Pharmazie Journal Impact Factor & Information

Publisher: Pharmazeutische Gesellschaft der DDR; Deutsche Arzneibuch-Kommission

Journal description

DiePharmazie is one of the world's leading pharmaceutical journals. As a peer-reviewed scientific journal, DiePharmazie is regularly indexed in Current Contents/Life Sciences, Excerpta Medica, Analytical Abstracts, International Pharmaceutical Abstracts, Beilstein Current Facts in Chemistry, Chemical Engineering and Biotechnology Abstracts (CEABA) and Science Citation Index. The journal DiePharmazie publishes reviews, experimental studies, letters to the editor, as well as book reviews. The following fields of pharmacy are covered: Pharmaceutical and medicinal chemistry, pharmaceutical analysis and drug control, pharmaceutical technolgy, biopharmacy (biopharmaceutics, pharmacokinetics, biotransformation), experimental and clinical pharmacology, pharmaceutical biology (pharmacognosy), history of pharmacy.

Current impact factor: 1.05

Impact Factor Rankings

2015 Impact Factor Available summer 2016
2014 Impact Factor 1.052
2013 Impact Factor 1.003
2012 Impact Factor 0.962
2011 Impact Factor 1.006
2010 Impact Factor 0.869
2009 Impact Factor 0.812
2008 Impact Factor 0.858
2007 Impact Factor 0.775
2006 Impact Factor 0.606
2005 Impact Factor 0.677
2004 Impact Factor 0.587
2003 Impact Factor 0.696
2002 Impact Factor 0.74
2001 Impact Factor 0.498
2000 Impact Factor 0.471
1999 Impact Factor 0.446
1998 Impact Factor 0.419
1997 Impact Factor 0.504
1996 Impact Factor 0.487
1995 Impact Factor 0.466
1994 Impact Factor 0.334
1993 Impact Factor 0.34
1992 Impact Factor 0.309

Impact factor over time

Impact factor

Additional details

5-year impact 1.06
Cited half-life >10.0
Immediacy index 0.19
Eigenfactor 0.00
Article influence 0.22
Website Pharmazie website
Other titles Pharmazie
ISSN 0031-7144
OCLC 1779245
Material type Periodical, Internet resource
Document type Journal / Magazine / Newspaper, Internet Resource

Publications in this journal

  • [Show abstract] [Hide abstract]
    ABSTRACT: APO866 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), and inhibits nicotinamide adenine dinucleotide (NAD) synthesis. Our previous study showed that APO866 inhibits the proliferation of C6 glioblastoma cells, but failed to induce apoptosis. Since APO866 inhibits cellular metabolism and such metabolic stress is closely related with autophagy, thus we determined whether APO866 can induce autophagy in C6 glioblastoma cells and whether the autophagy induced by APO866 is pro-death or prosurvival. Using LC3 immunofluorescence imaging and transmission electron microscopy detection, we found that APO866 at 1-100 nM induced autophagy in C6 glioblastoma cells. APO866 at 1 nM mainly induced initial autophagic vacuoles. Whereas APO866 at 100 nM induced degrading autophagic vacuoles, as well as induced nuclei malformation and mitochondria swelling. In addition, APO866 concentration-dependently decreased the cell viability of C6 glioblastoma cells, and this effect was attenuated by autophagy inhibitors, including 3-methyladenine and LY294002. APO866 concentration-dependently decreased intracellular NAD level. Interestingly, APO866 at 1 nM slightly decreased intracellular NAD level, but dramatically increased autophagy-positive cells. The dramatical cell viability decreasing required the decreasing of intracellular NAD level to a very low threshold. Thus, our results indicated that APO866 induced pro-death autophagy in C6 glioblastoma cells by decreasing intracellular NAD, and low concentration of APO866 can be used as an autophagy inducer in autophagic-death sensitive glioblastoma.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5614
