Mir Azam Khan

Comparative chemical profiling, cholinesterase inhibitions and anti-radicals properties of essential oils from Polygonum hydropiper L: A Preliminary anti- Alzheimer’s study

BackgroundCholinesterase inhibition is a vital target for the development of novel and mechanism based inhibitors, owing to their role in the breakdown of acetylcholine (ACh) neurotransmitter to treat various neurological disorders including Alzheimer’s disease (AD). Similarly, free radicals are implicated in the progression of various diseases like neurodegenerative disorders. Due to lipid solubility and potential to easily cross blood brain barrier, this study was designed to investigate the anticholinesterase and antioxidant potentials of the standardized essential oils from the leaves and flowers of Polygonum hydropiper.MethodsEssential oils from the leaves (Ph.LO) and flowers (Ph.FO) of P. hdropiper were isolated using Clevenger apparatus. Oil samples were analyzed by GC-MS to identify major components and to attribute the antioxidant and anticholinesterase activity to specific components. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potentials of the samples were determined following Ellman’s assay. Antioxidant assays were performed using 1,1-diphenyl,2-picrylhydrazyl (DPPH), 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) and hydrogen peroxide (H2O2) free radical scavenging assays.ResultsIn the GC-MS analysis 141 and 122 compounds were indentified in Ph.LO and Ph.FO respectively. Caryophylene oxide (41.42xa0%) was the major component in Ph.FO while decahydronaphthalene (38.29xa0%) was prominent in Ph.LO. In AChE inhibition, Ph.LO and Ph.FO exhibited 87.00** and 79.66***% inhibitions at 1000xa0μg/ml with IC50 of 120 and 220xa0μg/ml respectively. The IC50 value for galanthamine was 15xa0μg/ml. In BChE inhibitory assay, Ph.LO and Ph.FO caused 82.66*** (IC50 130xa0μg/ml) and 77.50***% (IC50 225xa0μg/ml) inhibitions respectively at 1000xa0μg/ml concentration. In DPPH free radical scavenging assay, Ph.LO and Ph.FO exhibited IC50 of 20 and 200xa0μg/ml respectively. The calculated IC50s were 180 & 60xa0μg/ml for Ph.LO, and 45 & 50xa0μg/ml for Ph.FO in scavenging of ABTS and H2O2 free radicals respectively.ConclusionsIn the current study, essential oils from leaves and flowers of P. hydropiper exhibited dose dependent anticholinesterase and antioxidant activities. Leaves essential oil were more effective and can be subjected to further in-vitro and in-vivo anti-Alzheimer’s studies.

Molecularly Characterized Solvent Extracts and Saponins from Polygonum hydropiper L. Show High Anti-Angiogenic, Anti-Tumor, Brine Shrimp, and Fibroblast NIH/3T3 Cell Line Cytotoxicity

Polygonum hydropiper is used as anti-cancer and anti-rheumatic agent in folk medicine. This study was designed to investigate the anti-angiogenic, anti-tumor, and cytotoxic potentials of different solvent extracts and isolated saponins. Samples were analyzed using GC, Gas Chromatography–Mass Spectrometry (GC–MS) to identify major and bioactive compounds. Quantitation of antiangiogenesis for the plants samples including methanolic extract (Ph.Cr), its subsequent fractions; n-hexane (Ph.Hex), chloroform (Ph.Chf), ethyl acetate (Ph.EtAc), n-Butanol (Ph.Bt), aqueous (Ph.Aq), saponins (Ph.Sp) were performed using the chick embryo chorioallantoic membrane (CAM) assay. Potato disc anti-tumor assay was performed on Agrobacterium tumefaciens containing tumor inducing plasmid. Cytotoxicity was performed against Artemia salina and mouse embryonic fibroblast NIH/3T3 cell line following contact toxicity and MTT cells viability assays, respectively. The GC–MS analysis of Ph.Cr, Ph.Hex, Ph.Chf, Ph.Bt, and Ph.EtAc identified 126, 124, 153, 131, and 164 compounds, respectively. In anti-angiogenic assay, Ph.Chf, Ph.Sp, Ph.EtAc, and Ph.Cr exhibited highest activity with IC50 of 28.65, 19.21, 88.75, and 461.53 μg/ml, respectively. In anti-tumor assay, Ph.Sp, Ph.Chf, Ph.EtAc, and Ph.Cr were most potent with IC50 of 18.39, 73.81, 217.19, and 342.53 μg/ml, respectively. In MTT cells viability assay, Ph.Chf, Ph.EtAc, Ph.Sp were most active causing 79.00, 72.50, and 71.50% cytotoxicity, respectively, at 1000 μg/ml with the LD50 of 140, 160, and 175 μg/ml, respectively. In overall study, Ph.Chf and Ph.Sp have shown overwhelming results which signifies their potentials as sources of therapeutic agents against cancer.

