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Ramesh A.,Vishnu Institute of Pharmaceutical Education and Research
Toxicology Mechanisms and Methods | Year: 2015

This study was undertaken to evaluate cardio protective effect of rutin against sodium fluoride (NaF)-induced oxidative stress-mediated cardiotoxicity and blood toxicity. Cardiac injury was induced by daily administration of NaF 600ppm in distilled water for four weeks. The animals exposed to NaF exhibited a significant increase in levels of cardiac serum markers, lipid peroxidative markers, serum total cholesterol, LDL, triglycerides and decrease in HDL levels. Decrease in hematological parameters, namely hemoglobin, red blood cells, mean corpuscular volume, mean corpuscular hemoglobin (MCH), MCH count and increase in white blood cells and erythrocyte sedimentation levels were also observed. Marked histopathological lesions and increased DNA fragmentation in cardiac tissues were observed. Activity of antioxidants-catalase, superoxide dismutase and reduced glutathione contents were decreased (p<0.01), whereas lipid peroxidation product (malondialdehyde) was increased. A significant decrease in body and heart weight was also observed. Treatment with rutin effectively ameliorated the alterations in the studied parameters of rat through its antioxidant nature. There was also significant improvement in hematological parameters. Thus, results of this study clearly demonstrated that treatment with rutin against NaF intoxication has a significant role in protecting F-induced cardiotoxicity, blood toxicity and dyslipidemia in rats. © 2015 Informa Healthcare USA, Inc. All rights reserved: reproduction in whole or part not permitted.


Mallikarjuna Setty C.,Vishnu Institute of Pharmaceutical Education and Research
Digest Journal of Nanomaterials and Biostructures | Year: 2012

The aim of the present study was to develop and characterize nanoemulsion formulation of tamoxifen citrate (TAM) for transdermal drug delivery system. Various oil-in-water nanoemulsions were prepared by the aqueous titration method. The prepared nanoemulsions were subjected to thermodynamic stability study and characterized for droplet size, transmission electron microscopy (TEM), viscosity studies. FTIR study was subjected to ensure the compatibility among its ingredients. Transdermal permeation of tamoxifen citrate through rat skin was determined by Keshary-Chien diffusion cell. Penetration enhancers effects on the skin permeation of TAM were investigated. Pharmacokinetic and pharmacodynamic parameter was determined on optimized formulations. Mean globule size and viscosity was found to be lowest in A1 formulation. TEM demonstrated spherical particle morphology and FTIR study revealed the compatibility among the ingredients. Significant increase in steady - state flux (Jss) was observed in optimized A1 and DA1 nanoemulsion. Of the various essential oils added, dill oil had the best enhancing ability. In pharmacokinetics study, transdermally applied nanoemulsion increased in bioavailability as compared to oral tablet formulation. In pharmacodynamic study RTV in mice receiving the optimized nanoemulsions was significantly reduced compared to control. Developed nanoemulsions can be used as potential vehicle for enhancement of bioavailability of TAM through transdermal application.


Rajendra Prasad V.V.S.,Vishnu Institute of Pharmaceutical Education and Research | Deepak Reddy G.,Vishnu Institute of Pharmaceutical Education and Research | Appaji D.,Vishnu Institute of Pharmaceutical Education and Research | Peters G.J.,VU University Amsterdam
Journal of Molecular Graphics and Modelling | Year: 2013

Calmodulin inhibitors have proved to play a significant role in sensitizing MDR cancer cells by interfering with cellular drug accumulation. The present investigation focuses on the evaluation of in vitro inhibitory efficacy of chloro acridones against calmodulin dependent cAMP phosphodiesterase (PDE1c). Moreover, molecular docking of acridones was performed with PDE1c in order to identify the possible protein ligand interactions and results thus obtained were compared with in vitro data. In addition an efficient pharmacophore model was developed from a set of 38 chemosensitizing acridones effective against doxorubicin resistant (HL-60/DX) cancer cell lines. Pharmacophoric features such as one hydrogen bond acceptor, one hydrophobic region, a positive ion group and three aromatic rings i.e., AHPRRR have been identified. Ligand based 3D-QSAR was also performed by employing partial least square regression analysis. © 2013 Elsevier Inc.


