keyword
MENU ▼
Read by QxMD icon Read
search

mechanism action

keyword
https://www.readbyqxmd.com/read/29684861/inhibition-of-gastric-cancer-by-local-anesthetic-bupivacaine-through-multiple-mechanisms-independent-of-sodium-channel-blockade
#1
Jiapeng Dan, Xiaodan Gong, Dezhan Li, Guanhua Zhu, Lishen Wang, Fang Li
BACKGROUND: Retrospective studies of patients undergoing cancer surgery suggest the use of local anesthesia may decrease tumor recurrence and improve survival. The mechanisms on the benefits of local anesthesia on cancer recurrence are complex and remain to be elucidated. METHODS: This study investigated the effects of bupivacaine on various cellular activities of gastric cancer using proliferation, migration, apoptosis assay. The underlying mechanism was analyzed focusing on mitochondrial functions and the activities of Rho family members...
April 20, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29684858/a-novel-triazine-ring-compound-md568-exerts-in-vivo-and-in-vitro-effects-on-lipid-metabolism
#2
Dan Jia, Ziwen Li, Ying Gao, Yifan Feng, Weimin Li
In this study, we investigated the toxicity and biological activity of a novel triazine ring compound named magnolol derivative 568 (MD568). The LD50 of MD568 was determined in Sprague-Dawley (SD) rats by intraperitoneal injection. Treatment of high fat diet-induced obese rats with MD568 demonstrated that MD568 displayed significant anti-obesity effects. MD568 markedly reduced body weight, blood lipid contents, white adipose tissue (WAT) and liver mass in obese rats. In addition, MD568 modulated lesions in WAT through regulating PPAR-Ɣ, C/EBP-a, SREBP-1c and FABP-4 proteins in the liver through regulating PPAR-α, SREBP-1c and FABP-4...
April 20, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29684755/impaired-tgf-%C3%AE-signaling-in-patients-with-active-systemic-lupus-erythematosus-is-associated-with-an-overexpression-of-il-22
#3
Raja Rekik, Monia Smiti Khanfir, Thara Larbi, Imen Zamali, Asma Beldi-Ferchiou, Ons Kammoun, Soumaya Marzouki, Saloua Hamzaoui, Skander Mrad, Mohamed Ridha Barbouche, Mohamed Habib Houman, Melika Ben Ahmed
The mechanisms leading to the disruption of self-tolerance in systemic lupus erythematosus (SLE) remain elusive. Herein, we aimed to decipher the molecular basis of the impaired response of mononuclear cells to TGF-β1. The Smad3-pathway was explored on CD3+ lymphocytes in either active or non active SLE patients. An impaired transcription of TGF-β1 target genes was demonstrated in the CD3+ lymphocytes of active SLE patients confirming that the defect involves T cells and pointing to its extrinsic nature. We further demonstrate that the defect did not result from an impaired TGF-βRII expression or Smad2/3 phosphorylation suggesting that the mechanism lies downstream Smad2/3 translocation...
April 20, 2018: Cytokine
https://www.readbyqxmd.com/read/29684705/dual-tail-arylsulfone-based-benzenesulfonamides-differently-match-the-hydrophobic-and-hydrophilic-halves-of-human-carbonic-anhydrases-active-sites-selective-inhibitors-for-the-tumor-associated-hca-ix-isoform
#4
Hany S Ibrahim, Heba Abdelrasheed Allam, Walaa R Mahmoud, Alessandro Bonardi, Alessio Nocentini, Paola Gratteri, Eslam S Ibrahim, Hatem A Abdel-Aziz, Claudiu T Supuran
The synthesis and characterization of two new sets of arylsulfonehydrazone benzenesulfonamides (4a-4i with phenyl tail and 4j-4q with tolyl tail) are reported. The compounds were designed according to a dual-tails approach to modulate the interactions of the ligands portions at the outer rim of both hydrophobic and hydrophilic active site halves of human isoforms of carbonic anhydrase (CA, EC 4.2.1.1). The synthesized sulfonamides were evaluated in vitro for their inhibitory activity against the following human (h) isoforms, hCA I, II, IV and IX...
