Journal of Pharmacy Research最新文献

Objective

Gallic acid, ellagic acid and quercetin are the important antioxidant compounds of Saraca asoca (Roxb.) de Wilde (Caesalpiniaceae). This report describes the determination of free radical scavenging activity in different plant parts (of S. asoca) by DPPH assay with correlation, and quantification of gallic acid, ellagic acid and quercetin in different plant parts by a simple, sensitive and validated HPTLC method.

Methodology

Methanolic extracts of bark, leaf and flowers of S. asoca were investigated for their antioxidant potential with the aid of DPPH assay followed by HPTLC analysis for quantitative evaluation of antioxidants (gallic acid, ellagic acid, and quercetin) in different plant parts.

Results

HPTLC analysis exhibited high amount of gallic acid and quercetin in flower (0.320% and 0.11% w/w respectively) and high amount of ellagic acid in bark (0.4805% w/w) which corresponds to low IC50 values of 6.83 ± 0.07 μg/ml and 6.6 ± 0.10 μg/ml respectively, indicating the remarkable antioxidant activity of these two plant parts whereas moderate amount of gallic acid (0.164 %w/w) and very low amount of quercetin (0.0445% w/w) and ellagic acid (0.04% w/w) correlate high IC50 value of 28.6 ± 0.62 μg/ml representing its poor antioxidant potential.

Conclusion

Consumption of bark and flower of S. asoca could be beneficial by virtue of its high antioxidant activity. The flower and bark may be considered as a source of gallic acid and ellagic acid respectively. The presence of moderate amount of gallic acid in leaf can be an alternative source.

Invertase, also called beta-fructofuranosidase cleaving the terminal non-reducing beta-fructofuranoside residues, is a glycoprotein with an optimum pH 4.5 and stability at 50 °C. It is widely distributed in the biosphere especially in plants and microorganisms. Saccharomyces cerevisiae commonly called baker's yeast is the chief strain used for the production and purification of the enzyme. Invertase in nature exists in different isoforms. In yeasts, it is present either as extracellular Invertase or intracellular Invertase. In plants, there are three isoforms each differing in biochemical properties and subcellular locations. Invertase in plants is essential not only for metabolism but also help in osmoregulation, development and defence system. In humans, the enzyme acts as an immune booster, as an anti-oxidant, an antiseptic and helpful for bone cancer or stomach cancer patients in some cases. The present study focuses upon the Invertase along with its application and purification from Saccharomyces cerevisiae. Invertase from baker's yeast was purified by concentrating the crude extract with ammonium sulphate (70%), dialyzed using sample buffer (0.1 M Tris, pH 7.2) and followed by centrifugation. The resultant supernatant was then applied on DEAE-cellulose column equilibrated with Tris buffer. The enzyme was eluted with a step gradient of NaCl (0–0.5 M) in starting buffer. Fractions showing highest activity were pooled. The result contains the purification summary with the purification fold of 27.13 and recovery of 31.93%. For the better understanding the mechanism and structure of the purified enzyme characterization is essential.

Various abiotic stresses lead to the overproduction of reactive oxygen species (ROS) in plants and animals which are highly reactive and toxic causing damage to proteins, lipids, carbohydrates and DNA thus leads to oxidative stress. This oxidative stress causes damage to tissues and results in large number of diseases. Antioxidants neutralize the effects of ROS and thus help in preventing diseases. Antioxidants can be natural or synthetic. Natural antioxidants can be taken up through diet as they are present in fruits, vegetables and spices. There are also certain synthetic antioxidants like BHT and BHA that also inhibit oxidation. However, these synthetic antioxidants have now been reported to be dangerous to humans so the search for non-toxic antioxidants have intensified in the recent years.

Background and aim

Alternanthera brasiliana belongs to the family, Amaranthaceae and is popularly known as Brazilian joyweed. It is a medicinal plant famous for its therapeutic effects in Brazil, South Africa and Nigeria amongst other countries. In the present study, the ethanol extract of the leaves of A. brasiliana was evaluated for its potential anti-oxidant activity.

Methods

This was carried out by determining the concentration of total phenols in the extract as well as using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging, iron (II)-chelating, nitric oxide radical-scavenging, ferrous sulphate and carbon tetrachloride-induced lipid peroxidation assays.

