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Pharmaceutical Applications (pharmaceutical + application)
Selected AbstractsApplications of Raman spectroscopy to pharmacyJOURNAL OF RAMAN SPECTROSCOPY, Issue 5 2004Giancarlo Fini Abstract This paper gives a summary of this special issue on ,Pharmaceutical Applications of Raman Spectroscopy'. It summarizes the papers collected and introduces the possible applications of classical Raman spectroscopy (macro and micro) and surface-enhanced Raman spectroscopy to the identification of pharmacologically active substances, their qualitative and quantitative analysis, characterization of crystalline forms and structure determination. Copyright © 2004 John Wiley & Sons, Ltd. [source] Pharmaceutical applications of mucoadhesion for the non-oral routesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 1 2005Katarina Edsman The adhesion of pharmaceutical formulations to the mucosal tissue offers the possibility of creating an intimate and prolonged contact at the site of administration. This prolonged residence time can result in enhanced absorption and, in combination with a controlled release of the drug, also improved patient compliance by reducing the frequency of administration. During the almost 30 years over which mucoadhesion has been studied, a considerable amount of knowledge has been gained, and much has been learned about the different mechanisms occurring at the formulation-mucus interface and the properties that affect these mechanisms. The in-vivo performance of a dosage form not only depends on the mechanisms occurring at the interface, but also on the properties of the total mucoadhesive complex: the dosage form, the mucosa and the interface between them. A wide variety of methods are used for studying mucoadhesion; some rather similar to the in-vivo situation and some mimicking the interface alone. In this review, the mucus surface, the methods used for the study of mucoadhesion, the different mechanisms involved in mucoadhesion and theories underpinning them have been described. The complexity of mucoadhesion when trying to systemize the subject will also be discussed. The last part of the review describes the buccal, nasal, ocular, vaginal and rectal routes and provides examples of what can be achieved in-vivo when using mucoadhesive formulations. [source] Analytical aspects of pharmaceutical grade chondroitin sulfatesJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 12 2007Nicola Volpi Abstract Chondroitin sulfate is a very heterogeneous polysaccharide in terms of relative molecular mass, charge density, chemical properties, biological and pharmacological activities. It is actually recommended by EULAR as a symptomatic slow acting drug (SYSADOA) in Europe in the treatment of knee osteoarthritis based on meta-analysis of numerous clinical studies. Chondroitin sulfate is also utilized as a nutraceutical in dietary supplements mainly in the United States. On the other hand, chondroitin sulfate is derived from animal sources by extraction and purification processes. As a consequence, source material, manufacturing processes, the presence of contaminants, and many other factors contribute to the overall biological and pharmacological actions of these agents. The aim of this review is to evaluate new possible more specific analytical approaches to the determination of the origin and purity of chondroitin sulfate preparations for pharmaceutical application and in nutraceuticals, such as the evaluation of the molecular mass values, the constituent disaccharides, and the specific and sensitive agarose-gel electrophoresis technique. Furthermore, a critical evaluation is presented, together with a discussion of the limits of these analytical approaches. Finally, the necessity for reference standards having high specificity, purity and well-known physico-chemical properties useful for accurate and reproducible quantitative analyses will be discussed. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 96: 3168,3180, 2007 [source] The antioxidant effect of hydroxyl-substituent Schiff bases on the free-radical-induced hemolysis of human erythrocytesCELL BIOCHEMISTRY AND FUNCTION, Issue 2 2007You-Zhi Tang Abstract The major objectives of the present work were focused on assessing the antioxidant capacities of two hydroxyl-substituent Schiff bases, 2-((o -hydroxylphenylimino)methyl)phenol (OSAP) and 2-((p -hydroxylphenylimino)methyl)phenol (PSAP) either used alone or in combination with some familiar water-soluble antioxidants i.e. 6-hydroxyl-2,5,7,8-tetramethylchroman-2-carboxylic acid (Trolox) and L-ascorbic acid (VC), and lipophilic ones i.e. ,-tocopherol (TOH) and L -ascorbyl-6-laurate (VC-12). 