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Sci. Pharm., Volume 77, Short Lectures (SL) (March 2009) – 32 articles , Pages 168-199

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220 KiB  
Abstract
Virtual and Real Screening of Natural Products to Find Effective Modulators of Protein Tyrosine Phosphatase PTP1B
by R. R. BAUMGARTNER, T. M. STEINDL, D. SCHUSTER, J. M. ROLLINGER, G. WOLBER, H. STUPPNER, A. G. ATANASOV, E. H. HEISS and V. M. DIRSCH
Sci. Pharm. 2009, 77(6), 199; https://doi.org/10.3797/scipharm.oephg.21.SL-32 - 16 Apr 2009
Viewed by 1028
Abstract
The protein tyrosine phosphatase 1B (PTP1B) is an important negative regulator of the insulin receptor. Elchebly M. et al showed that PTP1B knockout mice enhanced insulin sensitivity and were completely healthy and resistant to weight gain when put on a high fat diet [...] Read more.
The protein tyrosine phosphatase 1B (PTP1B) is an important negative regulator of the insulin receptor. Elchebly M. et al showed that PTP1B knockout mice enhanced insulin sensitivity and were completely healthy and resistant to weight gain when put on a high fat diet (1). This makes PTP1B a promising target for diabetes type 2 and metabolic syndrome. Full article
199 KiB  
Abstract
Austrian Red Wine Samples Reveal Enhanced Activity of the Enzyme Endothelial Nitric Oxide Synthase
by O. DONATH, R. EDER, G. REZNICEK and V. M. DIRSCH
Sci. Pharm. 2009, 77(6), 198; https://doi.org/10.3797/scipharm.oephg.21.SL-31 - 16 Apr 2009
Viewed by 720
Abstract
Red wine polyphenol extracts (RWPE) have been shown to increase nitric oxide (NO) release from EA.hy926 endothelial cells [1]. Trans-resveratrol seems to partly contribute to this effect by inducing endothelial NO-synthase (eNOS) expression [1]. Aim of this study is to identify further major [...] Read more.
Red wine polyphenol extracts (RWPE) have been shown to increase nitric oxide (NO) release from EA.hy926 endothelial cells [1]. Trans-resveratrol seems to partly contribute to this effect by inducing endothelial NO-synthase (eNOS) expression [1]. Aim of this study is to identify further major active component(s) by bio-assay guided fractionation. Full article
199 KiB  
Abstract
Expression of Sulfotransferases and Sulfatases in Human Breast Cancer: Impact on Resveratrol Metabolism
by M. MIKSITS, K. WLCEK, M. SVOBODA, T. THALHAMMER and W. JÄGER
Sci. Pharm. 2009, 77(6), 197; https://doi.org/10.3797/scipharm.oephg.21.SL-30 - 16 Apr 2009
Viewed by 654
Abstract
Resveratrol is a naturally occurring anticancer compound present in grapes and wine that undergoes pronounced metabolism in human intestine and liver. In order to determine whether resveratrol is also biotransformed in human breast carcinoma, metabolism experiments were conducted in breast tumor and adjacent [...] Read more.
Resveratrol is a naturally occurring anticancer compound present in grapes and wine that undergoes pronounced metabolism in human intestine and liver. In order to determine whether resveratrol is also biotransformed in human breast carcinoma, metabolism experiments were conducted in breast tumor and adjacent non-tumorous specimens from 13 patients. Resveratrol was metabolized in cytosolic tissue fractions to resveratrol-3-O-sulfate: the formation rates were up to 33.5-fold higher in cancer samples than in peritumoral tissue. Full article
197 KiB  
Abstract
Expression of Organic Anion Transporter Polypeptides (OATPs) in Human Breast Carcinoma
by K. WLCEK, M. SVOBODA, T. THALHAMMER and W. JÄGER
Sci. Pharm. 2009, 77(6), 196; https://doi.org/10.3797/scipharm.oephg.21.SL-29 - 16 Apr 2009
Cited by 1 | Viewed by 701
Abstract
Organic anion transporter polypeptides (OATPs) mediate the transmembrane uptake of endogenous compounds and clinically important drugs in various tissues thereby effecting drug disposition and tissue penetration. OATPs have also been identified in gastric, pancreatic, and colon carcinomas but little is known about their [...] Read more.
