2,519 results match your criteria inhibition 182


Exploring biologically active hybrid pharmacophore N-substituted hydrazine-carbothioamides for urease inhibition: In vitro and in silico approach.

Int J Biol Macromol 2021 Apr 9;182:534-544. Epub 2021 Apr 9.

Institute of Chemical Sciences, Bahauddin Zakariya University, Multan 60800, Pakistan. Electronic address:

Urease is potential target for various human's health complications, such as peptic ulcer, gastric cancer and kidney stone formation. The present study was based on synthesis of new hybrid pharmacophore N-substituted hydrazine-carbothioamides as potential urease inhibitors. Presented method gave excellent yield in range of 85-95% for hydrazine-carbothioamides derivatives (3a-s) after reaction of mono- and disubstituted hydrazides (1a-k) and substituted isothiocyanates (2a-d). Read More

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Antibacterial potency, cell viability and morphological implications of copper oxide nanoparticles encapsulated into cellulose acetate nanofibrous scaffolds.

Int J Biol Macromol 2021 Apr 7;182:464-471. Epub 2021 Apr 7.

Department of Chemistry, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. Electronic address:

It is generally believed that the most challenging impediment for the utilization of cellulose acetate (CA) in the medical field is its hydrophobicity and disability to poison the harmful microbes. Therefore, in this contribution, we aimed to prepare an environmentally scaffold-based CA loaded with copper nanoparticles (CuONPs), which are expected to not only improve the hydrophilicity of the prepared nanofibers, but also have an effective ability to kill such harmful and infectious microbes that are abundant in wounds. The obtained results attested that the generated nanofibers became thicker with increasing the content of CuONPs in CA nanofibers. Read More

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Preparation of TiO/cellulose nanocomposites as antibacterial bio-adsorbents for effective phosphate removal from aqueous medium.

Int J Biol Macromol 2021 Apr 7;182:434-444. Epub 2021 Apr 7.

Centre for Future Materials, University of Southern Queensland, Springfield 4300, Australia.

The design of environmentally benign bio-adsorbents for the removal of phosphate from aqueous medium was an economic and effective way for controlling eutrophication. Herein, we prepared three kinds of TiO/cellulose (CE-Ti) nanocomposites by a facile hydrolysis-precipitation method, and used them as antibacterial bio-adsorbents for the removal of phosphate from aqueous medium. Multiple techniques including Fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS), scanning electron microscope (SEM), transmission electron microscopy (TEM), X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) and thermogravimetric analysis (TGA) were employed to characterize the nanostructure and characteristics of the prepared CE-Ti nanocomposite. Read More

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The characterization of optimal selenized garlic polysaccharides and its immune and antioxidant activity in chickens.

Int J Biol Macromol 2021 Apr 5;182:136-143. Epub 2021 Apr 5.

School of Veterinary Medicine, Yangzhou University, Yangzhou 225009, PR China; Jiangsu Co-innovation Center for Prevention and Control of Important Animal Infectious Diseases and Zoonoses, Yangzhou 225009, PR China; Joint International Research Laboratory of Agriculture and Agri-Product Safety, the Ministry of Education of China, Yangzhou University, Yangzhou, Jiangsu 225009, PR China. Electronic address:

The purpose of this study was to optimize modification conditions of selenized garlic polysaccharides (sGPS) and investigate its structural characterization, immune and antioxidant activities. Herein, selenized garlic polysaccharides (sGPS) were prepared using by HNO-NaSeO selenylation method. And then modification conditions of sGPS were optimized through L (3) orthogonal test. Read More

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Melatonin regulates the cross-talk between autophagy and apoptosis by SIRT3 in testicular Leydig cells.

Biochem Biophys Res Commun 2021 Apr 3;555:182-189. Epub 2021 Apr 3.

Reproductive Medicine Center, Zhongnan Hospital of Wuhan University, Wuhan, 430071, Hubei, PR China; Clinical Medicine Research Center of Prenatal Diagnosis and Birth Health in Hubei Province, Wuhan, 430071, Hubei, PR China. Electronic address:

Autophagy and apoptosis, as major modes of cell death, play critical roles in cellular homeostasis. Our previous study demonstrated that the cross-talk between autophagy and apoptosis regulated cadmium-induced testicular injury and self-recovery, influencing male fertility. However, the underlying mechanism remains blurry. Read More

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Structural and kinetic characterization of glutaminyl cyclase.

Biol Chem 2021 Apr 7. Epub 2021 Apr 7.

Department of Biological Sciences, School of Science, Xi'an Jiaotong-Liverpool University, Suzhou, Jiangsu215123, China.

is a bacterial species known to be involved in the pathogenesis of chronic periodontitis, that more recently has been as well associated with Alzheimer's disease. expresses a glutaminyl cyclase (PgQC) whose human ortholog is known to participate in the beta amyloid peptide metabolism. We have elucidated the crystal structure of PgQC at 1. Read More

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Estradiol-induced inhibition of endoplasmic reticulum stress normalizes splenic CD4 + T lymphocytes following hemorrhagic shock.

