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https://www.readbyqxmd.com/read/28543784/improvement-of-hydration-and-epidermal-barrier-function-in-human-skin-by-a-novel-compound-isosorbide-dicaprylate
#1
Ratan K Chaudhuri, Krzysztof Bojanowski
OBJECTIVE: The study involved the synthesis of a novel derivative of caprylic acid - isosorbide dicaprylate (IDC) - and the evaluation of its potential in improving water homeostasis and epidermal barrier function in human skin. METHODS: The effect of IDC on gene expression was assayed in skin organotypic cultures by DNA microarrays. The results were then confirmed for a few key genes by quantitative PCR, immuno- and cytochemistry. Final validation of skin hydration properties was obtained by four separate clinical studies...
May 24, 2017: International Journal of Cosmetic Science
https://www.readbyqxmd.com/read/28540463/investigating-the-organic-and-conventional-production-type-of-olive-oil-with-target-and-suspect-screening-by-lc-qtof-ms-a-novel-semi-quantification-method-using-chemical-similarity-and-advanced-chemometrics
#2
Natasa P Kalogiouri, Reza Aalizadeh, Nikolaos S Thomaidis
The discrimination of organic and conventional production has been a critical topic of public discussion and constitutes a scientific issue. It remains a challenge to establish a correlation between the agronomical practices and their effects on the composition of olive oils, especially the phenolic composition, since it defines their organoleptic and nutritional value. Thus, a liquid chromatography-electrospray ionization-quadrupole time of flight tandem mass spectrometric method was developed, using target and suspect screening workflows, coupled with advanced chemometrics for the identification of phenolic compounds and the discrimination between organic and conventional extra virgin olive oils...
May 25, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28539726/development-and-validation-of-a-simultaneous-rp-hplcuv-dad-method-for-determination-of-polyphenols-in-gels-containing-s-terebinthifolius-raddi-anacardiaceae
#3
Melina G Carvalho, Cícero F S Aragão, Fernanda N Raffin, Túlio F A de L Moura
Topical gels containing extracts of Schinus terebinthifolius have been used to treat bacterial vaginosis. It has been reported that this species has antimicrobial, anti-inflammatory and anti-ulcerogenic properties, which can be attributed to the presence of phenolic compounds. In this work, a sensitive and selective reversed-phase HPLC-UV/DAD method for the simultaneous assay of six polyphenols that could be present in S. terebinthifolius was developed. The method was shown to be accurate and precise. Peak purity and similarity index both exceeded 0...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28534261/the-role-of-drug-metabolites-in-the-inhibition-of-cytochrome-p450-enzymes
#4
Momir Mikov, Maja Đanić, Nebojša Pavlović, Bojan Stanimirov, Svetlana Goločorbin-Kon, Karmen Stankov, Hani Al-Salami
Following the drug administration, patients are exposed not only to the parent drug itself, but also to the metabolites generated by drug-metabolizing enzymes. The role of drug metabolites in cytochrome P450 (CYP) inhibition and subsequent drug-drug interactions (DDIs) have recently become a topic of considerable interest and scientific debate. The list of metabolites that were found to significantly contribute to clinically relevant DDIs is constantly being expanded and reported in the literature. New strategies have been developed for better understanding how different metabolites of a drug candidate contribute to its pharmacokinetic properties and pharmacological as well as its toxicological effects...
May 22, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28533956/toxicity-repellency-and-flushing-out-in-triatoma-infestans-hemiptera-reduviidae-exposed-to-the-repellents-deet-and-ir3535
#5
Mercedes M N Reynoso, Emilia A Seccacini, Javier A Calcagno, Eduardo N Zerba, Raúl A Alzogaray
DEET and IR3535 are insect repellents present worldwide in commercial products; their efficacy has been mainly evaluated in mosquitoes. This study compares the toxicological effects and the behavioral responses induced by both repellents on the blood-sucking bug Triatoma infestans Klug (Hemiptera: Reduviidae), one of the main vectors of Chagas disease. When applied topically, the Median Lethal Dose (72 h) for DEET was 220.8 µg/insect. Using IR3535, topical application of 500 µg/insect killed no nymphs. The minimum concentration that produced repellency was the same for both compounds: 1,15 µg/cm(2)...