Organic anion transporter polypeptides (OATPs) mediate the transmembrane uptake of endogenous compounds and clinically important drugs in various tissues thereby effecting drug disposition and tissue penetration. OATPs have also been identified in gastric, pancreatic, and colon carcinomas but little is known about their expression in breast carcinoma. We therefore analyzed the expression pattern of all 11 known OATPs in three breast cancer cell lines (MCF-7, ZR-75-1, MDA-MB-231) and one immortalized breast epithelial cell line (MCF-10A) using quantitative PCR. Transcripts of 7/11 OATP genes with a remarkable heterogeneity in their expression profile were detected in control and/or cancer cell lines.[...] Full article
216 KiB  
Abstract
Absolute Bioavailability and Metabolism of Dodeca-2E,4E,8E,10E/Z-tetraenoic acid isobutylamides (“tetraene”) after Intravenous and Oral Single Doses to Rats
by K. WÖLKART, R. FRYE, H. DERENDORF, R. BAUER and V. BUTTERWECK
Sci. Pharm. 2009, 77(6), 195; https://doi.org/10.3797/scipharm.oephg.21.SL-28 - 16 Apr 2009
Viewed by 683
Abstract
This study assessed the absolute and relative bioavailabilities of dodeca-2E,4E,8E,10E/Z-tetraenoic acid isobutylamides (tetraene), one of the main bioactive constituents in Echinacea, administered as pure compounds or as an Echinacea purpurea root extract preparation. Ten rats [...] Read more.
This study assessed the absolute and relative bioavailabilities of dodeca-2E,4E,8E,10E/Z-tetraenoic acid isobutylamides (tetraene), one of the main bioactive constituents in Echinacea, administered as pure compounds or as an Echinacea purpurea root extract preparation. Ten rats received 0.75 mg/kg dodeca-2E,4E,8E,10E/Z-tetraenoic acid isobutylamides oral, pure and within 158.6 mg/kg Echinacea purpurea extract, or intravenous.[...] Full article
200 KiB  
Abstract
Reverse Chemical Proteomics in Drug Discovery
by M. GOTSBACHER and P. KARUSO
Sci. Pharm. 2009, 77(6), 194; https://doi.org/10.3797/scipharm.oephg.21.SL-27 - 16 Apr 2009
Viewed by 774
Abstract
With advances in separation technology and structure elucidation, the main bottleneck limiting drug development from natural products is the identification of their cellular targets. Although effective therapeutic agents can be developed and successfully administered without knowledge of the underlying mechanism of action, elucidation [...] Read more.
With advances in separation technology and structure elucidation, the main bottleneck limiting drug development from natural products is the identification of their cellular targets. Although effective therapeutic agents can be developed and successfully administered without knowledge of the underlying mechanism of action, elucidation of drug target proteins is essential in the design of new compounds with improved safety and efficacy [1].[...]
Full article
217 KiB  
Abstract
Falcarinol Content in Carrot Genotypes Determined by LC-MS
by V. GETZINGER, E. M. PFERSCHY-WENZIG, O. KUNERT, K. WÖLKART, J. ZAHRL and R. BAUER
Sci. Pharm. 2009, 77(6), 193; https://doi.org/10.3797/scipharm.oephg.21.SL-26 - 16 Apr 2009
Viewed by 786
Abstract
For the determination of falcarinol [(3R,9Z)-heptadeca-1,9-diene-4,6-diyn-3-ol] in various genotypes of carrots (Daucus carota L.) a new LC–MS method has been developed and validated. The method consists of accelerated solvent extraction (ASE) of lyophilized carrot root samples with ethyl acetate and LC–ESI MS [...] Read more.
For the determination of falcarinol [(3R,9Z)-heptadeca-1,9-diene-4,6-diyn-3-ol] in various genotypes of carrots (Daucus carota L.) a new LC–MS method has been developed and validated. The method consists of accelerated solvent extraction (ASE) of lyophilized carrot root samples with ethyl acetate and LC–ESI MS analysis of the extracts.[...] Full article
200 KiB  
Abstract
Antiasthmatic Compounds Isolated from Antiasthmatic “JAMU” Ingredient Legundi Leaves (Vitex trifolia L.)
by S. WAHYUONO, G. ALAM, Z. IKAWATI, H. TIMMERMAN and K. MAEYAMA
Sci. Pharm. 2009, 77(6), 192; https://doi.org/10.3797/scipharm.oephg.21.SL-25 - 16 Apr 2009
Cited by 1 | Viewed by 862
Abstract
“JAMU” Indonesian traditional medicine preparations have been utilized extensively by Indonesian people. Due to lack of scientific and clinical data, JAMU has not been recommended for formal medication although it has been practiced long before recorded history. Therefore, this study aimed to screen [...] Read more.