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    ABSTRACT: Here we examined the effects of a DNA methylation inhibitor, 5-azacytidine, on melanogenesis in Mel-Ab cells. We found that 5-azacytidine decreased the melanin content and tyrosinase activity in these cells in a dose-dependent manner; importantly, 5-azacytidine was not cytotoxic at the concentrations used in these experiments. On the other hand, 5-azacytidine did not affect tyrosinase activity in a cell-free system, indicating that 5-azacytidine is not a direct tyrosinase inhibitor. Instead, 5-azacytidine decreased the protein levels of microphthalmia-associated transcription factor (MITF) and tyrosinase. Thus, we investigated the effects of 5-azacytidine on signal transduction pathways related to melanogenesis. However, 5-azacytidine did not have any effect on either Akt or glycogen synthase kinase 3β (GSK3β) phosphorylation. The phosphorylation of cAMP response element-binding protein (CREB) is well known to regulate MITF expression, thereby also regulating tyrosinase expression. We found that 5-azacytidine decreased the phosphorylation of CREB. Therefore, we propose that 5-azacytidine may decrease melanin synthesis by downregulating MITF and tyrosinase via CREB inactivation.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5621
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    ABSTRACT: Rituximab (RTX), a monoclonal antibody against CD20, is known to cause fewer side effects than conventional anti-cancer drugs; however, infusion reaction (IR), which is specific to monoclonal antibody therapy, is frequently triggered by RTX. Therefore, we designed this study to identify risk factors based on clinical test values for developing IR after RTX administration. Eighty-nine patients with B-cell non-Hodgkin's lymphoma who had received RTX for the first time between February 2010 and March 2013, at the Gifu Municipal Hospital were enrolled as subjects. Analysis of data was conducted for 87 patients, after excluding patients whose data were missing. Univariate analysis showed significant differences in the number of patients exhibiting a soluble interleukin-2 receptor (sIL-2R) level > 2,000 U/L and hemoglobin (Hb) 2,000 U/L [odds ratio (OR), 4.463; 95% confidence interval (CI), 1.262-15.779; P = 0.020], Hb P = 0.038], and steroid administration [OR, 0.284; 95% CI, 0.094-0.852; P = 0.025]. Our findings show that sIL-2R > 2,000 U/L, Hb Document Type: Research Article DOI: Publication date: October 1, 2015 More about this publication? Pharmazie is one of the world's leading pharmaceutical journals. As a peer-reviewed scientific journal, DiePharmazie is regularly indexed in Current Contents/Life Sciences, Excerpta Medica, Analytical Abstracts, International Pharmaceutical Abstracts, Beilstein Current Facts in Chemistry, Chemical Engineering and Biotechnology Abstracts (CEABA) and Science Citation Index. Information for Authors Submit a Paper Subscribe to this Title Terms & Conditions ingentaconnect is not responsible for the content or availability of external websites $(document).ready(function() { var shortdescription = $(".originaldescription").text().replace(/\\&/g, '&').replace(/\\, '<').replace(/\\>/g, '>').replace(/\\t/g, ' ').replace(/\\n/g, ''); if (shortdescription.length > 350) { shortdescription = "" + shortdescription.substring(0,250) + "... more"; } $(".descriptionitem").prepend(shortdescription); $(".shortdescription a").click(function(e) { e.preventDefault(); $(".shortdescription").hide(); $(".originaldescription").slideDown(); }); }); govi/pharmaz/2015/00000070/00000010/art00009 dcterms_title,dcterms_description,pub_keyword 6 5 20 40 5 GA_googleFillSlot("Horizontal_banner_bottom");
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5620
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    ABSTRACT: 3'4'7-Trihydroxyflavone is a flavonoid from ladino clover, alfalfa, and Albizzia julibrissin. In the present study, we found that 3'4'7-trihydroxyflavone markedly inhibited the receptor activator of nuclear factor kappa B ligand (RANKL) induced osteoclastic differentiation from mouse bone marrow derived macrophages (BMMs). 3'4'7-trihydroxyflavone also reduced the mRNA expression level of osteoclastic marker genes including calcitonin receptor (CTR), Cathepsin K, v-ATPase V0 subunit d2 (ATP6v0d2), and dendritic cell-specific transmembrane protein (DC-STAMP). In addition, 3'4'7-trihydroxyflavone decreased the bone resorption activity of osteoclasts on dentin slices. We found that 3'4'7-trihydroxyflavone inhibited RANKL-induced expression of nuclear factor of activated T cells c1 (NFATc1), a key transcription factor of osteoclast differentiation. Furthermore, 3'4'7-trihydroxyflavone attenuated RANKL-induced activation of p38 mitogenactivated protein kinase (MAPK) and expression of B lymphocyte-induced maturation protein 1 (Blimp1), a repressor of negative regulators of NFATc1. Taken together, our data suggest that 3'4'7-trihydroxyflavone inhibits osteoclastogenesis via NFATc1.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5575