2017: PeerJ
https://www.readbyqxmd.com/read/28530145/bioengineered-liposome-scaffold-composites-as-therapeutic-delivery-systems
#6
Claudia Zylberberg, Sandro Matosevic
The therapeutic potential of liposomes can be amplified when combined with biomaterial scaffolds. Such configurations overcome the convergent demands of therapies by enabling enhanced delivery, environmental responsiveness and potency. Liposomes benefit from the increased physical and mechanical strength, favorable rheological properties and natural environment conducive to improved tissue formation that scaffolds provide, while enabling biocompatible delivery of hydrophilic and lipophilic compounds that can be further functionalized to achieve targeted delivery...
June 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/28525834/exposure-to-phenols-parabens-and-uv-filters-associations-with-loss-of-function-mutations-in-the-filaggrin-gene-in-men-from-the-general-population
#7
Ulla N Joensen, Niels Jørgensen, Jacob P Thyssen, Jørgen Holm Petersen, Pal B Szecsi, Steen Stender, Anne-Maria Andersson, Niels E Skakkebæk, Hanne Frederiksen
BACKGROUND: Filaggrin is an epidermal protein that is important for normal skin barrier functions. Up to 10% of Europeans and Asians carry filaggrin gene (FLG) loss-of function mutations that appear to facilitate trans-epidermal penetration of certain chemicals. We previously showed that mutation carriers have higher internal exposure to certain phthalates, compared to controls, and hypothesized that they could have increased trans-epidermal penetration of other chemicals. OBJECTIVES: We investigated exposure to non-persistent chemicals in young Danish men with and without FLG mutations...
May 16, 2017: Environment International
https://www.readbyqxmd.com/read/28525344/morphometric-abnormalities-in-spleen-and-kidney-of-the-progeny-of-mice-fed-american-cranberry-extract-vaccinium-macrocarpon-during-pregnancy-and-lactation
#8
B J Bałan, S Lewicki, A K Siwicki, M Stelmasiak, P Skopiński, E Skopińska-Różewska, A Wasiutyński, R Zdanowski
Cranberries and cranberry-derived diet supplements are often recommended for the treatment of urinary tract infections, also during pregnancy. These products contain strongly anti-angiogenic chemical compounds which could not be indifferent to the developing fetus. In the present work we evaluated the effect of feeding pregnant and lactating mice American cranberry extract (daily dose 0.88 mg) on the morphology and some parameters of spleen and kidney function of their adult progeny. Six weeks after delivery the morphometry of spleen and kidney, cytometric analysis of spleen lymphocytes, evaluation of humoral response to SRBC (Sheep Red Blood Cells), and examination of serum creatinine/urea concentration, were performed in the offspring...
March 28, 2017: Polish Journal of Veterinary Sciences
https://www.readbyqxmd.com/read/28524727/e-cadherin-%C3%AE-catenin-complex-a-target-for-anticancer-and-antimetastasis-plants-plant-derived-compounds
#9
Majid Tafrihi, Roohollah Nakhaei Sistani
Plants reputed to have cancer-inhibiting potential and putative active components derived from those plants have emerged as an exciting new field in cancer study. Some of these compounds have cancer-inhibiting potential in different clinical staging levels, especially metastasis. A few of them which stabilize cell-cell adhesions are controversial topics. This review article introduces some effective herbal compounds that target E-cadherin/β-catenin protein complex. In this article, at first, we briefly review the structure and function of E-cadherin and β-catenin proteins, Wnt signaling pathway, and its target genes...
May 19, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28523898/case-series-study-of-the-efficacy-of-compounded-antibacterial-steroid-and-moisturizer-in-atopic-dermatitis
#10
Fatima Lakhani, Kachiu Lee, Peter A Lio
BACKGROUND/OBJECTIVES: Previous studies have demonstrated that the use of a topical antimicrobial combined with a steroid may benefit patients with atopic dermatitis (AD), but modern guidelines discourage the use of antimicrobials in treating this condition. We sought to evaluate the degree of improvement in the severity and extent of AD lesions after using a compounded antibacterial, steroid, and moisturizer (CASM). METHODS: This was a nonblinded retrospective review of patients with AD treated using CASM...
