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Journal of Pharmacy Research
ISSN NO: 0974-6943
The Journal of Pharmacy Research is an online Journal, publishing of correct version and document can be modified when, we/or author get comments from any readers. The journal is devoted to the promotion of Pharmaceutical sciences and related disciplines (including Pharmacy, medical, Biotech, Botany, organic and medicinal chemistry,  Nursing, Paramedical, prescription etc  fields).
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Journal Metrics for this Journal of Pharmacy Research (Source ID: 21100325431): 2015(SNIP) Source Normalized Impact Per Paper : 0.575; SCImago Journal Rank (SJR):0.787; Impact Per Publication : 0.789 CiteScore 2016: 0.93(Top level : Life Science)

Year SJR Cites per document Year Value
2014 0.607 Cites / Doc. (4 years) 2014 0.607
2015 0.787 Cites / Doc. (4 years) 2015 0.789
2016 0.926 Cites / Doc. (4 years) 2016 0.926
    Cites / Doc. (3 years) 2014 0.607
    Cites / Doc. (3 years) 2015 0.789
    Cites / Doc. (2 years) 2014 0.607
    Cites / Doc. (2 years) 2015 0.789
2016   Cites / Doc. (4 years) 2016 0.926
Cites Year Value
External Cites per document 2014 0.607
External Cites per document 2015 0.789
External Cites per document 2016 0.926
Cites per document 2014 0.607
Cites per document 2015 0.789
Cites per document 2016 0.926

Manuscripts Published

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PC-0000104
Title: Synthesis and molecular docking studies of few novel Pyrimidine derivatives
Category: Pharmaceutical Chemistry
Section: Research Article
Country: India
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This study was designed to synthesize some novel pyrimidine derivatives by using chalcone and thiourea. 10 different compounds thus formed were further reacted with ethylchloroacetate and then with hydrazine hydrochloride. The synthesized pyrimidinethioester hydrazide were subjected to docking studies against protein Human Cyclin Dependent Kinase 2 Complexed with the CDK4 Inhibitor (1GII) using Argus Lab software. The result indicates that the synthesized derivatives shows ligand bind pose energy varies from -8.35388 kcal/mol to -10.7195 kcal/mol. Of the 10 compounds, compound IV shows ligand bind pose energy -10.0084 kcal/mol with 4 hydrogen bond having best anticancer activity. This study also suggested that all the synthesized pyrimidine derivatives show potent anticancer activity than the standard drug 6-mercaptopurine.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-EEM-0000103
Title: Antimicrobial activity of Vitex negundo against pathogenic bacteria
Category: Extract Effect on Microbes
Section: Research Article
Country: India
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The present investigation indicates that C. Albicans was most sensitive towards the methanolic extract where as S. mutase was least sensitive towards methanolic extract of Vitex negundo. The maximum zone of inhibition (28 mm) was shown by both leaf and bark chloroform and methanolic extract against C. Albicans. The minimum zone of inhibition (12 mm) was shown by leaf methanolic extract against S. mutase.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PC-0000128
Title: Synthesis and Molecular Docking of Isoquinoline derivatives as Potential Antitumor Agents
Category: Pharmaceutical Chemistry
Section: Research Article
Country: India
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Aim: In an effort to establish new candidates with improved antitumor activity, series of Indolo[2,1-a]isoquinoline derivatives were synthesized and characterized. The synthesized compounds were docked in-silico onto the binding site of tyrosine kinase enzyme. Methods:The desired compounds 3a-l were synthesized regioselectively by the palladium-catalyzed preferential addition of N-heterocycles on to ortho-haloarylalkynes followed by intramolecular C-2 arylation without isolating enamine intermediate generated in in situ in the reaction, using an inexpensive and air stable 2-benzotriazolyl pyridine as novel bidentate ligand. Docking was performed by using the AutodockVina and integrated with Hex 6.0 to understand the binding preference of synthesized compound with target enzyme tyrosine kinase at default parameters. Result:The results obtained indicate that, out of our designed isoquinoline derivatives one has showed binding energy of -10.3kcal/mol and it was showing best interaction with tyrosine kinase. To explore drug like behavior Quantum mechanical studies of that compound was also been carried out. Conclusion: The present investigation may find applications in developing an easy protocol for the formation of Indolo[2,1-a]isoquinoline derivatives and efforts to screen tyrosine kinase inhibitor using semi flexible manner by AutodockVina17 and Hex 6.018 at default parameters.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PB-0000127
Title: Lactobacillus Derived Silver Nano Particles as a Potent Antibacterial Agent
Category: Pharmaceutical Biotechnology
Section: Research Article
Country: India