PubMed | Emcure Pharmaceuticals Ltd., VU University Amsterdam and Vishnu Institute of Pharmaceutical Education and Research
Type: | Journal: Bioorganic chemistry | Year: 2016

A series of nitric oxide donating acridone derivatives are synthesized and evaluated for in vitro cytotoxic activity against different sensitive and resistant cancer cell lines MCF7/Wt, MCF7/Mr (BCRP overexpression) and MCF7/Dx (P-gp expression). The results showed that NO-donating acridones are potent against both the sensitive and resistant cells. Structure activity relationship indicate that the nitric oxide donating moiety connected through a butyl chain at N(10) position as well as morpholino moiety linkage through an amide bridge on the acridone ring system at C-2 position, are required to exert a good cytotoxic effect. Further, good correlations were observed when cytotoxic properties were compared with in vitro nitric oxide release rate, nitric oxide donating group potentiated the cytotoxic effect of the acridone derivatives. Exogenous release of nitric oxide by NO donating acridones enhanced the accumulation of doxorubicin in MCF7/Dx cell lines when it was coadministered with doxorubicin, which inhibited the efflux process of doxorubicin. In summary, a nitric oxide donating group can potentiate the anti-MDR property of acridones.


Babu Y.R.,Gland Institute of Pharmaceutical science | Bhagavanraju M.,Gland Institute of Pharmaceutical science | Reddy G.D.,Vishnu Institute of Pharmaceutical Education and Research | Peters G.J.,VU University Amsterdam | And 2 more authors.
Archiv der Pharmazie | Year: 2014

In a quest for finding potent cytotoxic molecules, we have designed and synthesized a new scaffold by tagging quinazolinones with an acridone moiety. The new acridone-4-carboximide derivatives were evaluated for their cytotoxic potentials against the MCF7 breast cancer cell line and three colon cancer cell lines (LS174T, SW1398, and WiDr). Compound 26 showed relatively potent cytotoxic activity among the derivatives, against all the cell lines tested. Mechanistic studies for the selected derivatives 7, 8, 16, 17, 25, and 26 were conducted through in vitro EGFR tyrosine kinase inhibition studies. The results indicate that compound 26 has a better EGFR tyrosine kinase inhibitory profile. The in vitro EGFR inhibition data was correlated with the cytotoxic properties, and molecular docking studies were performed with regard to the receptor autophosphorylation sites of the protein kinase domain of the EGFR. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Setty C.M.,Vishnu Institute of Pharmaceutical Education and Research | Deshmukh A.S.,Shree Dhanvantary Pharmacy College | Badiger A.M.,BDR Pharmaceuticals International Private Ltd
International Journal of Biological Macromolecules | Year: 2014

The present study investigates the pharmaceutical application of hydrolyzed polyacrylamide grafted carboxymethylxyloglucan (HPam-g-CMXG), as promising polymeric material for the development of pH responsive microbeads. The graft copolymer was synthesized by conventional free radical polymerization method and saponified to enhance its functionality and characterized. An acute oral toxicity study ensured the bio-safety of developed copolymer for clinical application. Various batches of pH responsive spherical microbeads were developed and evaluated for the effect of process parameters on their overall performance. Result of in vitro drug release study (USP Type-II, paddle method) carried out in two different pH media (pH 1.2 and pH 7.4) showed a triphasic drug release pattern in all the formulations. Both the drug release and swelling of microbeads were significantly higher in simulated intestinal (alkaline) pH compared to simulated gastric (acidic) pH and this nature is desirable for targeted drug delivery. A strong correlation was observed between the process parameters and matrix composition and it directly influenced the drug transport mechanism. In conclusion, the hydrolyzed polyacrylamide grafted carboxymethylxyloglucan holds an immense potential to be explored pharmaceutically as new matrix material for the design of targeted drug delivery system. © 2014 Elsevier B.V.


