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Editorial: Colchicine: Conventional and Contemporary Indications.
PMID: 29768995 [PubMed - in process] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 18, 2018 Category: Drugs & Pharmacology Authors: Vrachatis DA, Giannopoulos G, Deftereos SG Tags: Curr Pharm Des Source Type: research

The Effects of Polymorphism on Physicochemical Properties and Pharmacodynamics of Solid Drugs.
CONCLUSION: As one of the significant factors to affect the quality and curative effect of solid drugs, polymorphism of drug substances has been investigated in the pharmaceutical field for over 50 years. Considerable studies indicate that comprehensive understanding of polymorphism is important for development, dosage form design, approval, production, quality control and curative effect of solid drugs. PMID: 29766778 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Zhou Y, Wang J, Xiao Y, Wang T, Huang X Tags: Curr Pharm Des Source Type: research

Technetium-99m-based Radiopharmaceuticals in Sentinel Lymph Node Biopsy: Gynecologic Oncology Perspective.
Abstract Technetium (99mTc)-radiolabeled colloids are popular tracers used to map lymphatic vessels and regional lymph nodes (LNs). The regional LN status is a significant determinant of cancer stage and patient prognosis, and strongly influences treatment. Regional LN dissection has become part of surgical treatment. However, not all patients with LN involvement benefit from extensive lymphadenectomy in terms of prolonged survival. Moreover, overtreatment of patients with localized disease carries unnecessary risk of complications. It is believed that sentinel LN biopsy (SLNB) allows to assess the involvement of ...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Zalewski K, Benke M, Mirocha B, Radziszewski J, Chechlinska M, Kowalewska M Tags: Curr Pharm Des Source Type: research

Soft Biomaterial-based nanocrystal in pharmaceutical.
CONCLUSION: The review enables an insightful discussion about the properties and the applications of existing bio-soft material. It may contribute to the further researches about bio-soft material development and analysis. PMID: 29766780 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Chen N, Su T, Cheng Z, An F Tags: Curr Pharm Des Source Type: research

Similar and distinct mechanisms in the protective processes of upper and lower gastrointestinal tract.
ár B, Zádori ZS Abstract Gastrointestinal (GI) mucosal integrity is based on the balance of aggressive and protective mechanisms. Mucosal damage may occur when the injurious factors become dominant or the mucosal defensive processes are impaired. The main target of the therapy against GI mucosal injury is the reduction of aggressive factors, however, the therapeutic possibilities for stimulation of mucosal defensive process are rather limited. This overview focuses on the gastric and intestinal mucosal protective mechanisms and discusses the main targets that increase protective process and increase ...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Gyires K, László SB, Lázár B, Zádori ZS Tags: Curr Pharm Des Source Type: research

Role of oxidative stress in diabetic retinopathy and the beneficial effects of flavonoids.
Abstract Diabetic retinopathy (DR) is one of the leading causes of decreased vision and blindness in developed countries. Diabetes-induced metabolic disorder is believed to increase oxidative stress in the retina. This results in deleterious changes through dysregulation of cellular physiology that damages both neuronal and vascular cells. Here in this review, we first highlight the evidence of potential metabolic sources and pathways which increase oxidative stress that contributes to retinal pathology in diabetes. As oxidative stress is a central factor in the pathophysiology of DR, antioxidants therapy would be...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Ola MS, Al-Dosari D, Alhomida AS Tags: Curr Pharm Des Source Type: research

Role Of Formyl Peptide Receptors In Gastrointestinal Healing.
Abstract The wound healing and the barrier restoration of the gastrointestinal (GI) mucosa must be continuously ensured to allow homeostasis of the gastrointestinal tract and of all the surrounding tissues. Several lines of the evidence report a key role of innate immunity, and in particular of Pattern Recognition Receptors (PRRs), in controlling the homeostasis of GI tract by sensing commensal and pathogen bacteria, activating the immune response and regulating epithelial repair, thus guaranteeing the morphological and functional recovery of the injured tissue. We will discuss the role of a particular class of PR...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Prevete N, Paulis A, Sgambato D, Melillo RM, D'Argenio G, Romano L, Zagari RM, Romano M Tags: Curr Pharm Des Source Type: research

