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Topical Compounds

Gillian A Ryan, Sarah M Nicholson, John J Morrison
Vaginal birth after caesarean (VBAC) delivery remains a controversial topic, and one for which there is a lack of robust data to guide clinicians and parturients regarding their best option for mode of delivery in a subsequent pregnancy. In many developed countries the trend observed in recent years is that of progressively reduced VBAC rates, and hence increased use of elective repeat caesarean section (ERCS). This factor has contributed, more than any other, to the disproportionately high caesarean section (CS) rates in many countries...
March 7, 2018: European Journal of Obstetrics, Gynecology, and Reproductive Biology
Jean-Francois Fournier, Claire Bouix-Peter, Denis Duvert, Anne-Pascale Luzy, Gilles Ouvry
Phototoxicity occurs when UV irradiation causes otherwise benign compounds to become irritant, sensitizers or even genotoxic. This toxicity is particularly a concern after topical application and in dermatological programs where skin irritation can be incompatible with the desired therapeutic outcome. This brief article establishes that the intrinsic Property Forecast Index (iPFI) can be used to evaluate the probability of a compound being phototoxic and gives medicinal chemists a practical tool to handle this liability...
March 16, 2018: Journal of Medicinal Chemistry
Kateřina Štulíková, Marcel Karabín, Jakub Nešpor, Pavel Dostálek
Hop ( Humulus lupulus L.), as a key ingredient for beer brewing, is also a source of many biologically active molecules. A notable compound, 8-prenylnaringenin (8-PN), structurally belonging to the group of prenylated flavonoids, was shown to be a potent phytoestrogen, and thus, became the topic of active research. Here, we overview the pharmacological properties of 8-PN and its therapeutic opportunities. Due to its estrogenic effects, administration of 8-PN represents a novel therapeutic approach to the treatment of menopausal and post-menopausal symptoms that occur as a consequence of a progressive decline in hormone levels in women...
March 15, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Andreu Presa, Guillem Vázquez, Leoní A Barrios, Olivier Roubeau, Luís Korrodi-Gregório, Ricardo Pérez-Tomás, Patrick Gamez
The development of photoactivatable metal complexes with potential anticancer properties is a topical area of current investigation. Photoactivated chemotherapy using coordination compounds is typically based on photochemical processes occurring at the metal center. In the present study, an innovative approach is applied that takes advantage of the remarkable photochemical properties of diarylethenes. Following a proof-of-concept study with two complexes, namely, C1 and C2, a series of additional platinum(II) complexes from dithienylcyclopentene-based ligands was designed and prepared...
March 15, 2018: Inorganic Chemistry
Ines Greco, Bernard D Hummel, Jaspreet Vasir, Jeffrey L Watts, Jason Koch, Johannes E Hansen, Hanne Mørck Nielsen, Peter Damborg, Paul R Hansen
Antimicrobial peptides (AMPs) hold promise as the next generation of antimicrobial agents, but often suffer from rapid degradation in vivo. Modifying AMPs with non-proteinogenic residues such as peptoids (oligomers of N -alkylglycines) provides the potential to improve stability. We have identified two novel peptoid-based compounds, B1 and D2 , which are effective against the canine skin pathogen Staphylococcus pseudintermedius , the main cause of antibiotic use in companion animals. We report on their potential to treat infections topically by characterizing their release from formulation and in vitro ADME properties...
March 10, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Marvin Pollum, Minh Lam, Steffen Jockusch, Carlos E Crespo-Hernández
Sulfur-substituted nucleobases (i.e. thiobases) are a prospective class of compounds for clinical and cosmetic topical phototherapies. Recent investigations of several thiobases have revealed the ultrafast and efficient population of reactive triplet states upon UVA irradiation and the subsequent generation of singlet oxygen in high yield. In this contribution, we examine the photosensitizing activities of three of the most promising thiobase derivatives discovered to date, 2,4-dithiothymine, 2,4-dithiouracil, and 2,6-dithiopurine...
March 12, 2018: ChemMedChem
Stephane Jeanmart, Julien Gagnepain, Pulakesh Maity, Clemens Lamberth, Fredrik Cederbaum, Ramya Rajan, Olivier Jacob, Mathias Blum, Stephane Bieri
Novel imidazole-based ketene dithioacetals show impressive in planta activity against the economically important plant pathogens Alternaria solani, Botryotinia fuckeliana, Erysiphe necator and Zymoseptoria tritici. Especially derivatives of the topical antifungal lanoconazole, which bear an alkynyloxy or a heteroaryl group in the para-position of the phenyl ring, exhibit excellent control of the mentioned phytopathogens. These compounds inhibit 14α -demethylase in the sterol biosynthesis pathway of the fungi...
