Journal of Pharmacy Research最新文献

{"title":"Study of phyto-chemical constituents of Ricinus communis Linn. under the influence of industrial effluent","authors":"Kavita Tyagi ,&nbsp;Sandhya Sharma ,&nbsp;Rajat Rashmi ,&nbsp;Sanjiv Kumar","doi":"10.1016/j.jopr.2013.08.005","DOIUrl":"10.1016/j.jopr.2013.08.005","url":null,"abstract":"<div><h3>Aims of the study</h3><p>To carried out the phyto-chemical constituents of <em>Ricinus communis</em> Linn. growing in a highly polluted and non-polluted sites.</p></div><div><h3>Method</h3><p>The industrial effluent was analysed by APHA method. The phyto-chemical constituents were analysed by Cromwell, 1955 &amp; Trease and Evans, 1983 were followed. TLC was analysed by WHO, 1998. Chlorophyll was estimated according to Arnon, 1949.</p></div><div><h3>Results</h3><p>The physico-chemical parameters of analysed effluent were found higher values as compared to standard values. Colour reaction tests showed the degree of changes in plants of polluted sites. The number of spots were decreased in the plant samples of polluted sites. Chlorophyll a, chlorophyll b and total chlorophyll were decreased in those leaves which were collected from polluted sites.</p></div><div><h3>Conclusion</h3><p>It may be concluded that the plants growing at non-polluted areas are not suitable for quality medicines, since, the study reveals quantitative alternations in the chemical constituents of plants growing in industrial areas and other parameters also found declining values in plants collected from polluted area.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 8","pages":"Pages 870-873"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85907049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Comparison of hepatoprotective activity of Swertia chirayita and Andrographis paniculata plant of North–East India against CCl4 induced hepatotoxic rats","authors":"Vinod Kumar Verma,&nbsp;Khomendra K. Sarwa,&nbsp;Atul Kumar,&nbsp;Md. Kamaruz Zaman","doi":"10.1016/j.jopr.2013.07.008","DOIUrl":"10.1016/j.jopr.2013.07.008","url":null,"abstract":"<div><h3>Background</h3><p>The aim of present study was to demonstrate and compare the hepatoprotective activity of ethanol extract of two well-known plants <em>Swertia chirayita</em> Buch-Ham and <em>Andrographis paniculata</em> (Burm.f.) Nees, in Swiss albino rats.</p></div><div><h3>Method</h3><p>The hepatotoxicity induced by single dose of CCl₄ dissolved in olive oil (1 ml/kg b.w.; p.o.) while vehicle control given food and water only. Vehicle as well as hepatotoxic rats were divided into groups (<em>n</em> = 6). Standard group treated with Silymarin (50 mg/kg b.w.; p.o.) daily for 16 days; and treated group received ethanol extract of plant <em>A. paniculata</em> and <em>S. chirayita</em> at the dose of 200 mg/kg b.w. p.o. daily for 16 days respectively.</p></div><div><h3>Results</h3><p>Ethanol extract of plant <em>S. chirayita</em> and <em>A. paniculata</em>, at a dose of 200 mg/kg body weight exhibited protective lowering effects of the serum enzyme levels SGPT, SGOT, GGTP and SALP to a significant extent. The pronounced activity observed in ethanol extract of <em>A. Paniculata</em> with dose of 200 mg/kg (b.w.) however decreases the elevated level of bilirubin, and lipid peroxidase (LPO). The decreased level of TP, GSH, SOD and CAT levels in CCl₄ induced hepatotoxic animal were significantly increase on treatment with ethanol extract of <em>A. Paniculata</em> and <em>S. chirayita</em> plant. The histopathological studies of liver were also supported hepatoprotective activity of <em>A. paniculata</em>.</p></div><div><h3>Conclusion</h3><p>Since results of biochemical studies conclude that the ethanol extract of <em>A. Paniculata</em> showed significant better hepatoprotective as compare to <em>S. chirayita</em>.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 647-653"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.008","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75307706","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Hibiscus tiliaceus: A possible immunomodulatory agent","authors":"Guduru Rajeswari ,&nbsp;Balugari Priyanka ,&nbsp;R.E. Amrutha ,&nbsp;Cuddapah Rajaram ,&nbsp;Rupesh S. Kanhere ,&nbsp;Sadhu Nelson Kumar","doi":"10.1016/j.jopr.2013.05.023","DOIUrl":"10.1016/j.jopr.2013.05.023","url":null,"abstract":"<div><h3>Objective</h3><p>The objective of the study is to evaluate the immunomodulatory effect of methanolic leaf extract of <em>Hibiscus tiliaceus</em> (MLHT) in pyrogallol induced immunosuppressed Wistar rats.