Scientia Pharmaceutica, Volume 77, Issue 7

Condor@Univie is a University of Vienna’s distributed systems web-based platform, developed to perform large-scale computations on a university-wide campus grid using the public domain middleware condor [1].

P-Glycoprotein (P-gp) is a member of the ABC (ATP binding cassette) super-family of transport proteins, which in addition to their physiological role in tissue protection, actively extrude a large variety of therapeutically administered drugs from th...

Current treatments of type 2 diabetes mellitus have sometimes severe side effects. Therefore, the identification of new treatments is still an urgent need. The binding of insulin to the extracellular part of the insulin receptor is a key step in the...

The human serotonin transporter (hSERT), embedded in the presynaptic membrane, is responsible for the reuptake of serotonin from the synaptic cleft, thus terminating neurotransmission. The structure of the SERT has not yet been resolved by experiment...

The human ATP-binding cassette transporter ABCB1 (P-glycoprotein, P-gp, MDR1), which is strongly related to multidrug resistance, is known for its high polyspecificity, thus binding a large number of structurally diverse molecules. The molecular basi...

The serotonin transporter (SERT) is a presynaptic membrane protein that terminates neuronal transmission of serotonin (5HT) by transporting its substrate into the emitting neuron. Recently new crystal structures of the Leucine Transporter (LeuT) with...

The hERG potassium channel is highly related to severe cardiac side effects. With the technique of homology modelling it is possible to model the homo tetrameric subunits of the hERG channel in the closed and open state, using KcsA and KirBac1.1 as w...

As part of the ATP-binding cassette transporter superfamily ABCB1 (P-gp) exports a multitude of xenobiotics and is strongly connected to multi-drug resistance (MDR). With the decreasing number of new drugs entering the market prediction of possible s...

The radical Kolbe electrolysis can be applied to synthesize non-proteinogenic amino acids starting from ʟ-glutamic acid (or L-aspartic acid, respectively). Using suitable protecting groups for both amino and carboxy functionalities, the retention of...

By using Kolbe electrolysis [1], an anodic oxidation, carboxylic acids are able to form dimers through precent decarboxylation and generation of radicals. The scope of the Kolbe reaction can be considerably enhanced by cross-reaction of two different...

Various staining methods for protein staining acrylamide gels exist. But as they all differ in their mechanism of action, sensitivity, linear range and the software tool required for analysis, not all of them can be used for the same issue of researc...

Resveratrol (3,3,4’-trans-trihydroxystilbene) is a polyphenolic phytoalexin that is produced by several plants as response to stress attack like UV exposure or fungus and bacteria infections [1]. It shows a variety of biological activities such as pr...

Malaria is one of the most dangerous diseases killing more than 880 000 people all over the world in 2006 [1]. Today the most effective drug against malaria is artemisinin which is seen as the last defence against this disease, because resistance to...

The bicyclic bases 4-(dimethylamino)-6,7-diphenylbicyclo[2.2.2]octan-2-ol 1e and N,N-dimethyl-7,8-diphenyl-2-azabicyclo[3.2.2]nonan-5-amine 2e exhibit distinct activity against Plasmodium falciparum and Trypanosoma b. rhodesiense [1, 2].[...]

Every year about half a million people are infected with Human African Trypanosomiasis (HAT) and more than 40.000 people die from this disease [1]. Infections with Trypanosoma brucei rhodesiense, which is the more virulent of the two causative organi...

The effects on ileal contraction of some synthetic derivatives of the bioactive [1–3] 3,4-secoisopimara-4(18),7,15-trien-3-oic acid (1) isolated from S. cinnabarina are reported.

Microbial diseases still pose a threat for the population as a consequence of increasing number of microbial strains resistant to antibiotics and chemo-therapeutics of common use. Their treatment remains an important and challenging worldwide problem...

Antisense and siRNA oligonucleotides have been widely used in the past decade as an efficient gene-silencing tool in molecular biological investigations. However, their therapeutic application has hitherto been hampered by their poor pharmacokinetic...

A diversity of disease processes and conditions such as Alzheimer´s disease, schizophrenia, epilepsy and stroke – although they are caused by different mechanism – share one common target: the NMDA-receptor [1]. Recent studies reported the presence a...

The blood-brain barrier (BBB) maintains the homeostasis between the central nervous system and the blood circulation [1]. One of the main efflux transporter proteins at the BBB is P-glycoprotein (P-gP) also known as ABCB1 or MDR1. Recently, transport...

The migration of substances between blood circulation and central nervous system (CNS) is regulated by the blood-brain barrier (BBB). Small lipophilic molecules such as carbon dioxide, oxygen or ethanol can pass the BBB by passive, transcellular diff...

The aim of this study was to synthesize three different dithiodibenzamides and to compare their effects on isolated heart and smooth muscle preparations [1]. The three compounds only differed in the substitution on the phenylendiamine moiety.[...]

In search of new antimycotic agents acting as ergosterol biosynthesis inhibitors we investigated widely new and optimized reaction pathways for preparing different types of triazasteroids [1, 2]. The various mono-, bi-, tri- and tetracyclic triazaste...

In many malaria stricken areas affordable medicines, such as chloroquine or mefloquine, which have been used for many years, are no longer effective, because the parasites have become resistant [1].