“JAMU” Indonesian traditional medicine preparations have been utilized extensively by Indonesian people. Due to lack of scientific and clinical data, JAMU has not been recommended for formal medication although it has been practiced long before recorded history. Therefore, this study aimed to screen those plant materials (0.25 and 0.50 mg/ml, n=3) for tracheospasmolytic activity in vitro (spasms induced by histamine 10-7-10-3 M) in order to obtain the promising active compounds to be studied for their mechanisms of actions. The leaves of Vitex trifolia were among the most promising material and further studied. By bioassay guided isolation, 3 compounds were isolated and identified as viteosin-A (1), vitexicarpin (2) and vitetrifolin-E (3) based on their spectroscopic and literature data. Compound 2 was the most active as compared to 1 and 3 in a tracheospasmolytic test using sensitized (ovalbumin 5, 50, 500, 5000 ng/ml, n=3) guinea pig trachea. These compounds were not harmful to the organ as it was proved by inducing the organ after the test with carbachol, followed by saturated KCl. Their mechanism seems to be non-competitive antagonistic to histamine, and the compounds are possibly able to stabilize the mast cells membrane function. Upon testing of those compounds (1 x 10-4 M) on RBL-2H3 (Rat Basophilic Leukemia cells represent mucosal mast cells) induced by DNA-BSA (Dinitrophenylated Bovine Serum Albumin), compound 2 still showed the strongest effect to inhibit the histamine release as compared to that of 1 and 2. Full article
217 KiB  
Abstract
Gadolinium-labeled PLGA Nanoparticles for Magnetic Resonance Imaging
by G. RATZINGER, P. AGRAWAL, M. WIRTH, W. KÖRNER, K. NICOLAY and F. GABOR
Sci. Pharm. 2009, 77(6), 191; https://doi.org/10.3797/scipharm.oephg.21.SL-24 - 16 Apr 2009
Viewed by 651
Abstract
To date, the main two classes of clinically used contrast agents for magnetic resonance imaging (MRI) are soluble paramagnetic gadolinium chelates and superparamagnetic iron oxide particles. While iron oxides predominantly increase T2-relaxivity and thus provide negative contrast, gadolinium chelates are often requested as [...] Read more.
To date, the main two classes of clinically used contrast agents for magnetic resonance imaging (MRI) are soluble paramagnetic gadolinium chelates and superparamagnetic iron oxide particles. While iron oxides predominantly increase T2-relaxivity and thus provide negative contrast, gadolinium chelates are often requested as they increase T1-relaxivity and enhance positive contrast. As particulate contrast agents are preferable due to a more favorable signal-to-noise ratio, the goal of our present work was the development of poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles labeled with chelated gadolinium. Full article
377 KiB  
Article
Differences in the Glycocalyx of 5637 and SV-HUC-1 Cells and their Impact on Lectin Targeting
by V. E. PLATTNER, F. GABOR, G. BORCHARD and M. WIRTH
Sci. Pharm. 2009, 77(6), 190; https://doi.org/10.3797/scipharm.oephg.21.SL-23 - 16 Apr 2009
Viewed by 748
Abstract
Background: Bladder cancer is one of the most common malignancies. Advances have been made in diagnosis, therapy, and surveillance resulting in increasing survival rates of patients, but the search for more effective therapies is imperative to be continued. Among others, lectin-mediated targeting might [...] Read more.
Background: Bladder cancer is one of the most common malignancies. Advances have been made in diagnosis, therapy, and surveillance resulting in increasing survival rates of patients, but the search for more effective therapies is imperative to be continued. Among others, lectin-mediated targeting might be a promising concept. Thus, the potential of fluorescein-labeled plant lectins was investigated using 5637 cells as a model for human urinary carcinoma [1] and SV-HUC-1 cells as a model for non-tumorigenic human uroepithelial cells. Full article
198 KiB  
Abstract
Influence of Microplate Mixing on Binding Assays
by C. FILLAFER, R. NOWOTNY, M. WIRTH and F. GABOR
Sci. Pharm. 2009, 77(6), 189; https://doi.org/10.3797/scipharm.oephg.21.SL-22 - 16 Apr 2009
Viewed by 643
Abstract
Introduction: Microplate-based analytical assays represent one of the most commonly used tools for the sensitive and reproducible detection of bioactive molecules. However, despite the widespread use of microplate assays, the degree of optimisation of the experimental procedures is questionable [1]. Effective mixing is [...] Read more.
Introduction: Microplate-based analytical assays represent one of the most commonly used tools for the sensitive and reproducible detection of bioactive molecules. However, despite the widespread use of microplate assays, the degree of optimisation of the experimental procedures is questionable [1]. Effective mixing is expected to shorten incubation periods, increase reproducibility and sensitivity. To investigate this, the association of cytoadhesive lectins and lectin-modified nanoparticles to epithelial cell monolayers was determined under stationary and mixing conditions. Full article
199 KiB  
Abstract
Cells “Feel” Their Surroundings – Implications for Biomedicine and Drug Delivery
by L. NEUTSCH, I. C. GEBESHUBER, F. AUMAYR and F. GABOR
Sci. Pharm. 2009, 77(6), 188; https://doi.org/10.3797/scipharm.oephg.21.SL-21 - 16 Apr 2009
Viewed by 653
Abstract
Cell-based research is a booming sector in life science. In vitro assays on cultured cells greatly foster the development of novel therapy concepts for a broad range of diseases, and upcoming techniques such as tissue engineering will soon bring benefits in the field [...] Read more.
