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Inhibitory control

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https://www.readbyqxmd.com/read/29778797/discovery-of-potent-%C3%AE-glucosidase-inhibitor-flavonols-insights-into-mechanism-of-action-through-inhibition-kinetics-and-docking-simulations
#1
Didem Şöhretoğlu, Suat Sari, Burak Barut, Arzu Özel
Beside other pharmaceutical benefits, flavonoids are known for their potent α-glucosidase inhibition. In the present study, we investigated α-glucosidase inhibitory effects of structurally related 11 flavonols, among which quercetin-3-O-(3″-O-galloyl)-β-galactopyranoside (8) and quercetin 3-O-(6″-O-galloyl)-β-glucopyranoside (9) showed significant inhibition compared to the positive control, acarbose, with IC50 values of 0.97 ± 0.02 and 1.35 ± 0.06 µM, respectively. It was found that while sugar substitution to C3-OH of C ring reduced the α-glucosidase inhibitory effect, galloyl substitution to these sugar units increased it...
May 17, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29777503/anti-tmv-effects-of-amaryllidaceae-alkaloids-isolated-from-the-bulbs-of-lycoris-radiata-and-lycoricidine-derivatives
#2
Dong-Qiong Yang, Zhao-Rong Chen, Duo-Zhi Chen, Xiao-Jiang Hao, Shun-Lin Li
Fifteen known amaryllidaceae alkaloids were isolated from the bulbs of Lycoris radiata. Some of the compounds and lycoricidine derivatives had been screened for the activities against tobacco mosaic virus (TMV) by the conventional half-leaf method. Lycoricidine derivatives were also carried out the assay of effect on systemic infection of TMV by western-blot and RT-PCR analysis. The tested compounds showed moderate inactivation effect, whereas the lycoricidine derivatives showed good protective effect. The protective inhibitory activity of compounds L1 (N-methyl-2,3,4-trimethoxylycoricidine) (60...
May 18, 2018: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/29777430/the-artificial-humic-substance-hs1500-does-not-inhibit-photosynthesis-of-the-green-alga-desmodesmus-armatus-in-vivo-but-interacts-with-the-photosynthetic-apparatus-of-isolated-spinach-thylakoids-in-vitro
#3
Matthias Gilbert, Hanno Bährs, Christian E W Steinberg, Christian Wilhelm
Humic substances (HSs) can influence the growth and composition of freshwater phytoplankton assemblage. Since HSs contain many phenolic and quinonic moieties and cause growth reductions in eco-physiological field experiments, HSs are considered photosystem II herbicides. To test this specific mode of action in vivo and in vitro, respectively, we used intact cells of the green alga Desmodesmus armatus, as well as thylakoids isolated from spinach (Spinacia oleracea) as a model system for the green algal chloroplast...
May 18, 2018: Photosynthesis Research
https://www.readbyqxmd.com/read/29777099/targeting-g-protein-coupled-receptor-signaling-at-the-g-protein-level-with-a-selective-nanobody-inhibitor
#4
Sahil Gulati, Hui Jin, Ikuo Masuho, Tivadar Orban, Yuan Cai, Els Pardon, Kirill A Martemyanov, Philip D Kiser, Phoebe L Stewart, Christopher P Ford, Jan Steyaert, Krzysztof Palczewski
G protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by mediating a GDP to GTP exchange in the Gα subunit. This leads to dissociation of the heterotrimer into Gα-GTP and Gβγ dimer. The Gα-GTP and Gβγ dimer each regulate a variety of downstream pathways to control various aspects of human physiology. Dysregulated Gβγ-signaling is a central element of various neurological and cancer-related anomalies. However, Gβγ also serves as a negative regulator of Gα that is essential for G protein inactivation, and thus has the potential for numerous side effects when targeted therapeutically...