2,2'-Azobis(2-amidinopropane hydrochloride) (AAPH). Induced hemolysis of human erythrocytes functioned as the evaluation experimental system in this research. The present findings showed that either OSAP or PSAP not only was an antioxidant with high activity in protecting erythrocytes against AAPH-induced hemolysis concentration-dependently, but can also protect erythrocytes by acting with Trolox, TOH, VC and VC-12 synergistically. Based on chemical kinetic deduction, the number of trapping peroxyl radicals, n, of the above-mentioned antioxidants can be calculated in relation to Trolox that traps two peroxyl radicals; thus, TOH can trap 3.83 peroxyl radicals, VC-12 traps 2.87 and VC can only trap 1.08. As for OSAP and PSAP, 8.71 and 13.7 peroxyl radicals can be trapped, respectively, indicating that they were the most efficient inhibitors against AAPH-induced hemolysis. Moreover, the total number of peroxyl radicals trapped by OSAP+Trolox, OSAP+TOH, OSAP+VC and PSAP+VC were higher than the sum of the above individual antioxidant used alone, demonstrating that a mutual promotive effect existed in the above mixed antioxidants. In contrast, owing to the fact that the total number of peroxyl radicals trapped by OSAP+VC-12, PSAP+Trolox, PSAP+TOH and PSAP+VC-12 were less than the sum of the above individual antioxidant used alone, a mutual antagonistic effect was suggested in these combinative usages. This information may be helpful in the pharmaceutical application of two Schiff bases. Copyright © 2005 John Wiley & Sons, Ltd. [source] Proteomics of snake venoms from Elapidae and Viperidae families by multidimensional chromatographic methodsELECTROPHORESIS, Issue 16 2003Jiraporn Nawarak Abstract Snake venoms contain a large number of biologically active substances and the venom components are very useful for pharmaceutical applications. Our goal is to separate and identify components of snake venoms in ten snake species from the Elapidae and Viperidae families using multidimensional chromatographic methods. The multidimensional chromatographic methods include reversed-phase high-performance liquid chromatography (RP-HPLC), sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), lab-on-a-chip, two-dimensional electrophoresis (2-DE), and mass spectrometry. The venoms of eight snake species demonstrated major differences in hydrophobicity, molecular weight separations, and 2-DE protein distribution patterns. The 2-DE images showed major differences between families, within each family and even between the same species. Venoms of the Elapidae family showed many basic proteins with a wide range of molecular weights, while venoms of the Viperidae family showed wide ranges of pI and molecular weights, especially for Trimeresurus sp. The multidimensional chromatographic methods revealed specific differences in venom proteins intra-species as well as between species and families. We have isolated and identified proteins that may be unique for each species for further studies in the proteome of snake venoms and their potentially use in the pharmaceutical applications. [source] Genetically engineered Pseudomonas: a factory of new bioplastics with broad applicationsENVIRONMENTAL MICROBIOLOGY, Issue 10 2001Elķas R. Olivera Summary New bioplastics containing aromatic or mixtures of aliphatic and aromatic monomers have been obtained using genetically engineered strains of Pseudomonas putida. The mutation (,) or deletion (,) of some of the genes involved in the ,-oxidation pathway (fadA,, fadB,,fadA or ,fad,BA mutants) elicits a strong intracellular accumulation of unusual homo- or co-polymers that dramatically alter the morphology of these bacteria, as more than 90% of the cytoplasm is occupied by these macromolecules. The introduction of a blockade in the ,-oxidation pathway, or in other related catabolic routes, has allowed the synthesis of polymers other than those accumulated in the wild type (with regard to both monomer size and relative percentage), the accumulation of certain intermediates that are rapidly catabolized in the wild type and the accumulation in the culture broths of end catabolites that, as in the case of phenylacetic acid, phenylbutyric acid, trans -cinnamic acid or their derivatives, have important medical or pharmaceutical applications (antitumoral, analgesic, radiopotentiators, chemopreventive or antihelmintic). Furthermore, using one of these polyesters (poly 3-hydroxy-6-phenylhexanoate), we obtained polymeric microspheres that could be used as drug vehicles. [source] Oxycellulose: Significant characteristics in relation to its pharmaceutical and medical applicationsADVANCES IN POLYMER TECHNOLOGY, Issue 3 2009Bajerovį Martina Abstract As a biomaterial, cellulose can be converted into a wide range of derivatives with desired properties for a variety of medical, biomedical, and pharmaceutical applications. The oxidation of cellulose yields oxidized cellulose (OC, oxycellulose, 6-carboxycellulose). OC represents an important class of biocompatible and bioresorbable polymers. In vivo bioabsorption of OC occurs via chemical depolymerization and enzymatic hydrolysis. Despite the fact OC is well established as a hemostatic agent and is widely used in a clinical practice, it still attracts a great interest and its new