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In a study Lactobacillus sp. derived silver nanoparticles were produced and characterized for the shape, size and appearance by using transmission electron microscope and further evaluated for its antibacterial activity against the P. vulgaris and K. pneumoniae. Synthesized nanoparticles of length 10±3 nm have the antibacterial activity against the pathogens tested. Conclusively, Lactobacillus derived nanoparticles shown ability to resist the bacterial growth and posses’ therapeutic value in treatment research.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PTD-0000126
Title: Formulation and evaluation of floating microspheres of Cefdinir
Category: Pharmaceutical Technology Development
Section: Research Article
Country: India
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Aim:Various approaches have been used to retain the dosage form in the stomach as a way ofincreasing the gastric residence time (GRT), including floatation systems; high-density systems;mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems; andsuperporous hydrogel systems. The aim of this study was to prepare and evaluate floatingmicrospheres of cefdinir for the prolongation of gastric residence time. Materials and methods:Themicrospheres were prepared byCapillary Extrusion method.A full factorial design was applied to optimize the formulation. Results:The optimum batch of microsphere exhibited smooth surfaces with good flow and packing properties, prolonged sustained drug release, remained buoyant for more than 12 hrs, high entrapment efficiency up to68%.Surface morphological studies by SEM analysis obtained showed good spherical shape and also surface morphological characters. Conclusion:The studies revealed that increase in concentration of gum Karaya increased the drug release from the floating microspheres.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PC-0000125
Title: Synthesis and antimicrobial activity of novel 4-amino/oxo-5-substituted-7-phenylpyrido[2,3-d]pyrimidines
Category: Pharmaceutical Chemistry
Section: Research Article
Country: India
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The rationale for the selection of pyrido[d]pyrimidine scaffold is dictated by the fact that these compounds are known to be active in a wide variety of biological assays. Four possible structural isomers of pyrido[d]pyrimidines exist. Among them, pyrido[3,2-d]pyrimidines (8-deazapteridines) and pyrido[2,3-d]pyrimidines (5-deazapteridines) are isosteres of quinazolines or pteridines. Pyrazoles, quinoline, pyridine and pyridopyrimidine were known for their promising biological activities such as antimicrobial, anti-inflammatory, anticancer and antiviral activities etc. The key synthon 2-amino-4-substituted-6-phenylnicotinonitriles (3a-c) were prepared by reaction of aldehydes (1a-c), acetophenone and ethanolic KOH yielded substituted-1-phenylprop-2-en-1-ones (2a-c) and subsequent cyclocondensation of 2a-c with malononitrile and ammonium acetate afforded 3a-c. Further, reaction of compounds 3a-c with urea, thiourea, formamide and formic acid yielded 4-amino-5-substituted-7-phenylpyrido[2,3-d]pyrimidin-2(1H)-ones (4a-c), 4-amino-5-substituted-7-phenylpyrido[2,3-d]pyrimidine-2(1H)-thiones (5a-c), 5-substituted-7-phenylpyrido[2,3-d]pyrimidin-4-amines (6a-c) and 5-substituted-7-phenylpyrido[2,3-d]pyrimidin-4(3H)-ones (7a-c), respectively. The structures of all these unknown compounds were characterized by their IR, 1HNMR, Mass and analytical data. The antimicrobial evaluation of synthesized compounds was carried out by cup-plate method. Antibacterial activity results suggested that compounds 3a, 5b, 5c and 6c showed good activity against gram +ve bacteria B. Substilus whereas compounds 3a, 4a, 4c and 7b exhibited maximum inhibition against E. Coli. Compounds 3a, 3b, 4a, 4b and 5a showed good activity against bacterial strain P. Aeruginosa. Compounds 5b and 7b displayed potent activity against S. Aureus. Antifungal activity results revealed that compounds 3c, 5a and 7b showed good activity against A. Flavus. Compounds 3c, 4a, 5a, 5b and 7c exhibited good zone of inhibition against A. Niger. An elegant method is described for the synthesis of novel pyrido[2,3-d]pyrimidine derivatives and the synthesized compounds were evaluated for antimicrobial activity.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PC-0000124
Title: Synthesis of ureides containing indole moiety bearing -4-oxazetidinone
Category: Pharmaceutical Chemistry
Section: Research Article
Country: India