</p></div><div><h3>Methods</h3><p>The methanolic extract of leaves of <em>H. tiliaceus</em> was administered orally at the dosage levels of 250 mg/kg/day and 500 mg/kg/day b.w in Wistar rats for 28 days. The assessment of immunomodulatory activity, humoral and cellular immunity was studied by hemagglutination antibody (HA) titer, delayed type hypersensitivity (DTH), Neutrophil adhesion test and carbon clearance test. In order to induce immunosuppression in rats pyrogallol (100 mg/kg/day, p.o.) is used and septilin syrup (1ml/100 g/day, p.o.) used as standard as it is immunostimulating agent. Hematological and biochemical were estimated by standard methods.</p></div><div><h3>Results</h3><p>Oral administration of MLHT showed a significant increase in the production of circulating antibody titer in response to sheep red blood cells (SRBCs). A significant (<em>P</em> &lt; 0.001) increase in both primary and secondary HA titer was observed when compared to control group, whereas in <em>H. tiliaceus</em> showed significant (<em>P</em> &lt; 0.001) increase in HA titer. MLHT significantly (<em>P</em> &lt; 0.001) potentiated the DTH reaction by facilitating the footpad thickness response to SRBCs in sensitized rats. Also MLHT evoked a significant (<em>P</em> &lt; 0.001) increase in percentage neutrophil adhesion to nylon fibers and phagocytic activity. It also enhanced the production of RBC, WBC and hemoglobin. It does not much affect the biochemical parameters.</p></div><div><h3>Conclusion</h3><p>An oral administration of the MLHT showed immunomodulatory effect in Wistar rats in a dose dependent manner. From the results obtained and reported phytochemical studies <em>H. tiliaceus</em> has a significant effect on both humoral and cellular immunity in experimental animals, this may be attributed to the polyphenols and flavonoid content of the plant extract.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 742-747"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.05.023","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80324747","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antioxidant potential of the flowers of Caesalpinia pulcherrima, Swartz in an in vitro system subjected to oxidative stress","authors":"S.T. Yamuna ,&nbsp;P.R. Padma","doi":"10.1016/j.jopr.2013.07.026","DOIUrl":"10.1016/j.jopr.2013.07.026","url":null,"abstract":"<div><h3>Background</h3><p>Oxidative stress leads to various pathological conditions including cancer. Antioxidant enzymes such as superoxide dismutase and catalase represent the cell defense mechanism for preventing oxidative damage. Recently many studies have focused on finding natural antioxidants, especially of plant origin for the treatment of oxidative stress associated diseases. The pharmacological and therapeutic properties of plants are attributed to the ability of antioxidants in them to scavenge free radicals.</p></div><div><h3>Objective</h3><p>In the present study, goat liver was selected as an <em>in vitro</em> model to determine the antioxidant effects of the three flowers (orange, pink and yellow) of <em>Caesalpinia pulcherrima</em> both in the presence and the absence of a standard oxidant (H₂O₂). The enzymic antioxidants (catalase, peroxidase, superoxide dismutase, glutathione reductase and glutathione S-transferase) and the non-enzymic antioxidants (vitamins A, C, E and reduced glutathione) were analysed.</p></div><div><h3>Results</h3><p>Treatment with hydrogen peroxide reduced the antioxidant levels in goat liver slices which were improved on co-treatment with the flower extracts, which proved the antioxidant efficacy of the flowers.</p></div><div><h3>Conclusion</h3><p>Our findings showed that the methanolic extract of the flowers of <em>C. pulcherrima</em> exhibits significant antioxidant activity against H₂O₂-induced oxidative stress in goat liver model.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 7","pages":"Pages 661-665"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.026","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88154791","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Chronic effects of anti-Alzheimer's drug, Galantamine hydrobromide on cholinergic system of mice brain","authors":"Yellamma Kuna ,&nbsp;Nirmala Kumari Borra","doi":"10.1016/j.jopr.2013.06.010","DOIUrl":"10.1016/j.jopr.2013.06.010","url":null,"abstract":"<div><h3>Objectives</h3><p>The present study emphasizes the prolonged effects of an anti-Alzheimer's drug, Galantamine hydrobromide (GHB) on morphometric, behavioural and cholinergic system in mice in the absence of the disease, AD.