March 9, 2018: Bioorganic & Medicinal Chemistry
Danielle H Dube
"Drug Discovery" is a 13-week lecture and laboratory-based course that was developed to introduce non-science majors to foundational chemistry and biochemistry concepts as they relate to the unifying theme of drug discovery. The first part of this course strives to build students' understanding of molecules, their properties, the differences that enable them to be separated from one another, and their abilities to bind to biological receptors and elicit physiological effects. After building students' molecular worldview, the course then focuses on four classes of drugs: antimicrobials, drugs that affect the mind, steroid-based drugs, and anti-cancer drugs...
March 12, 2018: Biochemistry and Molecular Biology Education
F Vizzarri, M Palazzo, S Bartollino, D Casamassima, B Parolini, P Troiano, C Caruso, C Costagliola
Ultraviolet-radiation exerts a well-known role in the development of various ocular diseases and may contribute to the progress of age-related macular degeneration. Therefore, the use of compounds able to protect the eyes from UV-induced cellular damage is challenging. The aim of this study has been to test the protective effects of an antioxidant topical formulation against UV-induced damage in rabbit eyes. Twelve male rabbits were used. Animals were divided into 4 groups of 3 animals each. Control group (CG) did not receive any irradiation and/or eye drop...
March 12, 2018: Physiological Research
J V Pergolizzi, R Taylor, J-A LeQuang, R B Raffa
WHAT IS KNOWN AND OBJECTIVE: Menthol has been used as a non-opioid pain reliever since ancient times. A modern understanding of its molecular mechanism of action could form the basis for generating targets for discovery of novel non-opioid analgesic drugs. METHODS: The PubMed database was queried using search words related to menthol, pain and analgesia. The results were limited to relevant preclinical studies and clinical trials and reviews published in English during the past 5 years, which yielded 31 reports...
March 10, 2018: Journal of Clinical Pharmacy and Therapeutics
Deepak Mehta, S Jyothi, Prashant Moogi, Werner J Finger, Keiichi Sasaki
OBJECTIVES: Aim of this clinical trial was to investigate the effect of a calcium phosphate based desensitizer paste applied prior to in-office tooth whitening on bleaching sensitivity (BS). METHODS: This crossover study was designed as randomized double-blinded, placebo-controlled trial. The desensitizer paste Teethmate AP (TAP) contains tetracalcium phosphate and dicalcium phosphate anhydrous in glycerol and polyethylene glycol, whereas placebo (PLA) is a calcium phosphate free analog...
March 9, 2018: Journal of Esthetic and Restorative Dentistry
Cícera Datiane de Morais Oliveira-Tintino, Renata Torres Pessoa, Maria Neyze Martins Fernandes, Isabel Sousa Alcântara, Bruno Anderson Fernandes da Silva, Maria Rayane Correia de Oliveira, Anita Oliveira Brito Pereira Bezerra Martins, Maria do Socorro da Silva, Saulo Relison Tintino, Fábio Fernandes Galvão Rodrigues, José Galberto Martins da Costa, Sidney Gonçalo de Lima, Marta Regina Kerntopf, Teresinha Gonçalves da Silva, Irwin Rose Alencar de Menezes
BACKGROUND: Inflammation makes up a set of vascularized tissue reactions acting in the defense of the body against harmful stimuli. Natural products are a lower cost alternative with better benefit, often used in popular medicine in the treatment of inflammatory processes. Several species from the genus Croton have scientifically proven anti-inflammatory action. PURPOSE: This study aims to analyze the chemical composition of the Croton campestris A. St.-Hil essential oil (EOCC), derived from fresh leaves, as well as to evaluate the anti-inflammatory potential and the possible mechanisms of action of the EOCC and its constituent β-caryophyllene...
March 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Caitlin V Bucher, A J Day, Maria Carvalho
Since the number of prescriptions for opioid medications have continued to rise, there have been questions about the safety of using opioids in pain management. Traditionally, opioid analgesics were reserved for a few select conditions, such as terminal illness and surgery, but currently opioids have been readily prescribed for multiple conditions. The objective of this manuscript is to clarify the current state of opioid use and to discuss alternative transdermal analgesic therapies in pain management. Transdermal compounded medications are patient-specific and customizable to include different types of drugs, in various dosage strengths, that are to be delivered simultaneously in one application...
January 2018: Journal of Opioid Management
Katrien Van Bocxlaer, Eric Gaukel, Deirdre Hauser, Seong Hee Park, Sara Schock, Vanessa Yardley, Ryan Randolph, Jacob J Plattner, Tejal Merchant, Simon L Croft, Robert T Jacobs, Stephen A Wring
Cutaneous leishmaniasis (CL) is caused by several species of the protozoan parasite Leishmania - affecting an estimated 10 million people worldwide. Previously reported strategies for the development of topical CL treatments have focussed primarily on drug permeation and formulation optimisation as the means to increase treatment efficacy.Our approach aims to identify compounds with anti-leishmanial activity and properties consistent with topical administration. Of the test compounds, five benzoxaboroles showed potent activity (EC50 < 5 μM) against intracellular amastigotes of at least one Leishmania species and acceptable activity (20 μM< EC50 <30 μM) against two more species...