applications, especially pharmaceutical, are investigated. The present review is focused on characterization of OC's physical and chemical properties. Its synthesis and mechanisms involved in its in vivo and in vitro biodegradation are discussed. Medical and biomedical applications of OC are summarized, and especially its hemostatic, enterosorbent, and wound-healing properties are described. In addition to these applications, OC could be used as a pharmaceutical excipient in solid (e.g., tablets, microparticles), semisolid (e.g., gels), as well as liquid (e.g., suspensions) dosage forms. © 2009 Wiley Periodicals, Inc. Adv Polym Techn 28:199,208, 2009; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/adv.20161 [source] Multivariate methods in pharmaceutical applicationsJOURNAL OF CHEMOMETRICS, Issue 3 2002Jon Gabrielsson Abstract This review covers material published within the field of pharmacy in the last five years. Articles concerning experimental design, optimization and applications of multivariate techniques have been published, from factorial designs to multivariate data analysis, and the combination of the two in multivariate design. The number of publications on this topic testifies to the good results obtained in the studies. Much of the published material highlights the usefulness of experimental design, with many articles dealing with optimization, where much effort is spent on getting useful results. Examples of multivariate data analysis are comparatively few, but these methods are gaining in use. The employment of multivariate techniques in different applications has been reviewed. The examples in this review represent just a few of the possible applications with different aims within pharmaceutical applications. A number of companies are using experimental design as a standard tool in preformulation and in combination with response surface modeling. The properties of e.g. a tablet can be optimized to fulfill a well-specified aim such as a specific release profile, hardness, disintegration time etc. However, none of the companies apply multivariate methods in all steps of the drug development process. As this is still very much a growing field, it is only a question of time before experimental design, optimization and multivariate data analysis are implemented throughout the entire formulation process, from performulation to multivariate process control. Copyright ©,2002 John Wiley & Sons, Ltd. [source] Mimicking biological delivery through feedback-controlled drug release systems based on molecular imprintingAICHE JOURNAL, Issue 6 2009David R. Kryscio Intelligent drug delivery systems (DDS) are able to rapidly detect a biological event and respond appropriately by releasing a therapeutic agent; thus, they are advantageous over their conventional counterparts. Molecular imprinting is a promising area that generates a polymeric network which can selectively recognize a desired analyte. This field has been studied for a variety of applications over a long period of time, but only recently has it been investigated for biomedical and pharmaceutical applications. Recent work in the area of molecularly imprinted polymers in drug delivery highlights the potential of these recognitive networks as environmentally responsive DDS that can ultimately lead to feedback controlled recognitive release systems. © 2009 American Institute of Chemical Engineers AIChE J, 2009. [source] Characterization of chitin,metal silicates as binding superdisintegrantsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 12 2009Iyad Rashid Abstract When chitin is used in pharmaceutical formulations, processing of chitin with metal silicates is advantageous, from both an industrial and pharmaceutical perspective, compared to processing using silicon dioxide. Unlike the use of acidic and basic reagents for the industrial preparation of chitin,silica particles, coprecipitation of metal silicates is dependent upon a simple replacement reaction between sodium silicate and metal chlorides. When coprecipitated onto chitin particles, aluminum, magnesium, or calcium silicates result in nonhygroscopic, highly compactable/disintegrable compacts. Disintegration and hardness parameters for coprocessed chitin compacts were investigated and found to be independent of the particle size. Capillary action appears to be the major contributor to both water uptake and the driving force for disintegration of compacts. The good compaction and compression properties shown by the chitin,metal silicates were found to be strongly dependent upon the type of metal silicate coprecipitated onto chitin. In addition, the inherent binding and disintegration abilities of chitin,metal silicates are useful in pharmaceutical applications when poorly compressible and/or highly nonpolar drugs need to be formulated. