Pub Date : 2013-08-01Epub Date: 2013-09-17DOI: 10.1016/j.jopr.2013.09.002
Sharad G. Jadhav, Rohan J. Meshram, Dhanaji S. Gond, Rajesh N. Gacche
Objective
In the present study series of selected coumarin derivatives (CDs) were assessed for their inhibition of growth of Helicobacter pylori (H. pylori) and its related urease. The selected CDs were docked in-silico onto the ligand binding site of H. pylori urease.
Methods
The anti-H. pylori studies were carried out using agar diffusion assay and minimum inhibitory concentrations (MICs) were calculated by microbroth dilution method. Urease inhibitory activity of H. pylori using selected CDs was determined by Berthelot reaction and their IC50 values were calculated using GraphPad Prism version 6.00 while, docking studies were performed by ArgusLab 4.0.1.
Result
The results obtained indicate that, most of the CDs showed considerable anti-H. pylori activity (MIC range of 10–40 μg/ml) as well as significant inhibition of H. pylori urease (IC50 of 48.90–72.56 μM). To a greater extent, the in-silico results were in agreement with in-vitro results of inhibition of H. pylori urease.
Conclusion
The present investigation may find applications in designing and developing a novel, safe and effective anti-H. pylori agents using coumarin scaffold.
目的评价香豆素衍生物对幽门螺杆菌及其相关脲酶生长的抑制作用。选择的CDs通过硅对接到幽门螺杆菌脲酶的配体结合位点上。MethodsThe anti-H。用琼脂扩散法对幽门螺杆菌进行研究，用微肉汤稀释法计算最低抑菌浓度(mic)。选择的CDs通过Berthelot反应测定幽门螺杆菌的脲酶抑制活性，使用GraphPad Prism version 6.00计算其IC50值，使用ArgusLab 4.0.1进行对接研究。结果结果表明，大多数CDs具有较强的抗h活性。抑制幽门螺杆菌脲酶(IC50为48.90 ~ 72.56 μM)。在很大程度上，计算机模拟结果与体外幽门螺杆菌脲酶抑制结果一致。结论本研究为设计和开发一种新型、安全、有效的抗h。利用香豆素支架治疗幽门螺杆菌。
{"title":"Inhibition of growth of Helicobacter pylori and its urease by coumarin derivatives: Molecular docking analysis","authors":"Sharad G. Jadhav, Rohan J. Meshram, Dhanaji S. Gond, Rajesh N. Gacche","doi":"10.1016/j.jopr.2013.09.002","DOIUrl":"10.1016/j.jopr.2013.09.002","url":null,"abstract":"<div><h3>Objective</h3><p>In the present study series of selected coumarin derivatives (CDs) were assessed for their inhibition of growth of <em>Helicobacter pylori</em> (<em>H. pylori</em>) and its related urease. The selected CDs were docked <em>in-silico</em> onto the ligand binding site of <em>H. pylori</em> urease.</p></div><div><h3>Methods</h3><p>The anti-<em>H. pylori</em> studies were carried out using agar diffusion assay and minimum inhibitory concentrations (MICs) were calculated by microbroth dilution method. Urease inhibitory activity of <em>H. pylori</em> using selected CDs was determined by Berthelot reaction and their IC<sub>50</sub> values were calculated using GraphPad Prism version 6.00 while, docking studies were performed by ArgusLab 4.0.1.</p></div><div><h3>Result</h3><p>The results obtained indicate that, most of the CDs showed considerable anti-<em>H. pylori</em> activity (MIC range of 10–40 μg/ml) as well as significant inhibition of <em>H. pylori</em> urease (IC<sub>50</sub> of 48.90–72.56 μM). To a greater extent, the <em>in-silico</em> results were in agreement with <em>in-vitro</em> results of inhibition of <em>H. pylori</em> urease.</p></div><div><h3>Conclusion</h3><p>The present investigation may find applications in designing and developing a novel, safe and effective anti-<em>H. pylori</em> agents using coumarin scaffold.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 8","pages":"Pages 705-711"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.09.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75940921","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}
Pub Date : 2013-07-01Epub Date: 2013-07-20DOI: 10.1016/j.jopr.2013.05.023
Guduru Rajeswari , Balugari Priyanka , R.E. Amrutha , Cuddapah Rajaram , Rupesh S. Kanhere , Sadhu Nelson Kumar
Objective
The objective of the study is to evaluate the immunomodulatory effect of methanolic leaf extract of Hibiscus tiliaceus (MLHT) in pyrogallol induced immunosuppressed Wistar rats.