Cell-based research is a booming sector in life science. In vitro assays on cultured cells greatly foster the development of novel therapy concepts for a broad range of diseases, and upcoming techniques such as tissue engineering will soon bring benefits in the field of regenerative medicine. Especially the beginning era of Nanomedicine, including e.g. the specific targeting of cells with drug-loaded particles, fundamentally depends on a profound initial characterization of the interaction process with the external surroundings. Full article
201 KiB  
Abstract
Identification of Privileged Atom-Types in Substrates of the ABC-Transporter ABCB1 (P-gp) by Random Forest Classification
by M. A. DEMEL, O. KRÄMER, P. ETTMAYER, E. E. J. HAAKSMA and G. F. ECKER
Sci. Pharm. 2009, 77(6), 187; https://doi.org/10.3797/scipharm.oephg.21.SL-20 - 16 Apr 2009
Viewed by 751
Abstract
The ABC-transporter ABCB1 (P-glycoprotein) is a drug efflux pump playing an important role in the transport route of drugs through tissue barriers, protection against xenobiotics, and in cancer drug resistance. Due to this, ABCB1 is notorious for limiting bioavailability of various chemical and [...] Read more.
The ABC-transporter ABCB1 (P-glycoprotein) is a drug efflux pump playing an important role in the transport route of drugs through tissue barriers, protection against xenobiotics, and in cancer drug resistance. Due to this, ABCB1 is notorious for limiting bioavailability of various chemical and functional unrelated drugs. Full article
211 KiB  
Abstract
Evaluation of a Blood-Brain Barrier in vitro Model Based on Primary Rat Cells
by W. NEUHAUS, E. SUBILEAU, C. CHESNE, D. GRUBER, S. TÖGEL, W. KLEPAL and C. R. NOE
Sci. Pharm. 2009, 77(6), 186; https://doi.org/10.3797/scipharm.oephg.21.SL-19 - 16 Apr 2009
Viewed by 707
Abstract
The blood-brain barrier (BBB) maintains the homeostasis between the central nervous system and the blood circulation [1]. Until now, no standard in vitro model of the BBB is available. In this contribution a novel BBB in vitro model based on primary rat brain [...] Read more.
The blood-brain barrier (BBB) maintains the homeostasis between the central nervous system and the blood circulation [1]. Until now, no standard in vitro model of the BBB is available. In this contribution a novel BBB in vitro model based on primary rat brain microvasculature endothelial cells (RBMEC) and primary rat glial cells (RGC) is introduced. The cells were isolated from Wistar rats and were provided by the company Biopredic Int. RBMEC were co-cultured with RGC in a 12-well Transwell system. The development of the barrier was monitored by the measurement of the transendothelial electrical resistance (TEER).[...] Full article
197 KiB  
Abstract
Behavioral and Endocrine Effects of Essential Oils in Humans
by I. STAPPEN, M. HÖFERL and E. HEUBERGER
Sci. Pharm. 2009, 77(6), 185; https://doi.org/10.3797/scipharm.oephg.21.SL-18 - 16 Apr 2009
Viewed by 770
Abstract
The influence of New Caledonian sandalwood oil on the autonomic nervous system and on the salvia cortisol level, on subjective evaluations on the Profile of Mood States (POMS), and the resulting perception of facial attractiveness were measured on 50 subjects (25 males and [...] Read more.