May 18, 2018: Nature Communications
https://www.readbyqxmd.com/read/29776929/antibacterial-effects-of-phage-lysin-lysgh15-on-planktonic-cells-and-biofilms-of-diverse-staphylococci
#5
Yufeng Zhang, Mengjun Cheng, Hao Zhang, Jiaxin Dai, Zhimin Guo, Xinwei Li, Yalu Ji, Ruopeng Cai, Hengyu Xi, Xinwu Wang, Yibing Xue, Changjiang Sun, Xin Feng, Liancheng Lei, Wenyu Han, Jingmin Gu
Treatment of infections caused by staphylococci has become more difficult because of the emergence of multidrug-resistant strains as well as biofilm formation. In this study, we observed the ability of the phage lysin LysGH15 to eliminate staphylococcal planktonic cells and biofilms formed by Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus and Staphylococcus hominis All these strains were sensitive to LysGH15, showing reductions in bacterial counts of approximately 4 log units within 30 min after treatment with 20 μg/mL LysGH15, and the minimum inhibitory concentrations (MICs) ranged from 8 μg/mL to 32 μg/mL...
May 18, 2018: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/29776859/increased-short-interval-intracortical-inhibition-in-un-medicated-patients-with-schizophrenia
#6
Martin Schecklmann, Carmen Weidler, Peter Eichhammer, Göran Hajak, Berthold Langguth
BACKGROUND: Schizophrenia is associated with changes in inhibitory and facilitatory brain networks which can be assessed by motor cortex excitability. OBJECTIVE: Here, we investigate differences between large cross-sectional samples of un-medicated and medicated patients with schizophrenia and healthy controls in single- and double-pulse transcranial magnetic stimulation parameters. METHODS: We measured right abductor digiti minimi muscle activity in 71 un-medicated, 43 medicated patients and 131 healthy controls...
May 4, 2018: Brain Stimulation
https://www.readbyqxmd.com/read/29775935/design-synthesis-antiproliferative-activity-and-docking-studies-of-quinazoline-derivatives-bearing-2-3-dihydro-indole-or-1-2-3-4-tetrahydroquinoline-as-potential-egfr-inhibitors
#7
Yiqiang OuYang, Wensheng Zou, Liang Peng, Zunhua Yang, Qidong Tang, Mengzi Chen, Shuang Jia, Hong Zhang, Zhou Lan, Pengwu Zheng, Wufu Zhu
Eight series of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline were designed, synthesized and evaluated for the IC50 values against three cancer cell lines (A549, MCF-7 and PC-3). Most of the forty nine target compounds showed excellent antiproliferative activity against one or several cancer cell lines. The compound 13a showed the best activity against A549, MCF-7 and PC-3 cancer cell lines, with the IC50 values of 1.09 ± 0.04 μM, 1.34 ± 0.13 μM and 1.23 ± 0...
May 9, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29775695/pulsatilla-decoction-inhibits-candida-albicans-proliferation-and-adhesion-in-a-mouse-model-of-vulvovaginal-candidiasis-via-the-dectin-1-signaling-pathway
#8
Lilin Yang, Haiwang Wu, Weiyu Qiu, Longyi Guo, Xin Du, Qingying Yu, Jie Gao, Songping Luo
ETHNOPHARMACOLOGICAL RELEVANCE: Pulsatilla decoction (PD) is a classical prescription in Traditional Chinese Medicine (TCM) and has been reported to have inhibitory effects on Candida albicans proliferation. STUDY AIM: To investigate the therapeutic effects of PD in the treatment of Vulvovaginal candidiasis (VVC) and elucidate the potential mechanism. MATERIALS AND METHODS: Female BALB/c mice (N=90) were randomized to six treatment groups, including the Control group, Model group, three PD groups and Fluconazole group which served as a positive control (20mg/kg weekly)...
