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Call For Paper
Bentham Science Publishers would like to invite you to submit your research paper for publishing in the Journal of
Current Pharmaceutical Design
Current Pharmaceutical Design
Tuesday, November 1, 2016
Highlighted Article: Antiepileptic Drugs Based on the α-Substituted Amide Group Pharmacophore: From Chemical Crystallography to Molecular Pharmaceutics
Antiepileptic Drugs Based on the α-Substituted Amide Group Pharmacophore: From Chemical Crystallography to Molecular Pharmaceutics
Author(s):
Arcadius V. Krivoshein Pages 5029 - 5040 ( 12 )
Abstract:
The antiepileptic activity of α-substituted acetamides, lactams, and cyclic imides has been known for over six decades. We recently proposed an α-substituted amide group as the minimum pharmacophore responsible for inhibition of neuronal nicotinic acetylcholine receptors by these compounds, with the implication that inhibition of these receptors in the brain might be the unifying mechanism of action for these classes of antiepileptic drugs. In order to realize the pharmacological potential of these orally administered drugs, the relevant aspects of solid-state chemistry and pharmaceutics (including solubility and stability) need to be addressed. A better - more cohesive and generalized - understanding of the solid-state properties of these drugs would pave the road for a rational approach to their development, formulation, and manufacturing. In this paper, Pharmaceutically relevant aspects of the crystal structure and solid-state chemistry of antiepileptic drugs containing the α-substituted amide bond pharmacophore - α-substituted acetamides, lactams, and cyclic imides and the structurally related barbiturates, hydantoins, and acetylureas are reviewed. The applicable experimental and computational approaches are also briefly mentioned.
Keywords:
Acetamides, lactams, cyclic imides, antiepileptic drugs, solid-state properties, crystal structure.
Affiliation:
Department of Physical & Applied Sciences, University of Houston - Clear Lake, 2700 Bay Area Boulevard, B3121-36, Houston, TX 77058-1002, USA.
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Sunday, October 23, 2016
Most Cited Article: The Role of ABC Transporters in Protecting Cells from Bilirubin Toxicity
The Role of ABC Transporters in Protecting Cells from Bilirubin
Toxicity
Author(s):
C. Bellarosa, G. Bortolussi and C.
TiribelliPages 2884-2892 (9)
Abstract:
The ATP-Binding Cassette (ABC) superfamily is the largest transporter family known to translocate a wide variety of exogenous and endogenous substrates across cell membranes. In this chapter we review the potential role of three ABC proteins in the transport of unconjugated bilirubin (UCB). These transporters are MRP1, MRP3 and PGP (MDR1). MRP1 is expressed at high levels in most epithelia, usually at the basolateral membrane. Among a multiplicity of substrates, MRP1 mediates the ATP-dependent cellular export of UCB, and its role has been demonstrated in protecting cells from UCB toxicity. MRP3 is an organic anion transporter whose major substrates are GSH conjugates of organic compounds. Among the MRP family members, MRP3 shares the highest degree of amino acid homology with MRP1. Although the hepatic expression of MRP3 has been reported to be up-regulated by bilirubin and bilirubin glucuronides, it is unknown whether MRP3 is also involved in the transport of UCB. PGP is expressed in organs involved in the elimination of endo- and xenobiotics and UCB is one of these substrates. Since the Km of PGP for UCB is well above pathophysiological levels of Bf, it remains uncertain whether it has a role in protecting against UCB cytotoxicity.
Keywords:
ATP-binding-cassette protein (ABC) protein,
multidrug-resistance-associated protein 1 (MRP1),
multidrugresistance-associated protein 3 (MRP3), P-glycoprotein (PGP),
unconiugated bilirubin, bilirubin neurocytotoxicity
Affiliation:
Centro Studi Fegato, Bldg Q -AREA Science Park
Basovizza, SS14 Km 163,5, 34012 Trieste, Italy.