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:4887,4901, 2009 [source] Recent pharmaceutical applications of raman and terahertz spectroscopiesJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 11 2008Cushla M. McGoverin Abstract This review outlines recent applications of Raman and terahertz spectroscopies within the field of pharmaceutical research. Of the two approaches, Raman is better established and more accessible, and is responsible for the majority of reviewed studies. Both techniques feature limitations, however, which are discussed in the context of methods used to circumvent apparent restrictions. Regardless, the diverse range of applications illustrates the flexibility of Raman and terahertz spectroscopies when characterizing pharmaceutical systems. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:4598,4621, 2008 [source] Using a modified shepards method for optimization of a nanoparticulate cyclosporine a formulation prepared by a static mixer techniqueJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 2 2008Dionysios Douroumis Abstract An innovative methodology has been used for the formulation development of Cyclosporine A (CyA) nanoparticles. In the present study the static mixer technique, which is a novel method for producing nanoparticles, was employed. The formulation optimum was calculated by the modified Shepard's method (MSM), an advanced data analysis technique not adopted so far in pharmaceutical applications. Controlled precipitation was achieved injecting the organic CyA solution rapidly into an aqueous protective solution by means of a static mixer. Furthermore the computer based MSM was implemented for data analysis, visualization, and application development. For the optimization studies, the gelatin/lipoid S75 amounts and the organic/aqueous phase were selected as independent variables while the obtained particle size as a dependent variable. The optimum predicted formulation was characterized by cryo-TEM microscopy, particle size measurements, stability, and in vitro release. The produced nanoparticles contain drug in amorphous state and decreased amounts of stabilizing agents. The dissolution rate of the lyophilized powder was significantly enhanced in the first 2 h. MSM was proved capable to interpret in detail and to predict with high accuracy the optimum formulation. The mixer technique was proved capable to develop CyA nanoparticulate formulations. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:919,930, 2008 [source] Identification and characterization of pharmaceuticals using Raman and surface-enhanced Raman scatteringJOURNAL OF RAMAN SPECTROSCOPY, Issue 5 2004Pīnzaru, S. Cīnt Abstract Many recent papers reflect ongoing research and development concerning pharmaceutical applications of Raman techniques. This short review highlights different Raman techniques (dispersive, Fourier transform, resonance Raman, SERS, SERRS, FT-SERS) employed in pharmaceutical investigations. Several Raman applications such as fundamental structural investigations, quantitative analysis, drug,excipient interaction, formulation, limit of detection, pH-dependent pharmaceutical species, adsorption geometry at a given surface and functional groups involved in adsorption for several widely used pharmaceutical compounds are presented. Copyright © 2004 John Wiley & Sons, Ltd. [source] Determination of adsorption isotherms by means of HPLC: Adsorption mechanism elucidation and separation optimizationJOURNAL OF SEPARATION SCIENCE, JSS, Issue 5-6 2009Nicola Marchetti Abstract The purpose of this review is to illustrate the most important techniques for isotherm determination by means of HPLC. Starting on the traditional Frontal Analysis approach, Frontal Analysis by Characteristic Point, Elution by Characteristic Point, Perturbation Method in its different applications will be considered to conclude with the most recent Inverse Method approach. Since many of these techniques are based on the fundamentals of nonlinear chromatography, a short overview of the theory of nonlinear chromatography is presented. Emphasis is given to the most recent applications of these techniques for pharmaceutical applications, characterization of binding mechanisms, bioaffinity studies, molecular and chiral recognition processes. [source] Capillary electrochromatographic chiral separations with potential for pharmaceutical analysisJOURNAL OF SEPARATION SCIENCE, JSS, Issue 8 2005Debby Mangelings Abstract The use of capillary electrochromatography as a chiral separation technique for pharmaceutical applications is reviewed. Publications of the past 10 years that provide a potential practical application in pharmaceutical analysis are considered. Method development or validation, separation strategies, and potential routine analysis by the methods/applications cited are the main subjects on which we focused our attention. The indirect chiral separation method was only used once in CEC mode. In the direct chiral separations, the use of chiral stationary phases was obviously preferred over the use of chiral mobile phases with non-chiral stationary phases. Amongst the chiral stationary phases, those based