Results

The results show that the concentration of total phenols in the extract was 0.031 ± 0.006 μg/ml of the extract. In addition, the percentage inhibition of DPPH radical exhibited by the increasing concentrations of the extract, iron (II)-chelating and nitric oxide radical-scavenging activities (in percent), percentage inhibitions of ferrous sulphate and carbon tetrachloride-induced lipid peroxidation by the extract ranged from 96.29% to 99.59%, 51.43% to 78.78%, 53.43% to 94.85%, 25.00% to 37.90% and 96.26% to 99.50% respectively. Results of the assays were comparable to those of the standard anti-oxidant (ascorbic acid).

Conclusion

The above data provide evidences that the ethanol extract of the leaves of A. brasiliana is rich in natural anti-oxidants and thus justify its use in folk medicine especially in the management of free radical-mediated disorders.

Background/objectives

Cerebral I/R injury is mainly characterized by oxidant production, complement activation, leukocyte–endothelial cell adhesion, platelet–leukocyte aggregation, increased microvascular permeability and decreased endothelium-dependent relaxation. I/R injury can lead to multiorgan dysfunction or death. In recent years, pyrimidines have received much attention of researchers because of their vasodilator, anti-inflammatory and antioxidant properties. Studies on cerebroprotective mechanism of pyrimidine derivatives on cerebral I/R injury are limited. Hence it is worthwhile to study the role of pyrimidines as cerebroprotective agents and evaluated for their possible inherent underlying mechanisms.

Methods

Experimental cerebral infarction was produced by bilateral common carotid artery occlusion (global cerebral ischemia) for 30 min followed by 4 h reperfusion in Wistar rats. The oxidative and anti-inflammatory biomarkers were estimated and percentage infarction was determined.

Results and conclusions

A dose dependent cerebroprotective action of pyrimidines (AUCP1 and AUCP2) in terms of limiting the infarct size was observed in the present in vivo model of cerebral I/R in Wistar rats. The antioxidant role of pyrimidines (AUCP1 and AUCP2) in cerebroprotection was confirmed by measuring SOD, CAT, MDA, levels. MDA levels were decreased; SOD and CAT levels were increased by treatment with pyrimidines (AUCP1 and AUCP2). The cerebroprotective actions of pyrimidines (AUCP1 and AUCP2) are partially attributed to their anti-inflammatory effects against I/R injury in rats as evidenced by significant reduction in pro-inflammatory markers MPO, TNF-α and significant increase in anti-inflammatory marker IL-10. Pyrimidines (AUCP1 and AUCP2) evaluated in the present investigation has offered significant cerebroprotection against ischemia-reperfusion induced cerebral infarction in rats.

Aim

A novel and quick HPTLC-densitometric method was developed for the simultaneous determination of Ketoprofen, Methyl Paraben, and Propyl Paraben.

Methods

Chromatographic separation of the drugs was performed on precoated silica gel 60 F₂₅₄ Merck plates using Toluene:Ethyl acetate:Glacial acetic acid (6.5:2.5:1.0 v/v/v) as a mobile phase. A TLC scanner set at 265 nm was used of Ketoprofen, Methyl Paraben, Propyl Paraben respectively were validated according to ICH guidelines. Forced degradation conditions of hydrolysis (neutral, acidic and alkaline), oxidation, photolysis and thermal stress, as suggested in the ICH guideline Q1A (R2).

Results

The three drugs were satisfactorily resolved with R_f values of 0.33 ± 0.05, 0.54 ± 0.05, 0.71 ± 0.05 for Ketoprofen, Methyl Paraben, Propyl Paraben respectively. Calibration curves were polynomial in the range 200–1000 ng/band, 200–1500 ng/band, 100–600 ng/band, for Ketoprofen, Methyl Paraben, and Propyl Paraben respectively. Correlation coefficient (r) values were 0.9917, 0.9927, 0.9906 Ketoprofen, Methyl Paraben, Propyl Paraben respectively. The percentage recovery ranges from 99 to 101%.

Conclusion

A low relative standard deviation (<2%) was found for both precision and robustness study showing that the proposed method was precise and robust. The method had an accuracy of 99.95%, 99.85% and 100.07 of Ketoprofen, Methyl Paraben, Propyl Paraben respectively were validated according to ICH guidelines. The drug showed instability in oxide, heat and UV light, while it remained stable in neutral conditions.

Aim

Novel heterocycle 3-cyano 6,9-dimethyl 4-imino 2-methylthio 4H pyrimido [2,1-b] [1,3] benzothiazole 3 has been prepared by using 2-amino 4,7-dimethtyl benzothiazole 1 and bis-methylthio methylene malononitrile 2.