The influence of New Caledonian sandalwood oil on the autonomic nervous system and on the salvia cortisol level, on subjective evaluations on the Profile of Mood States (POMS), and the resulting perception of facial attractiveness were measured on 50 subjects (25 males and 25 females) in a within subjects experiment. The study focused on the possible aphrodisiac effect of sandalwood oil and its potentially identifiable effect between the sexes. Each participant was tested in three sessions where either sandalwood oil or geranium oil was vaporised or no odor was present. The order of introducing the oils or clean air was arbitrary, and unlike other studies [1, 2] the subjects did not know that odors were present in the room. At the beginning and at the end of each session, blood pressure was measured, and the participants had to fill in a questionnaire concerning their subjective emotional status. In addition, saliva samples were collected in order to determine saliva cortisol. During the sessions various physiological parameters were recorded, and the subjects judged the attractiveness of a series of male and female faces presented briefly on a computer monitor using a 5-point visual rating scale. At the end of the last session participants were debriefed and rated the oils on their familiarity and pleasantness. The results indicated no significant influence of New Caledonian sandalwood oil on the parameters of the autonomic nervous system or on the mood status, and no endocrine effects were found. For both sexes the perceived attractiveness was significantly higher under the influence of sandalwood oil in comparison with geranium oil or clean air. The evaluation of the oils’ familiarity showed a significant difference between the sexes: sandalwood oil is less and geranium oil is more recognizable for men than for women. Full article
210 KiB  
Abstract
Inside the Brain: Fragrance Effects on Human Attention
by S. M. FRIEDL, E. LAISTLER, E. MOSER and E. HEUBERGER
Sci. Pharm. 2009, 77(6), 184; https://doi.org/10.3797/scipharm.oephg.21.SL-17 - 16 Apr 2009
Viewed by 805
Abstract
Understanding the nature of attention seemed intractable until recent develop-ments in neuroimaging and cognitive psychology have allowed for providing specific anatomical and cognitive details about the attention systems of the human brain. Full article
194 KiB  
Abstract
Improved “General Unknown” Drug Screening Using GCxGCqMS
by S. BÖHME and M. BÖTTCHER
Sci. Pharm. 2009, 77(6), 183; https://doi.org/10.3797/scipharm.oephg.21.SL-16 - 16 Apr 2009
Viewed by 703
Abstract
Drug screening in the clinical setting is very often started or even solely performed with a limited selection of enzyme immunoassays in urine samples. As a general rule positive results must be confirmed by more specific and sensitive methods like GC/MS or LC/MS(-MS). [...] Read more.
Drug screening in the clinical setting is very often started or even solely performed with a limited selection of enzyme immunoassays in urine samples. As a general rule positive results must be confirmed by more specific and sensitive methods like GC/MS or LC/MS(-MS). GC/MS full scan mode giving the highest level of specificity often faces the problem of co-elution which esp. at high concentrations cannot be circumvented even with modern deconvolution software in many cases. However, broad, undirected “general unknown” screening for drugs of abuse not covered by the EIA/GC/MS-SIM combinations is of increasing importance. In the present study we therefore investigated if the common drawbacks encountered in a standard GC/MS full-scan method could be improved by increased chromatographic resolution by means of comprehensive GCxqGCMS in full-scan mode [1]. To perform comprehensive GCxGC measurements a two stage loop modulator (ZOEX cooperation USA) was used. By use of a modulation frequency of 6 seconds together with the selected GC parameters results in 3 modulated peaks per compound. The results out of the comprehensive GCxGCqMS were compared with the one dimensional data set. Full article
193 KiB  
Abstract
Nucleofection® & other Technologies Enabling Advances in Pharmaceutical Research
by K. J. MOBBS and N. FAUST
Sci. Pharm. 2009, 77(6), 182; https://doi.org/10.3797/scipharm.oephg.21.SL-15 - 16 Apr 2009
Viewed by 691
Abstract
The maintenance of physiological relevance in cell models while introducing nucleic acids and other molecules is key to effective life science research and the efficient development of novel therapies. The increasing drive toward use of primary cells is triggered by the limitations of [...] Read more.
The maintenance of physiological relevance in cell models while introducing nucleic acids and other molecules is key to effective life science research and the efficient development of novel therapies. The increasing drive toward use of primary cells is triggered by the limitations of ‘easy-to-use’ cell lines, such as their predictive power regarding whole-organism physiology. The use of physiologically relevant and validated cell models together with technologies enabling the fine dissection of signal transduction and metabolic pathways is pivotal in increasing the efficiency of pharmaceutical research and development. Full article
209 KiB  
Abstract
Using Multiple Approaches in Docking Pose Evaluation – Application to the GABAA Receptor
by L. RICHTER, M. ERNST, W. SIEGHART and G. F. ECKER
Sci. Pharm. 2009, 77(6), 181; https://doi.org/10.3797/scipharm.oephg.21.SL-14 - 16 Apr 2009
Viewed by 713
Abstract
Most docking programs are able to generate conformations similar to crystallographically determined protein/ligand complex structures. However, scoring function have problems at distinguishing conformations from the set of docked poses. The task becomes even more challenging, if the precise induced fit structure is not [...] Read more.