The genus Magnolia plays a role in American as well as in Asian medicinal systems such as TCM or Japanese Kampo medicine [1, 2]. Main lignan constituents in the seeds of the north american Magnolia grandiflora are honokiol (1) and 4'-O-methyl-honokio...

Honokiol, a neolignan compound isolated from Magnolia species has been suggested to interact with GABA_A receptors. Evidence comes from honokiol-induced enhanced [³H]muscimol binding [1] and anxiolytic action in behavioural studies [2]. The molecular...

Inhibition of hERG channels prolongs the ventricular action potential and correspondingly the QT-interval with the risk of torsade de pointes arrhythmias which may result in sudden cardiac death.[...]

Introduction: When collecting saliva for routine diagnostic purposes a number of basic problems should be prevented: analytes should not be unspecifically absorbed in or on the collection device, analyte stability should be assured and the sample vol...

The reversal (synthetic mode) of the maltose cleavage reaction catalyzed by maltose phosphorylase from Enterococcus sp. was utilized to synthesize maltose analogs such as D-glucosyl-D-xylose.

Cellobiose phosphorylase from Clostridium thermocellum was examined for its ability to catalyze the synthesis of cellobiose derivatives with glucose-1-phosphate as the donor and azido analogues of glucose as acceptors. We have prepared the 2-azido-2-...

During the recent decade, the interest on probiotic products has been growing due to the increasing evidence of health benefits associated with their use. The essential step for the development of such products is the stabilization (drying) of probio...

Recently, supplementaries containing probiotic microorganisms are getting more and more important. Due to the fact that synthetic excipients are limited in the preparation of nutritional supplements, an increasing trend for using excipients from natu...

Monosaccharide analysis of the deacetylated polysaccharide from Sterculia urens was performed by thin-layer chromatography and by High-pH-Anion Exchange (Dionex) chromatography.[...]

For over 50 years, cellulose derivatives have been used as excellent pharmaceutical excipients. Commercially, cellulose products are designated with viscosity grade, proportional to the molecular weight or chain length, which identifies the product n...

Aliphatic polyesters are biodegradable polymers most frequently used in drug delivery systems.[...]

Particles from poly(D,L-lactide-co-glycolide) (PLGA) can be covalently modified for active targeting with biorecognitive molecules. Usually, steric stabilizers are added that build an adsorptive layer on the particle surface.[...]

Microspheres loaded with carnosic acid (CA) as an active ingredient which was extracted from various species of Salvia L., were prepared by a spray drying technology. The matrix of the microspheres consisted of 85% deacetylated chitosan (average MW 5...

In recent years, intraarticular inflammation has been recognized to contribute to the symptoms and progression of osteoarthritis (OA). Inflammation in OA is associated with increased levels of catabolic enzymes and inflammatory mediators such as nitr...

Gum resin extracts of Boswellia serrata have been traditionally applied in folk medicine for the treatment of various inflammatory diseases. Analyses of these extracts identified a group of pentacyclic triterpenes, the boswellic acids (BAs), as activ...

Herbal drugs used in Traditional Chinese Medicine (TCM) for anti-inflammatory purposes have been examined regarding their impact on cyclooxygenase-2 (COX-2) in an in vitro COX-2 gene expression assay.[...]

Peroxisome proliferator-activated receptors (PPARs) are transcription factors that belong to the nuclear receptor super family and represent promising therapeutic targets for several inflammatory and metabolic disorders. Nuclear factor-κB (NF-κB) is...

The norepinephrine (= noradrenaline) transporter (NET) belongs besides serotonin and dopamine transporters to the family of monoamine transporters and mediates the re-uptake of norepinephrine released from neurons. Therefore, it is an important regul...

It was previously shown by us that resveratrol (RV) is able to inhibit the angiotensin (Ang) II-induced phosphorylation of the protein kinase Akt in vascular smooth muscle cells (VSMC).[...]

In cardiovascular diseases such as atherosclerosis or restenosis, migration of vascular smooth muscle cells (VSMC) from the media into the intima of blood vessels is an early and crucial step.[...]

During the pathology of atherosclerosis and restenosis, hyperproliferation and migration of vascular smooth muscle cells (VSMC) contribute to lumen loss of the vessel and neointima formation [1]. Drugs interfering with both, proliferation and migrati...

Tylophorine, a phenanthroindolizidine alkaloid, is the main active component of Tylophora indica (Asclepiadaceae) which is used in ayurvedic medicine to treat various alleTylophora indica (Asclepiadaceae)rgic and inflammatory disorders, including bro...

Saussurea lappa Clarke (Asteraceae) is native to China, India and Pakistan. Traditionally, decoctions of the roots have been used, amongst others, for abdominal pain, tenesmus, nausea and cancer.[...]

Antibiotic resistance has become a serious problem for human health.[...]

The purpose of this study was to examine the effectiveness of essential oils from Tanacetum vulgare L., and Salvia officinalis L. for control of growth and survival of selected microorganisms.

Antioxidant activity [1] plays an important role in some biological effects of genus Ligustrum (on the cardiovascular system [2], immunomodulant [3] activity etc.). This activity can be caused by a wide range of constituents, mostly phenolic and terp...