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   2015| July-September  | Volume 6 | Issue 3  
    Online since July 27, 2015

 
 
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ORIGINAL ARTICLES
Synthesis, antifungal and antibacterial activity of novel 1,2,4-triazole derivatives
Deepa Gupta, DK Jain
July-September 2015, 6(3):141-146
DOI:10.4103/2231-4040.161515  PMID:26317080
A large number of 1,2,4-triazole-containing ring system have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, central nervous system stimulants, antianxiety, and antimicrobial agents. To overcome the rapid development of drug resistance, new agents should preferably have chemical characteristics that clearly differ from those of existing agents. Thus led to the design and synthesize the new antimicrobial agents. A novel series of Schiff bases based on of 4-(benzylideneamino)-5-phenyl-4H-1,2,4-triazole-3-thiol scaffold was prepared by heating thiocarbohydrazide and substituted benzoic acid and subsequently, treating with substituted benzaldehydes. Seventeen derivatives were synthesized and were biologically screened for antifungal and antibacterial activity. The newly synthesized derivatives of triazole showed antifungal activity against fungal species, Microsporum gypseum; and antibacterial activity against bacterial species, Staphylococcus aureus. It was observed that none of the compounds tested showed positive results for fungi Candida albicans fungi Aspergillus niger, nor against bacterial strain Escherichia coli. Strong antifungal effects were obtained for the synthesized compounds against M. gypseum and were superior or comparable to standard drug ketoconazole. Similarly, all of the synthesized compounds exhibit strong antibacterial activity against S. aureus and were superior or comparable to standard drug streptomycin. It was found that among the triazole derivatives so synthesized, six of them, showed antifungal activity superior to ketoconazole while one of them, showed antibacterial activity superior to streptomycin. Thus, these can be the potential new molecule as an antimicrobial agent.
  4,657 782 34
Development, validation of liquid chromatography-tandem mass spectrometry method for simultaneous determination of rosuvastatin and metformin in human plasma and its application to a pharmacokinetic study
P Pavan Kumar, T. E. G. K. Murthy, MV Basaveswara Rao
July-September 2015, 6(3):118-124
DOI:10.4103/2231-4040.157982  PMID:26317076
A new, simple and accurate liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for simultaneous determination of rosuvastatin (ROS) and metformin (MET) in human plasma was developed. The assay procedure involved simple protein precipitation with acetonitrile. Following precipitation, fraction of supernatant was decanted and evaporated under gentle stream of nitrogen at 40΀C. The residue was reconstituted in mobile phase and injected. The chromatographic separation was achieved with Thermo Hypurity C18 column (50 mm Χ 4.6 mm, 5 μ) using a mobile phase composition containing 0.1% v/v formic acid in water and acetonitrile (30:70, v/v) at a flow rate of 0.4 mL/min. The total run time was 3.5 min. The method showed good linearity in the range 0.5-200 ng/mL for ROS and 2-2000 ng/mL for MET with correlation coefficient (r) >0.9994 for both the analytes. The intra and inter-day precision values for ROS and MET met the acceptance criteria as per regulatory guidelines. The battery of stability studies viz., bench-top, freeze-thaw and long term stability were performed. The developed method was applied to a pharmacokinetic study.
  4,243 588 9
Chalcone derivatives as potential antifungal agents: Synthesis, and antifungal activity
Deepa Gupta, DK Jain
July-September 2015, 6(3):114-117
DOI:10.4103/2231-4040.161507  PMID:26317075
Much research has been carried out with the aim to discover the therapeutic values of chalcone derivatives. Chalcones possess wide range of pharmacological activity such as antibacterial, antimalarial, antiprotozoal, antitubercular, anticancer, and antifungal agents etc. The presence of reactive α,β-unsaturated keto group in chalcones is found to be responsible for their biological activity. The rapid developments of resistance to antifungal agents, led to design, and synthesize the new antifungal agents. The derivatives of chalcones were prepared using Claisen-Schmidt condensation scheme with appropriate tetralone and aldehyde derivatives. Ten derivatives were synthesized and were biologically screened for antifungal activity. The newly synthesized derivatives of chalcone showed antifungal activity against fungal species, Microsporum gypseum. The results so obtained were superior or comparable to ketoconazole. It was observed that none of the compounds tested showed positive results for fungi Candida albicans nor against fungi Aspergillus niger. Chalcone derivatives showed inhibitory effect against M. gypseum species of fungus. It was found that among the chalcone derivatives so synthesized, two of them, that is, 4-chloro derivative, and unsubstituted derivative of chalcone showed antifungal activity superior to ketoconazole. Thus, these can be the potential new molecule as antifungal agent.