Polyphenols, their metabolites and derivatives as drug leads.
Abstract In this non-comprehensive review, the potential of natural polyphenols as lead compounds for the design and synthesis of new molecules with potential application in several diseases was highlighted. Organic synthesis has been essential for the development of new analogues of naturally found polyphenols, providing a wide range of structural modifications for structure-activity relationship studies and improving or modulating the biological activity of the promising compounds. PMID: 29766784 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Almeida FA, Dos Santos CN, Ventura MR Tags: Curr Pharm Des Source Type: research

Pharmaceutical Strategies for Stabilizing Drug Nanocrystals.
CONCLUSION: Studies on stabilizers used in the production of drug nanocrystals are ongoing; various factors, such as the effect of zeta potential on the stability of drug nanosuspensions, have already been revealed. However, it is necessary to determine the most appropriate stabilizer experimentally based on the various mechanisms and factors have been reviewed since the possible interactions between each drug and stabilizer are diverse. PMID: 29766785 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Yang H, Kim H, Jung S, Seo H, Nida SK, Yoo SY, Lee J Tags: Curr Pharm Des Source Type: research

Nanocrystals: The preparation, precise control, and application toward the pharmaceutics and foods industry.
Abstract Crystallization is a significant process employed to produce a wide variety of materials in pharmaceutical and food area. The control of crystal dimension, crystallinity, and shape is very important because they will affect the subsequent filtration, drying and grinding performance as well as the physical and chemical properties of the material. This review summarizes the special features of crystallization technology and the preparation methods of nanocrystals, and discusses analytical technology which is used to control crystal quality and performance. The crystallization technology applications in phar...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Wu C, Chen Z, Hu Y, Rao Z, Wu W, Yang Z Tags: Curr Pharm Des Source Type: research

Nanocrystal technology as a strategy to improve drug bioavailability and antitumor efficacy for the cancer treatment.
CONCLUSION: This review is likely to enable a detailed insight on nanocrystal technology as a strategy to improve drug bioavailability and antitumor efficacy for the cancer treatment and be of particular interest to pharmaceutical industry. PMID: 29766787 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Fan M, Geng S, Liu Y, Wang J, Wang Y, Zhong J, Yan Z, Yu L Tags: Curr Pharm Des Source Type: research

Microbial genetic screens for monitoring protein misfolding associated with neurodegeneration: tools for identifying disease-relevant genes and for screening synthetic and natural compound libraries for the discovery of potential therapeutics.
Abstract Neurodegenerative diseases (ND) are a major threat to the aging population and the lack of a single preventive or disease-modifying agent only serves to increase their impact. In the past few years, protein misfolding and the subsequent formation of neurotoxic oligomeric/aggregated protein species have emerged as a unifying theme underlying the pathology of these complex diseases. Recently developed microbial genetic screens and selection systems for monitoring ND-associated protein misfolding have allowed the establishment of high-throughput assays for the identification of cellular factors and processes...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Kostelidou K, Matis I, Skretas G Tags: Curr Pharm Des Source Type: research

Metabolomics: a high-throughput screen for biochemical and bioactivity diversity in plants and crops.
Abstract Plants and crops contain a staggering diversity of compounds, many of which have pharmacological activity towards a variety of diseases. These properties have been exploited by traditional and modern medicine providing important sources of healthcare to this day. The contribution of natural products (such as plant-derived) to the modern pharmacopeia is indeed significant; however, the process of identifying novel bioactive compounds from biological sources has been a central challenge in the discovery of natural products. The resolution of these challenges relied extensively on the use of hyphenated mass ...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Foito A, Stewart D Tags: Curr Pharm Des Source Type: research

MALT Lymphoma, Stress Ulcer and Cholinergic Nerves from the Viewpoint of Bilateral and Unilateral Truncal Vagotomy and Substance P.
In conclusion, vagotomy enhanced gastric MALT lymphoma development possibly through the substance P-neurokinin-1 receptor pathway. PMID: 29766790 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Kodama Y, Sasaki K, Murasato F, Øverby A, Takahashi S, Murayama SY, Matsui H, Nakamura M Tags: Curr Pharm Des Source Type: research