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The article is aimed to synthesize,characterize and screening the biological activity of a series of Synthesis of N-((3-(4-chloro-3-oxo-1-((4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)amino)azetidin-2-yl)-1H-indol-1-yl)methyl)piperidine-1-carboxamide 11(a) Indole-3-carbaldehyde and chloro ethyl acetate were dissolved in DMF.To this reaction mixture anhydrous K2CO3 was added and the reaction mixture was stirred at room temperature(350C) for 8 hours .To afford 2-(3-formyl-1H-indol-1-yl)acetate(A). To this reaction mixture Equimolar quantity of hydrazinecarbothioamide were dissolved in absolute alcohol, to this three drops of aceticacid was added then heated on a steam bath for 5-6hrs at 1000C to obtain Ethyl2-(3-((2-carbamoylhydrazono)methyl)-1H-indol-1-yl)acetate(3).To this reaction mixture a-halo ketones (chloro aceto phenone , cloro acetone) 10mM and the mixture stirred at roomtemperature for 30min. compound (3) Ethyl 2-(3-((2-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)hydrazono)methyl)-1H-indol-1-yl)acetate was obtained.To this reaction mixture Monocholoroacetyl chloride(0.01)was added drop wise to schiffs base (0.01) and triethylamine (0.02mol) in dioxane(25ml) at room temperature.To obtain Ethyl 2-(3-(4-chloro-3-oxo-1-((4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)amino) azetidin-2-yl)-1H-indol-1-yl)acetate(5).After hydrolysis to this reaction mixture isobutyl chloroformate (1:1eq) was added stirred for 30min, and aq NaN3 (3eq) was added and stirred for 20min at 00C. To obtain 2-(3-(4-chloro-3-oxo-1-((4-(4-(trifluoromethyl) phenyl) thiazol-2-yl)amino)azetidin-2-yl)-1H-indol-1-yl)acetyl azide.The reaction mixture is treated with mannich bases to obtain of N-((3-(4-chloro-3-oxo-1-((4-(4-(trifluoromethyl) phenyl) thiazol-2-yl)amino)azetidin-2-yl)-1H-indol-1-yl)methyl)piperidine-1-carboxamide 11(a) was obtained. The structure of these newly synthesized compounds were characterised by 1H NMR,13CNMR , Mass, IR, and elemental analysis. The antimicriobial activity of the novel compounds was screened by agar discdiffusion method.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-MB-0000123
Title: In vitro anti-Fungal activity of benzene and hydro-alcoholic leaves extract of Albizia lebbeck
Category: Microbiology
Section: Research Article
Country: India
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Objective: The present study was aimed to evaluate the in vitro anti-Fungal activity of benzene and hydro-alcoholic leaves extract of Albizia lebbeck. Materials and methods: Preliminary phytochemical investigations were carried out for qualitative detection of phytoconstituents by standard procedures, anti fungal activity of benzene and hydro-alcoholic leaves of Albizia lebbeck plant extracts was compared with that of standard Flucanozole (10µg/ml) by measuring the diameter of the Zone of Inhibitions of test and standard samples. Results: Hydro-Alcoholic extract (1000µg/ml) obtained from leaves of Albizia lebbeck showed excellent activity on comparing to that of standard drug Fluconazole (10µg/ml) and benzene extract. Conclusion: In conclusion the present study supports the traditional medicine use of Albizia lebbeck plant extracts in treating different infections caused by pathogenic fungi either by using a single or combined extracts.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-NN-0000122
Title: Extracellular biosynthesis of silver nanoparticles using Cassia fistula extract and in-vitro antimicrobial studies
Category: Nanotechnology & Nanomedicine
Section: Research Article
Country: India
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The synthesis of extracellular silver nanoparticles by biological method is one of the easier and convenient than that of the physical or chemical method of synthesis. The silver nanoparticles are synthesized using the dried plant leaves of Cassia fistula treated with silver nitrate solution. Silver nanoparticles are synthesized due to the reduction of the silver ions. The synthesized silver nanoparticles are characterized in different ways such as UV-Visible Spectrophotometer, XRD analysis, EDX analysis, HR-TEM analysis. The characterized silver nanoparticles are studied for their antibacterial and antifungal activities against different pathogenic microorganisms. From the antimicrobial study, it has been found that the synthesized silver nanoparticles are susceptible to Pseudomonas aeruginosa and Curvularia lipolytica which shows maximum zone of inhibition. The plant material mediated synthesis of silver nanoparticles is comparatively faster and less expensive and has wide application in antibacterial and antifungal therapy in modern medicine.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-MB-0000121
Title: Increasing Prevalence of Extended Spectrum Beta Lactamase Producing Microorganisms: A review
Category: Microbiology
Section: Review Article
Country: India