Most docking programs are able to generate conformations similar to crystallographically determined protein/ligand complex structures. However, scoring function have problems at distinguishing conformations from the set of docked poses. The task becomes even more challenging, if the precise induced fit structure is not known. Functional data may provide indirect structural information, and biochemical structure mapping methods have been developed to provide structural information for hard to crystallize biomolecules. In this study we wish to report a novel approach utilizing a statistical evaluation of docking poses with respect to their ability to fit experimental data.The FlexE docking tool was applied to dock nine benzodiazepines into an array of homology models of the benzodiazepine binding site of the α1β2γ2GABAA-receptor. Docking into an array of models with FlexE takes into consideration both receptor uncertainty and side chain flexibility. Subsequently, we screened for ligand orientations which support the maximum common binding mode [1] hypothesis. In an initial coarse step, poses were clustered merely using a RMSD matrix of their common scaffold (csRMSD). Cluster number was set to 30, resulting in an average scaffold-RMSD of about 2Å within a cluster. Only three out of 30 clusters were able to accommodate all ligands at this coarse level. In a second more precise step, for each of the three clusters, receptor atoms forming the binding site for the common scaffold were identified. Finally the scaffold atoms and identified receptor atoms of each pose within a cluster were used to calculate a fused RMSD (fRMSD) matrix. Subsequently in each cluster the fRMSD matrix was used to form homogeneous groups that contain all ligands. These groups of poses were then evaluated in view of homogeneity, energetic scoring values and accordance with biological data. This procedure enabled us to identify one single homogenous group of docking poses which harbors 9 different benzodiazepines. Full article
195 KiB  
Abstract
Validation of Fluorimetric Assay of Histone Deacetylase for Inhibitors from Plant Origin
by S. M. KRASTEVA and L. KRENN
Sci. Pharm. 2009, 77(6), 180; https://doi.org/10.3797/scipharm.oephg.21.SL-13 - 16 Apr 2009
Viewed by 642
Abstract
Histone deacetylase inhibitors (HDACi) have received high interest as anti-cancer agents recently. HDACi may influence tumor growth by an inhibition of angiogenesis as well as by increasing tumor cell immunogenicity [1]. In many clinical trials the effect of several HDACi on different tumors [...] Read more.
Histone deacetylase inhibitors (HDACi) have received high interest as anti-cancer agents recently. HDACi may influence tumor growth by an inhibition of angiogenesis as well as by increasing tumor cell immunogenicity [1]. In many clinical trials the effect of several HDACi on different tumors are studied at the moment [2]. Full article
214 KiB  
Abstract
Pluronic® F-68 Enhances the Nanoparticle-Cell Interaction
by V. KERLETA, I. ANDRLIK, M. SCHNEIDER, T. FRANKE, M. WIRTH and F. GABOR
Sci. Pharm. 2009, 77(6), 179; https://doi.org/10.3797/scipharm.oephg.21.SL-12 - 16 Apr 2009
Cited by 5 | Viewed by 931
Abstract
Nowadays, the various surfactants find wide application in pharmaceutical industry. The nanoparticle preparation process by emulsion techniques essentially requires a surfactant, most commonly Pluronic® F-68 [1]. This non-ionic tenside influences cell physiology and was tested in clinical trial for the treatment of [...] Read more.
Nowadays, the various surfactants find wide application in pharmaceutical industry. The nanoparticle preparation process by emulsion techniques essentially requires a surfactant, most commonly Pluronic® F-68 [1]. This non-ionic tenside influences cell physiology and was tested in clinical trial for the treatment of sickle cell disease [2] and myocardial infarction [3]. Out of these reasons, even residual tenside in nanoparticle preparations might influence the cells as well as their interaction with the colloidal carriers. At this, Caco-2 single cells were incubated with fluorescent polystyrene nanoparticles, in presence of increasing amounts of Pluronic® F-68 and cell-associated nanoparticles were detected by flow cytometry. Independent from incubation temperature, the cell-associated fraction of nanoparticles concurrently increased with the tenside concentration. Ongoing from micropipette aspiration experiments this effect could be attributed to an increase of membrane stiffness of Caco-2 cells in presence of Pluronic® F-68. Furthermore, the toxicity assay revealed that viability of the cells remained unaffected at any concentration of Pluronic® F-68. Full article
329 KiB  
Abstract
An Acoustically-Driven Biochip: Particle-Cell In-teractions Under Physiological Flow Conditions
by C. FILLAFER, G. RATZINGER, J. NEUMANN, S. DISSAUER, M. WIRTH, F. GABOR and M. SCHNEIDER
Sci. Pharm. 2009, 77(6), 178; https://doi.org/10.3797/scipharm.oephg.21.SL-11 - 16 Apr 2009
Viewed by 691
Abstract
Introduction: The interaction of particulate drug carriers with cells has generally been assessed in stationary microplate assays. These setups fail to reflect the flow conditions in vivo which generate substantial hydrodynamic drag forces [1]. In order to address this shortcoming, a microfluidic biochip [...] Read more.
Introduction: The interaction of particulate drug carriers with cells has generally been assessed in stationary microplate assays. These setups fail to reflect the flow conditions in vivo which generate substantial hydrodynamic drag forces [1]. In order to address this shortcoming, a microfluidic biochip with the capability of imitating a wide range of shear rates and pulsation modes has been developed. This device, which is based on an incorporated surface acoustic wave pump, was used to study the interaction of targeted microparticles with epithelial cells under flow conditions.