GABAA receptors: Various stoichiometrics of subunit arrangement in α1β3 and α1β3ε receptors.
GABAA receptors: Various stoichiometrics of subunit arrangement in α1β3 and α1β3ε receptors. Curr Pharm Des. 2018 May 15;: Authors: Has ATC, Chebib M Abstract GABAA receptors (GABAARs) are members of the Cys-loop ligand-gated ion channel (LGIC) superfamily, which includes nicotinic acetylcholine, glycine, and serotonin (5HT3) receptors [1,2,3,4]. LGICs typically mediate fast synaptic transmission via the movement of ions through channels gated by neurotransmitters, such as acetylcholine for nicotinic receptors and GABA for GABAARs [5]. The term Cys-loop receptors originat...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Has ATC, Chebib M Tags: Curr Pharm Des Source Type: research

Engineering of Microbial Cell Factories for the Production of Plant Polyphenols with Health-Beneficial Properties.
Abstract Polyphenols form a group of important natural bioactive compounds with numerous ascribed health-beneficial attributes (e.g. antioxidant, anti-inflammatory, anti-microbial and tumor-suppressing properties). Some polyphenols can also be used as natural dyes or plastic precursors. Notwithstanding their relevance, production of most of these compounds still relies on extraction from plant material, which for most of it is a costly and an inefficient procedure. The use of microbial cell factories for this purpose is an emerging alternative that could allow a more efficient and sustainable production. The most ...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Dudnik A, Gaspar P, Neves AR, Forster J Tags: Curr Pharm Des Source Type: research

Chitosan-coated C-phycocyanin liposome for extending the neuroprotective time window against ischemic brain stroke.
This study sought to verify if muco-adhesive chitosan coating improves the neuroprotective potential of the pre-proven C-Phycocyanin-pertaining liposome (C-Pc liposome). The use of chitosan-coated liposomes extended the neuroprotective time window by 6 h after reperfusion, and further improved the neuroprotection efficiency of the C-Pc liposome in a rat middle cerebral artery occlusion (MCAO) model. Beneficial changes in mRNA expressions of antioxidants, inflammatory cytokines and glia scar proteoglycans were evident in the C-Pc liposomes. In addition, in the cultured astrocytes, the chitosan-coated C-Pc liposome expressed...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Chung GY, Shim KH, Kim HJ, Min SK, Shin HS Tags: Curr Pharm Des Source Type: research

Carboxymethyl-hexanoyl Chitosan Nanodroplets for Ultrasonic Imaging and Drug Delivery to Tumor.
CONCLUSIONS: CHC-PFP-DOX holds great promise in simultaneous cancer-targeting US imaging and ultrasound-mediated delivery for cancer theranostics. PMID: 29766795 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Jinsui Y, Bing S, Muhua L, Yue L, Jianyi L, Meng D, Kuan C, Chaopin Y, Hui Z, Zhiyi C Tags: Curr Pharm Des Source Type: research

Anti-aging and anti-aggregation properties of polyphenolic compounds in C. elegans.
Abstract Polyphenols constitute a group of compounds that have been highly investigated for their beneficial effects against various pathologic and non-pathologic conditions and diseases. Among their multi-faceted properties, their anti-oxidant potential nominates them as ideal protective candidates for conditions characterized by elevated levels of oxidative stress, including aging and age-related diseases. The nematode Caenorhabditis elegans is a multicellular model organism that is highly exploited in studies related to aging and age-associated diseases. In this review, we will summarize studies where polypheno...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Papaevgeniou N, Chondrogianni N Tags: Curr Pharm Des Source Type: research

Defense mechanisms against acid exposure by dental enamel formation, saliva and pancreatic juice production.
Abstract The pancreas, the salivary glands and the dental enamel producing ameloblasts have marked developmental, structural and functional similarities. One of the most striking similarities is their bicarbonate-rich secretory product serving acid neutralization. An important difference between them is that while pancreatic juice and saliva are delivered into a lumen where they can be collected and analyzed, ameloblasts produce locally precipitating hydroxyapatite which cannot be easily studied. Interestingly, the ion and protein secretion by the pancreas, the salivary glands, and maturation ameloblasts are all t...
Source: Current Pharmaceutical Design - May 15, 2018 Category: Drugs & Pharmacology Authors: Racz R, Nagy A, Rakonczay Z, Dunavari EK, Gerber G, Varga G Tags: Curr Pharm Des Source Type: research