Sci Rep 2021 Apr 5;11(1):7508. Epub 2021 Apr 5.

Institute of Microcirculation, Hebei North University, Diamond South Road 11, Zhangjiakou, Hebei, 075000, People's Republic of China.

The aim is to investigate that 17β-estradiol (E2)/estrogen receptors (ERs) activation normalizes splenic CD4 + T lymphocytes proliferation and cytokine production through inhibition of endoplasmic reticulum stress (ERS) following hemorrhage. The results showed that hemorrhagic shock (hemorrhage through femoral artery, 38-42 mmHg for 90 min followed by resuscitation of 30 min and subsequent observation period of 180 min) decreased the CD4 T lymphocytes proliferation and cytokine production after isolation and incubation with Concanavalin A (5 μg/mL) for 48 h, induced the splenic injury with evidences of missed contours of the white pulp, irregular cellular structure, and typical inflammatory cell infiltration, upregulated the expressions of ERS biomarkers 78 kDa glucose-regulated protein (GRP78) and activating transcription factor 6 (ATF6). Either E2, ER-α agonist propyl pyrazole triol (PPT) or ERS inhibitor 4-Phenylbutyric acid administration normalized these parameters, while ER-β agonist diarylpropionitrile administration had no effect. Read More

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Investigations of Olive Oil Industry By-Products Extracts with Potential Skin Benefits in Topical Formulations.

Pharmaceutics 2021 Mar 30;13(4). Epub 2021 Mar 30.

Research Institute for Medicine (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisbon, Portugal.

The by-products of olive oil industry are a major ecological issue due to their phenolic content, highly toxic organic load, and low pH. However, they can be recovered and reused, since their components have antioxidant, anti-inflammatory, and photoprotector properties. In this work, oil-in-water creams containing three different olive oil industry by-products extracts were produced without the use of organic solvents. Read More

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Antioxidant activity of calycosin against α-synuclein amyloid fibrils-induced oxidative stress in neural-like cells as a model of preventive care studies in Parkinson's disease.

Int J Biol Macromol 2021 Mar 30;182:91-97. Epub 2021 Mar 30.

Department of Cerebrovascular Diseases, The Second Affiliated Hospital of Zhengzhou University, Zhengzhou, China. Electronic address:

Protein misfolding and aggregation result in induction of a number of neurodegenerative diseases. In the present study, the anti-fibrillation activity of calycosin and its influence on the amyloid formation of α-synuclein (α-syn) and associated cytotoxicity on neuron-like cells (PC-12) as a model of Parkinson's disease were explored. Therefore, in combination with ThT and ANS fluorescence assay, CD, Congo red absorbance, TEM and cytotoxicity assays (MTT, ROS, SOD activity, CAT activity, GSH content, and caspase-3 activity assays), we showed that calycosin remarkably inhibits α-syn fibril formation through a concentration-dependent manner. Read More

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A comprehensive review on oncogenic miRNAs in breast cancer.

J Genet 2021 ;100

Department of Fetomaternal, Faculty of Medicine, Shariati Hospital, Tehran University of Medical Sciences, Tehran 14155-6559, Iran.

A growing body of evidence demonstrates that the oncogenic miRNAs are critical components that are involved in breast cancer (BC) progression. Thus, they are attracting a great deal of consideration as they provide opportunities for the novel avenues for developing BC targeted therapy. In the current review, we try to discuss the key oncogenic miRNAs implicated in cell migration, invasion and metastasis (e. Read More

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January 2021

miR-182-5p and miR-96-5p Target and Mediate the Negative Feedback Regulatory Loop between PIAS1 and STAT3 in Endometrial Cancer.

DNA Cell Biol 2021 Apr 22;40(4):618-628. Epub 2021 Mar 22.

Department of Obstetrics and Gynecology, The Second Xiangya Hospital, Central South University, Changsha, China.

The expressions and roles of protein inhibitor of activated STAT (PIAS) proteins, a group of proteins with STAT inhibition and SUMOylation E3 ligase activity, are rarely revealed in endometrial cancer (EC). In this study, we analyzed the expressions of PIASs and their relationships with clinical features by mining online data through web servers, including UALCAN and Gene Expression Profiling Interactive Analysis (GEPIA) in EC. The expressions of PIASs in EC tissues were further validated by immunohistochemistry (IHC). Read More

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SNHG15 facilitated malignant behaviors of oral squamous cell carcinoma through targeting miR-188-5p/DAAM1.

J Oral Pathol Med 2021 Mar 20. Epub 2021 Mar 20.

