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Topical Compounds

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https://www.readbyqxmd.com/read/28318723/pan-european-survey-of-the-topical-ocular-use-of-cyclosporine-a
#1
A Labbé, C Baudouin, D Ismail, M Amrane, J-S Garrigue, A Leonardi, F C Figueiredo, G Van Setten, M Labetoulle
OBJECTIVE: To assess medical practices surrounding the use of topical ocular cyclosporine A across European Union nations. METHODS: Key stakeholders (ophthalmologists, hospital pharmacists, regulatory health authorities) from European Union member states were interviewed by telephone using a semi-structured, open-ended questionnaire. Ophthalmologists responded to questions about practice patterns of cyclosporine A use (prescription frequency, indication, dosage), pharmacists about cyclosporine A formulations (composition, manufacturing process, quality control, distribution), and the regulatory authorities about market authorization and pharmacovigilance for various cyclosporine A products...
March 16, 2017: Journal Français D'ophtalmologie
https://www.readbyqxmd.com/read/28318351/retinoids-a-journey-from-the-molecular-structures-and-mechanisms-of-action-to-clinical-uses-in-dermatology-and-adverse-effects
#2
Samar Khalil, Tara Bardawil, Carla Stephan, Nadine Darwiche, Ossama Abbas, Abdul Ghani Kibbi, Georges Nemer, Mazen Kurban
Retinoids are a class of compounds derived from vitamin A or have structural and/or functional similarity with vitamin A. They are classified into three generations based on their molecular structures. Inside the body, retinoids bind to several classes of proteins including retinoid-binding proteins and retinoid nuclear receptors. This eventually leads to the activation of specific regulatory regions of DNA - called the retinoic acid response elements - involved in regulating cell growth, differentiation and apoptosis...
March 20, 2017: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/28297727/new-knowledge-about-old-drugs-the-anti-inflammatory-properties-of-cardiac-glycosides
#3
Robert Fürst, Ilse Zündorf, Theo Dingermann
In the 19th century, cardio-active steroid glycosides, shortly cardiac glycosides, were scientifically established as drugs against heart failure. Their in vivo, cellular, and molecular actions as well as their predominant target, Na(+)-K(+)-ATPase, have been comprehensively investigated in the 20th century and the discovery of endogenous cardiac glycosides has fostered this research field. In the last years, however, results from clinical trials and meta-analyses have questioned their therapeutic value due to efficacy and safety issues...
March 15, 2017: Planta Medica
https://www.readbyqxmd.com/read/28294050/an-integrated-multi-qsar-modeling-approach-for-designing-knoevenagel-type-indoles-with-enhancing-cytotoxic-profiles
#4
Sk Abdul Amin, Nilanjan Adhikari, Tarun Jha, Shovanlal Gayen
BACKGROUND: Unconventional Knoevenagel-type indoles have been the topic of interest of many synthetic chemists because of its promising efficacy in different diseases including in cancer. OBJECTIVE: To explore the structural requirements of Knoevenagel-type cytotoxic indoles for higher efficacy. METHODS: Multi-QSAR modeling (MLR, ANN, SVM, Bayesian classification, HQSAR and Topomer CoMFA) was performed on these analogs. RESULTS: All these modeling techniques were validated individually and interpreted with the experimental SAR observations...
March 9, 2017: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/28291591/the-inma-infancia-y-medio-ambiente-environment-and-childhood-project-more-than-10-years-contributing-to-environmental-and-neuropsychological-research
#5
REVIEW
Mireia Gascon, Mònica Guxens, Martine Vrijheid, Maties Torrent, Jesús Ibarluzea, Eduardo Fano, Sabrina Llop, Ferran Ballester, Mariana F Fernández, Adonina Tardón, Ana Fernández-Somoano, Jordi Sunyer
BACKGROUND: In 2003 the INMA-INfancia y Medio Ambiente (Environment and Childhood) project, a Spanish national network of birth cohorts including more than 3500 participants, was set up with the aim to assess the health impacts of pre- and postnatal environmental exposures on children. The project has published more than 60 papers on maternal and environmental factors related to neuropsychological development in children, one of the main research interests within the project. With the present review, we evaluate the evidence provided by the INMA project on this topic and discuss how the data can contribute to cover the challenges that children's environmental health research will face in the coming years...