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    ABSTRACT: Pharmacogenomics explores the variations in both the benefits and the adverse effects of a drug among patients in a target population by analyzing genomic profiles of individual patients. Minerals and trace elements, which can be found in human tissues and maintain normal physiological functions, are also in the focus of pharmacogenomic research. Single-nucleotide polymorphisms (SNPs) affect the metabolism, disposition and efficacy of minerals and trace elements in humans, resulting in changes of body function. This review describes some of the recent progress in pharmacogenomic research related to minerals and trace elements.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5591
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    ABSTRACT: After Estonia, Latvia and Lithuania proclaimed their independence in 1918 and began to create their national health care systems, one of their stated priorities was the formulation and publication of national pharmacopoeias. In order to accomplish this, working groups as well as commissions composed of pharmacists, medical specialists and even linguists had to be formed. The process was long and difficult. New terminology in native languages had to be created. Sources for the monographs had to be chosen, researched, analyzed and compared. There were organizational and financial problems. Nevertheless, by the late 1930s, all three Baltic States published their national pharmacopoeias. Officially, they were not able to use them for long because during World War II all three were occupied and annexed by the Soviet Union. Pharmacists in those countries were obliged to use the Soviet pharmacopoeias, although unofficially, they also made good use of their national ones. Currently, the European Pharmacopoeia is in use in Estonia, Latvia and Lithuania.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5082
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    ABSTRACT: This study aimed to monitor liquid-liquid extraction of Gardenia jasminoides Ellis (Zhizi in Chinese) using in-line near-infrared spectroscopy. Shanzhiside (SZS), deacetyl asperulosidic acid methyl ester (DAAME), genipin-1-β-D-gentiobioside (GG), geniposide (GS), total acids (TA) and soluble solid content (SSC) were selected as quality control indicators, and measured by reference methods. Both partial least-squares regression (PLSR) and back propagation artificial neural networks (BP-ANN) were applied to create models to predict the content of above indicators. Paired-samples t-test and nonparametric test were used to compare differences in predictive values between two models of each indicator. Relative standard error of prediction (RSEP) and mean absolute percentage error (MAPE) were used to evaluate the predictive accuracy of the established models. The results showed that there was no significant difference in predicting DAAME, GS and TA between two models. However, PLSR model gave better accuracy in predicting GG and SZS than BP-ANN model. The BP-ANN model of SSC was better than PLSR model. This study shows that NIR spectroscopy can be used for rapid and accurate analysis of quality control indicators in the liquid-liquid extraction of Zhizi. Simultaneously, this study can serve as technical support for the application of NIR spectroscopy in the industrial production process.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.4173
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    ABSTRACT: MicroRNA-184 (miR-184) is found to be significantly deregulated in human cancers associated with tumorigenesis and progression. In this study, we aimed to investigate the role and mechanism of miR-184 expression in epithelial ovarian cancer (EOC). Relative expression of miR-184 was measured by quantificational real-time polymerase chain reaction assay (qRT-PCR) in 80 EOC patients. Kaplan-Meier curve and the log-rank test were conducted to detect the prognostic value of miR-184. Function assays including cell proliferation, apoptosis and inflammation were further explored in vitro. We found that miR-184 was down-regulated in EOC tissues and cell lines compared with paired non-cancerous tissues and IOSE, respectively. Moreover, miR-184 was expressed at significantly lower levels in late-stage (III/IV) EOC tissues. Cox regression multivariate analysis indicated that miR-184 and FIGO stage were independent prognostic indicators for EOC patients. Patients with high miR-184 level achieved significantly a higher 5-year survival rate compared with low level group (P in vitro. Altogether, our results suggest that miR-184 together with pathologic diagnosis is critical for prognosis determination in EOC patients and help select treatment strategy.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5577