Methods
The methanolic extract of leaves of H. tiliaceus 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.
Results
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 (P < 0.001) increase in both primary and secondary HA titer was observed when compared to control group, whereas in H. tiliaceus showed significant (P < 0.001) increase in HA titer. MLHT significantly (P < 0.001) potentiated the DTH reaction by facilitating the footpad thickness response to SRBCs in sensitized rats. Also MLHT evoked a significant (P < 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.
Conclusion
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 H. tiliaceus 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.
{"title":"Hibiscus tiliaceus: A possible immunomodulatory agent","authors":"Guduru Rajeswari , Balugari Priyanka , R.E. Amrutha , Cuddapah Rajaram , Rupesh S. Kanhere , 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> < 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> < 0.001) increase in HA titer. MLHT significantly (<em>P</em> < 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> < 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}
Pub Date : 2013-07-01Epub Date: 2013-08-20DOI: 10.1016/j.jopr.2013.07.008
Vinod Kumar Verma, Khomendra K. Sarwa, Atul Kumar, Md. Kamaruz Zaman
Background
The aim of present study was to demonstrate and compare the hepatoprotective activity of ethanol extract of two well-known plants Swertia chirayita Buch-Ham and Andrographis paniculata (Burm.f.) Nees, in Swiss albino rats.
Method
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 (n = 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 A. paniculata and S. chirayita at the dose of 200 mg/kg b.w. p.o. daily for 16 days respectively.
Results
Ethanol extract of plant S. chirayita and A. paniculata, 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 A. Paniculata 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 A. Paniculata and S. chirayita plant. The histopathological studies of liver were also supported hepatoprotective activity of A. paniculata.
Conclusion
Since results of biochemical studies conclude that the ethanol extract of A. Paniculata showed significant better hepatoprotective as compare to S. chirayita.
{"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, Khomendra K. Sarwa, Atul Kumar, 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 CCl<sub>4</sub> 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 CCl<sub>4</sub> 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}
Pub Date : 2013-07-01Epub Date: 2013-08-19DOI: 10.1016/j.jopr.2013.07.026
S.T. Yamuna , P.R. Padma
Background
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.
Objective
In the present study, goat liver was selected as an in vitro model to determine the antioxidant effects of the three flowers (orange, pink and yellow) of Caesalpinia pulcherrima 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.
Results
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.
Conclusion
Our findings showed that the methanolic extract of the flowers of C. pulcherrima exhibits significant antioxidant activity against H2O2-induced oxidative stress in goat liver model.
{"title":"Antioxidant potential of the flowers of Caesalpinia pulcherrima, Swartz in an in vitro system subjected to oxidative stress","authors":"S.T. Yamuna , 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 (H<sub>2</sub>O<sub>2</sub>). 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 H<sub>2</sub>O<sub>2</sub>-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}
Pub Date : 2013-07-01Epub Date: 2013-07-27DOI: 10.1016/j.jopr.2013.06.010
Yellamma Kuna , Nirmala Kumari Borra
Objectives
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.
Methods
One month old male albino mice, Mus musculus (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.
Results
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.
Conclusions
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.
{"title":"Chronic effects of anti-Alzheimer's drug, Galantamine hydrobromide on cholinergic system of mice brain","authors":"Yellamma Kuna , 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 ED<sub>50</sub> 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}
Pub Date : 2013-07-01Epub Date: 2013-07-27DOI: 10.1016/j.jopr.2013.06.021
Sapna S. Ingle, Chandrahas N. Khobragade
Aim
To investigate potent tyrosinase inhibitor by drug docking analysis.