Immunometabolic changes in hepatocytes arising from obesity and the practice of physical exercise.
ra FS Abstract Over the recent years, a particular interest was shown towards understanding the roles of excessive hepatic fat accumulation and the development of obesity-related diseases. While hepatic triacylglycerol accumulation seems to be a response to the systemic increase of insulin release, fatty acid metabolites contribute to the progression of non-alcoholic fatty liver disease (NAFLD) to non-alcoholic steatohepatitis (NASH). It is widely accepted that NAFLD is a polygenic and multifactorial disease under the influence of critical behavioral factors such as overeating and sedentary lifestyles. The progres...
Source: Current Pharmaceutical Design - May 14, 2018 Category: Drugs & Pharmacology Authors: Monteiro PA, Prado W, Dos Santos Tenório TR, Tomaz LM, St-Pierre DH, Lira FS Tags: Curr Pharm Des Source Type: research

Biological and in silico studies on synthetic analogues of tyrosine betaine as inhibitors of neprilysin, a drug target for the treatment of heart failure.
CONCLUSIONS: Tyrosine betaine remains as a starting point for the development of NEP inhibitors because of the low probability of BBB permeation and, consequently, of NEP inhibition at the Central Nervous System, which is associated to an increment in the Aβ levels and, accordingly, with a higher risk for the onset of Alzheimer's disease. PMID: 29766796 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 14, 2018 Category: Drugs & Pharmacology Authors: Kawano DF, de Carvalho MR, Machado MFM, Carmona AK, Braga GUL, Carvalho I Tags: Curr Pharm Des Source Type: research

Internal and External Triggering Mechanism of "Smart" Nanoparticle-Based DDSs in Targeted Tumor Therapy.
CONCLUSION: In this review article, we summarize and classify the internal and external triggering mechanism of "smart" nanoparticle-based DDSs in targeted tumor therapy, and the most recent research advances are illustrated for better understanding. PMID: 29745324 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - May 9, 2018 Category: Drugs & Pharmacology Authors: Qiana XL, Li J, Wei R, Lin H, Xiong LX Tags: Curr Pharm Des Source Type: research

Life style and peptic ulcer disease.
Abstract The risk of developing peptic ulcer disease (PUD) was shown to be associated with genetic inheritance, life-style and social status of the patients. Unhealthy lifestyle habits and failure in coping with stress have been closely associated with the occurrence of PUD. In contrary, limiting the use of analgesic drugs and glucocorticoids, controlling environmental and socioeconomic factors that predispose to H. Pylori infection, having a balanced diet, exercising regularly, coping successfully with stress, avoiding smoking, limiting alcohol intake and getting sufficient night sleep are essential in prevention...
Source: Current Pharmaceutical Design - May 9, 2018 Category: Drugs & Pharmacology Authors: Yegen BC Tags: Curr Pharm Des Source Type: research

Otilonium bromide: a drug with a complex mechanism of action.
Abstract Otilonium bromide (OB) is a drug with spasmolytic activity belonging to quaternary ammonium derivatives and extensively used to treat patients affected by the irritable bowel syndrome (IBS). Thanks to its peculiar pharmacokinetic, OB concentrates in the large bowel wall and acts locally. From the pharmacodynamics point of view, OB is able to inhibit i) the main patterns of human colonic motility in vitro; ii) the contractility caused by excitatory motor neurons stimulation (pre-synaptic action) and iii) the contractility caused by the direct action of excitatory neurotransmitters (post-synaptic action). I...
Source: Current Pharmaceutical Design - May 7, 2018 Category: Drugs & Pharmacology Authors: Evangelista S, Traini C, Vannucchi MG Tags: Curr Pharm Des Source Type: research

Editorial: The Advances in Treatment for Coronary Artery Disease, Voices from Interventional Cardiologists at the Fortieth Year of Percutaneous Coronary Intervention.
PMID: 29701573 [PubMed - in process] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 28, 2018 Category: Drugs & Pharmacology Authors: Wu W Tags: Curr Pharm Des Source Type: research