Department of Stomatology, First People's Hospital of Lianyungang, Lianyungang, Jiangsu, China.

Background: Long non-coding RNA (lncRNA) small nucleolar RNA host gene 15 (SNHG15) has been discovered and demonstrated to have significant function in multiple cancers. Nevertheless, how it participates in the progression of oral squamous cell carcinoma (OSCC) and its potential regulatory system are still unclear.

Methods: RT-qPCR detected the expression of SNHG15, miR-188-5p, and DAAM1. Read More

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Mitochondrial DNA enables AIM2 inflammasome activation and hepatocyte pyroptosis in non-alcoholic fatty liver disease.

Am J Physiol Gastrointest Liver Physiol 2021 Mar 17. Epub 2021 Mar 17.

Department of Oncology, Xuzhou City Cancer Hospital, China.

Nonalcoholic fatty liver disease (NAFLD) is typified by accumulating excess liver triacylglycerol, inflammation, and liver dysfunction. This study was aimed to investigate the role of mitochondrial DNA synthesis-induced activation of Absent in melanoma 2 (AIM2) inflammasome and pyroptosis in NAFLD. Mice were raised on a high-fat diet for 24 weeks to establish NAFLD models. Read More

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Myricetin exhibits anti-glioma potential by inducing mitochondrial-mediated apoptosis, cell cycle arrest, inhibition of cell migration and ROS generation.

J BUON 2021 Jan-Feb;26(1):295

Department of Neurosurgery, LiShui People Hospital, LiShui, Zhejiang 323000, P.R.China.

The Editors of JBUON issue an Expression of Concern to 'Myricetin exhibits anti-glioma potential by inducing mitochondrial-mediated apoptosis, cell cycle arrest, inhibition of cell migration and ROS generation', by Hu-Guang Li, Jun-Xia Chen, Jun-Hui Xiong, Jin-Wei Zhu, JBUON 2016;21(1):182-190; PMID:27061547. Following the publication of the above article, readers drew to our attention that part of the data was possibly unreliable. We sent emails to the authors with a request to provide the raw data to prove the originality, but received no reply. Read More

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MicroRNA-182 inhibits osteogenic differentiation of bone marrow mesenchymal stem cells by targeting Smad1.

J Biol Regul Homeost Agents 2021 Mar 11;35(2). Epub 2021 Mar 11.

Department of Orthopaedics, Yongjia People's Hospital, Wenzhou, China.

The present study aimed to screen abnormally expressed microRNAs (miRs/miRNAs) in patients with postmenopausal osteoporosis (POP) and explore their mechanisms via functional verification. Bone marrow mesenchymal stem cells (BMSCs) were extracted from healthy controls and patients with POP. Differences in osteogenic differentiation and proliferation of human BMSCs were compared between the two groups using Cell Counting Kit-8 (CCK-8) assay and alizarin red staining. Read More

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Long-Term Dipeptidyl Peptidase 4 Inhibition Worsens Hypertension and Renal and Cardiac Abnormalities in Obese Spontaneously Hypertensive Heart Failure Rats.

J Am Heart Assoc 2021 Mar 8;10(6):e020088. Epub 2021 Mar 8.

Department of Pharmacology and Chemical Biology University of Pittsburgh School of Medicine Pittsburgh PA.

Background The long-term effects of dipeptidyl peptidase 4 (DPP4) inhibitors on blood pressure and cardiovascular and renal health remain controversial. Herein, we investigated the extended (>182 days) effects of DPP4 inhibition in a model of spontaneous hypertension, heart failure, diabetes mellitus, obesity and hyperlipidemia. Methods and Results Adult obese spontaneously hypertensive heart failure rats (SHHF) were implanted with radio transmitters for measurement of arterial blood pressures. Read More

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Genome sequence analysis and bioactivity profiling of marine-derived actinobacteria, Brevibacterium luteolum, and Cellulosimicrobium funkei.

Arch Microbiol 2021 Mar 7. Epub 2021 Mar 7.

Microbiology and Biotechnology Research Lab, Department of Biotechnology, Fatima Jinnah Women University, Rawalpindi, 46000, Pakistan.

Genome analysis gives important insights into the biosynthetic potential of marine actinobacteria. The genomes of two marine actinomycetes Brevibacterium luteolum MOSEL-ME10a and Cellulosimicrobium funkei MOSEL-ME6 were sequenced to identify the biosynthetic gene clusters (BGCs). Additionally, anti-proliferative, antioxidant, and enzyme inhibitory activities were studied in vitro. Read More

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SIRT1 alleviates hepatic ischemia-reperfusion injury via the miR-182-mediated XBP1/NLRP3 pathway.

Mol Ther Nucleic Acids 2021 Mar 26;23:1066-1077. Epub 2020 Nov 26.