  4,125 674 31
Evaluation of wound healing activity of Thunbergia laurifolia supercritical carbon dioxide extract in rats with second-degree burn wounds
Juthaporn Kwansang, Chandhanee Itthipanichpong, Wacharee Limpanasithikul
July-September 2015, 6(3):103-107
DOI:10.4103/2231-4040.157984  PMID:26317073
Thunbergia laurifolia Lindl (TL) has been traditionally used as an antidote, anti-inflammatory, and anti-drug addiction. This study investigated the burn wound healing activity of TL leaf extract (TLL) from supercritical CO 2 extraction in rats. The extract was prepared to 2.5%, 5%, and 10% gel (TLL gel). Rats were induced to second-degree burn wounds. They were randomly divided into six groups (six rats/group), which five groups were topically applied gel base, 1% silver sulfadiazine gel, 2.5%, 5%, and 10% TLL gel, respectively, for 14 days. Six untreated burn rats were used as the control group. The rats in each group were evaluated for wound healing rate, histological parameters, and wound collagen content. Rats treated with 10% TLL gel had a higher wound healing rate than rats in the control and untreated groups. An increase in collagen content, which indicates good regeneration of wound skin, was observed in the TLL treated rats from a pathological study by Masson's trichrome and collagen content assay. The results from this study suggest that T. laurifolia leaf extract obtained by supercritical CO 2 extraction promotes the recovery of wound skin by shortening the inflammation phase, increasing collagen content, and stimulating fibroblasts proliferation and migration in wound healing.
  4,144 595 3
Application of quality by design approach to optimize process and formulation parameters of rizatriptan loaded chitosan nanoparticles
Ajinath Eknath Shirsat, Sohan S Chitlange
July-September 2015, 6(3):88-96
DOI:10.4103/2231-4040.157983  PMID:26317071
The purpose of present study was to optimize rizatriptan (RZT) chitosan (CS) nanoparticles using ionic gelation method by application of quality by design (QbD) approach. Based on risk assessment, effect of three variables, that is CS %, tripolyphosphate % and stirring speed were studied on critical quality attributes (CQAs); particle size and entrapment efficiency. Central composite design (CCD) was implemented for design of experimentation with 20 runs. RZT CS nanoparticles were characterized for particle size, polydispersity index, entrapment efficiency, in-vitro release study, differential scanning calorimetric, X-ray diffraction, scanning electron microscopy (SEM). Based on QbD approach, design space (DS) was optimized with a combination of selected variables with entrapment efficiency > 50% w/w and a particle size between 400 and 600 nm. Validation of model was performed with 3 representative formulations from DS for which standard error of − 0.70-3.29 was observed between experimental and predicted values. In-vitro drug release followed initial burst release 20.26 ± 2.34% in 3-4 h with sustained drug release of 98.43 ± 2.45% in 60 h. Lower magnitude of standard error for CQAs confirms the validation of selected CCD model for optimization of RZT CS nanoparticles. In-vitro drug release followed dual mechanism via, diffusion and polymer erosion. RZT CS nanoparticles were prepared successfully using QbD approach with the understanding of the high risk process and formulation parameters involved and optimized DS with a multifactorial combination of critical parameters to obtain predetermined RZT loaded CS nanoparticle specifications.