Full article
221 KiB  
Abstract
Cyclodextrins as Natural Co-Stabilising Agents in Submicron Emulsions
by V. KLANG and C. VALENTA
Sci. Pharm. 2009, 77(6), 177; https://doi.org/10.3797/scipharm.oephg.21.SL-10 - 16 Apr 2009
Viewed by 639
Abstract
Purpose: Development and physicochemical characterisation of eudermic submicron emulsions (SE) based on natural surfactants (lecithin, sucrose stearate) with different cyclodextrins as co-stabilising agents. Full article
198 KiB  
Abstract
Increased Skin Permeation of Acyclovir by Incorporation into Chitosan-Tripolyphosphate Nanoparticles
by A. HASANOVIC
Sci. Pharm. 2009, 77(6), 176; https://doi.org/10.3797/scipharm.oephg.21.SL-09 - 16 Apr 2009
Viewed by 663
Abstract
Purpose: To create a skin delivery system based on chitosan-tripolyphosphate nanoparticles (cs-tpp np) for acyclovir with enhanced chemical stability and satisfying permeation through skin. Full article
192 KiB  
Abstract
UPLC Analysis of Herbal Plant Extracts
by H. U. KUFFNER
Sci. Pharm. 2009, 77(6), 175; https://doi.org/10.3797/scipharm.oephg.21.SL-08 - 16 Apr 2009
Viewed by 687
Abstract
UPLC (ultraperformance liquid chromatography) has become commercially available in 2004. Like other chromatographic techniques using sub two micron (STM) particles, UPLC is capable of accelerating existing HPLC methods by a factor of 10 to16. However, analyzing plant extracts, a gain in separation power [...] Read more.
UPLC (ultraperformance liquid chromatography) has become commercially available in 2004. Like other chromatographic techniques using sub two micron (STM) particles, UPLC is capable of accelerating existing HPLC methods by a factor of 10 to16. However, analyzing plant extracts, a gain in separation power is often of greater importance than a gain in speed. This requires the use of columns generating backpressures up to and exceeding 15000psi (1000bar). The theory of UPLC is briefly explained and the benefits of UPLC vs. HPLC are illustrated by several examples, incl. ginkgo, kava, black cohosh, milk thistle, and passion flower extracts. Full article
197 KiB  
Abstract
Speeding Up Pharmaceutical U-HPLC Method Development with an Integrated, Ultrafast Automated Method Scouting Solution
by H. HERRMANN, S. GHIRLANDA, F. STEINER and R. SWART
Sci. Pharm. 2009, 77(6), 174; https://doi.org/10.3797/scipharm.oephg.21.SL-07 - 16 Apr 2009
Viewed by 704
Abstract
HPLC method development is still considered to be one of the crucial bottlenecks that impede productivity in analytical laboratories. Due to the variety of available columns, the proper selection of the stationary phase usually represents the greatest challenge. With the progress in U-HPLC [...] Read more.
HPLC method development is still considered to be one of the crucial bottlenecks that impede productivity in analytical laboratories. Due to the variety of available columns, the proper selection of the stationary phase usually represents the greatest challenge. With the progress in U-HPLC which enables generic gradient separations within 5 minutes or less, ultrafast method development techniques become possible. While conventional LC rarely supported more than one generic gradient run per hour, U-HPLC can do a multitude of chromatographic runs in the same amount of time. This allows changing the experimental approach from thoroughly designing a small number of initial experiments towards a more comprehensive screening along any possible combination of column/eluent/temperature. Thanks to the very short run times of U-HPLC, this can be accomplished within the same time frame as the conventional approach. However this screening provides a significantly broader set of results, more information on the influence of the parameters within the design space, and thus more confidence in the robustness of the new method. Full article
198 KiB  
Abstract
LC-MS-MS Can Distinguish Between Toxic and Non-Toxic Pyrrolizidine Alkaloids in Plants
by J. N. ELOFF and M. RÖSEMANN
Sci. Pharm. 2009, 77(6), 173; https://doi.org/10.3797/scipharm.oephg.21.SL-06 - 16 Apr 2009
Viewed by 715
Abstract
Several plants including medicinal plants and weeds that contaminate food crops contain pyrrolizidine alkaloids (PA). In the case of medicinal plants not used regularly, a low level of PA can be accommodated, but because food is consumed over a long time the allowable [...] Read more.