</p></div><div><h3>Methods</h3><p>One month old male albino mice, <strong><em>Mus musculus</em></strong> (20 ± 2 g) were selected as experimental model and GHB as the test drug. The ED₅₀ dose (5 mg/kg body weight) was given to experimental mice once in a day up to 180 days continuously.</p></div><div><h3>Results</h3><p>Observations on the morphometric aspects such as weight, size and also changes in the behaviour pattern of both control and experimental mice were recorded with help of the Morris water maze technique. Various constituents of the cholinergic system viz. acetylcholine content and acetylcholinesterase level were estimated in different regions of brain such as Olfactory Lobe, Hippocampus, Cerebral Cortex, Cerebellum, Pons-medulla and Spinal cord on selected days during the entire treatment schedule lasting for 180 days through standard biochemical assay techniques. From the results, it was evident that GHB exerted severe perturbations in the cholinergic system in all regions of brain on chronic exposure, thus eventually leading to behavioural changes.</p></div><div><h3>Conclusions</h3><p>From this, it was concluded that GHB, even though exerted positive effects on all the above mentioned parameters which were of course short-lived and during later stages, GHB exerted ill effects. In view of this, particularly, children are cautioned not to consume indiscriminately any kind of memory enhancing drugs or any formulated health drinks containing these chemicals either directly or indirectly for improvement of their cognitive skills.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 714-719"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.010","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78408342","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phenolic content of Ruprechtia salicifolia leaf and its immunomodulatory, anti-inflammatory, anticancer and antibacterial activity","authors":"Eman G. Haggag,&nbsp;Mohamed I.S. Abdelhady,&nbsp;Amel M. Kamal","doi":"10.1016/j.jopr.2013.07.015","DOIUrl":"10.1016/j.jopr.2013.07.015","url":null,"abstract":"<div><h3>Objectives</h3><p>This work aimed to isolate phenolics from leaves of <em>Ruprechtia salicifolia</em> and evaluate its immunomodulatory, anti-inflammatory, anticancer and antibacterial activity.</p></div><div><h3>Methods</h3><p>80% MeOH leaf extract was subjected to chromatographic separation, structures of the isolated compounds were established by different chromatographic and spectral techniques UV, MS, ¹H and ¹³C NMR. Immunomodulatory was evaluated through RAW 264.7 macrophages proliferation by MTT assay. Anti-inflammatory was evaluated by inhibition of NO and TNF-α factor generation in LPS-stimulated cells through bicinchoninici acid assay and ELISA assay, respectively. Cytotoxicity estimated through Hep-G2, MCF-7 and HCT-116 cell lines measured by MTT assay. Antibacterial activity tested by agar diffusion method.</p></div><div><h3>Results</h3><p>Eleven known phenolic compounds were isolated for the first time from this species including five flavonoid glycosides <em>viz</em>; Rutin <strong>3</strong>, quercetin 3-<em>O</em>-arabinoglucoside <strong>4</strong>, apigenin 7-<em>O</em>-β-<span>d</span>-glucoside <strong>5</strong>, quercetin 3-<em>O</em>-<em>α-</em><span>l</span>-arabinofuranoside <strong>6</strong> and isoquercetin <strong>7</strong> along with four aglycones <em>viz</em>; kaemferide <strong>8</strong>, apigenin <strong>9</strong>, quercetin <strong>10</strong> and naringenin <strong>11</strong> and two phenolic acids; caffeic <strong>1</strong> and gallic <strong>2</strong>. Compounds <strong>5</strong> showed the most activity increasing macrophage proliferation implying immunomodulatory activity. 80% MeOH extract, <strong>4</strong>, <strong>5</strong> and <strong>11</strong> inhibited nitrite oxide by 68.19%, 52.95%, 20.33% and 15.22%, respectively and TNF-α generation by 70.82%, 29.88%, 13.13% and 6.14%, respectively in LPS-stimulated cells implying anti-inflammatory activity. 80% MeOH leaf extract and the tested compounds <strong>4</strong> and <strong>5</strong> were safe possessing no cytotoxic activity against hepatocellular carcinoma (Hep-G2), breast adenocarcinoma (MCF-7) and colon carcinoma (HCT-116), while Compound <strong>11</strong> had cytotoxicity against only HCT-116 cells (IC₅₀ = 27.67 μg/ml). Also 80% MeOH leaf extract showed antibacterial activity against both G +ve and G −ve bacteria, moreover it inhibits growth of <em>Klebsiella pneumonia</em> strain, which is resistant to Ciprofloxacin broad-spectrum antibiotic.