May 2017: Pediatric Dermatology
https://www.readbyqxmd.com/read/28511906/design-synthesis-and-anti-tumor-activity-study-of-novel-histone-deacetylase-inhibitors-containing-isatin-based-caps-and-o-phenylenediamine-based-zinc-binding-groups
#11
Shuai Gao, Jie Zang, Qianwen Gao, Xuewu Liang, Qinge Ding, Xiaoyang Li, Wenfang Xu, C James Chou, Yingjie Zhang
As a hot topic of epigenetic studies, histone deacetylases (HDACs) are related to lots of diseases, especially cancer. Further researches indicated that different HDAC isoforms played various roles in a wide range of tumor types. Herein a novel series of HDAC inhibitors with isatin-based caps and o-phenylenediamine-based zinc binding groups have been designed and synthesized through scaffold hopping strategy. Among these compounds, the most potent compound 9n exhibited similar if not better HDAC inhibition and antiproliferative activities against multiple tumor cell lines compared with the positive control entinostat (MS-275)...
March 19, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28511597/understanding-sleep-wake-mechanisms-and-drug-discovery
#12
Ana Clementina Equihua-Benítez, Khalil Guzmán-Vásquez, René Drucker-Colín
Although not discernible at first glance, sleep is a highly active and regulated brain state. Although we spend practically one third of our lifetimes in this stage, its importance is often taken for granted. Sleep loss can lead to disease, error and economic loss. Our understanding of how sleep is achieved has greatly advanced in recent years, and with that, the management of sleep disorders has improved. Nevertheless, there is still room for improvement and recently many new compounds have reached clinical trials with a few being approved for commercial use...
May 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28509652/risk-assessment-of-zinc-oxide-a-cosmetic-ingredient-used-as-a-uv-filter-of-sunscreens
#13
Kyu-Bong Kim, Young Woo Kim, Seong Kwang Lim, Tae Hyun Roh, Du Yeon Bang, Seul Min Choi, Duck Soo Lim, Yeon Joo Kim, Seol-Hwa Baek, Min-Kook Kim, Hyo-Seon Seo, Min-Hwa Kim, Hyung Sik Kim, Joo Young Lee, Sam Kacew, Byung-Mu Lee
Zinc oxide (ZnO), an inorganic compound that appears as a white powder, is used frequently as an ingredient in sunscreens. The aim of this review was to examine the toxicology and risk assessment of ZnO based upon available published data. Recent studies on acute, sub-acute, and chronic toxicities of ZnO indicated that this compound is virtually non-toxic in animal models. However, it was reported that ZnO nanoparticles (NP) (particle size, 40 nm) induced significant changes in anemia-related hematologic parameters and mild to moderate pancreatitis in male and female Sprague-Dawley rats at 536...
2017: Journal of Toxicology and Environmental Health. Part B, Critical Reviews
https://www.readbyqxmd.com/read/28504367/neuroprotective-natural-products-for-the-treatment-of-parkinson-s-disease-by-targeting-the-autophagy-lysosome-pathway-a-systematic-review
#14
REVIEW
Zi-Ying Wang, Jing-Yi Liu, Chuan-Bin Yang, Sandeep Malampati, Ying-Yu Huang, Mei-Xiang Li, Min Li, Ju-Xian Song
The autophagy-lysosome pathway (ALP) is a primary means by which damaged organelles and long-lived proteins are removed from cells and their components recycled. Impairment of the ALP has been found to be linked to the pathogenesis of Parkinson's disease (PD), a chronic neurodegenerative disorder characterized by the accumulation of protein aggregates and loss of dopaminergic neurons in the midbrain. In recent years, some active compounds derived from plants have been found to regulate the ALP and to exert neuroprotective effects in experimental models of PD, raising the possibility that autophagy enhancement may be an effective therapeutic strategy in PD treatment...
May 15, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28497304/acaricidal-activity-of-havardia-albicans-and-caesalpinia-gaumeri-methanolic-leaf-extracts-on-rhipicephalus-microplus-and-its-toxicity-to-laboratory-animals
#15
José A Rosado-Aguilar, Roger I Rodríguez-Vivas, Rocío Borges-Argaez, Karen A Arjona-Cambranes
The acaricidal activity of methanolic extracts from the leaves of Havardia albicans (Kunth Britton and Rose) and Caesalpinia gaumeri (Greenm) were tested on the larvae and adults of the cattle tick Rhipicephalus microplus Canestrini using the larval immersion test and the adult immersion test, respectively. The toxicity of these extracts was also evaluated on laboratory animals using toxicity bioassays at different concentrations: skin irritability (500 mg/ml), acute oral toxicity (5000 mg/kg), ocular irritability (1000 mg/ml) and dermal toxicity (5000 mg/kg)...