Method

Compound 3 prepared from 2-amino 4,7-dimethyl benzothiazole 1 was refluxed with bis-methylthio methylene malononitrile 2 in presence of anhydrous potassium carbonate and N,N-dimethyl formamide as solvent. Compound 3 possesses replaceable methylthio functionality at 2-postion, which was replaced by using selected different nucleophiles like phenols/aryl amines/heteryl amines and compounds containing active methylene group to afford 2-substituted derivatives 4–7 of compound 3.

Results

Heterocyclic compounds containing benzothiazoles fused with pyrimidines, pyrazoles reported to possess activity against the different types of cancers. Compound 3 and it's selected derivatives 4–7 were screened for their in-vitro anticancer activity towards 60 Human cancer cell lines at National Cancer Institute, Maryland USA. Many compounds exhibited remarkable activity against 60 human cell lines.

Conclusion

The compounds 3, 4-a, 4-d, 5-a, 6-a, 6-b exhibited maximum in-vitro anticancer activity against different cancers lines.

Aims

To determine the influence of location, seasonal variation and solvent system in production of phytochemicals and antioxidants from ginkgo leaves.

Methods

Total phenolic and flavonoid contents and antioxidant activity in ginkgo leaf extracts were estimated spectrophotometrically. Factorial analysis was performed to correlate the influence of location, season and solvent on production of phytochemicals and antioxidants.

Results

Total phenolic and flavonoid contents as well as the antioxidants were estimated maximum in autumn. Among solvents, acetone/water extracts gave best results for phenolic and flavonoid contents while methanolic extracts were best for antioxidants. Phenolic content, the predominant indicator of phytochemicals, showed significant correlation with antioxidant activity.

Conclusion

Factorial analysis among location, season and solvent with respect to the phytochemicals and antioxidants, was found to be statistically significant. Presence of phytochemicals along with the protective feature in the form of antioxidants is indicative of the importance of this species in pharmacological industry.

Objective

In the present study, we investigated the appropriate ratio of vancomycin with l-arginine, a non antibiotic adjuvant (NAA) and ceftriaxone against some selected clinical isolates. Furthermore, having determined the ratio, in vitro susceptibility studies were conducted.

Methods

The in vitro interaction between vancomycin with l-arginine and ceftriaxone was carried out on the chosen strains using agar dilution checkerboard method and results were presented as fractional inhibitory concentration (FIC) index. Susceptibility studies were carried out according to Clinical and Laboratory Standards Institute methods.

Results

Results of our study revealed that vancomycin with l-arginine and ceftriaxone at ratio, showed the lowest FICs, <0.5, for all selected positive controls as well as clinical isolates. The synergy between vancomycin with l-arginine and ceftriaxone was also confirmed by broth dilution, agar diffusion and time kill curve methods. In broth dilution and agar diffusion methods, vancomycin with l-arginine and ceftriaxone produced 4–5 fold lower minimum inhibitory concentration (MIC) and demonstrated greater zone of inhibition (≥5 mm) when compared with individual ceftriaxone and vancomycin. Approximately 10⁴–10⁵ log of killing reduction was observed with vancomycin with l-arginine and ceftriaxone in time kill curve study.

Conclusion

This study suggests that vancomycin with l-arginine and ceftriaxone could be an alternative regimen in combating antibiotic resistance among MRSA and hGISA.

Background

The leaves of Phyllanthus amarus (family: Euphorbiaceae) is reported to have good medicinal values such as antitussive properties. However the extract of the plant is very bitter, this constitutes a challenge in formulating an acceptable oral liquid dosage form. Therefore, the aim of this study is to develop a pleasant tasting liquid preparation of the extract by a taste masking technique as well as evaluate some physicochemical properties of the formulation that relate to its stability.

Methods

Six formulations (A–F) of the extract were prepared. To obtain the most stable and acceptable taste of the herbal syrup the physicochemical properties such as: colour, taste, pH, specific gravity, as well as its antioxidant activity were evaluated.

Results and discussion

Formulation C which contains ethanol, citric acid, glycerin and syrup BP as the taste masking agents was adjudged to have the most acceptable taste and stability. Generally formulations C showed a pH of 6.61 ± 0.02 and 6.62 ± 0.04, specific gravity of 1.24 ± 0.02 g/ml and 1.28 ± 0.01 g/ml immediately after formulation and after storage for 10 weeks respectively.

Conclusion

Formulating P. amarus extract with ethanol, citric acid, glycerin and syrup BP produced palatable and stable herbal syrup.