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The development of antibiotic resistance in various species of bacteria following introduction of antimicrobial agents has emerged as an important medical problem everywhere in the world including India. Extended spectrum beta lactamases (ESBLs) are rapidly evolving group of beta lactamase enzymes produced by the Gram negative bacteria. Beta-lactam antibiotics are the largest and most commonly used group of antimicrobial agents world-wide. They show very good tolerability and many of the drugs can be administrated orally. Bacteria expressing extended-spectrum beta-lactamases (ESBLs), enzymes hydrolyzing penicillins and cephalosporins, may not respond to therapy using some of these antibiotics. These enzymes are found most commonly in the Enterobacteriaceae family, and organisms that produce ESBLs are often resistant to non-beta lactam antibiotics, such as fluoroquinolones and aminoglycosides, by additional mechanisms, thus further limiting treatment options. At present, ESBLs has been increasing as a serious nosocomial and community pathogen having the property multidrug resistance. It is a great challenge for clinician to treat these bacterial infections. There was a limited number of drugs sensitive for these bacteria, the only drug of choice is imipenem, followed by amikacin in injectable form. But most probably in near future, if this irrational use is not stopped, infection with that Gram negative bacteria increase the rate of resistant to drugs that are now sensitive, resulting increase morbidity and mortality. Infection-control practitioners and clinicians need the clinical laboratory to rapidly identify and characterize different types of resistant bacteria specially ESBLs efficiently to minimize the spread of these bacteria and help to select more appropriate antibiotics.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-P'Col-0000120
Title: Prevalence and impact of cardiovascular risk factors among patients with acute coronary syndrome: a review
Category: Pharmacology
Section: Review Article
Country: India
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A dramatic increase in the number of deaths related to coronary artery disease has been observed world-wide, from 7.3 million deaths in 2008 to 11.1 million deaths in 2020 (estimated). The trend is believed to be due, in part, to the steeply increasing incidence of CAD in developing countries undergoing rapid westernization. This article provides a selective review of the effects of cardiovascular risk factors on the onset of acute coronary syndrome (ACS). ACS is a complex, multifactorial disorder in which interactions among various genetic and environmental influences play an important role. Coronary atherosclerosis results from excessive inflammatory and fibro proliferative responses to various forms of insults to the endothelium and smooth muscle of the artery wall, responses in which a large number of growth factors, cytokines, and vasoregulatory molecules participate. In this review, the prevalence of cardiovascular risk factors and their impact on patients presenting with ACS are discussed. Some of the known risk for ACS includes smoking, high blood cholesterol, physical inactivity, diabetes, high blood pressure, being overweight or obese, depression and social isolation. These were the risk factors that can be reduced by specific preventative methods, such as pharmacotherapy and lifestyle changes. Age, gender and a family history of coronary heart disease are some risk factors which cannot be reduced. The more the cardiovascular risk factor a patient has the higher the risk of ACS. Lack of knowledge and changes in the life style, food habits, psychological factors contribute to the progression of ACS. By providing patient education the quality of life can be improved and thereby preventing the ACS morbidity and mortality.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PHDRS-0000119
Title: anti-fertility activity and lipid peroxidatation effects of Clerodendrum serratum in male rats
Category: Pharmacognosy and Herbal Drugs related study
Section: Research Article
Country: India
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Aim:The objective of the present study is to explore anti-fertility and lipid peroxidation properties of methanolic extract of Clerodendrum Serratum aerial plant. Methods:The different dose of methanolic extracts were given by gavage to rats in the In Vivo test at a dose of 100, 300, 500mg/kg of body weight to rats in group II, II & III respectively, along with control dose. At the end of study various parameter such as biochemical and testicular lipid peroxidation levelwere analyzed. Result:Finding of this study explored a significantly decrease (p<0.05) the Alanine amino transferase, Aspartate aminotransferase and Alkaline phosphatase levels in methanolic extract of Clerodendrum Serratum treated rats when compared to control. But Malondialdehyde levels were significantly increased in methanolic extract of Clerodendrum Serratum treated rats testicular tissues in dose dependent manner when compared with control. Conclusion:The present study, it concluded that methanolic extract of Clerodendrum Serratum aerial parts have antifertility effects in male rats.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PCS-0000117
Title: Formulation by 23 factorial design and evaluation of controlled release transdermal patches of metoprolol succinate
Category: Pharmaceutics
Section: Research Article
Country: India