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    ABSTRACT: Although chemical trapping has been widely used to evaluate cytochrome P450-mediated drug bioactivation, thus far, only a few in vitro-trapping studies have been performed on UDP-glucuronosyltransferase (UGT)-mediated drug bioactivation. In this study, we used cysteine (Cys) as trapping agent to gain new insights into the UGT-mediated bioactivation involving acyl glucuronides of carboxylic acid drugs. Diclofenac, ketoprofen and ibuprofen were incubated in human liver microsomes with UDPGA and Cys, followed by analysis using ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS). The N-acyl-Cys amide adduct of diclofenac was characterized by mass analysis and was detectable even in photodiode array analysis. Our data indicated that the formation of such adducts reflects the reactivity of the corresponding acyl glucuronides. In addition, it was suggested that the adduct formation requires an N-terminal Cys moiety with both a free amine and a free thiol group, from the results using various cysteine derivatives. We propose that the S-acyl-Cys thioester adduct can form via transacylation of an acyl glucuronide and can then form to an N-acyl-Cys amide adduct through intramolecular S- to N-acyl rearrangement. This series of the reactions has important implications as a possible bioactivation mechanism for covalent binding of carboxylic acid drugs to macromolecules.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5636
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    ABSTRACT: Regulatory B cells (Breg) are a distinct B cell subset, which contribute to the pathogenesis of autoimmune disorders. Interleukin-10 (IL-10) plays a pivotal function to Breg. It is well described in adults but little is known in a pediatric population. This study was to investigate the role of IL-10-producing B cell (B10) and its association with Treg and Th17 subsets in the children with inflammatory bowel diseases (IBD). Peripheral blood mononuclear cells from IBD children patients and controls were stimulated with PMA, ionomycin, and brefeldin A. The frequencies of CD19+IL-10+ B cells, CD3+CD4+IL-17+Th17 cells, and CD4 + CD25hiFoxp3+ Treg cells were analyzed by flow cytometry. The mRNA expression of Foxp3, IL-17a and RORγt was detected by real-time quantitative PCR. The number of B10 cells was elevated in IBD children patients. There was a positive correlation between B10 cells and Tregs in IBD. The ratio of Treg/Th17 decreased in IBD, and it strongly correlated with B10 cells. The frequency of B10 cells is elevated in IBD and it correlates with both the Tregs counts and the Treg/Th17 ratio. B10 cells to regulate functional T cell subsets might be impaired in paediatric patients with IBD.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.5606
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    ABSTRACT: Process analytical technology is important for the analysis and control of manufacturing processes. Near-infrared spectroscopy is widely used in various process analytical technologies for the analysis of the chemical componentsof solid dosage forms. Lubrication is an important process carried out before a tablet is produced. In this process, the concentration of lubricant, such as magnesium stearate (StMg), might change for one of many reasons during powder transport, which would be a critical problem such as variation in tablet compressibility and dissolution failure of compressed tablets. Our group investigated the feasibility of the quantitative monitoring of a change in the concentration of StMg in the feeder tube of tableting equipment employing real-time near-infrared spectroscopy.