</p></div><div><h3>Conclusions</h3><p><em>R. salicifolia</em> contain phenolics of immunomodulatory anti-inflammatory, cytotoxicity and antibacterial activity, giving <em>R. salicifolia</em> grate potential as a medicinal natural drug.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 696-703"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.015","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81634953","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In silico drug docking and screening for the drug discovery of new tyrosinase inhibitors","authors":"Sapna S. Ingle,&nbsp;Chandrahas N. Khobragade","doi":"10.1016/j.jopr.2013.06.021","DOIUrl":"10.1016/j.jopr.2013.06.021","url":null,"abstract":"<div><h3>Aim</h3><p>To investigate potent tyrosinase inhibitor by drug docking analysis.</p></div><div><h3>Methods</h3><p>The study involved the protein structure of tyrosinase of <em>B. megaterium</em> to investigate the drugs designed by Chem office and drug docking was performed by AutoDock to investigate QSAR activity of the drug.</p></div><div><h3>Results</h3><p>Tyrosinase is an important enzyme linked with disorders like Parkinson's, melanogenesis, and hyper pigmentation, and studies on selection tyrosinase inhibitor and its implication in drug therapy is an urgent need. We have investigated five drugs which showcased tyrosinase inhibitor activity when tested by QSAR analysis in AutoDock. Docking study was done with the tyrosinase of <em>B. megaterium</em>, and results highlighted potent binding affinity of the drugs with binding energy in the range of −06.00 kcal/mol. In view, designed drugs show potential as tyrosinase inhibitor and may be used further for study.</p></div><div><h3>Conclusion</h3><p>All five drugs docked successfully with binding energy in the range of −06.00 kcal/mol suggested significant results.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 704-708"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.021","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81738482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Matrix type transdermal patches of captopril: Ex vivo permeation studies through excised rat skin","authors":"Rajesh Sreedharan Nair,&nbsp;Tai Nyet Ling,&nbsp;Mohamed Saleem Abdul Shukkoor,&nbsp;Balamurugan Manickam","doi":"10.1016/j.jopr.2013.07.003","DOIUrl":"10.1016/j.jopr.2013.07.003","url":null,"abstract":"<div><h3>Background/objectives</h3><p>Captopril, \"an ACE inhibitor\" has comparatively short elimination half life and its oxidation rate in dermal homogenate is significantly lower than that in intestinal homogenate. So as to enhance the bioavailability and to reduce the difficulties associated with captopril, it is decided to design a transdermal drug delivery system for this drug. So the objective of this present work is to formulate and evaluate the matrix type transdermal drug delivery systems of captopril, with different polymer combinations and penetration enhancers.</p></div><div><h3>Methods</h3><p>Eight formulations (F1–F8) were prepared by the solvent casting technique using varying proportions of polymers such as hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG) 400, along with the permeation enhancers such as menthol and <em>aloe vera</em> at different concentrations.</p></div><div><h3>Results</h3><p>The FTIR results showed no abnormal peaks and thus concluded that no incompatibility between the drug and polymers. The skin irritation studies were performed on rabbits, the results showed no noticeable skin reactions, pointed out the compatibility of drug as well as polymer matrix with the skin. The uniformity of drug content was evidenced by low standard deviation (S.D) values. High folding endurance (&gt;280) revealed that the prepared films have good flexibility. The weight of patches were uniform and thickness varied from 0.05 to 0.13 mm. <em>Ex vivo</em> permeation studies through excised rat skin were carried out using modified Franz diffusion cell, and the results showed that film (F6) containing HPMC and PEG 400 (1:1) with menthol as a permeation enhancer demonstrated the highest drug permeation (90.04%) at 24 h (<em>p</em> &lt; 0.05) with the transdermal flux of 54.5 μg/cm²/h.