April 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29684682/identification-and-validation-nucleolin-as-a-target-of-curcumol-in-nasopharyngeal-carcinoma-cells
#5
Juan Wang, Jiacai Wu, Xumei Li, Haowei Liu, Jianli Qin, Zhun Bai, Bixia Chi, Chen Xu
Identification of the specific protein target(s) of a drug is a critical step in unraveling its mechanisms of action (MOA) in many natural products. Curcumol, isolated from well known Chinese medicinal plant Curcuma zedoary, has been shown to possess multiple biological activities. It can inhibit nasopharyngeal carcinoma (NPC) proliferation and induce apoptosis, but its target protein(s) in NPC cells remains unclear. In this study, we employed a mass spectrometry-based chemical proteomics approach reveal the possible protein targets of curcumol in NPC cells...
April 20, 2018: Journal of Proteomics
https://www.readbyqxmd.com/read/29684665/anti-trypanosoma-cruzi-action-of-a-new-benzofuran-derivative-based-on-amiodarone-structure
#6
Andrea Pinto-Martinez, Vanessa Hernández-Rodríguez, Jessica Rodríguez-Durán, Elżbieta Hejchman, Gustavo Benaim
Chagas disease is a neglected tropical affection caused by the protozoan parasite Trypanosoma cruzi. There is no current effective treatment since the only two available drugs have a limited efficacy and produce side effects. Thus, investigation efforts have been directed to the identification of new drug leads. In this context, Ca2+ regulating mechanisms have been postulated as targets for antiparasitic compounds, since they present paramount differences when compared to host cells. Amiodarone is an antiarrhythmic with demonstrated trypanocidal activity acting through the disruption of the parasite intracellular Ca2+ homeostasis...
April 11, 2018: Experimental Parasitology
https://www.readbyqxmd.com/read/29684626/multi-scale-structural-design-and-biomechanics-of-the-pistol-shrimp-snapper-claw
#7
Shahrouz Amini, Maryam Tadayon, J Q Isaiah Chua, Ali Miserez
The Arthropoda, the largest phylum of the Animal Kingdom, have successfully evolved to survive various ecological constraints under a wide range of environmental conditions. Central to this survival are the structural designs developed in their exoskeletons and their raptorial appendages for protection and hunting. One such example, the pistol shrimp, is a shallow-water crustacean that is well-known for its aggressive hunting behavior, using its snapper claw to trigger the nucleation of cavitation bubbles that strike targets...
April 20, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29684590/a-synthetic-snake-venom-based-tripeptide-glu-val-trp-protects-pc12-cells-from-mpp-toxicity-by-activating-the-ngf-signaling-pathway
#8
Carolina P Bernardes, Neife A G Santos, Flavia M Sisti, Rafaela Scalco Ferreira, Norival A Santos-Filho, Adélia C O Cintra, Eduardo M Cilli, Suely V Sampaio, Antonio C Santos
Venom small peptides that target neurotrophin receptors might be beneficial in neurodegeneration, including Parkinsońs disease (PD). Their small size, ease of synthesis, structural stability and target selectivity make them important tools to overcome the limitations of endogenous neurotrophins as therapeutic agents. Additionally, they might be optimized to improve resistance to enzymatic degradation, bioavailability, potency and, mainly, lipophilicity, important to cross the blood brain barrier (BBB). Here, we evaluated the neuroprotective effects and mechanisms of the synthetic snake-venom-based peptide p-BTX-I (Glu-Val-Trp) in PC12 cells treated with MPP+ (1-methyl-4-phenylpyridinium), a dopaminergic neurotoxin that induces Parkinsonism in vivo...
April 20, 2018: Peptides
https://www.readbyqxmd.com/read/29684532/a-complicated-complex-ion-channels-voltage-sensing-cell-membranes-and-peptide-inhibitors
#9
REVIEW
Alan H Zhang, Gagan Sharma, Eivind A B Undheim, Xinying Jia, Mehdi Mobli
Voltage-gated ion channels (VGICs) are specialised ion channels that have a voltage dependent mode of action, where ion conduction, or gating, is controlled by a voltage-sensing mechanism. VGICs are critical for electrical signalling and are therefore important pharmacological targets. Among these, voltage-gated sodium channels (NaV s) have attracted particular attention as potential analgesic targets. NaV s, however, comprise several structurally similar subtypes with unique localisations and distinct functions, ranging from amplification of action potentials in nociception (e...
April 20, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29684456/radioprotective-effect-of-orally-administered-beta-d-glucan-derived-from-saccharomyces-cerevisiae
#10
Fang Liu, Zhuanzi Wang, Jia Liu, Wenjian Li
The present study was to evaluate the in vivo radioprotective effect of oral administration of Saccharomyces cerevisiae-derived-beta-d-glucan (S. cerevisiae-BG) and to investigate the protective mechanism. The results demonstrated that oral pretreatment with 350 mg/kg S. cerevisiae-BG once daily for 14 consecutive days significantly increased the survival rate of mice from 6 Gy X-rays irradiation. At the 30th day after irradiation, cellularity and the percentage of hematopoietic stem/progenitor cells in bone marrow (BM) of surviving mice were increased by S...