on macrocyclic antibiotics and polysaccharide selectors were the most frequently used. Monolithic stationary phases also have several applications, but not so extended as those with packed capillary electrochromatography. The considered papers not only describe the applicability of the technique for relatively large sets of chiral analytes, they also showed that various types of stationary phases can be produced in-house in a simple manner. However, to survive as a mature separation technique, considerable time and effort are still needed to solve some disadvantages currently characterizing capillary electrochromatography. [source] Preparation of microparticulate ,-glucan from Saccharomyces cerevisiae for use in immune potentiationLETTERS IN APPLIED MICROBIOLOGY, Issue 4 2002K.W. Hunter Jr Aims: To develop a method for the preparation of an immunologically active, homogeneous, nonaggregated, microparticulate ,-glucan-containing material from the budding yeast Saccharomyces cerevisiae. Methods and Results: Using a combination of sonication and spray-drying, a homogeneous preparation of 1,2-µ diameter ,-glucan-containing particles was made from alkali- and acid-insoluble yeast cell wall material. This microparticulate ,-glucan remained in suspension longer and, following oral administration at 0·1 mg kg,1 for 14 d, enhanced phagocytosis of mouse peritoneal macrophages significantly better than did aggregated ,-glucan particles. Conclusions: A new sonication and spray-drying method can be employed to overcome the problem of aggregation of ,-glucan microparticles in aqueous media. Significance and Impact of the Study: A microparticulate form of ,-glucan that remains in suspension longer for pharmaceutical applications and has superior immune potentiation characteristics has been developed. [source] Pharmacology and structure-activity relationships of bioactive polycyclic cage compounds: A focus on pentacycloundecane derivativesMEDICINAL RESEARCH REVIEWS, Issue 1 2005Werner J. Geldenhuys Abstract The chemistry of organic polycyclic cage compounds has intrigued medicinal chemists for over 50 years, yet little is published about their pharmacological profiles. Polycyclic cage compounds have important pharmaceutical applications, ranging from the symptomatic and proposed curative treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's disease (e.g., amantadine and memantine), to use as anti-viral agents against influenza and the immunodeficiency virus (HIV). The polycyclic cage appears to be a useful scaffold to yield drugs with a wide scope of applications, and can be used also to modify and improve the pharmacokinetic and pharmacodynamic properties of drugs in current use. This review attempts to summarize the pharmacological profiles of polycyclic cage compounds with an emphasis on the lesser known pentacycloundecanes, homocubanes, and trishomocubanes. © 2004 Wiley Periodicals, Inc. [source] Liposome/water lipophilicity: Methods, information content, and pharmaceutical applicationsMEDICINAL RESEARCH REVIEWS, Issue 3 2004Georgette Plemper van Balen Abstract This review discusses liposome/water lipophilicity in terms of the structure of liposomes, experimental methods, and information content. In a first part, the structural properties of the hydrophobic core and polar surface of liposomes are examined in the light of potential interactions with solute molecules. Particular emphasis is placed on the physicochemical properties of polar headgroups of lipids in liposomes. A second part is dedicated to three useful methods to study liposome/water partitioning, namely potentiometry, equilibrium dialysis, and 1H-NMR relaxation rates. In each case, the principle and limitations of the method are discussed. The next part presents the structural information encoded in liposome/water lipophilicity, in other words the solutes' structural and physicochemical properties that determine their behavior and hence their partitioning in such systems. This presentation is based on a comparison between isotropic (i.e., solvent/water) and anisotropic (e.g., liposome/water) systems. An important factor to be considered is whether the anisotropic lipid phase is ionized or not. Three examples taken from the authors' laboratories are discussed to illustrate the factors or combinations thereof that govern liposome/water lipophilicity, namely (a) hydrophobic interactions alone, (b) hydrophobic and polar interactions, and (c) conformational effects plus hydrophobic and ionic interactions. The next part presents two studies taken from the field of QSAR to exemplify the use of liposome/water lipophilicity in structure,disposition and structure,activity relationships. In the conclusion, we summarize the interests and limitations of this technology and point to promising developments. © 2004 Wiley Periodicals, Inc. Med Res Rev, 24, No. 3, 299,324, 2004 [source] Mixture and mixture,process variable experiments for pharmaceutical applicationsPHARMACEUTICAL STATISTICS: THE