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The aim of present investigation is the development and evaluation of Transdermal drug delivery system for Selective β1 receptor blocker of Metoprolol succinate. Optimization of formulations of matrix transdermal patches was carried out by 23 factorial design. Formulation of controlled release matrix transdermal patches of Metoprolol succinate was done by solvent casting method by using different polymers like HPMC K4M, PVP K30 and Eudragit RL100. Formulated matrix transdermal patches were evaluated for physiochemical parameters like thickness and weight, Flatness, Folding endurance, Mechanical strength, Percentage moisture absorption, Percentage moisture loss, Water vapor transmission rate and Drug content. Surface morphology was examined by Scanning electron microscopy. All prepared formulations indicated good physical stability. Skin irritation studies were performed through rat skin by Draize scoring method. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. The satisfactory results were obtained in all prepared formulation and based on the results MP14 (HPMCK4M-71.25mg, PVP K30-4.75mg and Eudragit RL100-19mg) was the best one when compared to other. The in-vitro kinetics shows the zero order drug release followed by non-fickian diffusion mechanism.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PC-0000116
Title: Development of Novel Indole Molecules for the Screening of Anti-inflammatory Activity
Category: Pharmaceutical Chemistry
Section: Research Article
Country: India
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In the present work, some new 5-[2(3)-dialkylamino alkoxy] Indole 2, 3-diones were prepared from 5-hydroxy isatin. A mixture of 5-hydroxy isatin, dialkylamino alkylhalide in alcoholic potassium hydroxide was stirred at room temperature for 6 hours to get the 5-[2(3)-dialkylamino alkoxy] Indole 2,3-diones. The structures of the products were characterized by IR, NMR, MASS Spectral studies. All the compounds were evaluated for anti-inflammatory activity. Some of these compounds showed good anti-inflammatory activity compared with standard compounds.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PA-0000115
Title: LC and LC/MS approach for quantification of everolimus and its degradants and application in stress analysis
Category: Pharmaceutical Analysis
Section: Research Article
Country: India
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Objective: Everolimus is the 40-O-(2-hydroxyethyl) derivative of sirolimus and a potent inhibitor of mammalian target of Rapamycin (mTOR). It is used as an immunosuppressant to prevent organ rejection, treatment of renal carcinoma and as restenotic inhibitor in drug eluting coronary stents. The objective of the present study is to develop an LC and LC/MS method for quantification and structural elucidation of everolimus and its degradants in various stress conditions and strategize the stability issues in various applications. Method: Everolimus was subjected to different ICH prescribed stress conditions of thermal stress, hydrolysis and photolysis. Quantification and further structural elucidation was done by a rapid and systematic strategy based liquid chromatography–mass spectrometry (LC–MS) and liquid chromatography–tandem mass spectrometry (LC–MS–MS) sub structural technique. An acceptable separation of degradants was achieved using a C -18 column with mobile phase comprising of 70:30 acetonitrile: water with 0.1% glacial acetic acid, pH 5.4 held isocratic for 10 min.. The PDA detection wavelength was from 200nm to 800nm. The scanning range of mass was set at 100 to 1030Daltons with capillary and cone voltages at 4.0 kV and 70.0V respectively. The source temperature was set at 1000C and desolvation temperature at 3500C. ESI micro mass quadrapole detector and data management software - Mass Lynx ver. 4.1 were used. Result: Subjecting everolimus to different stress conditions resulted in degradants of different molecular weights. Molecular weights of the degradants are found to be 634, 559, 507, 437,309 Daltons (Da) in basic condition 707, 633, 549, 431, 298 Da in acidic condition and 633, 559, 429, 780, 707 Da under accelerated conditions of temperature. Conclusion: The results indicate that everolimus is highly sensitive to acid, base, light and temperature. The present method developed helped in proposing structures of degradants and further provide base for future work involving the analysis of everolimus.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-ND-0000114
Title: Potential Effect of Alpinia purpurata rhizome against Free radicals and Lipidperoxidation
Category: Natural Drugs
Section: Research Article
Country: India