April 20, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29684379/effect-of-a-long-term-treatment-with-metformin-in-dystrophic-mdx-mice-a-reconsideration-of-its-potential-clinical-interest-in-duchenne-muscular-dystrophy
#11
Paola Mantuano, Francesca Sanarica, Elena Conte, Maria Grazia Morgese, Roberta Francesca Capogrosso, Anna Cozzoli, Adriano Fonzino, Angelo Quaranta, Jean-Francois Rolland, Michela De Bellis, Giulia Maria Camerino, Luigia Trabace, Annamaria De Luca
The pharmacological stimulation of AMP-activated protein kinase (AMPK) via metabolic enhancers has been proposed as potential therapeutic strategy for Duchenne muscular dystrophy (DMD). Metformin, a widely-prescribed anti-hyperglycemic drug which activates AMPK via mitochondrial respiratory chain, has been recently tested in DMD patients in synergy with nitric oxide (NO)-precursors, with encouraging results. However, preclinical data supporting the use of metformin in DMD are still poor, and its actions on skeletal muscle appear controversial...
April 20, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29684344/er-stress-attenuation-by-aloe-derived-polysaccharides-in-the-protection-of-pancreatic-%C3%AE-cells-from-free-fatty-acid-induced-lipotoxicity
#12
K S Kim, M H Chung, S Y Park, J M Cha, J H Baek, S Y Lee, S-Y Choi
Insulin resistance, a pathophysiology of type 2 diabetes, is associated with obesity. Lipotoxicity in obesity leads to the dysfunction and death of pancreatic β-cells and inadequate insulin production, thereby aggravating type 2 diabetes. The present study was conducted to determine the effect of Aloe vera polysaccharides (APs) as an anti-hyperglycemic agent and their mechanisms of action. Gel polysaccharides from Aloe extracts were separated using ultrafiltration devices with molecular weight-cutoff membranes, and the protective effect of APs on pancreatic β-cells in response to free fatty acids (FFAs) was determined...
April 20, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29684102/nitric-oxide-boosting-effects-of-the-mediterranean-diet-a-potential-mechanism-of-action
#13
Oliver M Shannon, Blossom C M Stephan, Anne-Marie Minihane, John C Mathers, Mario Siervo
No abstract text is available yet for this article.
April 19, 2018: Journals of Gerontology. Series A, Biological Sciences and Medical Sciences
https://www.readbyqxmd.com/read/29684039/development-and-validation-of-brain-target-controlled-infusion-of-propofol-in-mice
#14
Brenna P Shortal, Sarah L Reitz, Adeeti Aggarwal, Qing C Meng, Andrew R McKinstry-Wu, Max B Kelz, Alex Proekt
Mechanisms through which anesthetics disrupt neuronal activity are incompletely understood. In order to study anesthetic mechanisms in the intact brain, tight control over anesthetic pharmacology in a genetically and neurophysiologically accessible animal model is essential. Here, we developed a pharmacokinetic model that quantitatively describes propofol distribution into and elimination out of the brain. To develop the model, we used jugular venous catheters to infuse propofol in mice and measured propofol concentration in serial timed brain and blood samples using high performance liquid chromatography (HPLC)...
2018: PloS One
https://www.readbyqxmd.com/read/29684018/wuschel-related-homeobox4-acts-as-a-key-regulator-in-early-leaf-development-in-rice
#15
Yukiko Yasui, Yoshihiro Ohmori, Yumiko Takebayashi, Hitoshi Sakakibara, Hiro-Yuki Hirano
Rice (Oryza sativa) has long and narrow leaves with parallel veins, similar to other grasses. Relative to Arabidopsis thaliana which has oval-shaped leaves, our understanding of the mechanism of leaf development is insufficient in grasses. In this study, we show that OsWOX4, a member of the WUSCHEL-RELATED HOMEOBOX gene family, plays important roles in early leaf development in rice. Inducible downregulation of OsWOX4 resulted in severe defects in leaf development, such as an arrest of vascular differentiation, a partial defect in the early cell proliferation required for midrib formation, and a failure to maintain cellular activity in general parenchyma cells...