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Tuesday, October 18, 2016
AFM-Based Single Molecule Techniques: Unraveling the Amyloid Pathogenic Species
AFM-Based Single Molecule Techniques: Unraveling the Amyloid Pathogenic Species
Author(s):
Francesco Simone Ruggeri, Johnny Habchi, Andrea Cerreta and Giovanni DietlerPages 3950-3970 (21)
Abstract:
Background: A wide class of human diseases and neurodegenerative disorders, such as Alzheimer’s disease, is due to the failure of a specific peptide or protein to keep its native functional conformational state and to undergo a conformational change into a misfolded state, triggering the formation of fibrillar cross-β sheet amyloid aggregates. During the fibrillization, several coexisting species are formed, giving rise to a highly heterogeneous mixture. Despite its fundamental role in biological function and malfunction, the mechanism of protein self-assembly and the fundamental origins of the connection between aggregation, cellular toxicity and the biochemistry of neurodegeneration remains challenging to elucidate in molecular detail. In particular, the nature of the specific state of proteins that is most prone to cause cytotoxicity is not established. Methods: In the present review, we present the latest advances obtained by Atomic Force Microscopy (AFM) based techniques to unravel the biophysical properties of amyloid aggregates at the nanoscale. Unraveling amyloid single species biophysical properties still represents a formidable experimental challenge, mainly because of their nanoscale dimensions and heterogeneous nature. Bulk techniques, such as circular dichroism or infrared spectroscopy, are not able to characterize the heterogeneity and inner properties of amyloid aggregates at the single species level, preventing a profound investigation of the correlation between the biophysical properties and toxicity of the individual species. Conclusion: The information delivered by AFM based techniques could be central to study the aggregation pathway of proteins and to design molecules that could interfere with amyloid aggregation delaying the onset of misfolding diseases.
Keywords:
Misfolding diseases, Alzheimer’s disease, amyloid, protein aggregation, single molecule biophysics, afm, nanomechanical properties, infrared nanospectroscopy.
Affiliation:
Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge, United Kingdom.
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Sunday, October 9, 2016
The Microbial Quality Aspects and Decontamination Approaches for the Herbal Medicinal Plants and Products: An in-Depth Review
The Microbial Quality Aspects and Decontamination Approaches for the Herbal Medicinal Plants and Products: An in-Depth Review
[ Vol. 22 , Issue. 27 ]
Author(s):
Daniela Dal Molim Ghisleni, Marina de Souza Braga, Irene Satiko Kikuchi, Mirela Braşoveanu, Monica R. Nemţanu, Kamal Dua and Terezinha de Jesus Andreoli PintoPages 4264-4287 (24)
Abstract:
Background: The present review article provides an overview of the published literature concerning microbial quality of medicinal plants and products and their decontamination methods. It is important to analyze different aspects regarding the cultivation, growing, harvesting, storage, manufacturing, and decontamination of medicinal plant products. Herbal medicinal plants bear a massive microbial load leading to contamination and mycotoxin, which needs to be considered, and properly controlled using suitable sterilization and decontamination methods. Methods: The main focus of this review is on the definition, advantages, disadvantages and applications of decontamination methods, particularly to show that one must consider the characteristics of the initial sample to be decontaminated. Results: The effects of various methods (ozone, plasma, irradiation) on medicinal herbs and products treated for microbiological decontamination are dependent on factors related to microbial load (i.e., nature and amount of initial contamination), herb/product matrix (i.e., complexity of chemical composition, physical state - solid or liquid) and treatment conditions (i.e., time, irradiation dose, absence or presence of oxygen). In addition, it is important to accept some loss of the chemical compounds, while decreasing microbial load to acceptable limits according to official herbal pharmacopoeias and literature, thus ensuring a final product with quality, safety and therapeutic efficacy. Conclusion: The conclusion, which comes from this contribution, is that herbal medicine has more contaminants than a chemically welldefined drug, thus, good manufacturing practices should be followed.
Keywords:
Herbal medicinal plants, herbal medicinal products, microbiological contamination, bio-burden, quality, decontamination, GMP.
