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https://www.readbyqxmd.com/read/28324846/novel-alk5-inhibitor-tp0427736-reduces-tgf-%C3%AE-%C3%A3-induced-growth-inhibition-in-human-outer-root-sheath-cells-and-elongates-anagen-phase-in-mouse-hair-follicles
#1
Takumi Naruse, Mari Aoki, Natsuko Fujimoto, Seiji Arase, Hajimu Oura, Yasuji Ueda, Akiko Ikeda
BACKGROUND: Androgenic alopecia (AGA) occurs as a result of the contraction of the anagen phase because of the action of androgens on hair follicles. TGF-β production from dermal papillae is enhanced by androgens, and growth inhibition of hair-follicle cells is induced by TGF-β, and the hair cycle progresses from the anagen phase to the catagen phase. We investigated both the in vitro and in vivo potency of the newly identified ALK5 inhibitor TP0427736 {6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole}...
January 25, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28324784/an-in%C3%A2-vivo-active-1-2-5-oxadiazole-pt-ii-complex-a-promising-anticancer-agent-endowed-with-stat3-inhibitory-properties
#2
Federica Porta, Giorgio Facchetti, Nicola Ferri, Arianna Gelain, Fiorella Meneghetti, Stefania Villa, Daniela Barlocco, Daniela Masciocchi, Akira Asai, Nao Miyoshi, Silvia Marchianò, Byoung-Mog Kwon, Yena Jin, Valentina Gandin, Cristina Marzano, Isabella Rimoldi
New Pt(II) complexes (Pt-1-3) bearing 1,2,5-oxadiazole ligands (1-3) were synthesized, characterized and evaluated for their ability to disrupt STAT3 dimerization. Ligand 3·HCl showed cytotoxic effects on HCT-116 cells (IC50 = 95.2 μM) and a selective ability to interact with STAT3 (IC50 = 8.2 μM) versus STAT1 (IC50 > 30 μM). Its corresponding platinum complex Pt-3 exhibited an increased cytotoxicity (IC50 = 18.4 μM) and a stronger interaction with STAT3 (IC50 = 1.4 μM), leading to inhibition of its signaling pathway...
March 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28324759/stability-and-instability-of-a-neuron-network-with-excitatory-and-inhibitory-small-world-connections
#3
Dongyuan Yu, Xu Xu, Jing Zhou, Eric Li
This study considers a delayed neural network with excitatory and inhibitory shortcuts. The global stability of the trivial equilibrium is investigated based on Lyapunov's direct method and the delay-dependent criteria are obtained. It is shown that both the excitatory and inhibitory shortcuts decrease the stability interval, but a time delay can be employed as a global stabilizer. In addition, we analyze the bounds of the eigenvalues of the adjacent matrix using matrix perturbation theory and then obtain the generalized sufficient conditions for local stability...
March 2, 2017: Neural Networks: the Official Journal of the International Neural Network Society
https://www.readbyqxmd.com/read/28324452/a-review-of-ranibizumab-for-the-treatment-of-diabetic-retinopathy
#4
REVIEW
Michael W Stewart
INTRODUCTION: Laser photocoagulation has been the standard treatment for diabetic macular edema (DME) and proliferative diabetic retinopathy (PDR) for several decades. The discovery of vascular endothelial growth factor (VEGF) and the subsequent determination of its critical role in the development DME and PDR has led to the development of VEGF inhibitory drugs. Ranibizumab was the first anti-VEGF drug approved for the treatment of both DME and diabetic retinopathy in eyes with DME. METHODS: Medline searches with the keywords "ranibizumab," "diabetic macular edema," and "proliferative diabetic retinopathy" were performed to identify pertinent pre-clinical studies and clinical trials...
March 21, 2017: Ophthalmology and Therapy
https://www.readbyqxmd.com/read/28324147/genotoxicity-kinetics-in-murine-normoblasts-as-an-approach-for-the-in-vivo-action-of-difluorodeoxycytidine
#5
Pedro Morales-Ramírez, Teresita Vallarino-Kelly, Virginia Cruz-Vallejo
PURPOSE: This study analyzed the kinetics of in vivo micronucleus induction in normoblasts by determining the kinetics of difluorodeoxycytidine (dFdC)-induced micronucleated polychromatic erythrocytes (MN-PCEs) in the peripheral blood of mice. The kinetic indexes of MN-PCE induction of dFdC were correlated with the previously reported mechanisms DNA damage induction by this compound. In general, this study aimed to establish an in vivo approach for discerning the processes underlying micronucleus induction by antineoplastic agents or mutagens in general...