Kishore T K.K.,Annamalai University | Ganugula R.,National Institute of Nutrition | Gade D.R.,Vishnu Institute of Pharmaceutical Education and Research | Reddy G.B.,National Institute of Nutrition | Nagini S.,Annamalai University
Tumor Biology | Year: 2015

Aberrant activation of oncogenic signaling pathways plays a central role in tumor development and progression. The aim of this present study was to investigate the chemopreventive effects of the neem limonoid gedunin in the hamster model of oral cancer based on its ability to modulate aldose reductase (AR), phosphatidyl inositol-3-kinase (PI3K)/Akt, and nuclear factor kappa B (NF-κB) pathways to block angiogenesis. Administration of gedunin suppressed the development of HBP carcinomas by inhibiting PI3K/Akt and NF-κB pathways through the inactivation of Akt and inhibitory kappa B kinase (IKK), respectively. Immunoblot and molecular docking interactions revealed that inhibition of these signaling pathways may be mediated via inactivation of AR by gedunin. Gedunin blocked angiogenesis by downregulating the expression of miR-21 and the pro-angiogenic factors vascular endothelial growth factor and hypoxia inducible factor-1 alpha (HIF-1α). In conclusion, the results of the present study provide compelling evidence that gedunin prevents progression of hamster buccal pouch (HBP) carcinomas via inhibition of the kinases Akt, IKK, and AR, and the oncogenic transcription factors NF-κB and HIF-1α to block angiogenesis. © 2015 International Society of Oncology and BioMarkers (ISOBM)


Kalshetti P.B.,Maharashtra Institute of Pharmacy | Alluri R.,Vishnu Institute of Pharmaceutical Education and Research | Thakurdesai P.A.,Indus Biotech Private Ltd
Brazilian Archives of Biology and Technology | Year: 2015

The objective of this work was to evaluate the effects of standardized hydroalcholic extract of Commiphora mukul (HECM) in animal model of chronic stress medicated depression, namely olfactory bulbectomy (OBX) model in rats. Effects of 14-day (subacute) oral pretreatment of HECM (50, 100 and 200 mg/kg) were evaluated on depression and stress related parameters on OBX rats. Separate groups for sham control, OBX control and positive controls namely imipramine (20 mg/kg), fluoxetine (30 mg/kg) and desipramine (15 mg/kg) were also maintained. Behavioral and physiological parameters in open field and elevated plus maze were recorded. HECM showed dose-dependent reversal of OBX-induced physiological effects such as reduction of body weight, body temperature, heart rate and serum sodium concentration. HECM also showed reversal effects on OBX induced food intake increase and hyperactivity in open field and elevated plus maze paradigm. In conclusion, HECM demonstrated restorative effects in OBX induced depression model in rats probably due to stress reliving mechanisms.


Chander P.A.,Vishnu Institute of Pharmaceutical Education and Research | Sri H.Y.,Vishnu Institute of Pharmaceutical Education and Research | Sravanthi N.B.M.,Vishnu Institute of Pharmaceutical Education and Research | Susmitha U.V.,Vishnu Institute of Pharmaceutical Education and Research
Asian Pacific Journal of Tropical Disease | Year: 2014

Objective: To study the anthelmintic activity of Barleria buxifolia leaf and to estimate the total flavonoid content. Methods: The aqueous and ethanolic leaf extracts were prepared and these were analyzed for total flavonoid content by aluminium chloride colorimetric method and Pheretima posthuma was used for anthelmintic activity by using the different concentrations (10, 20, 40, 80 and 100 mg/mL). Results: All the investigational extracts showed an anthelmintic activity at concentration of 10 mg/mL. The ethanolic extract of 100 mg/mL has produced an significant effect (P<0.001) when compared to aqueous extract. The total flavonoid content was found to be 5.67 mg QE/100 g. Conclusions: From the above study, the leaf extract has shown a good anthelmintic activity. © 2014 Asian Pacific Tropical Medicine Press.


Vanitasagar S.,Vishnu Institute of Pharmaceutical education and research | Subhashini N.J.P.,Osmania University
International Journal of Pharma and Bio Sciences | Year: 2013

Fenofibrate is a very potent and highly effective lipid lowering agent, used in the treatment of hypercholesteremia with poor water solubility and dissolution rate. The objective of the study was to develop SNEDDS of fenofibrate with improved dissolution rate and to characterize for particle size, self-nanoemulsification, and dissolution enhancement. Solubility of fenofibrate was determined in various oils, surfactants, and cosurfactants. meglyoil was selected as oil phase, Cremophore RH-40 as surfactant, and PEG-400 as cosurfactant due to their higher solubilization effect. The Results of the present research indicates that the in-vitro dissolution and intestinal permeability of the developed formulation was increased when compared with that of pure drug. The mean globule size (n=3) was observed to be (< 100nm), and the zeta potential was negative which may not interfere in the absorption of the formulation. Therefore the optimised formulation exhibits improved dissolution rate when compares with pure drug.

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