Affiliation:
Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, São Paulo, Rua Professor Lineu Prestes 05508-000, Cidade Universitária, Brazil.
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Wednesday, October 5, 2016
New Issue ::: Current Pharmaceutical Design , 22 Issue 27
Current Pharmaceutical Design publishes timely in-depth reviews and research articles from leading pharmaceutical researchers in the field, covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area guest edited by an acknowledged authority in the field.
Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design including: medicinal chemistry, pharmacology, drug targets and disease mechanism
Articles from the journal Current Pharmaceutical Design , 22 Issue 27
- Editorial (Thematic Issue: Perspectives and Challenges in Rational Exploitation of Phytochemicals in Cure, Control and Management of Diseases)
- Phytochemicals: Potential in Management of Climacteric Neurobiology
- Phytochemicals as Inhibitors of Candida Biofilm
- Challenges in the Development of Antifungal Agents Against Candida: Scope of Phytochemical Research
- Historical Spice as a Future Drug: Therapeutic Potential of Piperlongumine
- Anticancer Potential of Ginger: Mechanistic and Pharmaceutical Aspects
- NF-κB Blockers Gifted by Mother Nature: Prospectives in Cancer Cell Chemosensitization
- Phytochemicals as Adjunctive with Conventional Anticancer Therapies
- Nanomedicine as a Strategy for Natural Compound Delivery to Prevent and Treat Cancers
- Exploring Nanotechnologies for the Effective Therapy of Malaria Using Plant-Based Medicines
- Lipid Based Nanosystems for Curcumin: Past, Present and Future
- Microemulsion and Microemulsion-Based Gels for Topical Antifungal Therapy with Phytochemicals
- The Microbial Quality Aspects and Decontamination Approaches for the Herbal Medicinal Plants and Products: An in-Depth Review
- Current Perspective in the International Trade of Medicinal Plants Material: An Update
For details on the articles, please visit this link :: http://bit.ly/2bwY2Bu
courtesy by : Bentham Insight
Current Pharmaceutical Design , 22 Issue 26
Current Pharmaceutical Design publishes timely in-depth reviews and research articles from leading pharmaceutical researchers in the field, covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area guest edited by an acknowledged authority in the field.
Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
Articles from the journal Current Pharmaceutical Design , 22 Issue 26
- Editorial (Thematic Issue: Current and Perspective Therapeutic Strategies for Alzheimer’s Disease)
- Protein Amyloidogenesis Investigated by Small Angle Scattering
- AFM-Based Single Molecule Techniques: Unraveling the Amyloid Pathogenic Species
- Heterocyclic Scaffolds for the Treatment of Alzheimer’s Disease
- Metal Ions and Metal Complexes in Alzheimer’s Disease
- Essential Oils and Pure Volatile Compounds as Potential Drugs in Alzheimer’s Disease Therapy: An Updated Review of the Literature
- Therapeutic Approaches Targeting Pathological Tau Aggregates
- Alzheimer’s Disease and Molecular Chaperones: Current Knowledge and the Future of Chaperonotherapy
- The Impact of Small Heat Shock Proteins (HspBs) in Alzheimer’s and Other Neurological Diseases
- Non-Demented Individuals with Alzheimer’s Disease Neuropathology: Resistance to Cognitive Decline May Reveal New Treatment Strategies
- The Potential Use of Piglets as Human Pediatric Surrogate for Preclinical Pharmacokinetic and Pharmacodynamic Drug Testing
- Macrocyclic Compounds: Emerging Opportunities for Current Drug Discovery
For details on the articles, please visit this link :: http://bit.ly/2bQsrvs
courtesy by : Bentham Insight
Friday, June 24, 2016
Lipid-Based Nanocarriers for RNA Delivery
Author(s):
Hui Yi Xue, Pengbo Guo, Wu-Cheng Wen and Ho Lun WongPages 3140-3147 (8)
Abstract:
RNA-interference (RNAi) agents such as small-interfering RNA (siRNA) and micro-RNA (miRNA) have strong potential as therapeutic agents for the treatment of a broad range of diseases such as malignancies, infections, autoimmune diseases and neurological diseases that are associated with undesirable gene expression. In recent years, several clinical trials of RNAi therapeutics especially siRNAs have been conducted with limited success so far. For systemic administration of these poorly permeable and easily degradable macromolecules, it is obvious that a safe and efficient delivery platform is highly desirable. Because of high biocompatibility, biodegradability and solid track record for clinical use, nanocarriers made of lipids and/or phospholipids have been commonly employed to facilitate RNA delivery. In this article, the key features of the major sub-classes of lipid-based nanocarriers, e.g. liposomes, lipid nanoparticles and lipid nanoemulsions, will be reviewed. Focus of the discussion is on the various challenges researchers face when developing lipid-based RNA nanocarriers, such as the toxicity of cationic lipids and issues related to PEGylated lipids, as well as the strategies employed in tackling these challenges. It is hoped that by understanding more about the pros and cons of these most frequently used RNA delivery systems, the pharmaceutical scientists, biomedical researchers and clinicians will be more successful in overcoming some of the obstacles that currently limit the clinical translation of RNAi therapy.