May 15, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29774435/neophobia-does-not-account-for-motoric-self-regulation-performance-as-measured-during-the-detour-reaching-cylinder-task
#9
M K Stow, A Vernouillet, D M Kelly
The ability to restrain a prepotent response in favor of a more adaptive behavior, or to exert inhibitory control, has been used as a measure of a species' cognitive abilities. Inhibitory control defines a spectrum of behaviors varying in complexity, ranging from self-control to motoric self-regulation. Several factors underlying inhibitory control have been identified, however, the influence of neophobia (i.e., aversion to novelty) on inhibitory control has not received much attention. Neophobia is known to affect complex cognitive abilities, but whether neophobia also influences more basic cognitive abilities, such as motoric self-regulation, has received less attention...
May 17, 2018: Animal Cognition
https://www.readbyqxmd.com/read/29774337/fermentation-alters-the-bioaccessible-phenolic-compounds-and-increases-the-alpha-glucosidase-inhibitory-effects-of-aronia-juice-in-a-dairy-matrix-following-in-vitro-digestion
#10
Xue Du, Angela D Myracle
The prevalence of diabetes reached 415 million worldwide in 2015. Polyphenol-rich food intake can benefit the glycemic control for individuals with diabetes. Fermentation may increase the bioavailability of polyphenols, which is generally low. Aronia (Aronia melanocarpa) is a polyphenol-rich berry that is native to North America. Proanthocyanins and anthocyanins are the major phenolic compounds in aronia. In this study, aronia kefir was made by fermenting cow's milk with added aronia juice. The changes in bioaccessible polyphenols of aronia kefir during digestion were assessed using an in vitro model...
May 18, 2018: Food & Function
https://www.readbyqxmd.com/read/29774109/sik2-attenuates-proliferation-and-survival-of-breast-cancer-cells-with-simultaneous-perturbation-of-mapk-and-pi3k-akt-pathways
#11
Neslihan Zohrap, Özge Saatci, Burcak Ozes, Ipek Coban, Hasan Murat Atay, Esra Battaloglu, Özgür Şahin, Kuyas Bugra
Salt Inducible Kinase2 (SIK2) has been shown to contribute to tumorigenesis in multiple tumor types in a dichotomous manner. However, little is known about its contribution to breast malignancies. Here, we report SIK2 as a potential tumor suppressor in breast cancer whose expression was reduced in tumor tissues and breast cancer cell lines compared to normal counterparts. In vitro loss- and gain-of-function experiments combined with xenograft studies demonstrated that SIK2-mediated attenuation of proliferation and survival of breast cancer cells with parallel inhibition of both Ras/Erk and PI3K/Akt pathways...
April 24, 2018: Oncotarget
https://www.readbyqxmd.com/read/29773923/brain-activity-low-self-control-and-delinquency-an-fmri-study-of-at-risk-adolescents
#12
Ryan Charles Meldrum, Elisa M Trucco, Lora M Cope, Robert A Zucker, Mary M Heitzeg
Purpose: A vast literature finds that low self-control is associated with a myriad of antisocial behaviors. Consequently, increasing attention has focused on the causes of low self-control. While criminologists have directed significant attention to studying its social causes, fewer studies have considered its neural bases. Methods: We add to this nascent body of research by using data collected on an at-risk sample of adolescents participating in the ongoing Michigan Longitudinal Study...
May 2018: Journal of Criminal Justice
https://www.readbyqxmd.com/read/29773680/macrophage-migration-inhibitory-factor-794-catt-microsatellite-polymorphism-and-risk-of-tuberculosis-a-meta-analysis
#13
Mingbiao Ma, Lvyan Tao, Aihua Liu, Zhang Liang, Jiaru Yang, Yun Peng, Xiting Dai, Ruolan Bai, Zhenhua Ji, Miaomiao Jian, Fukai Bao
Tuberculosis (TB) is a chronic infectious disease that has been threatening public health for many years. Several studies have shown the relationship between the macrophage migration inhibitory factor-794CATT ( MIF-794CATT ) microsatellite polymorphism and susceptibility of tuberculosis ( TB ). However, the results remain inconclusive. Therefore, we aim to find out the impact of MIF-794 CATT microsatellite polymorphism on risk of TB by a comprehensive meta-analysis. We conducted a systematic study search in PubMed,Embase, the Cochrane Library, and the China National Knowledge Infrastructure ( CNKI ) up to October, 2017...