March 5, 2018: Antimicrobial Agents and Chemotherapy
Kerstin Reisinger, Veronika Blatz, Joep Brinkmann, Thomas R Downs, Anja Fischer, Frank Henkler, Sebastian Hoffmann, Cyrille Krul, Manfred Liebsch, Andreas Luch, Ralph Pirow, Astrid A Reus, Markus Schulz, Stefan Pfuhler
Recently revised OECD Testing Guidelines highlight the importance of considering the first site-of-contact when investigating the genotoxic hazard. Thus far, only in vivo approaches are available to address the dermal route of exposure. The 3D Skin Comet and Reconstructed Skin Micronucleus (RSMN) assays intend to close this gap in the in vitro genotoxicity toolbox by investigating DNA damage after topical application. This represents the most relevant route of exposure for a variety of compounds found in household products, cosmetics, and industrial chemicals...
March 2018: Mutation Research
Sharon Elad, Kevin Zinchuk, Shuli Li, Corey Cutler, Jane Liesveld, Nathaniel Treister
BACKGROUND: Chronic graft-versus-host disease (cGVHD) frequently affects the oral mucosa and is generally responsive to topical immunomodulatory therapies. Clinicians may benefit from guidance in choosing the most appropriate therapy with respect to practicality and cost. OBJECTIVE: To assess the economic considerations related to topical immunomodulatory treatments for management of oral mucosal cGVHD and their practical implications. METHOD: Topical treatments used for management of oral cGVHD were obtained from the NIH Consensus document for ancillary and supportive care...
March 1, 2018: Biology of Blood and Marrow Transplantation
Takeru Ehara, Christopher M Adams, Doug Bevan, Nan Ji, Erik L Meredith, David B Belanger, James Powers, Mitsunori Kato, Catherine Solovay, Donglei Liu, Michael Capparelli, Philippe Bolduc, Jonathan E Grob, Matthew H Daniels, Luciana Ferrara, Louis Yang, Byron Li, Christopher S Towler, Rebecca C Stacy, Ganesh Prasanna, Muneto Mogi
Soluble guanylate cyclase (sGC), the endogenous receptor for nitric oxide (NO), has been implicated in several diseases associated with oxidative stress. In a pathological oxidative environment, the heme group of sGC can be oxidized becoming unresponsive to NO leading to a loss in the ability to catalyze the production of cGMP. Recently a dysfunctional sGC/NO/cGMP pathway has been implicated in contributing to elevated intraocular pressure associated with glaucoma. Herein we describe the discovery of molecules specifically designed for topical ocular administration, which can activate oxidized sGC restoring the ability to catalyze the production of cGMP...
March 2, 2018: Journal of Medicinal Chemistry
Ai-Min Bao, Dick F Swaab
The quality of postmortem research depends strongly on a thorough clinical investigation and documentation of the patient's disorder and therapies. In addition, a systematic and professional neuropathologic investigation of both cases and controls is absolutely crucial. In the experience of the Netherlands Brain Bank (NBB), about 20% of clinical neurologic diagnoses, despite being made in first-rate clinics, have to be revised or require an extra diagnosis after a complete and thorough review by the NBB. The neuropathology examination may reveal for instance that the "controls" already have preclinical neurodegenerative alterations...
2018: Handbook of Clinical Neurology
Thaiene Avila Reis, Ana Elise Jaculi, Rubens da Costa Alves, Tais Gratieri, Ricardo Bentes Azevedo, Graziella Anselmo Joanitti, Guilherme Martins Gelfuso, Marcilio Cunha-Filho
Considering the feasibility of the aluminum phthalocyanine chloride (AlPcCl) application in the topical photodynamic therapy of cutaneous tumors and the lack of HPLC methods capable of supporting skin permeation experiments using this compound, the aim of this study was to obtain a simple and selective chromatographic method for AlPcCl determination in skin matrices. A HPLC-UV/Vis method was developed using a normal-phase column operating at 30°C, an isocratic mobile phase of methanol : phosphoric acid (0...
2018: Journal of Analytical Methods in Chemistry
Claudio Vernieri, Federico Nichetti, Alessandra Raimondi, Sara Pusceddu, Marco Platania, Franco Berrino, Filippo de Braud
In recent years, calorie-restricted dietary regimens and compounds such as vitamins, curcumin, green tea extracts and omega-3 fatty acids have attracted attention for their potential anticancer effects. While definitive conclusions cannot be drawn in this field, many patients adopt complementary antitumor therapies aiming to improve efficacy or reduce toxicity of chemotherapy, with uncertain benefits and the risk of additional toxicities or antagonistic interactions with standard therapies. In this manuscript, we review the different levels of available evidence to suggest or discourage specific dietary changes or supplement use in the context of cancer prevention, reduction of tumor recurrences and survival prolongation in advanced cancers...
March 2018: Critical Reviews in Oncology/hematology
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