Keywords:
Drug delivery, lipid, nanocarrier, RNA interference, small-interfering RNA.
Affiliation:
School of Pharmacy, Temple University, 3307 North Broad Street, Philadelphia, Pennsylvania, US 19140.
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Recent advances in the fundamental understanding of adhesive mixtures for inhalation
Author(s):
Floris Grasmeijer, Niels Grasmeijer, Paul Hagedoorn, Henderik Willem Frijlink and Anne Haaije de BoerPages 5900-5914 (15)
Abstract:
Adhesive mixtures for inhalation are the most widely used type of formulation in dry powder inhalation products. Although they have been the subject of active research, the relationships between properties of the starting materials, the mixing and dispersion processes, and the dispersion performance of this type of formulation are generally poorly understood. Interactions between relevant variables have been mentioned as an important cause. By reviewing the effects on mixture dispersion performance of the most widely studied formulation variables we try to find out whether or not the understanding of adhesive mixtures has improved in recent years. We furthermore propose an approach that may potentially accelerate the process of understanding. General conclusions concerning the effects of the variables considered cannot be drawn, because inconsistent findings are reported throughout the literature for all of them. These inconsistencies are indeed largely the result of interactions between variables of the formulation and dispersion processes. Mechanisms for most of the observed effects and interactions have been proposed, but they often remain unproven and, therefore, speculative. We have attempted to condense the knowledge from the literature into a theoretical framework that is intended to help explain the interplay between variables. According to this framework, only few mixture properties are key to understanding the effects of and interactions between formulation variables. Therefore, we suggest that the development or optimisation of techniques to accurately characterise these mixture properties could be an effective approach to further the fundamental understanding of adhesive mixtures for inhalation and enable their rational engineering.
Keywords:
Carrier particle size distribution, carrier surface roughness, cohesion-adhesion balance, drug content, fines, interactive mixtures, ordered mixtures, powder dispersion.
Affiliation:
University of Groningen, Department of Pharmaceutical Technology and Biopharmacy, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
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Evolving Drug Delivery Strategies to Overcome the Blood Brain Barrier
Author(s):
David S. Hersh, Aniket S. Wadajkar, Nathan B. Roberts, Jimena G. Perez, Nina P. Connolly, Victor Frenkel, Jeffrey A. Winkles, Graeme F. Woodworth and Anthony J. KimPages 1177-1193 (17)
Abstract:
The blood-brain barrier (BBB) poses a unique challenge for drug delivery to the central nervous system (CNS). The BBB consists of a continuous layer of specialized endothelial cells linked together by tight junctions, pericytes, nonfenestrated basal lamina, and astrocytic foot processes. This complex barrier controls and limits the systemic delivery of therapeutics to the CNS. Several innovative strategies have been explored to enhance the transport of therapeutics across the BBB, each with individual advantages and disadvantages. Ongoing advances in delivery approaches that overcome the BBB are enabling more effective therapies for CNS diseases. In this review, we discuss: (1) the physiological properties of the BBB, (2) conventional strategies to enhance paracellular and transcellular transport through the BBB, (3) emerging concepts to overcome the BBB, and (4) alternative CNS drug delivery strategies that bypass the BBB entirely. Based on these exciting advances, we anticipate that in the near future, drug delivery research efforts will lead to more effective therapeutic interventions for diseases of the CNS.