March 21, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28324061/progesterone-protects-against-bpa-induced-arrhythmias-in-female-rat-cardiac-myocytes-via-rapid-signaling
#6
Jianyong Ma, Kui Hong, Hong-Sheng Wang
Bisphenol A (BPA) is an estrogenic endocrine disrupting chemical (EDC) that has a range of potential adverse health effects. Previously we showed that acute exposure to BPA promoted arrhythmias in female rat hearts through estrogen receptor rapid signaling. Progesterone (P4) and estrogen have antagonistic or complementary actions in a number of tissues and systems. In the current study, we examined the influence, and possible protective effect, of P4 on the rapid cardiac actions of BPA in female rat cardiac myocytes...
January 25, 2017: Endocrinology
https://www.readbyqxmd.com/read/28324026/gonadotropin-inhibitory-hormone-gnih-the-piscine-ortholog-of-lpxrfa-participates-in-17%C3%AE-estradiol-feedback-in-female-goldfish-reproduction
#7
Xin Qi, Wenyi Zhou, Qingqing Wang, Liang Guo, Danqi Lu, Haoran Lin
Gonadotropin-inhibitory hormone (GnIH) plays a critical role in regulating GnRH, GtH and steroidogenesis in teleosts. In the present study, we sought to determine whether E2 (17β-estradiol) acts directly on GnIH neurons to regulate reproduction in goldfish, a seasonal breeder, and we investigated the role of estrogen receptors in mediating this process. We found that GnIH neurons co-express three types of ERs. Ovariectomy and letrozole implantation into female goldfish at the vitellogenic stage elicited a significant decrease in the expression of GnIH mRNA, and E2 supplementation abolished this effect...
January 4, 2017: Endocrinology
https://www.readbyqxmd.com/read/28323879/mir-181b-regulates-vascular-stiffness-age-dependently-in-part-by-regulating-tgf-%C3%AE-signaling
#8
Daijiro Hori, Brittany Dunkerly-Eyring, Yohei Nomura, Debjit Biswas, Jochen Steppan, Jorge Henao-Mejia, Hideo Adachi, Lakshmi Santhanam, Dan E Berkowitz, Charles Steenbergen, Richard A Flavell, Samarjit Das
BACKGROUND: Endothelial dysfunction and arterial stiffening play major roles in cardiovascular diseases. The critical role for the miR-181 family in vascular inflammation has been documented. Here we tested whether the miR-181 family can influence the pathogenesis of hypertension and vascular stiffening. METHODS AND RESULTS: qPCR data showed a significant decrease in miR-181b expression in the aorta of the older mice. Eight miR-181a1/b1-/- mice and wild types (C57BL6J:WT) were followed weekly for pulse wave velocity (PWV) and blood pressure measurements...
2017: PloS One
https://www.readbyqxmd.com/read/28323870/contribution-of-sortase-srta2-to-lactobacillus-casei-bl23-inhibition-of-staphylococcus-aureus-internalization-into-bovine-mammary-epithelial-cells
#9
Renata F S Souza, Julien Jardin, Chantal Cauty, Lucie Rault, Damien S Bouchard, Luis G Bermúdez-Humarán, Philippe Langella, Vicente Monedero, Núbia Seyffert, Vasco Azevedo, Yves Le Loir, Sergine Even
Probiotics have been considered as a promising strategy to prevent various diseases in both humans and animals. This approach has gained interest in recent years as a potential means to control bovine mastitis. In a previous study, we found that several L. casei strains, including BL23, were able to inhibit the internalization of S. aureus, a major etiologic agent of mastitis, into bovine mammary epithelial cells (bMEC). This antagonism required a direct contact between L. casei and bMEC or S. aureus, suggesting the inhibition relied on interactions between L...
2017: PloS One
https://www.readbyqxmd.com/read/28323850/ligand-guided-homology-modelling-of-the-gabab2-subunit-of-the-gabab-receptor
#10
Thibaud Freyd, Dawid Warszycki, Stefan Mordalski, Andrzej J Bojarski, Ingebrigt Sylte, Mari Gabrielsen
γ-aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the central nervous system, and disturbances in the GABAergic system have been implicated in numerous neurological and neuropsychiatric diseases. The GABAB receptor is a heterodimeric class C G protein-coupled receptor (GPCR) consisting of GABAB1a/b and GABAB2 subunits. Two GABAB receptor ligand binding sites have been described, namely the orthosteric GABA binding site located in the extracellular GABAB1 Venus fly trap domain and the allosteric binding site found in the GABAB2 transmembrane domain...