  3,947 622 9
Comparison of the efficacy of cardamom (Elettaria cardamomum) with pioglitazone on dexamethasone-induced hepatic steatosis, dyslipidemia, and hyperglycemia in albino rats
GM Nitasha Bhat, Nagendra Nayak, K Vinodraj, N Chandralekha, Paul Mathai, J Cherian
July-September 2015, 6(3):136-140
DOI:10.4103/2231-4040.157981  PMID:26317079
To evaluate the efficacy of cardamom with pioglitazone on dexamethasone-induced hepatic steatosis, dyslipidemia, and hyperglycemia in albino rats. There were four groups of 6 rats each. First group received dexamethasone alone in a dose of 8 mg/kg intraperitoneally for 6 days to induce metabolic changes and considered as dexamethasone control. Second group received cardamom suspension 1 g/kg/10 mL of 2% gum acacia orally 6 days before dexamethasone and 6 days during dexamethasone administration. Third group received pioglitazone 45 mg/kg orally 6 days before dexamethasone and 6 days during dexamethasone administration. Fourth group did not receive any medication and was considered as normal control. Fasting blood sugar, lipid profile, blood sugar 2 h after glucose load, liver weight, liver volume were recorded, and histopathological analysis was done. The effects of cardamom were compared with that of pioglitazone. Dexamethasone caused hepatomegaly, dyslipidemia and hyperglycemia. Both pioglitazone and cardamom significantly reduced hepatomegaly, dyslipidemia, and hyperglycemia (P < 0.01). Reduction of blood sugar levels after glucose load was significant with pioglitazone in comparison to cardamom (P < 0.01). Cardamom has comparable efficacy to pioglitazone in preventing dexamethasone-induced hepatomegaly, dyslipidemia, and fasting hyperglycemia.
  3,855 464 12
A comparative study of neuroprotective effect of angiotensin converting enzyme inhibitors against scopolamine-induced memory impairments in rats
Talha Jawaid, Shah Jahan, Mehnaz Kamal
July-September 2015, 6(3):130-135
DOI:10.4103/2231-4040.161514  PMID:26317078
The comparative study of neuroprotective effect of angiotensin converting enzyme inhibitors against scopolamine-induced neuroinflammation in albino Wistar rats was studied. Male albino rats were administered with scopolamine to induce memory impairment. The standard nootropic agent, piracetam (200 mg/kg b.w., [i.p.]), perindopril (0.1 mg/kg b.w., [i.p.]), enalapril (0.1 mg/kg b.w., [i.p.]), and ramipril (0.1 mg/kg b.w., [i.p.]) were administered in different group of animals for 5 days. On 5 th day, scopolamine (1 mg/kg b.w., i.p.) was administered after 60 min of the last dose of test drug. Memory function was evaluated in Morris water maze (MWM) test and pole climbing test (PCT). Biochemical estimations like glutathione (GSH), malondialdehyde (MDA), and acetylcholinesterase activity in the brain were estimated after completion of behavior study. All three test groups shows improvement in learning and memory in comparison to control group. Perindopril treated group showed a more effective significant decrease in escape latency time and transfer latency time compared to enalapril and ramipril treated group on day 4 in MWM test and PCT, respectively. Perindopril shows a significant reduction in MDA level and acetylcholinesterase activity and a significant rise in GSH level compared to enalapril and ramipril. The finding of this study indicates that Perindopril is more effective in memory retention compared to enalapril and ramipril.