A potential therapeutic target RNA-binding protein, Arid5a for the treatment of inflammatory disease associated with aberrant cytokine expression.
CONCLUSION: Thus, Arid5a contributes to the activation of macrophages and T cells through positive control of mRNA half-lives of inflammatory cytokines and its related molecules, which might lead to cytokine storm. Interestingly, Arid5a was identified from an inhibitory effect of CPZ on IL-6 production in macrophages activated by LPS. Therefore, CPZ derivatives or Arid5a inhibitors may have a potential to suppress severe sepsis through control of post-transcriptional gene expression. PMID: 29701145 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 25, 2018 Category: Drugs & Pharmacology Authors: Masuda K, Kishimoto T Tags: Curr Pharm Des Source Type: research

Role of melatonin in the inflammatory process and its therapeutic potential.
Abstract Melatonin is an indolamine synthesized and secreted by the pineal gland along with other sources including immune system cells, the brain, skin and the gastrointestinal tract. Growing interest in this compound as a potential therapeutic agent in several diseases stems from its pleiotropic effects. Thus, melatonin plays a key role in various physiological activities that include regulation of circadian rhythms, immune responses, the oxidative process, apoptosis or mitochondrial homeostasis. Most of these processes are altered during inflammatory pathologies, among which neurodegenerative and bowel diseases...
Source: Current Pharmaceutical Design - April 25, 2018 Category: Drugs & Pharmacology Authors: Carrascal L, Nunez-Abades P, Ayala A, Cano M Tags: Curr Pharm Des Source Type: research

Molecular targets of phytochemicals for skin inflammation.
Abstract Skin is a protective organ and the largest of the human body. Due to its pivotal role in aesthetic appearance, skin health has a significant impact on quality of life. Chronic inflammation of the skin often marks the beginning of various skin diseases. Immune-mediated responses serve to protect the body from external insults and require succinct control, and can lead to ongoing cellular damage and various skin conditions if left unchecked. Studies have shown that phytochemicals can alter processes involved in skin inflammation and alleviate the effects of aging, cancer, atopic dermatitis, psoriasis, and v...
Source: Current Pharmaceutical Design - April 25, 2018 Category: Drugs & Pharmacology Authors: Kim JE, Lee KW Tags: Curr Pharm Des Source Type: research

Editorial: Inflammation and Heart Diseases.
PMID: 29671718 [PubMed - in process] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 21, 2018 Category: Drugs & Pharmacology Authors: Yue-Chun L Tags: Curr Pharm Des Source Type: research

N-Acetyl Cysteine and Vitamin D Supplementation in Treatment Resistant Obsessive- compulsive Disorder Patients: a General Review.
CONCLUSIONS: Nutraceutical supplementation in treatment resistance OCD may be important not only for improving obsessive-compulsive symptomatology, but also from a psychological perspective, given its better acceptance by the patients compared to pharmacological treatment. PMID: 29663874 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 17, 2018 Category: Drugs & Pharmacology Authors: di Michele F, Siracusano A, Alessandra T, Niolu C Tags: Curr Pharm Des Source Type: research

Heterocyclic N-oxides - A Promising Class of Agents Against Tuberculosis, Malaria and Neglected Tropical Diseases.
Abstract Heterocyclic N-oxides have emerged as promising agents against a number of diseases and disorders, especially infectious diseases. This review analyzes the emergence and development of this scaffold in the medicinal chemistry, focusing mainly on the discovery of new heterocyclic N-oxide compounds with potent activity against tuberculosis, malaria and neglected tropical diseases (i.e. leishmaniasis and Chagas disease). A number of heterocyclic N-oxide are described herein, nevertheless, the following chemical classes deserve to be highlighted due to the large number of reports in the literature about their...
Source: Current Pharmaceutical Design - April 17, 2018 Category: Drugs & Pharmacology Authors: Dos Santos Fernandes GF, Pavan AR, Dos Santos JL Tags: Curr Pharm Des Source Type: research

Antimicrobial Peptides as Mediators of Innate Immunity.
PMID: 29663872 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 15, 2018 Category: Drugs & Pharmacology Authors: Emilio J, Magrone T Tags: Curr Pharm Des Source Type: research