2017: PloS One
https://www.readbyqxmd.com/read/28323646/endothelial-cells-and-lymphatics-at-the-interface-between-the-immune-and-central-nervous-systems-implications-for-multiple-sclerosis
#11
Céline Meyer, Guillaume Martin-Blondel, Roland S Liblau
PURPOSE OF REVIEW: The central nervous system (CNS) has a unique relationship with the immune system. This review highlights the distinct roles of lymphatic vessels and endothelial cells in the interface between CNS and immune cells and invites to revisit the concept of CNS immune privilege. RECENT FINDINGS: T cells can follow several routes to penetrate the CNS parenchyma but may also benefit, together with antigen-loaded presenting cells, from the newly described lymphatic network to exit the CNS...
March 18, 2017: Current Opinion in Neurology
https://www.readbyqxmd.com/read/28323619/fast-spiking-gaba-circuit-dynamics-in-the-auditory-cortex-predict-recovery-of-sensory-processing-following-peripheral-nerve-damage
#12
Jennifer Resnik, Daniel B Polley
Cortical neurons remap their receptive fields and rescale sensitivity to spared peripheral inputs following sensory nerve damage. To address how these plasticity processes are coordinated over the course of functional recovery, we tracked receptive field reorganization, spontaneous activity, and response gain from individual principal neurons in the adult mouse auditory cortex over a 50-day period surrounding either moderate or massive auditory nerve damage. We related the day-by-day recovery of sound processing to dynamic changes in the strength of intracortical inhibition from parvalbumin-expressing (PV) inhibitory neurons...
March 21, 2017: ELife
https://www.readbyqxmd.com/read/28323517/differences-in-adolescent-emotion-regulation-and-impulsivity-a-group-comparison-study-of-school-based-recovery-students
#13
Beth S Russell, Anne Thompson Heller, Morica Hutchison
BACKGROUND: Recovery high schools (RHS) vary in organization and operating philosophy, but are designed to support the unique needs of students struggling with substance use disorders (SUD). Previous research on youth risk taking behaviors suggests emotion regulation is a key predictor of outcomes. Specifically, the ability to respond in adaptive rather than maladaptive ways is often associated with challenges of impulsivity, poor distress tolerance, and adolescent substance use. OBJECTIVES: The current study considers data from RHS students in order to answer research questions concerning impulsivity and emotion regulation of youth working to change their risk trajectories in comparison to group of typically developing youth...
March 21, 2017: Substance Use & Misuse
https://www.readbyqxmd.com/read/28323499/antiproliferative-activity-of-egg-yolk-peptides-in-human-colon-cancer-cells
#14
Marwa N Yousr, Akram A Aloqbi, Ulfat M Omar, Nazlin K Howell
Egg yolk peptides were successfully prepared from egg yolk protein by-products after lecithin extraction. Defatted egg yolk protein was hydrolyzed with pepsin and pancreatin and purified by gel filtration to produce egg yolk gel filtration fraction (EYGF-33) with antiproliferative activity. The highlight of this study was that the peptide EYGF-33 (1.0 mg/ml) significantly inhibits cell viability of colon cancer cells (Caco-2) with no inhibitory effects on the viability of human colon epithelial normal cells (HCEC) after 48 h...
March 21, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28323438/green-tea-polyphenols-inhibit-colorectal-tumorigenesis-in-azoxymethane-treated-f344-rats
#15
Xingpei Hao, Hang Xiao, Jihyeung Ju, Mao-Jung Lee, Joshua D Lambert, Chung S Yang
In studying the cancer-preventive activities of green tea polyphenols, we previously demonstrated that dietary administration of polyphenon E (PPE) inhibited the formation of aberrant crypt foci (ACF) in the colon of azoxymethane (AOM)-treated F344 rats. Herein, we reported cancer-preventive activity of PPE using colorectal cancer as an end point. F344 rats were given two weekly injections of AOM, and then maintained on a 20% high-fat diet with or without 0.24% PPE for 34 wk. In the control group, 83% of rats developed colorectal tumors...