    Pharmazie 10/2015; 70(10). DOI:10.1691/ph.2015.4219
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    ABSTRACT: Schisandrin B (Sch B), the most abundant dibenzocyclooctadiene lignan isolated from the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill, possesses various biological activities, such as hepatic protection, anti-tumor, anti-inflammatory and anti-cardiovascular properties. However, the effect of Sch B on inflammatory bowel disease (IBD) is not yet known. The aim of this study was to investigate whether Sch B has protective effect against dextran sulfate sodium (DSS)-induced colitis in a mouse model. The acute mouse model of IBD was induced by drinking 2.5% DSS water for 5 days. Sch B was administered orally in doses of 10, 40, and 100 mg/kg respectively. It significantly reduced concentration of TNF-α, IL-1β, INF-γ and IL-6 in colon tissue as well as the mRNA expression levels. In addition, we demonstrated that Sch B blocked the phosphorylation of IκBα, nuclear factor-κB (NF-κB) p65, p38 mitogen-activated protein kinase (MAPK), c-Jun NH2-terminal kinase, and extracellular signal regulated kinase in DSS-induced acute colitis. In conclusion, these results indicated that Sch B could exert beneficial effects on experimental IBD induced by DSS and may represent a novel treatment strategy for IBD.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5561
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    ABSTRACT: Rapamycin, a classical inhibitor of the mammalian target of rapamycin (mTOR), has been intensively studied for its role in metabolism and verified to induce metabolic defects through mTORC2/Akt pathway. However, disparity of the results exists depending on the differences of the animal models or the detailed procedures. Moreover, data regarding the effect of rapamycin treatment in diabetic models are sparse. Therefore, we investigated its influence on glucose and lipid metabolism, and further analyzed its effect on the mTORC2/Akt pathway in a high-fat diet- and streptozotocin-induced diabetic mice model. Three-weeks old C57BL/6J mice were fed with a high fat diet (60 kcal% fat) and intraperitoneally injected with streptozotocin (100 mg/kg) at 6 weeks of age. Rapamycin (2 mg/kg) was orally given to the mice daily for consecutive 6 weeks. Body weight, blood lipid parameters and HbA1c% values were evaluated. Oral glucose test and insulin tolerance test were performed. Furthermore, western blot assay was applied to investigate the protein epression levels of Akt and PKC , two key targets of the mTORC2/Akt pathway. Rapamycin-treated diabetic mice demonstrated less weight gain, more profound symptoms of polydipsia, polyphagia and polyuria, significant liver fat accumulation and exacerbated metabolic disorders including insulin resistance, hyperglycemia and dyslipidemia. Contrary to what have been expected, though significantly inhibiting mTORC1/S6K1 signaling, chronic rapamycin treatment failed to down-regulate mTORC2/Akt pathway. Our findings provide evidence that chronic rapamycin treatment may exacerbate metabolism in diabetic subjects and does not down-regulate mTORC2/Akt signialing in a high-fat diet- and streptozotocin- induced diabetic mice model.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.4847
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    ABSTRACT: Niemann-Pick C1-like 1 (NPC1L1) protein is the key transporter responsible for dietary cholesterol absorption. Recent studies indicated that several functional polymorphisms of NPC1L1 were associated with coronary heart disease (CHD) and response to ezetimibe therapy. The aim of the present study was to analyze the allele frequency and haplotype distribution of NPC1L1 polymorphisms in Chinese Hans and to compare them with those of other ethnic populations reported before. Blood samples were collected from 424 unrelated Chinese Hans (246 males and 178 females). Ten NPC1L1 polymorphisms (-762T > C, -133A > G, -18C > A, 1721C > T, 1735C > G, 1764T > C, 1767G > A, 27677T > C, 25342A > C and 28650A > G) were genotyped by direct sequencing or polymerase chain reaction–restriction fragment length polymorphism (PCR-RFLP) assay. Among the variants, the minor allele frequency of -762T > C and 1735C > G were 35.0% and 37.0%, respectively. Furthermore, these two polymorphisms were highly linked with a D' value of 0.80. The observed frequencies of two major haplotypes were 59.1% for T-762/C1735 and 30.1% for C-762/G1735, respectively. The frequencies of the rest variants were extremely low (1.8% for-133G, 1.5% for -18A, 0.9% for 1721T and only 0.2% for 27677C allele, respectively) or even not detected (1764T > C, 1767G > A, 25342A > C and 28650A > G) in our study population. Comparison with other ethnic populations revealed a remarkable genetic variability in the incidences of NPC1L1 polymorphisms. The frequencies of NPC1L1 polymorphisms in Chinese Hans are comparable to Japanese population but totally different from Caucasians, African-Americans and Hispanic individuals. This is the first study to report the ethnic difference in the frequencies of NPC1L1 functional polymorphisms in detail. -762T > C and 1735C > G are two prevalent NPC1L1 variants which need further studies to explore their clinical impact on CHD prevalence and response to ezetimibe therapy in Chinese Hans.