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The aim of the study was to determine the free radical scavenging activities as well as the inhibition of in vitro lipid peroxidation evoked by Alpinia purpurata rhizome. The ethanolic extract of Alpinia purpurata was studied for its free radical scavenging property on different in vitro models like, Hydroxyl radical scavenging, Nitric Oxide Radical Scavenging, Super oxide radical scavenging activity and in vitro antilipidperoxidative assay using goat liver homogenate and RBC Ghost model. The results of ethanolic extract of Alpinia purpurata rhizome showed that a dose dependent increase in Hydroxyl radical scavenging, Nitric Oxide Radical Scavenging and Super oxide radical scavenging activity. In vitro anti-lipid peroxidative assay using goat liver homogenate and RBC Ghost model. The in vitro Lipid peroxidation (LPO) was inhibited to a good extent by the Alpinia purpurata rhizome ethanolic extract and the extent of inhibition being higher in the RBC membrane model than the liver homogenate model. The ethanolic extract showed good dose dependent free radical scavenging property in both the models. This study showed that inhibition of LPO and Hydroxyl radical, Nitric Oxide Radical and Super oxide radical scavenging abilities of Alpinia purpurata rhizome could be related to the presence of phenolic and flavonoid compounds. Therefore, the ethanolic extract of the rhizome may be a good source of natural antioxidative agent.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PHDRS-0000113
Title: Preliminary phytochemical screening and in vitro antioxidant activity of Banana flower (Musa paradisiaca AAB Nendran variety)
Category: Pharmacognosy and Herbal Drugs related study
Section: Research Article
Country: India
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Preliminary phytochemical screening, total polyphenol content, total flavonoid content and antioxidant activity of the extracts from banana flower (Musa paradisiaca AAB Nendran variety) were studied. Six different extracts using water, ethanol, methanol, chloroform, ethyl acetate and acetone were prepared by maceration process and evaporated using rotary evaporator. Total Polyphenol Content (TPC) and Total Flavonoid Content (TFC) in the extracts were determined by UV visible spectrophotomery and antioxidant activity was measured by in vitro DPPH assay method. The results showed that ethanol extract having more amount of flavonoid (0.67%) and polyphenol content (1.92 mg Eq of GA) than other extracts. In addition, the ethanol extract exhibited more antioxidant activity with IC50value 63 µg/ml. This study indicated that ethanol extract of banana flower (Musa paradisiaca AAB Nendran variety) exhibited more antioxidant property due to the presence of high content of polyphenols and flavonoids.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-MB-0000112
Title: Evaluation of antimicrobial activity and radical scavenging potential of lipopeptide biosurfactant from Klebsiella pneumoniae MSO-32
Category: Microbiology
Section: Research Article
Country: India
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Objective: In the present study we evaluated the antimicrobial and antiradical potential of a lipopeptide biosurfactant isolated from a soil bacterium, Klebsiella pneumoniae MSO-32 strain. Methods: Biosurfactant was produced by shake flask fermentation and purified by column chromatography. Its antimicrobial activity was estimated against gram-positive and gram-negative bacteria using agar well diffusion method. MIC and MBC values were determined to find efficacy of biosurfactant against test bacteria. The effect of biosurfactant on cell wall integrity of sensitive strain M. luteus was determined in terms of leakage of UV absorbing intracellular components. Antiradical potential and metal chelation capacity of biosurfactant was determined by using DPPH and hydroxyl radical scavenging assay and iron chelation activity respectively. Results: Chemically, biosurfactant was lipopeptide in nature and exhibited notable antimicrobial activity against all test bacteria. M. luteus displayed highest sensitivity with MIC at 10µg/ml and MBC at 30µg/ml. The biosurfactant caused gradual leakage of proteins, DNA and RNA from treated cells and showed concentration dependent scavenging effect on DPPH, hydroxyl radical and ferrous ion. Conclusion: The biosurfactant of K. pneumoniae MSO-32 exhibited promising antimicrobial and antiradical potential.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PC-0000111
Title: Molecular docking studies: 1, 3-thiazine and 1,3-oxazine dervatives
Category: Pharmaceutical Chemistry
Section: Research Article
Country: India
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Some novel derivatives of 1, 3 thiazines and 1, 3 oxazines were synthesized from five different chalcones with thiobenzamide and benzamide respectively. The synthesized five 1,3 thiazines and 1,3 oxazines derivatives were subjected to molecular docking docking studies against cytochrome p450 14 alpha sterol demethylase from mycobacterium tuberculosis using Argus Lab software .The results indicated that the chalcone derivatives of 1,3 thiazines (ligand binding energy varies from -12.135kcal/molto-14.2547 kcal/mol) shows considerable anti-fungal activity than the chalcone derivatives of 1,3 0xazines (ligand binding energy varies from -11.3042kcal/mol to -13.0389kcal/mol) against cytochrome p450 alpha sterol demethylase from Mycobacterium tuberculosis. Out of 10 derivatives, 3a (Methyl substituted 1, 3 thiazine) possess best ligand pose energy (-13.9505kcal/mol) and have one hydrogen bond .This study suggested that 1, 3 thiazine derivatives could be a potent antifungal activity than 1, 3 oxazine derivatives.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-P'Col-0000110