  3,427 370 9
In-silico study of small cell lung cancer based on protein structure and function: A new approach to mimic biological system
Nidhi Sood, Sameer Chaudhary, Tanvee Pardeshi, Shama Mujawar, Krishna Balaji Deshmukh, Saba Afrin Sheikh, Preety Sharma
July-September 2015, 6(3):125-129
DOI:10.4103/2231-4040.161513  PMID:26317077
Lung cancer being the most common disease worldwide that leads to a number of deaths. A huge amount of effort has been done in screening trials for early diagnose treatment which increases the disease-free survival rate. Based on the expression of protein of mouse double minute 2 and tumor protein 53 complex, we have identified the antagonist for this complex that would facilitate the treatment for specific lung cancer. It is a complex disease that involves vast investigation for the characterization of a lung cancer and thus, computational study is being developed to mimic the in vivo system. In this work, a computational process was employed for the identification of these proteins, with a short and simple method to discover protein-protein interactions. Moreover, these proteins have more similarities in their function with the known cancer proteins as compared to those identified from the protein expression specific profiles. A new method that utilizes experimental information to improve the extent of numerical calculations based on free energy profiles from molecular dynamics simulation. The experimental information guides the simulation along relevant pathways and decreases overall computational time. This method introduces umbrella sampling simulations. A new technique umbrella sampling is described where the high efficacy100 of this technique enables uniform sampling with several degrees of freedom. Here, we review the protein interactions techniques and we focus on main concepts in the molecular of in-silico study in lung cancer. This study recruiting new methods proved the efficiency and showed good results.
  3,171 418 -
Pharmacognostic evaluation with reference to catechin content and antioxidant activities of pale catechu in Thailand
Thidarat Duangyod, Chanida Palanuvej, Nijsiri Ruangrungsi
July-September 2015, 6(3):97-102
DOI:10.4103/2231-4040.161505  PMID:26317072
Pale catechu, a well-known crude drug, has been widely used for anti-diarrhea. Due to its medicinal usage, this study was performed to evaluate the pharmacognostic and antioxidant properties as well as catechins contents of pale catechu in Thailand. Twenty samples of pale catechu collected from traditional drug stores throughout Thailand were investigated. Antioxidant activities, total phenolic, nontannin phenolic, and total tannin contents were evaluated. (+)-catechin and (−)-epicatechin were quantitatively analyzed by high performance liquid chromatography. The results revealed that most of pale catechu samples were adulterated according to high ash values. Qualified pale catechu in Thailand were demonstrated for their average contents of total ash, acid insoluble ash, loss on drying, and moisture as 5.20 ± 0.19, 1.61 ± 0.17, 13.14 ± 0.10, and 13.20 ± 1.07 g/100 g of dry weight, respectively. The ethanol and water soluble extractive matters were 91.66 ± 5.16 and 44.59 ± 3.18 g/100 g of dry weight respectively. (+)-catechin in theses samples was 478.87 ± 2.77 μg/mg of crude drug, whereas (−)- epicatechin was found to be trace (< limit of quantitation). The promising antioxidant activities were demonstrated compared to (+)- catechin hydrate.
  3,187 378 1
A reverse phased high-pressure liquid chromatographic method for the estimation of a poisonous matter in Strychnos nux-vomica
Achu Hashim, Rafique Mohammed, Dilshad Umar, Vaswani R Veena, Basheer Bahija, Baroudi Kusai
July-September 2015, 6(3):108-113
DOI:10.4103/2231-4040.161506  PMID:26317074
Seeds of Strychnos nux-vomica were subjected to preliminary phytochemical tests and its presence was confirmed by thin layer chromatography (TLC) method. The TLC profile of the methanolic extract of seeds of S. nux-vomica was developed using the solvent system toluene:chloroform:methanol in the ratio 8:2:1. The plate was observed in visible light after spraying with Dragendorff's reagent (specific method). High-performance liquid chromatography (HPLC) profile of the methanolic extracts of S. nux-vomica was developed, and the amount of strychnine seems to be 0.36% (w/w) in the seeds. The TLC and HPLC profiles developed are very valuable for the identification of the original drug from their adulterants. The TLC profile identifies the presence of strychnine in the plant material. The quantification method for the strychnine in the seeds can be used for the quality standardization of the raw drug because the strychnine is reported to have some toxicity.
  2,819 390 -
EDITORIAL
Era of pharmacovigilance: Revolution in healthcare
Upendra Nagaich
July-September 2015, 6(3):87-87
DOI:10.4103/2231-4040.161501  PMID:26317070
  2,110 342 -
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