Methods
The study involved the protein structure of tyrosinase of B. megaterium to investigate the drugs designed by Chem office and drug docking was performed by AutoDock to investigate QSAR activity of the drug.
Results
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 B. megaterium, 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.
Conclusion
All five drugs docked successfully with binding energy in the range of −06.00 kcal/mol suggested significant results.
{"title":"In silico drug docking and screening for the drug discovery of new tyrosinase inhibitors","authors":"Sapna S. Ingle, 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}
Pub Date : 2013-07-01Epub Date: 2013-07-31DOI: 10.1016/j.jopr.2013.07.015
Eman G. Haggag, Mohamed I.S. Abdelhady, Amel M. Kamal
Objectives
This work aimed to isolate phenolics from leaves of Ruprechtia salicifolia and evaluate its immunomodulatory, anti-inflammatory, anticancer and antibacterial activity.
Methods
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.
Results
Eleven known phenolic compounds were isolated for the first time from this species including five flavonoid glycosides viz; Rutin 3, quercetin 3-O-arabinoglucoside 4, apigenin 7-O-β-d-glucoside 5, quercetin 3-O-α-l-arabinofuranoside 6 and isoquercetin 7 along with four aglycones viz; kaemferide 8, apigenin 9, quercetin 10 and naringenin 11 and two phenolic acids; caffeic 1 and gallic 2. Compounds 5 showed the most activity increasing macrophage proliferation implying immunomodulatory activity. 80% MeOH extract, 4, 5 and 11 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 4 and 5 were safe possessing no cytotoxic activity against hepatocellular carcinoma (Hep-G2), breast adenocarcinoma (MCF-7) and colon carcinoma (HCT-116), while Compound 11 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 Klebsiella pneumonia strain, which is resistant to Ciprofloxacin broad-spectrum antibiotic.
Conclusions
R. salicifolia contain phenolics of immunomodulatory anti-inflammatory, cytotoxicity and antibacterial activity, giving R. salicifolia grate potential as a medicinal natural drug.
目的从水杨树叶中分离酚类物质，并评价其免疫调节、抗炎、抗癌和抗菌活性。方法对80%的MeOH叶提取物进行色谱分离，通过不同的色谱和光谱技术(UV、MS、1H和13C NMR)建立化合物的结构。MTT法检测RAW 264.7巨噬细胞增殖的免疫调节作用。分别通过双霉素酸法和ELISA法检测lps刺激细胞对NO和TNF-α因子生成的抑制作用。MTT法测定Hep-G2、MCF-7和HCT-116细胞株的细胞毒性。琼脂扩散法测定抗菌活性。结果首次从该属植物中分离到6个已知的酚类化合物，包括5个类黄酮苷类化合物;芦丁3、槲皮素3- o -阿拉伯葡萄糖苷4、芹菜素7- o -β-d-葡萄糖苷5、槲皮素3- o -α-l-阿拉伯葡萄糖苷6、异槲皮素7及4种糖苷元;山柰素8、芹菜素9、槲皮素10、柚皮素11和两种酚酸;咖啡因和没食子。化合物5对巨噬细胞增殖的促进作用最大，表明其具有免疫调节作用。80% MeOH提取物、4、5和11对lps刺激细胞中亚硝酸盐的抑制作用分别为68.19%、52.95%、20.33%和15.22%，对TNF-α的抑制作用分别为70.82%、29.88%、13.13%和6.14%。80% MeOH叶提取物和化合物4、5对肝细胞癌(Hep-G2)、乳腺癌(MCF-7)和结肠癌(HCT-116)均无细胞毒活性，化合物11仅对HCT-116细胞有细胞毒活性(IC50 = 27.67 μg/ml)。80% MeOH叶提取物对G +ve和G−ve菌均有抑菌活性，且对肺炎克雷伯菌生长有抑制作用，该菌对环丙沙星广谱抗生素具有耐药性。水杨花含有免疫调节、抗炎、细胞毒性和抗菌活性的酚类物质，具有天然药用价值。
{"title":"Phenolic content of Ruprechtia salicifolia leaf and its immunomodulatory, anti-inflammatory, anticancer and antibacterial activity","authors":"Eman G. Haggag, Mohamed I.S. Abdelhady, 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, <sup>1</sup>H and <sup>13</sup>C 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 (IC<sub>50</sub> = 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}
Cuscuta reflexa Roxb., (Convolvulaceae), is well known medicinal plant in Indian System of Medicine for various ailments. We have explored antiproliferative properties of Cuscuta reflexa (whole plant).