Title: Pharmacological investigation on the diuretic activity of the aqueous fruit extract of Neolamarckia cadamba (Roxb) bosser
Category: Pharmacology
Section: Research Article
Country: India
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The study was formulated to evaluate the efficacy of aqueous fruit extract of Neolamarckia cadamba on diuretic property in albino rats. Adult albino rats were randomly divided into five groups (n=8). All groups received normal saline (25 ml/kg). Group I which served as control received normal saline and animals which received standard diuretic drug furosemide (750mg/kg) were taken as diuretic control (group 2). Group 3 and group 4 received the fruit extract at a dose of 200 mg/kg and 400 mg/kg body weight. 24 h urine samples were collected by keeping the animals in metabolic cages. After 24 hrs of experiment, blood samples were collected from tail vein and serum was analyzed for creatinine concentration. Urine samples were analyzed for volume, pH, conductivity, urinary excretion, electrolyte concentration (Na+, K+, Cl-), Ca2+ , creatinine, creatinine clearance, glomerular filtration rate (GFR), saluretic, natriuretic and diuretic activity. The results were expressed in mean ± SE and analyzed with one way ANOVA. P< 0.05 was considered statistically significant. Significant dose dependant increase in serum creatinine, urine creatinine, creatinine clearance, glomerular filtration rate, saluretic and natriuretic activity was observed in the fruit extract treated groups. Urine volume, urinary excretion, electrolyte concentration and Ca2+ were also increased in the fruit extract treated groups when compared with controls. At a dose of 200mg/kg extract had moderate diuretic activity and a higher dose of 400mg/kg had good diuretic activity. The present study confirmed the effectiveness of aqueous fruit extract of N. cadamba as diuretic agent.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PTD-0000109
Title: Design and Development of chronopharmaceutical Drug Delivery of Lansoprazole
Category: Pharmaceutical Technology Development
Section: Research Article
Country: India
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The aim of the present investigation is to develop a pulsatile drug delivery system basedon an insoluble capsule body filled with Lansoprazole matrix tablet and sealed with HPMC K 100 plug. The Lansoprazole matrix tablets were prepared by wet granulation method. The plugs of varying thickness and hardness were prepared by direct compression which was then placed in the capsule opening. The drug delivery system was designed to deliver the drug at such a time when it was needed (nocturnal time). Dissolution studies of pulsatile capsule device in media with different pH (1.2, 7.4 and6.8) showed that drug release in colon could be modulated by optimizing the concentration of polymers in the plug and also the position of plug. The study showed that, lag time prior to drugrelease was highly affected by the plug position. The dissolution data revealed that the plug position and the composition of plug were very important to achieve a optimum formulation. Drug–polymer interaction studies indicated no interaction or complexation in between the drug and the polymer.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PC-0000108
Title: Artemisinin analogues selection in linear and non-linear QSAR
Category: Pharmaceutical Chemistry
Section: Research Article
Country: India
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Artificial neural networks (ANNs) and multiple linear regressions (MLR) controlled non-linear and linear quantitative structure activity relationship (QSAR) models were established for a set of (32) Artemisinin derivative (ART). QSAR models derived from MLR and ANN yielded appreciable internal and external predictability. Using the pertinent descriptors calculate from this study that the activity dependent especially on substituent R and hydrogen liaison du substituent R2 by different descriptors coding for same structural properties and energies and associated properties of the molecules are identified and discussed as overlapping structure features in linear and non-linear QSAR models. The independent variables selected in relation with concentration of 50% inhibition are BHA(R), W(R), and WM (R2), processed by leave one-out cross validation and Y-scrambling technique. The test set (N=6) presented an external prediction power of 94%: In conclusion these overlapping features may reveal fundamental structural properties which convert a linear relationship to non-linear and better identifications of bio-chemical aspects of QSAR models to medicinal chemists.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-Tox-0000107
Title: Evaluation of skin corrosive property of ethanolic leaf extract of Acyranthus aspera by in vitro Transcutaneous Electrical Resistance Test and Human skin Model Test.