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5582
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    ABSTRACT: Historical research may be able to contribute to the exploration of traditional knowledge about medicinal plants and promising attempts have been made investigating Byzantine texts, Early Modern herbals, and writings of Christian missionaries. In this pilot study it should be explored if publications, travel reports, diaries or correspondence of the botanical explorers of the 19th and early 20th centuries may serve a source of ethnopharmacological information as well and may be able to guide modern phytopharmacological research. Writings of Berthold Seemann (1825-1871), a German investigator exploring the botany of Middle America, the Fiji islands and other regions, are investigated as a first example. It could be shown that Seemann’s heritage mainly kept at Kew Garden Archives, does contain ethnopharmacological information which in part has already been confirmed by recent study results indicating some reliability of his observations. However, there are also reports about traditional medicinal plants scarcely investigated so far, including Schultesia stenophylla Mart. (syn. S. guainensis (Aubl.) Malme), Trixis inula Crantz,Waltheria glomerata Presl., Gonophlebium attenuatum (Humb. & Bonpl. Es Willd) C. Presl., or Pseudoelephantopus spicatus (Juss ex Aubl.) C.F. Baker. It is suggested to further explore their potential as medicinal plants. In general, as Seemann’s example has shown, publications and correspondence of botanical explorers of the past seem to be a valuable and hitherto almost neglected source of information to be considered in further historical and ethnopharmacological research.
    Pharmazie 09/2015; 70(9):616-626. DOI:10.1691/ph.2015.5601
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    ABSTRACT: Breviscapine (BE) is a standardized Chinese herbal medicine extracted from Erigeron breviscapus (Vant.) Hand.-Mazz. It has been widely used to treat cardiovascular and cerebrovascular diseases. However, there are no reports on the protective effects and underlying molecular mechanisms of BE action on myocardial ischemia/reperfusion (MI/R)-induced cardiomyocyte apoptosis. In the present study, we aimed to confirm the cardioprotective effect of BE from MI/R injury in vivo, and investigate the potential molecular mechanisms against simulated ischemia/reperfusion (SI/R)-induced cardiomyocyte apoptosis in vitro. The rat model of MI/R injury was induced by 30 min of transient vessel occlusion followed by 3 h of reperfusion. BE significantly reduced the myocardium infarct size and production of cardiac troponin (cTnI) in serum. In an in vitro experiment, H9c2 cardiomyocytes were incubated with vehicle or ischemic buffer during hypoxia; then, they were reoxygenated with or without BE. BE markedly improved the cell viability and decreased lactate dehydrogenase (LDH) release. We confirmed the anti-apoptotic effect of BE with the Hoechst 33258 staining assay, and this effect was associated with an increase in Bcl-2 and a decrease in active caspase-3 expression. Western blot analysis also showed that BE increased the phosphorylation of Akt and eNOS in H9c2 cells, and the protective effects of BE were partially inhibited by the phosphatidylinositol 3'-kinase (PI3K) specific inhibitor LY294002. Our results suggested that BE could provide significant cardioprotection against MI/R injury, and the potential mechanisms might involve suppression of cardiomyocyte apoptosis through activating the PI3K/Akt/eNOS signaling pathway.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5552
