ml). Analysis of the culture supernatant showed that the enzyme activity rise from 126.20 U/ml on the fifth day to 141.11 U/ml on the 10th day which its peak enzyme production activity. Different carbon sources such as starch, mannitol, lactose, sucrose, and glucose were amended in asparagine-modified Czapek Dox broth to determine their impact on l-asparaginase production. Biosynthesis of l-asparaginase by S. griseoplanus strain has been reported to be higher when the basal medium was supplemented with starch. For the production of l-asparaginase by S. griseoplanus strain, yeast extract has been reported as a good nitrogen source. According to the properties of the enzyme, the maximum activity was achieved at 45°C. The half-lives of the free enzyme were calculated to be 521 min (8.5 h) at 50°C, 312.6 min (5.2 h) at 55°C, and 195.2 min (3.25 h), at 60°C.
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