Evaluation of antidiabetic and antihyperlipidemic activity of Artemisia indica linn (aeriel parts) in Streptozotocin induced diabetic rats

ETHNOPHARMACOLOGICAL RELEVANCEnDiabetes mellitus is a major metabolic disorder affecting a huge population all over the world. Artemisia species have been extensively used for the management of diabetes in folkloric medicine. The present study is designed to investigate the antidiabetic and antihyperlipidemic effects of aeriel parts of Artemisia indica.nnnMATERIALS AND METHODSnHydromethanolic crude extracts, chloroform, ethyl acetate and n-butanol fractions of aerial parts of Artemisia indica were tested for their antidiabetic potential in Streptozotocin (STZ) (50mg/kg, i.p.) induced diabetic Sprague-Dawley rats. Blood glucose level, body weight, serum lipid profile and activities of liver enzymes were determined. The extracts were further subjected to preliminary phytochemical analysis.nnnRESULTSnA daily oral dose of hydromethanolic crude extracts (200 and 400mg/kg b.w.) and chloroform fraction (200mg/kg b.w.) of Artemisia indica for 15 days showed a significant reduction in blood glucose level which was comparable to that of the standard antidiabetic drug, glibenclamide (500 μg/kg, p.o.). Artemisia indica extracts also showed reduction in total cholesterol, triglycerides and low density lipoproteins as well as serum creatinine level, serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT) and alkaline phosphatase (ALP) in diabetic rats.nnnCONCLUSIONnAccording to the results Artemisia indica possesses hypoglycemic, antihyperlipidemic and valuable effects on liver and renal functions in diabetic rats, which seems to validate its traditional usage.

Evaluation of Prunus domestica gum as a novel tablet binder

The present study was initiated with the objective of studying the in vitro dissolution behavior of gliclazide from its solid dispersion with polyethylene glycol 6000. In this work, a solid dispersion of gliclazide with polyethylene glycol was prepared by the fusion method. In vitro dissolution study of gliclazide, its physical mixture and solid dispersion were carried out to demonstrate the effect of PEG 6000. Analytical techniques of FT-IR spectroscopy, differential scanning calorimetry and X-ray diffractometry were used to characterize the drug in the physical mixtures and solid dispersions. The dissolution studies of solid dispersion and physical mixture showed greater improvement compared to that of the pure drug. The mechanisms for increased dissolution rate may include reduction of crystallite size, a solubilization effect of the carrier, absence of aggregation of drug crystallites, improved wettability and dispersbility of the drug from the dispersion, dissolution of the drug in the hydrophilic carrier or conversion of drug to an amorphous state. The FT-IR spectra suggested that there was no interaction between gliclazide and PEG 6000 when prepared as a solid dispersion. DSC and XRD study indicated that the drug was converted in the amorphous form.