Category: Toxicology
Section: Research Article
Country: India
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Objective: The present article is an attempt to investigate the corrosive property of ethanolic leaf extract of Achyranthus aspera (Amaranthaceae) by in vitro transcutaneous electrical resistance (TER) test and in vitro human skin model test before conducting wound healing experiments on rats to know instead of wound healing activity, whether it is having skin corrosion property or not. Methods: In TER test, application of extract for up to 24 hours to the epidermal surfaces of skin discs in a two-compartment test system in which the skin discs function as the separation between the compartments. Corrosive substances will be identified by their ability to produce a loss of normal stratum corneum integrity and barrier function, which was measured as a reduction in the TER below a threshold level (5 KW). In human skin model test, the extract is applied topically to a three-dimensional human skin model, comprising reconstructed epidermis with a functional stratum corneum for 1 hour. Corrosive substances are identified by their ability to penetrate the stratum corneum by diffusion or erosion, and cytotoxic to the underlying cell layers to produce a decrease in cell viability below threshold levels (15 %). Results: The ethanolic extract of Achyranthus aspera does not show corrosive property in both transcutaneous electrical resistance and human skin model test. Conclusion: The results obtained in these studies suggest a significant scope for the isolation of biological active components for further studies.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-ERS-0000106
Title: Optimization of Polygalacturonase using isolated Bacillus subtilis C4 by submerged fermentation
Category: Enzyme Related Study
Section: Research Article
Country: India
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Aim: Pectinases are an enzyme group that catalyzes pectin substance degradation through depolymerization (hydrolases and lyases) and deesterification (esterases) reactions. Method: The present investigation is envisaged to study the production of alkaline and thermostable polygalacturonase using isolated soil Bacillus subtilis(C4) by submerged fermentation. The potential of the isolate was compared with that of procured ones. Effect of fermentation factors like incubation time, temperature, pH, inoculum age, inoculum volume, agitation speed, carbon and nitrogen sources were optimized. Effect of crude substrates like corn, bajra, white jower, yellow jower, wheat bran, lemon peel, lemon pulp, papaya peel, mango peel, apple pomace and orange peel were tested. Result: Process parameters like incubation time (19.65U/mL), temperature (28.08 U/mL), pH 10.0, inoculum volume(1mL), inoculum age (24h) and agitation (150rpm) were studied for maximum production of polygalacturonase. To the optimized medium, different carbon, nitrogen and amino acids supplements were used for the enhancement of enzyme activity. Polygalacturonase production significantly improved when yellow jower was used as a carbon source(42.64U/mL) and casein (45.69 U/mL) as nitrogen sources. Cysteine, glycine, arginine and histidine also stimulated polygalacturonase activity. Conclusion: The present study suggests that the new soil isolate Bacillus subtilis C4 is a good producer of polygalacturonase. Yellow jower as a carbon source significantly influenced enzyme activity. Considering the process advantages of thermostable enzyme and wide applications of alkaline polygalacturonase, the new soil isolate Bacillus subtilis C4 is a potential candidate for commercial exploitations.

Journal: Journal of Pharmacy Research , Volume: 8, Issue: 2.
Article Id: JPRS-PDD-0000105
Title: Synthesis and characterization of biocompatible gold nanoparticles stabilized with hydrophilic polymer coated hesperetin drug for sustained drug delivery to treat hepatocellular carcinoma-derived ca
Category: Process Development of Drugs
Section: Research Article
Country: India
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The biological application of polymer coated gold nanoparticles in the recent chemotherapeutic work on drug delivery as a carrier has been effective for the treatment of cancer. Obviously in the production of pharmaceutical anticancer drugs, the factors like solubility, bioavailability, biocompatibility, limited chemical stability etc., are necessary with a special formulation technology in effective drug delivery. Our aim of the present study was to improve the solubility of the drug and reduce the side effects of chemotherapy drugs. Therefore, we report a simple and efficient method to synthesize a biocompatible nano carrier (polymer functionalized gold nanoparticles) to load the partially soluble drug (Hesperetin). Initially the carrier viz., the polymer functionalized gold nanoparticles (Au- mPEG (5000)-SH) was synthesized by reacting the tetrachloroauric acid (HAuCl4) with polymer (O-[2-(3-Mercaptopropionylamino) ethyl]-O’-methylpolyethylene glycol). Then, the anti-liver cancer drug viz., hesperetin (HP) was loaded on to the Au- mPEG (5000)-SH to treat the hepatocellular carcinoma. The formation of polymer functionalized gold nanoparticles and drug loaded polymer gold nanoparticles were characterized using UV-VIS spectrophotometer, HR-TEM with EDAX, and DLS with Zeta potential techniques. The in vitro drug release was carried out in PBS at pH 7.4 for Au- mPEG (5000)-S-HP and compared with the control pure hesperetin (HP). The in vitro cytotoxicity was studied using Hep3B human hepatocellular carcinoma cell line and observed that the cellular uptake of Au- mPEG (5000)-S-HP was higher when compare with pure drug (HP). These consistent results suggest that mPEG (5000)-S-HP functionalized Au nanoparticles could be used as an efficient drug for in vivo to treat hepatocellular carcinoma in animals.