</p></div><div><h3>Conclusions</h3><p>The formulation coded as F6 was found to be the ideal patch, shown the maximum drug permeation of 90.04% at the end of 24 h followed Higuchi diffusion kinetics.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 774-779"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73749167","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis of novel indole based scaffolds holding pyrazole ring as anti-inflammatory and antioxidant agents","authors":"Vishwanath Sharath ,&nbsp;Honnaiah Vijay Kumar ,&nbsp;Nagaraja Naik","doi":"10.1016/j.jopr.2013.07.002","DOIUrl":"10.1016/j.jopr.2013.07.002","url":null,"abstract":"<div><h3>Aim</h3><p>To synthesize substituted indole based scaffolds having pyrazole ring and evaluate for their anti-inflammatory activity and antioxidant.</p></div><div><h3>Method</h3><p>The structures of newly synthesized compounds were elucidated by spectroscopic methods such as IR, ¹H NMR, ¹³C NMR, mass, ¹H NMR spectra and elemental analysis. Antioxidant assays like 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2-azino <em>bis</em> (3-ethylbenzothiazoline-6-sulfonic acid) (<span><math><mrow><msup><mrow><mtext>ABTS</mtext></mrow><mrow><mtext><mglyph></mglyph></mtext><mo>+</mo></mrow></msup></mrow></math></span>) radical ion decolorization assay and lipid peroxidation activity (LPO) were performed. Anti-inflammatory activity was studied using linoleic acid as substrate and lipoxidase enzyme.</p></div><div><h3>Results</h3><p>Among the synthesized analogues compound <strong>7d</strong> revealed broad-spectrum of antioxidant activity and on the other hand compound <strong>7c</strong> exhibits a promising anti-inflammatory activity.</p></div><div><h3>Conclusion</h3><p>The achieved results prove that the distinctive compounds could serve as promising lead candidates and also for acclimatization and investigation to construct more active analogues.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 785-790"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77493974","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacogenomics of drug resistance in Breast Cancer Resistance Protein (BCRP) and its mutated variants","authors":"Sugunakar Vuree ,&nbsp;Nageswara Rao Dunna ,&nbsp;Imran Ali Khan ,&nbsp;Khalid K. Alharbi ,&nbsp;Satti Vishnupriya ,&nbsp;Divya Soni ,&nbsp;Pratik Shah ,&nbsp;Harshpreet Chandok ,&nbsp;Mukesh Yadav ,&nbsp;Anuraj Nayarisseri","doi":"10.1016/j.jopr.2013.06.020","DOIUrl":"10.1016/j.jopr.2013.06.020","url":null,"abstract":"<div><h3>Aim</h3><p>Drugs in breast cancer treatment suffer resistance and drug efflux from ATP-binding cassette (ABC) efflux transporter protein. Drugs inhibiting BCRP suffer activity alteration due to sequence variants. It is imperative to investigate role of mutant variants using structure based aspects of drug binding.</p></div><div><h3>Method</h3><p>In present work, we included single nucleotide polymorphisms like F208S, S248P and F431L in BCRP structure and evaluated their role in alteration of drug binding affinities using computational approaches. Comparative modeling of BCRP 3D structure was achieved using various tools available followed by structure validation. Mutagenesis and its impact by SNPs was attained in 3D structure of BCRP. A set of selected and established BCRP inhibitors were further docked into binding site to record the drug resistance in mutant variants.</p></div><div><h3>Results</h3><p>Nucleotide binding (NB) domain (258 AA) and transmembrane (TM) domain (291 AA) of BCRP were modeled separately and assembled together to generate a single structure. Ramachandran Plot confirmed quality of modeled structures along with main chain and side chain parameters. Mutagenesis included three main variants (F208S, S248P and F431L) using Triton program. Molecular docking results showed inhibitor CID_25223199 binding effectively to wild and F431L mutant structure of BCRP while inhibitors CID_25223002 to F208S and CID_119373 to S248P.</p></div><div><h3>Conclusion</h3><p>Distortion in spatial arrangement of amino acids in BCRP protein due to mutations led to low efficacy in drug response with respect to wild isoform. Results of present work demand to probe pharmacogenomic aspects in drug development efforts for breast cancer.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 791-798"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.020","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76188395","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}