JOURNAL OF APPLIED STATISTICS IN THE PHARMACEUTICAL INDUSTRY, Issue 4 2004Christine M. Anderson-Cook Abstract Many experiments in research and development in the pharmaceutical industry involve mixture components. These are experiments in which the experimental factors are the ingredients of a mixture and the response variable is a function of the relative proportion of each ingredient, not its absolute amount. Thus the mixture ingredients cannot be varied independently. A common variation of the mixture experiment occurs when there are also one or more process factors that can be varied independently of each other and of the mixture components, leading to a mixture,process variable experiment. We discuss the design and analysis of these types of experiments, using tablet formulation as an example. Our objective is to encourage greater utilization of these techniques in pharmaceutical research and development. Copyright © 2004 John Wiley & Sons Ltd. [source] Polymeric gels and hydrogels for biomedical and pharmaceutical applicationsPOLYMERS FOR ADVANCED TECHNOLOGIES, Issue 1 2010Joseph Jagur-Grodzinski Abstract Hydrogels are formed when a three-dimensional polymeric network is loosely crosslinked. They are swollen by water but not dissolved in it. Hydrogels may display reversible sol,gel transitions, induced by changes in the environmental conditions such as temperature, pH, ionic strength, phase separation, wave length of light, crystallinity, etc. Hydrogel is described as smart or intelligent when sharp transition is induced by small change in such conditions. For the shape-memory hydrogels, reversible change in shape may also be induced by such stimuli. The preparation and applications of the molecularly imprinted polymeric hydrogels (MIPs) are illustrated by a few examples. The use of shape sensitive hydrogels in microfluidic is mentioned. Application of hydrogels for chronobiology and chronotherapy is outlined. The conversion of hydrogels into aerogels and their respective properties is discussed. Copyright © 2009 John Wiley & Sons, Ltd. [source] A new generation of protein display scaffolds for molecular recognitionPROTEIN SCIENCE, Issue 1 2006Ralf J. Hosse Abstract Engineered antibodies and their fragments are invaluable tools for a vast range of biotechnological and pharmaceutical applications. However, they are facing increasing competition from a new generation of protein display scaffolds, specifically selected for binding virtually any target. Some of them have already entered clinical trials. Most of these nonimmunoglobulin proteins are involved in natural binding events and have amazingly diverse origins, frameworks, and functions, including even intrinsic enzyme activity. In many respects, they are superior over antibody-derived affinity molecules and offer an ever-extending arsenal of tools for, e.g., affinity purification, protein microarray technology, bioimaging, enzyme inhibition, and potential drug delivery. As excellent supporting frameworks for the presentation of polypeptide libraries, they can be subjected to powerful in vitro or in vivo selection and evolution strategies, enabling the isolation of high-affinity binding reagents. This article reviews the generation of these novel binding reagents, describing validated and advanced alternative scaffolds as well as the most recent nonimmunoglobulin libraries. Characteristics of these protein scaffolds in terms of structural stability, tolerance to multiple substitutions, ease of expression, and subsequent applications as specific targeting molecules are discussed. Furthermore, this review shows the close linkage between these novel protein tools and the constantly developing display, selection, and evolution strategies using phage display, ribosome display, mRNA display, cell surface display, or IVC (in vitro compartmentalization). Here, we predict the important role of these novel binding reagents as a toolkit for biotechnological and biomedical applications. [source] A Simple, Non-Nucleosidic Base Surrogate Increases the Duplex Stability of DNA Containing an Abasic SiteCHEMISTRY & BIODIVERSITY, Issue 2 2004Simon Abasic sites represent a common type of lesion in DNA. If not repaired, they can lead to mutations during replication or to cell death. Due to their biological importance, there is a strong interest in methods of recognizing abasic sites in DNA both for diagnostic and also for potential pharmaceutical applications. Extended aromatic residues can have a substantial positive influence on the stability of double-stranded DNA containing abasic sites. We report here the use of a simple, non-nucleosidic phenanthrene as a base surrogate, which effectively enhances the duplex stability of DNA with an abasic site. The influence of the linker length on the stability of the duplex is investigated. Data and model considerations indicate that stabilization is a result of stacking interactions between the phenanthrene and DNA base pairs. [source] | ||||||||||||||||