Effects of Rubus coreanus extract on visual processes in bullfrog's eye

ETHNOPHARMACOLOGICAL RELEVANCEnThe fruit of Rubus coreanus (Rosaceae) is traditionally used as an aphrodisiac, astringent, restorative and tonic in Asian countries. It is advised for treating diseases related to liver, kidney and urinary dysfunction, premature greying, blurred vision, infertility, impotence and premature ejaculation. Additionally, there is a long history of different parts of the plants being used in the treatment of ophthalmic diseases. However, no scientific studies have been undertaken to determine the effects of Rubus coreanus in visual processes of the vertebrate retina.nnnAIM OF STUDYnThe purpose of the present study was to investigate the positive effects of Rubus coreanus extracts on visual processes in the vertebrates eye.nnnMATERIALS AND METHODSnElectroretinogram (ERG) techniques were used to record the responses from a bullfrogs eye cup preparations. Active pharmacological agents were used to block specific receptors in the retina and to leave others unaffected. Lipid peroxidation in the retina was generated by adding FeSO(4)+Na-ascorbate.nnnRESULTSnIt was observed that both dark- and light-adapted ERG b-wave peak amplitude significantly increases with Rubus coreanus treatment. It was found that Rubus coreanus acts as a retinal neural antagonist but not as GABA receptor antagonist. Rubus coreanus treatment lowered the duration of rhodopsin regeneration. The results obtained indicated that Rubus coreanus protects against lipid peroxidation drop off ERG amplitude in retina.nnnCONCLUSIONnBased on results obtained, it is suggested that Rubus coreanus can potentially improve visual sensitivity and can be used to treat pathophysiological conditions of eye.

Aceclofenac nanocrystals with enhanced in vitro, in vivo performance: formulation optimization, characterization, analgesic and acute toxicity studies

This study was aimed to enhance the dissolution rate, oral bioavailability and analgesic potential of the aceclofenac (AC) in the form of nanosuspension using cost-effective simple precipitation–ultrasonication approach. The nanocrystals were produced using the optimum conditions investigated for AC. The minimum particle size (PS) and polydispersity index was found to be 112±2.01 nm and 0.165, respectively, using hydroxypropyl methylcellulose (1%, w/w), polyvinylpyrrolidone K30 (1%, w/w) and sodium lauryl sulfate (0.12%, w/w). The characterization of AC was performed using zeta sizer, scanning electron microscopy, transmission electron microscopy, powder X-ray diffraction and differential scanning calorimetry. The saturation solubility of the AC nanocrystals was substantially increased 2.6- and 4.5-fold compared to its unprocessed active pharmaceutical ingredient in stabilizer solution and unprocessed drug. Similarly, the dissolution rate of the AC nanocrystals was substantially enhanced compared to its other counterpart. The results showed that >88% of AC nanocrystals were dissolved in first 10 min compared to unprocessed AC (8.38%), microsuspension (66.65%) and its marketed tablets (17.65%). The in vivo studies of the produced stabilized nanosuspension demonstrated that the Cmax were 4.98- and 2.80-fold while area under curve from time of administration to 24 h (AUC0→24 h) were found 3.88- and 2.10-fold greater when compared with unprocessed drug and its marketed formulation, respectively. The improved antinociceptive activity of AC nanocrystals was shown at much lower doses as compared to unprocessed drug, which is purely because of nanonization which may be attributed to improved solubility and dissolution rate of AC, ultimately resulting in its faster rate of absorption.

Mentha piperita in nephrotoxicity - a possible intervention to ameliorate renal derangements associated with gentamicin

Objective: Free radical generation has a strong role in the pathogenesis of renal damage associated with the use of gentamicin. Therefore, the present study was carried out to evaluate the renoprotective effect of Mentha piperita against gentamicin induced nephrotoxicity. Materials and Methods: A total of 24 male rabbits were divided into 4 groups receiving normal saline, gentamicin, M. piperita extract and co-therapy of extract and gentamicin respectively. Gentamicin was provided as 80 mg/kg/day intramuscularly and extract was given 200 mg/kg/day orally for a period of 21 days. Serum and urinary biochemical parameters and histological changes were studied for each group. The impact of the extract on the antibacterial action of gentamicin was also evaluated. Results: Animals treated with gentamicin showed derangements in serum and urinary biochemical parameters. These alterations were reversed by treatment with M. piperita extract. The histological changes showed in gentamicin group were also reverted by treatment with the extract. Further the plant did not influence the efficacy of gentamicin with respect to its antimicrobial properties. Conclusion: Co-therapy of M. piperita with gentamicin successfully attenuated biochemical kidney functioning derangements and morphological changes associated with gentamicin.