Inflammation and Heart Diseases.
PMID: 29663873 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 15, 2018 Category: Drugs & Pharmacology Authors: Yue-Chun L Tags: Curr Pharm Des Source Type: research

Foreword: The Year in Review: Comments on Plants, Cyclodextrins, Microbiota, and Diabetes.
PMID: 29648525 [PubMed - in process] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 14, 2018 Category: Drugs & Pharmacology Authors: Banks WA Tags: Curr Pharm Des Source Type: research

Cytochrome P450s And Alcoholic Liver Disease.
Abstract Alcohol consumption causes liver diseases, designated as alcoholic liver disease (ALD). Because alcohol is detoxified by alcohol dehydrogenase (ADH), a major ethanol metabolism system, the development of ALD was initially believed to be due to malnutrition caused by alcohol metabolism in liver. The discovery of the microsomal ethanol oxidizing system (MEOS) changed this dogma. Cytochrome P450 enzymes (CYP) constitute the major components of MEOS. Cytochrome P450 2E1 (CYP2E1) in MEOS is one of the major ROS generators in liver and is considered to be contributive to ALD. Our labs have been studying the rel...
Source: Current Pharmaceutical Design - April 9, 2018 Category: Drugs & Pharmacology Authors: Lu Y, Cederbaum AI Tags: Curr Pharm Des Source Type: research

Advances in the use of anti-inflammatory agents to manage chemotherapy-induced oral and gastrointestinal mucositis.
Abstract Mucositis is a side effect associated with the use of chemotherapy, and has a significant impact on the quality of life. Mucositis, by definition, refers to the inflammation of the mucosa and occurs throughout the alimentary tract from the mouth to anus. Nuclear factor kappa B (NFκB) encompasses a family of transcription factors, which upregulate pro-inflammatory cytokines. Both are recognized as key targets in developing therapeutic interventions for chemotherapy-induced mucositis, and cyclooxygenase (COX)-2 inhibition may also be beneficial in reducing the severity and duration. This review focuse...
Source: Current Pharmaceutical Design - April 8, 2018 Category: Drugs & Pharmacology Authors: Mahendran VJ, Stringer AM, Semple SJ, Song Y, Garg S Tags: Curr Pharm Des Source Type: research

Comparative study of the effects exerted by N-Valproyl-L-Phenylalanine and N-valproyl-L-tryptophan on CA1 hippocampal epileptiform activity in rat.
CONCLUSIONS: Both VPA-Phen and VPA-Tryp exert significant inhibitory effects on hippocampal burst activity parameters. Although of comparable magnitude, VPA-Phen-dependent effects have shorter duration than VPA-Tryp-induced ones. Nevertheless, the present results confirm that the conjugation between VPA and aminoacids represents a valid tool to improve the efficacy of antiepileptic drugs and, as well as for VPA-Tryp, propose VPA-Phen as a novel VPA derivative with enhanced pharmacological features Highlights - Effects of VPA-Phen and VPA-Tryp on CA1 epileptiform bursting activity were compared - 0.2, 0.5 and 1 mM drug conc...
Source: Current Pharmaceutical Design - April 8, 2018 Category: Drugs & Pharmacology Authors: Carletti F, Rizzo V, Gambino G, De Caro V, Sutera FM, Giannola LI, Ferraro G, Sardo P Tags: Curr Pharm Des Source Type: research

A Novel Fluorescence-Labeled Curcumin Conjugate: Synthesis, Evaluation And Imaging On Human Cell Lines.
In conclusion we successfully synthesized a novel water-soluble fluorescent curcumin conjugate which showed a strong preference for CAL-72 osteosarcoma cells in vitro. PMID: 29623828 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 5, 2018 Category: Drugs & Pharmacology Authors: Sheikh S, Sturzu A, Kalbacher H, Nagele T, Weidenmaier C, Horger M, Schwentner C, Ernemann U, Heckl S Tags: Curr Pharm Des Source Type: research

The potential mechanisms of exercise-induced cognitive protection: A literature review.
Abstract Dementia has become a major health concern for the aging population of the United States. Studies indicate that participation in moderate exercise, with training, has been shown to have a beneficial impact on cognition. Thus, exercise and its effects on cognitive function has become an important area of research. This review summarizes the current literature on the potential mechanisms of the benefits of exercise for cognitive function. PMID: 29623829 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 5, 2018 Category: Drugs & Pharmacology Authors: Norman JE, Rutkowsky J, Bodine S, Rutledge JC Tags: Curr Pharm Des Source Type: research