Several plants including medicinal plants and weeds that contaminate food crops contain pyrrolizidine alkaloids (PA). In the case of medicinal plants not used regularly, a low level of PA can be accommodated, but because food is consumed over a long time the allowable levels must be much lower [1]. Maize and soybean farmers in South Africa suffer economic losses due to the presence of Crotalaria sphaerocarpa seed pods in crops by the implementation of current regulations [1]. Because many Crotalaria species contain toxic PAs, there is a limit on the quantity of seeds that are allowed in the grain. C. sphaerocarpa undoubtedly contains pyrrolizidine alkaloids but toxicity to animals could not be established in several unpublished trials. Full article
203 KiB  
Abstract
Discovery of Chemosensitizing Flavonoids from Eriobotrya japonica Using in silico and HPLC-SPE-NMR Techniques
by P. H. PFISTERER, P. SCHNEIDER, A. RUDY, J. M. ROLLINGER, A. M. VOLLMAR and H. STUPPNER
Sci. Pharm. 2009, 77(6), 172; https://doi.org/10.3797/scipharm.oephg.21.SL-05 - 16 Apr 2009
Viewed by 736
Abstract
Mimetics of the second mitochondria-derived activator of caspases (Smac) increase the sensitivity of tumor cells towards chemotherapeutics in cancer therapy [1]. Our aim was the discovery of naturally derived small molecule Smac-mimetics from the medicinal plant Eriobotrya japonica Lindl. (Rosaceae), which is known [...] Read more.
Mimetics of the second mitochondria-derived activator of caspases (Smac) increase the sensitivity of tumor cells towards chemotherapeutics in cancer therapy [1]. Our aim was the discovery of naturally derived small molecule Smac-mimetics from the medicinal plant Eriobotrya japonica Lindl. (Rosaceae), which is known to contain cytotoxic constituents [2]. Using a previously generated and validated pharmacophore model [3] 122 3D-molecules (ERIO-database) of known constituents from the leaves of E. japonica were subjected to virtual screening. We focused on acylated flavonol monorhamnosides (AFMR) as promising phytochemical class due to the statistical evaluation of the virtual hits. AFMR were identified in the methanol extract by LC-MS and enriched by different chromatographic methods. In the Nicoletti test [4], the combination of the AFMR-mixture with sub-optimal concentrations of the chemotherapeutic etoposide strongly induced cell death in S-Jurkat and XIAP overexpressing Jurkat cells. Since the AFMR-mixture was not separable by conventional methods, we used an HPLC-SPE-NMR approach for the structural identification of single compounds. The combination of the in silico and HPLC-SPE-NMR techniques enabled the insight into ligand-target interactions of single compounds from a complex mixture. Full article
198 KiB  
Abstract
Targeted Delivery of siRNA to Tumor Cells with Designed Ankyrin Repeat Protein Nanocomplexes
by J. WINKLER and U. ZANGEMEISTER-WITTKE
Sci. Pharm. 2009, 77(6), 171; https://doi.org/10.3797/scipharm.oephg.21.SL-04 - 16 Apr 2009
Viewed by 682
Abstract
Specific delivery to tumors and efficient cellular uptake of nucleic acids are major challenges for gene-targeted cancer therapies. Tumor-targeted delivery using antibody fragments or immunoliposomes have already been demonstrated to enhance cellular uptake of nucleic acids by receptor-mediated endocytosis. Here we report the [...] Read more.
Specific delivery to tumors and efficient cellular uptake of nucleic acids are major challenges for gene-targeted cancer therapies. Tumor-targeted delivery using antibody fragments or immunoliposomes have already been demonstrated to enhance cellular uptake of nucleic acids by receptor-mediated endocytosis. Here we report the first use of an epithelial cell adhesion molecule (EpCAM)-specific designed ankyrin repeat protein (DARPin) as a carrier for siRNA. Designed ankyrin repeat proteins are a novel class of non-immunoglobulin binding proteins relying on the modularity of ankyrins. Their short length, high stability, and the lack of intramolecular cysteines facilitate proper folding, result in high-yield expression in E. coli, and allow engineering procedures usually not well tolerated by antibodies. A DARPin binding to EpCAM was derived from a designed protein library using ribosome display. Full article
195 KiB  
Abstract
How to Deal with Ion Suppression – the Foe of HPLC-MS/MS
by C. SEGER and A. GRIESMACHER
Sci. Pharm. 2009, 77(6), 170; https://doi.org/10.3797/scipharm.oephg.21.SL-03 - 16 Apr 2009
Viewed by 642
Abstract
It is well accepted, that a HPLC-MS/MS assay can outperform immunoassays in therapeutic drug monitoring (TDM) due to its increased accuracy, sensitivity, and precision. However, the occurrence of sudden and unpredictable ion yield attenuation, can hamper assay performance. Such “ion suppression effects” are [...] Read more.
It is well accepted, that a HPLC-MS/MS assay can outperform immunoassays in therapeutic drug monitoring (TDM) due to its increased accuracy, sensitivity, and precision. However, the occurrence of sudden and unpredictable ion yield attenuation, can hamper assay performance. Such “ion suppression effects” are considered a central analytical problem if using an MS/MS detector in bio-analysis. Since pathological patient specimen compositions or individual co-medications may be major causes for ion yield fluctuations, measures have to be taken to evaluate these interferences prior to transferring an HPLC-MS/MS assay to routine use. Full article
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