Nephro-protective potential of Morus alba, a prospective experimental study on animal models

Abstract Context: Morus alba L. (Moraceae) is traditionally used for the treatment of urinary incontinency due its strong diuretic properties. Objective: The present study explores the renal protective effects of M. alba, due to its free radical scavenging properties, in order to provide experimental evidence for its established use. Materials and methods: Ethanolic extract (200u2009mg/kg/d) derived from M. alba fruit was employed in rabbits as a co-therapy (GM-al) with gentamicin (80u2009mg/kg/d) for a period of 3u2009weeks. Biochemical kidney functioning parameters, urinary isozymes, and histopathological examination were performed. Results: The results showed that ethanol extract of Morus alba L. prevented alterations in serum creatinine (4.02u2009±u20090.14, pu2009<u20090.0001), blood urea nitrogen (54.18u2009±u20092.60, pu2009<u20090.0001), and serum uric acid levels (2.34u2009±u20090.12, pu2009<u20090.001). However, a decrease in creatinine clearance and urinary volume was observed in experimental groups. Histopathological examination and urinary enzymes excretion also suggested the protective role of the extract. Discussion and conclusions: The co-administration of M. alba with gentamicin prevented renal functioning alterations expected with the use of gentamicin alone. Therefore, it can be concluded that M. alba to protect from kidney damage, which may be because of its free radical scavenging and diuretic properties.

Evaluation of Paeonia emodi and its gold nanoparticles for cardioprotective and antihyperlipidemic potentials

Paeonia emodi Wall. ex Royle is an important member of family Paeoniaceae and folklorically used for constipation, hysteria, respiratory diseases, epilepsy and cardiac diseases like hypertension, palpitations, congestive heart failure and atherosclerosis. In the present study, ethyl acetate fraction of P. emodi (Pe.EA) was subjected to column chromatography to obtain sub- fractions. These sub-fractions were screened for their cardioprotective activity in isoproterenol hydrochloride (ISO) induced myocardial infarction (MI) in mice. The most active fraction Pe. EA 40 was used for its gold nanoparticles synthesis (Pe.EA 40-AuNPs). Pe.EA 40 and Pe.EA 40-AuNPs were investigated for their cardioprotective, antihyperlipidemic, DNA fragmentation assay and histopathological study. Pe.EA 40 (80u202fmg/kg body weight) significantly reduced the serum levels of Alanine Aminotransferase (ALT), Aspartate Aminotransferase (AST), Lactate Dehydrogenase (LDH), Creatine Phosphokinase (CPK) to 66.07u202f±u202f1.54, 77.08u202f±u202f1.79, 84.86u202f±u202f1.34 and 265.34u202f±u202f4.34u202fIU/L respectively as compared to ISO treated group. Pe.EA 40-AuNPs (40u202fmg/kg) reduced the levels of ALT, AST, CPK and LDH to 60.74u202f±u202f2.79, 75.47u202f±u202f1.67, 80.48u202f±u202f2.64 and 247.54.u202f±u202f5.57u202fIU/L respectively. A significant reduction was observed in lipid profile, protection in DNA damage and restoration of histopathological changes as compared to ISO treated group. Based on the results, it can be suggested that preparation of Pe.EA 40-AuNPs enhances the therapeutic potential of plant extract for the treatment of atherosclerosis and MI.

Multi-Agent based Functional Testing in the Distributed Environment

Verification and testing are two formal techniques of defect reduction applied on designing and development phases of SDLC to rationalize quality assurance activities. The process of testing applications in the distributed environment becomes too complex. This study discusses a distributed testing framework that consists of many parallel tester components. The idea is based on utilizing client server environment to conduct software testing efficiently and in a short span of time. It is pertinent to mention that this study is restricted to testing of functional aspects of the software while testing of performance and other quality-of-service aspects are outside the scope of the study. An important factor influencing the use of agent technology in software testing is the dynamic nature of events. Since agents are characterized by intelligence and autonomy, their ability to interact with the environment offers added functionality to make decisions based on the needs of the scenarios that are dynamic in nature. This study shows that the use of agents to build a dynamic model for software testing in the distributed environment results in a more robust and efficient design. The proposed framework is based on distribution of test cases among multiple agents deployed across a distributed system which collaborate with each other to perform testing in an efficient manner. The proposed framework also provides an in-depth visibility into the software quality by providing the defect statistics on-the-fly. The experiments have been conducted using Selenium test automation tool. The test cases along with their test scripts and the test run results are described herein.