March 21, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28320163/inhibition-of-17-beta-estradiol-on-neuronal-excitability-via-enhancing-girk1-mediated-inwardly-rectifying-potassium-currents-and-girk1-expression
#16
Yuwen Zhang, Yian Huang, Guoxiang Wang, Xin Wang, Yun Wang
BACKGROUND: Catamenial epilepsy is a common central nervous system disease in female, which is influenced by the 17-β-estradiol (estrogen) level during the menstrual cycle. Low level (<0.05ng/ml) of estrogen normally accompanies with the perimenstrual classification of catamenial epilepsy, however, without clear mechanism. In previous studies, estrogen has been demonstrated to possess widely regulatory effects on potassium channels. Here, the effect of 17-β-estradiol on modulating inwardly rectifying K(+) (Kir) currents was investigated in cultured hippocampal neurons...
April 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28320095/dt-13-a-saponin-monomer-13-of-the-dwarf-lilyturf-tuber-synergized-with-vinorelbine-to-induce-mitotic-arrest-via-activation-of-erk-signaling-pathway-in-nci-h1299-cells
#17
Hongyang Li, Li Sun, Hang Li, Xiaodan Lv, Herve Semukunzi, Ruiming Li, Jun Yu, Shengtao Yuan, Sensen Lin
Vinorelbine (NVB) is a semi-synthetic vinca alkaloid that is approved for the clinical therapy of lung cancer. However, the clinical application of NVB was limited because of the acquisition of resistance and inacceptable toxicity. Therefore, it is of great interest to develop low-cytotoxic drugs that can synergize with NVB. DT-13, a saponin monomer 13 of the Dwarf lilyturf tuber, showed inhibitory effects on tumor metastasis and angiogenesis in the previous studies. Here, we found that DT-13 combined with NVB exhibited synergistic effect to inhibit the cell proliferation in human lung cancer NCI-H1299 cells rather than human embryonic lung fibroblasts WI-38...
March 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28319828/genistein-affects-proliferation-and-migration-of-bovine-oviductal-epithelial-cells
#18
Daniela C García, Pablo A Valdecantos, Dora C Miceli, Mariela Roldán-Olarte
Genistein is one of the most abundant isoflavones in soybean. This molecule induces cell cycle arrest and apoptosis in different normal and cancer cells. Genistein has been of considerable interest due to its adverse effects on bovine reproduction, altering estrous cycle, implantation and fetal development and producing subfertility or infertility. The objective of this work was to study the effects of genistein on the expression of selected genes involved in the regulation of cell cycle and apoptosis. Primary cultures of bovine oviductal epithelial cells (BOEC) were treated with different genistein concentrations (0...
March 8, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28319780/new-bis-hydroxymethyl-alkanoate-curcuminoid-derivatives-exhibit-activity-against-triple-negative-breast-cancer-in%C3%A2-vitro-and-in%C3%A2-vivo
#19
Min-Tsang Hsieh, Ling-Chu Chang, Hsin-Yi Hung, Hui-Yi Lin, Mei-Hui Shih, Chang-Hai Tsai, Sheng-Chu Kuo, Kuo-Hsiung Lee
Novel bis(hydroxymethyl) alkanoate curcuminoid derivatives were designed, synthesized and screened for in vitro antiproliferative and in vivo antitumor activity. Selected new compound 9a and curcumin were further evaluated for inhibitory activity against ER(+)/PR(+) breast cancer (MCF-7, T47D), HER 2(+) breast cancer (SKBR3, BT474, and MDA-MB-457) and triple negative breast cancer (TNBC) (HS-578T, MDA-MB-157, and MDA-MB-468) cell lines. In addition, compound 9a was evaluated in the MDA-MB-231 xenograft nude mice model...
March 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28319746/predicting-biphasic-responses-in-binary-mixtures-pelargonic-acid-versus-glyphosate
#20
Regina G Belz, Hans-Peter Piepho
Predicting hormesis in mixtures is challenging, but essential considering that chemical exposures often occur in mixtures and at low doses. This study investigated mixture effects with two herbicides prone to induce hormesis and to interact, namely pelargonic acid versus glyphosate. Five independent mixture experiments were conducted in vitro to assess effects on root growth of lettuce. Mixture effects on the dose were analyzed using classical joint-action models in terms of deviation from the reference model of concentration addition...
March 13, 2017: Chemosphere
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