The effects of coenzyme Q10 supplementation on lipid profiles among patients with metabolic diseases: a systematic review and meta-analysis of randomized controlled trials.
CONCLUSIONS: CoQ10 supplementation may significantly reduce serum triglycerides levels, and help to improve lipid profiles in patients with metabolic disorders. Additional prospective studies are recommended using higher supplementation doses and longer intervention period. PMID: 29623830 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 5, 2018 Category: Drugs & Pharmacology Authors: Sharifi N, Tabrizi R, Moosazadeh M, Mirhosseini N, Lankarani KB, Akbari M, Chamani M, Kolahdooz F, Asemi Z Tags: Curr Pharm Des Source Type: research

Comparative Assay of 2D and 3D Cell Culture Models: Proliferation, Gene Expression and Anticancer Drug Response.
Abstract In vitro tests allow establishing experimental variables. However, in vitro results cannot be extrapolated to in vivo tests. Considering that three-dimensional (3D) culture has been one of the best ways to portray the in vivo system of most cell types, it is possible to carry out assays with a great clinical relevance for the analysis of the screening, action and resistance of antitumor drugs. Thus, the objective of the present study was to compare between 2D and 3D cell culture forms to conclude which is the most suitable model for preclinical in vitro drug testing. We evaluated the proliferation, geneti...
Source: Current Pharmaceutical Design - April 4, 2018 Category: Drugs & Pharmacology Authors: Souza AG, Silva IBB, Campos-Fernandez E, Barcelos LS, Souza JB, Marangoni K, Goulart LR, Alonso-Goulart V Tags: Curr Pharm Des Source Type: research

Antimicrobial peptides: Phylogenic Sources and Biological Activities. First of Two Parts.
Abstract Antimicrobial peptides (AMPs) are phylogenetically ancient substances released by living organisms for self protection against a broad variety of microbes. Moreover, AMPs are endowed with immune modulatory activities, linking innate and adaptive immunity together. Lantibiotics are AMPs of bacterial origin currently investigated for the generation of a new class of anti-infective compounds, owing to the phenomenon of antibiotic resistance against a broad variety of bacteria. Also, plants and marine AMPs are screened as novel drugs against human pathogens. Human AMPs encompass defensins and cathelicidins pr...
Source: Current Pharmaceutical Design - April 3, 2018 Category: Drugs & Pharmacology Authors: Magrone T, Russo MA, Jirillo E Tags: Curr Pharm Des Source Type: research

The role of formyl peptide receptors for immunomodulatory activities of antimicrobial peptides and peptidomimetics.
Abstract In recent years, the therapeutic potential of antimicrobial peptides (AMPs) as immunomodulators has become generally accepted. Nevertheless, only very few AMP-based compounds have progressed into clinical trials. This paradox may be explained by the fact, that some of the intrinsic properties of natural peptides, such as proteolytic and oxidative instability, render them inconvenient as therapeutics. Therefore, substantial research efforts have been dedicated to mimick the physico-chemical properties as well as biological activities of AMPs by designing and identifying more stable peptidomimetics displayi...
Source: Current Pharmaceutical Design - April 3, 2018 Category: Drugs & Pharmacology Authors: Skovbakke SL, Holdfeldt A, Forsman H, Bylund J, Franzyk H Tags: Curr Pharm Des Source Type: research

Virtual screening studies for discovery of novel inhibitors of inflammatory process targets.
Abstract Inflammation has been very evident in infectious diseases, but in recent times research has increasingly shown that a range of non-infectious diseases may present with inflammatory conditions. This fact becomes important as new anti-inflammatory drugs emerge with different targets for treatment of diseases. Virtual screening (VS) involves applying computational methods to discover new ligands for biological structures from the formation of large libraries composed of a large number of compounds. This review aims to report several studies employing a variety of VS: ligand-based and structure-based VS are b...
Source: Current Pharmaceutical Design - April 3, 2018 Category: Drugs & Pharmacology Authors: Scotti MT, Alves MF, Herrera-Acevedo CA, Scotti L Tags: Curr Pharm Des Source Type: research