April 23, 2018: PLoS Genetics
https://www.readbyqxmd.com/read/29683647/structure-activity-relationships-of-pan-g%C3%AE-q-11-coupled-muscarinic-acetylcholine-receptor-positive-allosteric-modulators
#16
Alice Berizzi, Aaron M Bender, Craig W Lindsley, P Jeffrey Conn, Patrick M Sexton, Christopher Langmead, Arthur Christopoulos
Recent years have seen a large increase in the discovery of allosteric ligands targeting muscarinic acetylcholine receptors (mAChRs). One of the challenges in screening such compounds is to understand their mechanisms of action and define appropriate parameter estimates for affinity, cooperativity and efficacy. Herein we describe the mechanisms of action and structure-activity relationships for a series of "pan-Gq-coupled" muscarinic acetylcholine (ACh) receptor (mAChR) positive allosteric modulators (PAMs)...
April 23, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29683518/the-function-and-failure-of-sensory-predictions
#17
REVIEW
Sonia Bansal, Judith M Ford, Miriam Spering
Humans and other primates are equipped with neural mechanisms that allow them to automatically make predictions about future events, facilitating processing of expected sensations and actions. Prediction-driven control and monitoring of perceptual and motor acts are vital to normal cognitive functioning. This review provides an overview of corollary discharge mechanisms involved in predictions across sensory modalities and discusses consequences of predictive coding for cognition and behavior. Converging evidence now links impairments in corollary discharge mechanisms to neuropsychiatric symptoms such as hallucinations and delusions...
April 23, 2018: Annals of the New York Academy of Sciences
https://www.readbyqxmd.com/read/29683487/regulation-of-primary-microrna-processing
#18
REVIEW
Antoine Creugny, Aurélie Fender, Sébastien Pfeffer
MicroRNAs (miRNAs) are evolutionarily conserved small regulatory RNAs that participate in the fine-tuning of many, if not all, fundamental biological processes. Molecular mechanisms involved in miRNA biogenesis and mode of action have been elucidated in the past two decades. Similar to many cellular pathways, miRNA processing and function can be globally or specifically regulated at several levels and by numerous proteins and RNAs. Given their role as fine-tuning molecules, it is essential for miRNA expression to be tightly regulated in order to maintain cellular homeostasis...
April 23, 2018: FEBS Letters
https://www.readbyqxmd.com/read/29682831/characterization-of-dcl4-missense-alleles-provides-insights-into-its-ability-to-process-distinct-classes-of-dsrna-substrates
#19
Thomas Montavon, Yerim Kwon, Aude Zimmermann, Philippe Hammann, Timothée Vincent, Valérie Cognat, Marc Bergdoll, Fabrice Michel, Patrice Dunoyer
In the model plant Arabidopsis thaliana, four Dicer-like proteins (DCL1-4) mediate the production of various classes of small RNAs (sRNAs). Among these four proteins, DCL4 is by far the most versatile RNaseIII-like enzyme and previously identified dcl4 missense alleles were shown to uncouple the production of the various classes of DCL4-dependent sRNAs. Yet, little is known about the molecular mechanism pertaining this uncoupled production. Here, by studying the subcellular localization, interactome and binding to the sRNA precursors of three distinct dcl4 missense alleles, we simultaneously highlight the absolute requirement of a specific residue in its helicase domain for efficient production of all DCL4-dependent sRNAs, and identify, within its PAZ domain, an important determinant of DCL4 versatility that is mandatory for efficient processing of intramolecular foldback dsRNA precursors but dispensable for the production of siRNAs from RDR-dependent dsRNA susbtrates...
April 22, 2018: Plant Journal: for Cell and Molecular Biology
https://www.readbyqxmd.com/read/29682608/-hallucinations-following-acute-cannabis-dosing-a-case-report-and-comparison-to-other-hallucinogenic-drugs
#20
Frederick S Barrett, Nicolas J Schlienz, Natalie Lembeck, Muhammad Waqas, Ryan Vandrey
Introduction: Cannabis has been historically classified as a hallucinogen. However, subjective cannabis effects do not typically include hallucinogen-like effects. Empirical reports of hallucinogen-like effects produced by cannabis in controlled settings, particularly among healthy research volunteers, are rare and have mostly occurred after administration of purified Δ-9 tetrahydrocannabinol (THC) rather than whole plant cannabis. Methods: The case of a healthy 30-year-old male who experienced auditory and visual hallucinations in a controlled laboratory study after inhaling vaporized cannabis that contained 25 mg THC (case dose) is presented...
2018: Cannabis and Cannabinoid Research
keyword
keyword
109270
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"