Keywords:
Central Nervous System (CNS), Blood-Brain Barrier (BBB), nanotechnology, ultrasound, immunotherapy.
Affiliation:
Department of Neurosurgery, University of Maryland School of Medicine, 22 South Greene Street, Baltimore, MD 21201., Departments of Neurosurgery and Pharmaceutical Sciences, University of Maryland, Baltimore, 655 W. Baltimore Street, Baltimore, MD 21201.
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The Therapeutic Aspects of the Endocannabinoid System (ECS) for Cancer and their Development: From Nature to Laboratory
Author(s):
Mohammed I. Khan, Anna A. Sobocińska, Anna M. Czarnecka, Magdalena Król, Bruno Botta and Cezary SzczylikPages 1756-1766 (11)
Abstract:
The endocannabinoid system (ECS) is a group of neuromodulatory lipids and their receptors, which are widely distributed in mammalian tissues. ECS regulates various cardiovascular, nervous, and immune system functions inside cells. In recent years, there has been a growing body of evidence for the use of synthetic and natural cannabinoids as potential anticancer agents. For instance, the CB1 and CB2 receptors are assumed to play an important role inside the endocannabinoid system. These receptors are abundantly expressed in the brain and fatty tissue of the human body. Despite recent developments in molecular biology, there is still a lack of knowledge about the distribution of CB1 and CB2 receptors in the human kidney and their role in kidney cancer. To address this gap, we explore and demonstrate the role of the endocannabinoid system in renal cell carcinoma (RCC). In this brief overview, we elucidate the therapeutic aspects of the endocannabinoid system for various cancers and explain how this system can be used for treating kidney cancer. Overall, this review provides new insights into cannabinoids’ mechanisms of action in both in vivo and in vitro models, and focuses on recent discoveries in the field.
Keywords:
CB1 and CB2 receptors, Cannabinoids, Endocannabinoid system, Renal cell carcinoma.
Affiliation:
Molecular Oncology Laboratory, Department of Oncology, Military Institute of Medicine, ul. Szaserów 128, 04-141 Warsaw, Poland
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Therapeutic Targets for Management of Periodontitis and Diabetes
Author(s):
Corneliu Sima and Thomas E. Van DykePages 2216-2237 (22)
Abstract:
The increasing incidence of diabetes mellitus (DM) and chronic periodontitis (CP) worldwide imposes a rethinking of individualized therapy for patients with both conditions. Central to bidirectional links between DM and CP is deregulated systemic inflammation and dysfunctional immune responses to altered-self and non-self. Control of blood glucose levels and metabolic imbalances associated with hyperglycemia in DM, and disruption of pathogenic subgingival biofilms in CP are currently the main therapeutic approaches for these conditions. Mounting evidence suggests the need to integrate immune modulatory therapeutics in treatment regimens that address the unresolved inflammation associated with DM and CP. The current review discusses the pathogenesis of DM and CP with emphasis on deregulated inflammation, current therapeutic approaches and the novel pro-resolution lipid mediators derived from -3 polyunsaturated fatty acids.
Keywords:
Diabetes mellitus, periodontitis, inflammation, lipid mediators, pro-resolution therapeutics.
Affiliation:
Corneliu Sima, 245 First Street, Room 5145, Cambridge, MA, 02142, USA.
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