Recent findings in molecular basis of inflammation and anti-inflammatory plants.
Abstract Inflammation is one of the most important body responses provided by the immune system since it ensures survival when tissues are affected by injuries or infections. The inflammatory response is an important process for maintenance of normal tissue homeostasis. In contrast to acute inflammation, chronic inflammation does not have a useful impact. Prevention and suppression of inflammation are necessary to reduce patient suffering and to preserve the integrity of multiple organs. Unfortunately, commercial available anti-inflammatory drugs are not free from side effects. Hence, there is an urgent need for i...
Source: Current Pharmaceutical Design - April 3, 2018 Category: Drugs & Pharmacology Authors: Kazemi S, Shirzad H, Rafieian-Kopaei M Tags: Curr Pharm Des Source Type: research

Systematic development and optimization of in-situ gelling system for Moxifloxacin Ocular nanosuspension using high pressure homogenization with improved encapsulation efficiency.
The objective of this study was to apply Quality by Design (QbD) principles on process parameter optimization for development of hybrid delivery system (combination of (SLNs) and In-situ gelling system) for hydrophilic drug Moxifloxacin Hydrochloride (MOX) to achieve its controlled delivery, which otherwise may not be possible through single type of technology. METHODS: Risk assessment studies were carried out to identify probable risks influencing CQAs on the product. In design of experiments (DoE), the process parameters (independent variables) i.e., chiller temperature X1, High pressure homogenization (HPH) pressur...
Source: Current Pharmaceutical Design - April 2, 2018 Category: Drugs & Pharmacology Authors: Khurana LK, Singh R, Singh H, Sharma M Tags: Curr Pharm Des Source Type: research

Human Oral Defensins Antimicrobial Peptides: A Future Promising Antimicrobial Drug.
Abstract The nature and structural composition of antimicrobial peptides are derived from their innate immune response and they are active against various bacteria, fungi and other microorganisms. The aim of this paper was to pool up the literature on the features of human oral defensins antimicrobial peptides. The defensins showed antimicrobial activity against Gram-positive and Gram-negative bacteria and various fungi and viruses. As with their other properties like antiviral, antifungal and antibacterial, human defensins peptides are thought to have a unique amino acid-based structure with Disulphide Bridge whi...
Source: Current Pharmaceutical Design - April 2, 2018 Category: Drugs & Pharmacology Authors: Khurshid Z, Zafar MS, Naseem M, Khan RS, Najeeb S Tags: Curr Pharm Des Source Type: research

Potential Use Of Nanomedicine For The Anti-Inflammatory Treatment Of Neurodegenerative Diseases.
Abstract Neurodegenerative diseases, like Alzheimer´s and Parkinson´s disease, are a group of disorders that have in common their increasingly high prevalence along with the shortage of effective treatments. In addition, the scientific community faces the challenge of getting the drugs used in these treatments to cross the blood-brain barrier (BBB) and reach the brain in sufficient concentration to be able to exert its effect. Hence, researchers across multiple disciplines are working together in order to improve the ability of therapeutics to penetrate the BBB. In this sense, the use of nanomedicine, ...
Source: Current Pharmaceutical Design - April 2, 2018 Category: Drugs & Pharmacology Authors: Cayero-Otero MD, Espinosa-Oliva AM, Herrera AJ, Garcia-Dominguez I, Fernandez-Arevalo M, Martin-Banderas L, de Pablos RM Tags: Curr Pharm Des Source Type: research

Management of antithrombotic therapy in patients with coronary artery disease or atrial fibrillation who underwent abdominal surgical operations.
CONCLUSIONS: Management of antithrombotics therapy during the perioperative period in patients undergoing abdominal surgery should follow a patient-centered approach according to a patient's medical history and thrombotic risk weighted for bleeding risk. PMID: 29611483 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Design)
Source: Current Pharmaceutical Design - April 2, 2018 Category: Drugs & Pharmacology Authors: Schizas D, Kariori M, Boudoulas KD, Siasos G, Patelis N, Kalantzis C, Carmen-Maria M, Vavuranakis M Tags: Curr Pharm Des Source Type: research