February 28, 2017: International Journal of Hygiene and Environmental Health
https://www.readbyqxmd.com/read/28280381/topical-phenytoin-for-the-treatment-of-neuropathic-pain
#6
David J Kopsky, Jan M Keppel Hesselink
We developed and tested a new putative analgesic cream, based on the anticonvulsant phenytoin in patients suffering from treatment refractory neuropathic pain. The use of commercial topical analgesics is not widespread due to the facts that capsaicin creams or patches can give rise to side effects, such as burning, and analgesic patches (e.g., lidocaine 5% patches) have complex handling, especially for geriatric patients. Only in a few countries, compounded creams based on tricyclic antidepressants or other (co-)analgesics are available...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28280377/promotion-of-anagen-increased-hair-density-and-reduction-of-hair-fall-in-a-clinical-setting-following-identification-of-fgf5-inhibiting-compounds-via-a-novel-2-stage-process
#7
Dominic Burg, Masakuni Yamamoto, Masato Namekata, Joseph Haklani, Koichiro Koike, Maria Halasz
BACKGROUND: There are very few effective, scientifically validated treatments with known mechanisms of action for treatment of hair loss in both men and women. Fibroblast growth factor 5 (FGF5) is an important factor in the irreversible transition from anagen to catagen, and inhibition of FGF5 prolongs anagen phase and reduces hair loss. OBJECTIVE: We aimed to screen botanically derived molecules for FGF5 inhibitory activity in vitro and assess efficacy in a clinical setting...
2017: Clinical, Cosmetic and Investigational Dermatology
https://www.readbyqxmd.com/read/28278501/standardization-of-an-in-vitro-model-for-evaluating-the-bioavailability-of-topically-applied-compounds-on-damaged-skin-application-to-sunscreen-analysis
#8
Carine Jacques-Jamin, Corinne Jeanjean-Miquel, Anaïs Domergue, Sandrine Bessou-Touya, Hélène Duplan
BACKGROUND: Information is lacking on the dermal penetration of topically applied formulations on in vitro skin models, under conditions where the stratum corneum (SC) is damaged. Therefore, we have developed a standardized in vitro barrier-disrupted skin model using tape stripping. METHODS: Different tape stripping conditions were evaluated using histology, transepidermal water loss, infrared densitometry, and caffeine absorption. RESULTS: The effects of tape stripping were comparable using pig and human skin...
March 10, 2017: Skin Pharmacology and Physiology
https://www.readbyqxmd.com/read/28274160/brucella-suis-carbonic-anhydrases-and-their-inhibitors-towards-alternative-antibiotics
#9
REVIEW
Stephan Köhler, Safia Ouahrani-Bettache, Jean-Yves Winum
Carbonic anhydrases have started to emerge as new potential antibacterial targets for several pathogens. Two β-carbonic anhydrases, denominated bsCA I and bsCA II, have been isolated and characterized from the bacterial pathogen Brucella suis, the causative agent of brucellosis or Malta fever. These enzymes have been investigated in detail and a wide range of classical aromatic and heteroaromatic sulfonamides as well as carbohydrate-based compounds have been found to inhibit selectively and efficiently Brucella suis carbonic anhydrases...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28271334/topical-treatments-for-localized-neuropathic-pain
#10
REVIEW
Roberto Casale, Z Symeonidou, M Bartolo
PURPOSE OF REVIEW: Topical therapeutic approaches in localized neuropathic pain (LNP) syndromes are increasingly used by both specialists and general practitioners, with a potentially promising effect on pain reduction. In this narrative review, we describe the available compounds for topical use in LNP syndromes and address their potential efficacy according to the literature. RECENT FINDINGS: Local anaesthetics (e.g., lidocaine, bupivacaine and mepivacaine), as well as general anaesthetic agents (e...