May 17, 2018: Bioscience Reports
https://www.readbyqxmd.com/read/29773202/impaired-short-term-plasticity-in-restless-legs-syndrome-a-pilot-rtms-study
#14
Giuseppe Lanza, Bartolo Lanuzza, Debora Aricò, Mariagiovanna Cantone, Filomena Irene Ilaria Cosentino, Rita Bella, Giovanni Pennisi, Raffaele Ferri, Manuela Pennisi
BACKGROUND: Previous studies showed an impairment of the LTP-like plasticity to TMS in restless legs syndrome (RLS). Clinically, repetitive TMS (rTMS) was effective in alleviating the sensory-motor complaints of patients, although the effects induced by low-frequency (inhibitory) rTMS have not yet been investigated. An impaired LTD-like mechanism of cortical plasticity has been hypothesized, which we have directly assessed in this pilot study. METHODS: Motor evoked potentials (MEPs) from the right first dorsal interosseus muscle were recorded at the stimulus intensity of 110% of the resting motor threshold (rMT) from 13 right-handed patients and ten age-matched right-handed healthy controls...
June 2018: Sleep Medicine
https://www.readbyqxmd.com/read/29773098/-polydatin-inhibits-cell-proliferation-and-expressions-of-inflammatory-cytokines-in-thp-1-cells-induced-by-ox-ldl-via-up-regulating-sirt1
#15
Yi Ma, Yunjun Ruan, Yuyan Wang, Saizhu Wu
Objective To investigate the effects of polydatin on cell proliferation and cytokine expression in THP-1 monocyte-derived macrophages (MDMs) induced by oxidized low-density lipoprotein (ox-LDL), and the possible mechanisms. Methods MDMs were divided into the control group (only treated with ordinary culture medium), ox-LDL group (treated wtih 80 μmol/L ox-LDL for 24 hours), polydatin treatment group (treated with 100 μmol/L polydatin for 2 hours prior to the treatment with 80 μmol/L ox-LDL for 24 hours) and EX-527 treatment group (treated with 10 μmol/L SIRT1 inhibitor EX-527 for 2 hours prior to the treatment with ox-LDL and polydatin)...
March 2018: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
https://www.readbyqxmd.com/read/29772445/the-protective-role-of-all-transretinoic-acid-atra-against-colorectal-cancer-development-is-achieved-via-increasing-mir-3666-expression-and-decreasing-e2f7-expression
#16
Weihong Liu, Yanqiu Song, Chenggui Zhang, Pengfei Gao, Bisheng Huang, Jianfang Yang
OBJECTIVE: Colorectal cancer (CRC) is one of the most common malignancies with high morbidity and mortality rates worldwide. This study aimed to investigate whether miR-3666 was involved in inhibitory effects of all-transretinoic acid (ATRA) on the development of colorectal cancer (CRC). MATERIAL AND METHODS: Surgical specimens of CRC tissues and adjacent non-tumor mucosa were collected for determining miR-3666 expression. Human CRC HCT116 cells were treated with different doses of ATRA (10, 20, 40, and 60 μM, respectively) and/or transfected with miR-3666 mimic, miR-3666 inhibitor, E2F7 siRNAs or their controls, respectively...