Methods
Three extracts (95% alcoholic, 50% hydro-alcoholic and aqueous) and four fractions (n-hexane, chloroform, n-butanol and aqueous) were prepared. In vitro cytotoxicity was observed by using SRB assay and in vivo antitumor activity was also performed using murine models.
Results
The alcoholic extract and its chloroform fraction were found to be most potent among three extracts and four fractions of alcoholic extract. It showed maximum cytotoxicity against human breast (MCF-7) cancer cell lines. The alcoholic extract showed significant (p < 0.05) tumor growth inhibition at 40 mg/kg which were 42.62% and 25.96% for Ehrlich tumor and Sarcoma −180 solid tumor model respectively. Similarly, chloroform fraction of alcoholic extract showed significant tumor growth inhibition of 48.98% and 44.11% for Ehrlich tumor and Sarcoma-180 solid tumor model at 10 mg/kg respectively.
Conclusion
This study indicates that the cytotoxic potential of Cuscuta reflexa lies in its alcoholic extract and chloroform fraction of alcoholic extract of the whole plant due to interference in cell proliferation.
{"title":"In vitro and in vivo antiproliferative potential of Cuscuta reflexa Roxb.","authors":"Madhulika Bhagat , Jatinder Singh Arora , Ajit Kumar Saxena","doi":"10.1016/j.jopr.2013.06.005","DOIUrl":"10.1016/j.jopr.2013.06.005","url":null,"abstract":"<div><h3>Background</h3><p><em>Cuscuta reflexa</em> Roxb., (Convolvulaceae), is well known medicinal plant in Indian System of Medicine for various ailments. We have explored antiproliferative properties of <em>Cuscuta reflexa</em> (whole plant).</p></div><div><h3>Methods</h3><p>Three extracts (95% alcoholic, 50% hydro-alcoholic and aqueous) and four fractions (n-hexane, chloroform, n-butanol and aqueous) were prepared. <em>In vitro</em> cytotoxicity was observed by using SRB assay and <em>in vivo</em> antitumor activity was also performed using murine models.</p></div><div><h3>Results</h3><p>The alcoholic extract and its chloroform fraction were found to be most potent among three extracts and four fractions of alcoholic extract. It showed maximum cytotoxicity against human breast (MCF-7) cancer cell lines. The alcoholic extract showed significant (<em>p</em> < 0.05) tumor growth inhibition at 40 mg/kg which were 42.62% and 25.96% for Ehrlich tumor and Sarcoma −180 solid tumor model respectively. Similarly, chloroform fraction of alcoholic extract showed significant tumor growth inhibition of 48.98% and 44.11% for Ehrlich tumor and Sarcoma-180 solid tumor model at 10 mg/kg respectively.</p></div><div><h3>Conclusion</h3><p>This study indicates that the cytotoxic potential of <em>Cuscuta reflexa</em> lies in its alcoholic extract and chloroform fraction of alcoholic extract of the whole plant due to interference in cell proliferation.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 690-695"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91193475","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}
To develop a stability-indicating reversed phase ultra performance liquid chromatographic (RP-UPLC) method for the determination of related substances in Metoclopramide bulk drugs and pharmaceutical dosage form.