March 2017: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/28266812/anticancer-activity-of-stilbene-based-derivatives
#11
Barbara De Filippis, Alessandra Ammazzalorso, Marialuigia Fantacuzzi, Letizia Giampietro, Cristina Maccallini, Rosa Amoroso
Anticancer Activity of Stilbene-based Derivatives Barbara De Filippis,* Alessandra Ammazzalorso, Marialuigia Fantacuzzi, Letizia Giampietro, Cristina Maccallini, Rosa Amoroso Dipartimento di Farmacia, Università "G. d'Annunzio", via dei Vestini 31, 66100 Chieti, Italy; * E-mail: barbara.defilippis@unich.it Stilbene is a very present structural scaffold in nature and stilbene-based compounds are largely described for their biological activity such as cardioprotective, potent antioxidant, anti-inflammatory, and anticancer agents...
March 7, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28262809/data-integration-aids-understanding-of-butterfly-host-plant-networks
#12
Ai Muto-Fujita, Kazuhiro Takemoto, Shigehiko Kanaya, Takeru Nakazato, Toshiaki Tokimatsu, Natsushi Matsumoto, Mayo Kono, Yuko Chubachi, Katsuhisa Ozaki, Masaaki Kotera
Although host-plant selection is a central topic in ecology, its general underpinnings are poorly understood. Here, we performed a case study focusing on the publicly available data on Japanese butterflies. A combined statistical analysis of plant-herbivore relationships and taxonomy revealed that some butterfly subfamilies in different families feed on the same plant families, and the occurrence of this phenomenon more than just by chance, thus indicating the independent acquisition of adaptive phenotypes to the same hosts...
March 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28262638/coulomb-correlations-in-4d-and-5d-oxides-from-first-principles-or-how-spin-orbit-materials-choose-their-effective-orbital-degeneracies
#13
Cyril Martins, Markus Aichhorn, Silke Biermann
The interplay of spin-orbit coupling and Coulomb correlations has become a hot topic in condensed matter theory and is especially at stake in 4d and 5d transition metal oxides, like iridates or rhodates. Here, we review recent advances in dynamical mean-field theory(DMFT)-based electronic structure calculations for treating such compounds, introducing all necessary implementation details. We also discuss the evaluation of Hubbard interactions in spin-orbit materials. As an example, we perform DMFT calculations on insulating strontium iridate (Sr<sub>2</sub>IrO<sub>4</sub>) and its 4d metallic counterpart strontium rhodate (Sr<sub>2</sub>RhO<sub>4</sub>)...
March 6, 2017: Journal of Physics. Condensed Matter: An Institute of Physics Journal
https://www.readbyqxmd.com/read/28262620/effects-of-jasminum-multiflorum-leaf-extract-on-rodent-models-of-epilepsy-motor-coordination-and-anxiety
#14
Jonas I Addae, Ramish Pingal, Kheston Walkins, Renee Cruickshank, Farid F Youssef, Shivananda B Nayak
Jasmine flowers and leaves are used extensively in folk medicine in different parts of the world to treat a variety of diseases. However, there are very few published reports on the neuropsychiatric effects of Jasmine extracts. Hence, the objectives of the present study were to examine the effects of an alcohol extract of Jasminum multiflorum leaves on topically-applied bicuculline (a model of acute simple partial epilepsy) and maximal electroshock (MES, a model of generalized tonic-clonic seizure) in male Sprague-Dawley rats...
February 28, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28259765/evaluating-the-transport-kinetics-of-a-model-compound-released-from-cellulosic-coacervate-compositions-into-artificial-sebum
#15
Nada H Baalbaki, Gerald B Kasting
Complex coacervates of cationic polymers and anionic surfactants, which are produced spontaneously during the use of rinse-off formulations, represent an important delivery vehicle for topical agents to the skin surface and appendages. In the present study, an artificial sebum-loaded cell culture insert method for determining the sebum diffusion properties of topical agents was optimized for in vitro release testing (IVRT). This method was subsequently used to evaluate the transport kinetics of a model compound, kinetin, released from semi-solid coacervate formulations into sebum...