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    ABSTRACT: Endonuclease G (Endo G) is a novel determinant of cardiac hypertrophy. Here, we report the characterization of Endo G and mitochondria-sarcoplasmic reticulum-related proteins during cardiac hypertrophy, and hypothesize that Endo G regulate mitochondrial function partly through Mfn2 and Jp2 during cardiac hypertrophy. Our results show that Endo G levels gradually increased at the beginning of phenylephrine-induced cardiac hypertrophy, accompanied by an abnormal mitochondrial membrane potential. The up-regulation of Mfn2, Jp2, and Endo G appeared at an early stage of cardiac hypertrophy, whereas PGC1 was not up-regulated until a later stage. Abolishing Endo G with siRNA led to the uncoupling of the mitochondrial electron transport chain from ATP production and decreased PGC1 expression, likely by affecting the juxtaposition of the mitochondria and the sarcoplasmic reticulum via Mfn2 and Jp2. Furthermore, abolishing Jp2 altered the expression of Endo G expression and induced mitochondrial dysfunction, suggesting that mitochondrial abnormalities in cardiac hypertrophy are most likely caused by Endo G. Taken together, our study established a link between Endo G and mitochondrial function during cardiac hypertrophy, partly through the effects of Endo G on Mfn2 and Jp2, and revealed a role for Endo G in the crosstalk between the processes controlled by Mfn2 and Jp2 in maladaptive cardiac hypertrophy.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5559
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    ABSTRACT: A capillary zone electrophoresis method for quantitative determination of doripenem in synthetic matrix was developed. The stability-indicating capability was performed applying stress testing protocols. The selected analytical conditions include 100 mM sodium borate buffer (pH 8.0) as run electrolyte, voltage of + 15 kV, hydrodynamic injection of 5 s (50 mBar), detection at 298 nm and temperature of analysis of 25 °C. The electrophoretic separation was carried out in a fused silica capillary (effective length 40 cm, 50 μm i.d.), using procainamide hydrochloride as internal standard. The proposed method showed quickness and reproducibility, with an analytical run in a total time of 5 min. The percentage of drug amount estimated was 101.33% (RSD=0.80), with satisfactory intra-day and inter-day precision. In the recovery test, the method was found to be reliable and accurate in the drug quantitation (mean recovery = 101.86%). The robustness was performed applying the Plackett–Burman experimental design which confirmed the assay reliability. Based on results from forced degradation study, the stability-indicating capability was established, being observed a major degradation in alkaline, photolytic and thermal conditions. In comparison to HPLC method previously developed, the proposed capillary electrophoresis assay is statistically equivalent.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5008
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    ABSTRACT: Several natural compound interfere with microtubules or the actin cytoskeleton. Compounds interfering with the microtubules like Vinca-alkaloids or taxanes, are extensively used for cancer therapy. In contrast, knowledge about pharmacological properties of actin binding drugs is poor and drugs interfering with actin are far from clinical use. Rhizopodin is a natural compound that strongly affects the actin cytoskeleton at nanomolar concentrations. Initial work revealed interesting anti-bacterial and cytotoxic effects, but the cellular effects and pharmacological properties of rhizopodin have not been characterized. We hypothesized that rhizopodin might exert anti-cancer activity. Therefore, the aim of this study was to characterize the cellular and pharmacological effects of rhizopodin in cancer. Effects of rhizopodin demonstrated prominent effects on the actin cytoskeleton as shown in the actin-pyrene assay and by immunostaining of cancer cells. To investigate cellular effects of rhizopodin, we analyzed cell proliferation, cell death induction by propidium iodide exclusion and western blot, as well as migration by impedance measurement using the xCELLligence device in MDA-MB-231 breast cancer and T24 bladder cancer cell lines. Rhizopodin inhibited proliferation and induced cell death of MDA-MB-231 and T24 cells at nanomolar concentrations. PARP cleavage by rhizopodin suggests caspase-dependent cell death induction. Importantly, rhizopodin potently inhibited MDA-MB-231 and T24 cancer cell migration at subtoxic doses where no actin aggregation was observed, indicating a specific underlying signaling of rhizopodin. In summary, our study elucidates rhizopodin as actin-binding natural compound that exerts potent anti-cancer effects. Therefore, our work provides the basis for further in depth characterization of rhizopodin as an antitumoral agent.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5579