May 11, 2017: Experimental & Applied Acarology
https://www.readbyqxmd.com/read/28494256/designing-multi-targeted-agents-an-emerging-anticancer-drug-discovery-paradigm
#16
REVIEW
Rong-Geng Fu, Yuan Sun, Wen-Bing Sheng, Duan-Fang Liao
The dominant paradigm in drug discovery is to design ligands with maximum selectivity to act on individual drug targets. With the target-based approach, many new chemical entities have been discovered, developed, and further approved as drugs. However, there are a large number of complex diseases such as cancer that cannot be effectively treated or cured only with one medicine to modulate the biological function of a single target. As simultaneous intervention of two (or multiple) cancer progression relevant targets has shown improved therapeutic efficacy, the innovation of multi-targeted drugs has become a promising and prevailing research topic and numerous multi-targeted anticancer agents are currently at various developmental stages...
May 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28488444/targeting-of-high-valent-iron-taml-activators-at-hydrocarbons-and-beyond
#17
Terrence J Collins, Alexander D Ryabov
TAML activators of peroxides are iron(III) complexes. The ligation by four deprotonated amide nitrogens in macrocyclic motifs is the signature of TAMLs where the macrocyclic structures vary considerably. TAML activators are exceptional functional replicas of the peroxidases and cytochrome P450 oxidizing enzymes. In water, they catalyze peroxide oxidation of a broad spectrum of compounds, many of which are micropollutants, compounds that produce undesired effects at low concentrations-as with the enzymes, peroxide is typically activated with near-quantitative efficiency...
May 10, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28485929/trans-metal-trapping-meets-frustrated-lewis-pair-chemistry-ga-ch2sime3-3-induced-c-h-functionalizations
#18
Marina Uzelac, Alan R Kennedy, Eva Hevia
Merging two topical themes in main-group chemistry, namely, cooperative bimetallics and frustrated-Lewis-pair (FLP) activity, this Forum Article focuses on the cooperativity-induced outcomes observed when the tris(alkyl)gallium compound GaR3 (R = CH2SiMe3) is paired with the lithium amide LiTMP (TMP = 2,2,6,6-tetramethylpiperidide) or the sterically hindered N-heterocyclic carbene (NHC) 1,3-bis(tert-butyl)imidazol-2-ylidene (I(t)Bu). When some previously published work are drawn together with new results, unique tandem reactivities are presented that are driven by the steric mismatch between the individual reagents of these multicomponent reagents...
May 9, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28474899/liquefaction-of-biopolymers-solvent-free-liquids-and-liquid-crystals-from-nucleic-acids-and-proteins
#19
Kai Liu, Chao Ma, Robert Göstl, Lei Zhang, Andreas Herrmann
Biomacromolecules, such as nucleic acids, proteins, and virus particles, are persistent molecular entities with dimensions that exceed the range of their intermolecular forces hence undergoing degradation by thermally induced bond-scission upon heating. Consequently, for this type of molecule, the absence of a liquid phase can be regarded as a general phenomenon. However, certain advantageous properties usually associated with the liquid state of matter, such as processability, flowability, or molecular mobility, are highly sought-after features for biomacromolecules in a solvent-free environment...
May 16, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28472063/occurrence-of-urea-based-soluble-epoxide-hydrolase-inhibitors-from-the-plants-in-the-order-brassicales
#20
Seiya Kitamura, Christophe Morisseau, Todd R Harris, Bora Inceoglu, Bruce D Hammock
Recently, dibenzylurea-based potent soluble epoxide hydrolase (sEH) inhibitors were identified in Pentadiplandra brazzeana, a plant in the order Brassicales. In an effort to generalize the concept, we hypothesized that plants that produce benzyl glucosinolates and corresponding isothiocyanates also produce these dibenzylurea derivatives. Our overall aim here was to examine the occurrence of urea derivatives in Brassicales, hoping to find biologically active urea derivatives from plants. First, plants in the order Brassicales were analyzed for the presence of 1, 3-dibenzylurea (compound 1), showing that three additional plants in the order Brassicales produce the urea derivatives...
2017: PloS One
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