May 14, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29772392/effects-of-task-repetition-but-no-transfer-of-inhibitory-control-training-in-healthy-adults
#17
Tobias Talanow, Ulrich Ettinger
Executive functions (EFs) comprise the updating, shifting and inhibition dimensions. According to the Unity and Diversity Model, the inhibition dimension is fully accounted for by a general EFs factor. This suggests that training of inhibition should transfer, in part, to updating and shifting. Therefore, we tested the effectiveness of a three-week inhibition training (high-conflict Stroop task) and explored near transfer effects to an untrained inhibition task (antisaccade task) and far transfer effects to untrained tasks demanding task-set shifting (number-letter-task), working memory updating (n-back task) and planning abilities (Stockings of Cambridge task)...
May 14, 2018: Acta Psychologica
https://www.readbyqxmd.com/read/29772243/synthesis-pharmacological-evaluation-and-docking-studies-of-progesterone-and-testosterone-derivatives-as-anticancer-agents
#18
Muafia Jabeen, Muhammad Iqbal Choudhry, Ghulam Abbas Miana, Khondaker Miraz Rahman, Umer Rashid, Hidayat-Ullah Khan, Arshia, Abdul Sadiq
Steroidal hormones progesterone and testosterone play a vital role in breast and prostate cancers. In this research, we have synthesized and characterized a total of thirty-one (31) new nitrogenous derivatives of progesterone and testosterone. The synthesized derivatives (1-31) were screened for their anti-cancer potential against MCF-7 and PC-3 cell lines of breast using MTT assay. The compounds 1-31exhibited significant inhibitory potentials against MCF-7 and PC-3 cell lines. In MCF-7 assay, compound 17 displayed IC50 value of 04 ±0...
May 14, 2018: Steroids
https://www.readbyqxmd.com/read/29771946/in-vitro-comparison-of-three-common-essential-oils-mosquito-repellents-as-inhibitors-of-the-ross-river-virus
#19
Miora Ralambondrainy, Essia Belarbi, Wildriss Viranaicken, Renata Baranauskienė, Petras Rimantas Venskutonis, Philippe Desprès, Pierre Roques, Chaker El Kalamouni, Jimmy Sélambarom
BACKGROUND: The essential oils of Cymbopogon citratus (CC), Pelargonium graveolens (PG) and Vetiveria zizanioides (VZ) are commonly used topically to prevent mosquito bites and thus the risk of infection by their vectored pathogens such as arboviruses. However, since mosquito bites are not fully prevented, the effect of these products on the level of viral infection remains unknown. OBJECTIVES: To evaluate in vitro the essentials oils from Reunion Island against one archetypal arbovirus, the Ross River virus (RRV), and investigate the viral cycle step that was impaired by these oils...
2018: PloS One
https://www.readbyqxmd.com/read/29771527/protoilludane-illudalane-and-botryane-sesquiterpenoids-from-the-endophytic-fungus-phomopsis-sp-tj507a
#20
Shuangshuang Xie, Ye Wu, Yuben Qiao, Yi Guo, Jianping Wang, Zhengxi Hu, Qing Zhang, Xiaonian Li, Jinfeng Huang, Qun Zhou, Zengwei Luo, Junjun Liu, Hucheng Zhu, Yongbo Xue, Yonghui Zhang
To explore the chemical diversity of metabolites from endophytic fungi, the strain Phomopsis sp. TJ507A, isolated from the medicinal plant Phyllanthus glaucus, was investigated. A 2,3- seco-protoilludane-type sesquiterpenoid (1), eight protoilludane-type sesquiterpenoids (2-9), four illudalane-type sesquiterpenoids (10a/10b, 11, and 12), and a botryane-type sesquiterpenoid (13) in addition to seven known sesquiterpenoids (14-20) were identified from the liquid culture of the fungus. Structures of the isolated compounds, including their absolute configurations, were elucidated based on extensive spectroscopic analyses, a modified Mosher analysis, electronic circular dichroism (ECD) calculations, and [Rh2 (OCOCF3 )4 ]-induced ECD spectra as well as X-ray crystallographic analyses...
May 17, 2018: Journal of Natural Products
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