Method
The chromatographic separation was achieved using a Waters X-terra RP18 (150 × 4.6 mm), 3.5 μm particle size column using the gradient program with mobile phase consisting of solvent A: 30 mM monobasic sodium phosphate and 2.3 mM of pentane-1-sulphonic acid sodium salt (pH 3.0 buffer) and solvent-B (Acetonitrile). A flow rate of 1.2 mL/min and UV detector at 273 nm was used. The runtime was 18 min within which Metoclopramide and its four impurities, ACETYLMETO, ACMA, CLEE and ACME were well separated.
Results and discussion
The drug was subjected to stress conditions such as oxidative, acid & base hydrolysis, thermal and photolytic degradation. Metoclopramide was found to degrade significantly in photolytic, oxidative & thermal stress conditions and stable in acid, base, hydrolytic & humidity stress conditions. The major degradation impurities in oxidation and photolytic degradation were identified by LCMS. The degradation products were well resolved from the main peak and its impurities, thus proved the stability-indicating power of the method.
Conclusion
The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness. The calibration curves obtained for the four impurities were linear over the range 0.062–3.040 μg/mL.
{"title":"Novel validated stability-indicating UPLC method for the determination of Metoclopramide and its degradation impurities in API and pharmaceutical dosage form","authors":"Prathyusha Sowjanya , Palani Shanmugasundaram , Petla Naidu , Sanjeev Kumar Singamsetty","doi":"10.1016/j.jopr.2013.07.004","DOIUrl":"10.1016/j.jopr.2013.07.004","url":null,"abstract":"<div><h3>Aim</h3><p>To develop a stability-indicating reversed phase ultra performance liquid chromatographic (RP-UPLC) method for the determination of related substances in Metoclopramide bulk drugs and pharmaceutical dosage form.</p></div><div><h3>Method</h3><p>The chromatographic separation was achieved using a Waters X-terra RP18 (150 × 4.6 mm), 3.5 μm particle size column using the gradient program with mobile phase consisting of solvent A: 30 mM monobasic sodium phosphate and 2.3 mM of pentane-1-sulphonic acid sodium salt (pH 3.0 buffer) and solvent-B (Acetonitrile). A flow rate of 1.2 mL/min and UV detector at 273 nm was used. The runtime was 18 min within which Metoclopramide and its four impurities, ACETYLMETO, ACMA, CLEE and ACME were well separated.</p></div><div><h3>Results and discussion</h3><p>The drug was subjected to stress conditions such as oxidative, acid & base hydrolysis, thermal and photolytic degradation. Metoclopramide was found to degrade significantly in photolytic, oxidative & thermal stress conditions and stable in acid, base, hydrolytic & humidity stress conditions. The major degradation impurities in oxidation and photolytic degradation were identified by LCMS. The degradation products were well resolved from the main peak and its impurities, thus proved the stability-indicating power of the method.</p></div><div><h3>Conclusion</h3><p>The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness. The calibration curves obtained for the four impurities were linear over the range 0.062–3.040 μg/mL.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 7","pages":"Pages 765-773"},"PeriodicalIF":0.0,"publicationDate":"2013-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81469690","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}
Pub Date : 2013-07-01Epub Date: 2013-07-22DOI: 10.1016/j.jopr.2013.07.003
Rajesh Sreedharan Nair, Tai Nyet Ling, Mohamed Saleem Abdul Shukkoor, Balamurugan Manickam
Background/objectives
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.
Methods
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 aloe vera at different concentrations.
Results
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 (>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. Ex vivo 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 (p < 0.05) with the transdermal flux of 54.5 μg/cm2/h.
Conclusions
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.
{"title":"Matrix type transdermal patches of captopril: Ex vivo permeation studies through excised rat skin","authors":"Rajesh Sreedharan Nair, Tai Nyet Ling, Mohamed Saleem Abdul Shukkoor, 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 (>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> < 0.05) with the transdermal flux of 54.5 μg/cm<sup>2</sup>/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}
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