March 1, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28258519/sirtuins-a-promising-target-in-slowing-down-the-ageing-process
#16
REVIEW
Wioleta Grabowska, Ewa Sikora, Anna Bielak-Zmijewska
Ageing is a plastic process and can be successfully modulated by some biomedical approaches or pharmaceutics. In this manner it is possible to delay or even prevent some age-related pathologies. There are some defined interventions, which give promising results in animal models or even in human studies, resulting in lifespan elongation or healthspan improvement. One of the most promising targets for anti-ageing approaches are proteins belonging to the sirtuin family. Sirtuins were originally discovered as transcription repressors in yeast, however, nowadays they are known to occur in bacteria and eukaryotes (including mammals)...
March 3, 2017: Biogerontology
https://www.readbyqxmd.com/read/28258218/structural-analyses-of-candida-albicans-sterol-14%C3%AE-demethylase-complexed-with-azole-drugs-address-the-molecular-basis-of-azole-mediated-inhibition-of-fungal-sterol-biosynthesis
#17
Tatiana Y Hargrove, Laura Friggeri, Zdzislaw Wawrzak, Aidong Qi, William J Hoekstra, Robert J Schotzinger, John D York, F Peter Guengerich, Galina I Lepesheva
With some advances in modern medicine (such as cancer chemotherapy, broad exposure to antibiotics, and immunosuppression) the incidence of opportunistic fungal pathogens such as Candida albicans has increased. Cases of drug resistance among these pathogens have become more frequent, requiring the development of new drugs and a better understanding of the targeted enzymes. Sterol 14α-demethylase (CYP51) is a cytochrome P450 enzyme required for biosynthesis of sterols in eukaryotic cells and the major target of clinical drugs for managing fungal pathogens, but some of the CYP51 key features important for rational drug design have remained obscure...
March 3, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28253633/fatty-acids-penetration-into-human-skin-ex-vivo-a-tof-sims-analysis-approach
#18
Vytis Čižinauskas, Nicolas Elie, Alain Brunelle, Vitalis Briedis
Linoleic, oleic, palmitoleic, palmitic, and stearic fatty acids (FAs) are commonly used in dermatological formulations. They differ by their structure, presence in the skin, and mode of application in pharmaceuticals and cosmetics compounding. These FAs are also known as chemical penetration enhancers, but their mechanisms of penetration enhancement and effect on barrier characteristics of the skin require additional study. In this study, the authors conducted an ex vivo analysis of the distribution of lipid components in the epidermis and dermis of human skin after applying individual FAs...
March 2, 2017: Biointerphases
https://www.readbyqxmd.com/read/28248487/practical-stereochemistry
#19
Richard M Kellogg
The relationship between fundamental and applied is often uneasy, particularly in modern political climates. A familiar political view, aimed negatively at the scientific community, is that the former is a waste of money whereas the latter gives value for investment. The answer that fundamental is required as the basis for practical suffers from the fact that the timelines between fundamental and practical are often long and the routes contorted and unexpected. This has been my experience. In this Account, examples are given from the research in which I have been involved wherein quite fundamental considerations have led to various applications...
March 1, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28243134/home-hemodialysis-a-comprehensive-review-of-patient-centered-and-economic-considerations
#20
REVIEW
Rachael C Walker, Kirsten Howard, Rachael L Morton
Internationally, the number of patients requiring treatment for end-stage kidney disease (ESKD) continues to increase, placing substantial burden on health systems and patients. Home hemodialysis (HD) has fluctuated in its popularity, and the rates of home HD vary considerably between and within countries although there is evidence suggesting a number of clinical, survival, economic, and quality of life (QoL) advantages associated with this treatment. International guidelines encourage shared decision making between patients and clinicians for the type of dialysis, with an emphasis on a treatment that aligned to the patients' lifestyle...
2017: ClinicoEconomics and Outcomes Research: CEOR
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