Department of Hepatic Surgery (II), Eastern Hepatobiliary Surgery Hospital, Naval Medical University (Second Military Medical University), Shanghai 200438, P.R. China.

The hepatoprotection of histone deacetylase sirtuin 1 (SIRT1) has been identified to attenuate ischemia-reperfusion (IR)-triggered inflammation and liver damage. This study was performed to characterize the function of SIRT1 in hepatic IR injury. In assays on liver-specific knockout mice of SIRT1, we first validated the effect of SIRT1 knockout on liver damage and XBP1/NLRP3 inflammasome activation. Read More

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Microstructural, mechanical, in vitro corrosion and biological characterization of an extruded Zn-0.8Mg-0.2Sr (wt%) as an absorbable material.

Mater Sci Eng C Mater Biol Appl 2021 Mar 30;122:111924. Epub 2021 Jan 30.

Section Medical Materials Science and Technology, University Hospital Tübingen, Osianderstrasse 2-8, Tübingen 72076, Germany. Electronic address:

Zinc (Zn) alloys seem to be promising candidates for application in orthopaedic or cardiovascular medical implants. In this area, high standards are required regarding the biocompatibility as well as excellent mechanical and tailored degradation properties. In the presented study, a novel Zn-0. Read More

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Inhibition of thrombin activity by a covalent-binding aptamer and reversal by the complementary strand antidote.

Chem Commun (Camb) 2021 Mar 24;57(20):2483-2486. Epub 2021 Feb 24.

Department of Engineering Science, Bioscience and Technology Program, The Graduate School of Informatics and Engineering, The University of Electro-Communications (UEC), 1-5-1 Chofugaoka, Chofu, Tokyo 182-8585, Japan.

Alleviating the potential risk of irreversible adverse drug effects has been an important and challenging issue for the development of covalent drugs. Here we created a DNA-aptamer-type covalent drug by introducing a sulfonyl fluoride warhead at appropriate positions of the thrombin binding aptamer to create weaponized covalent drugs. We showed the de-activation of thrombin by the novel modality, followed by its re-activation by the complementary strand antidote at an arbitrary time. Read More

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Activation of G-protein coupled estradiol receptor 1 in the dorsolateral striatum attenuates preference for cocaine and saccharin in male but not female rats.

Horm Behav 2021 Apr 19;130:104949. Epub 2021 Feb 19.

Psychology Department, University of Michigan, Ann Arbor, MI, 48109, USA; Michigan Neuroscience Institute, University of Michigan, Ann Arbor, MI, 48109, USA. Electronic address:

There are sex differences in the response to psychomotor stimulants, where females exhibit a greater response than males, due to the presence of the gonadal hormone estradiol (E2). Extensive research has shown that E2 enhances drug-seeking and the rewarding properties of cocaine for females. The role of E2 in male drug-seeking, however, is not well understood. Read More

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Immune-related Gene Expression Predicts Response to Neoadjuvant Chemotherapy but not Additional Benefit from PD-L1 Inhibition in Women with Early Triple-negative Breast Cancer.

Clin Cancer Res 2021 Feb 16. Epub 2021 Feb 16.

Department of Pathology, Philipps-University Marburg and University Hospital Marburg (UKGM), Marburg, Germany.

Purpose: We evaluated mRNA signatures to predict response to neoadjuvant PD-L1 inhibition in combination with chemotherapy in early triple-negative breast cancer.

Experimental Design: Targeted mRNA sequencing of 2,559 transcripts was performed in formalin-fixed, paraffin-embedded samples from 162 patients of the GeparNuevo trial. We focused on validation of four predefined gene signatures and differential gene expression analyses for new predictive markers. Read More

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February 2021

Development of portable CdS QDs screen-printed carbon electrode platform for electrochemiluminescence measurements and bioanalytical applications.

Talanta 2021 Apr 17;225:122029. Epub 2020 Dec 17.

Center for Cooperative Research in Biomaterials (CIC BiomaGUNE), Basque Research and Technology Alliance (BRTA), Paseo de Miramon 182, 20014, Donostia San Sebastián, Spain. Electronic address:

In this work, a portable and disposable screen-printed electrode-based platform for CdS QDs electrochemiluminescence (ECL) detection is presented. CdS QDs were synthesized in aqueous media and placed on top of carbon electrodes by drop casting. The CdS QDs spherical assemblies consisted of nanoparticles about 4 nm diameters and served as ECL sensitizers to enzymatic assays. Read More

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Identification of chicken-derived scFv against N-glycolylneuraminic acid retrieved from an immune library by phage display.

Protein Expr Purif 2021 Jun 11;182:105841. Epub 2021 Feb 11.

Key Laboratory of Zoonosis Research, Ministry of Education, College of Veterinary Medicine, Jilin University, Changchun, 130062, PR China. Electronic address:

N- glycolylneuraminic acid (Neu5Gc) is a type of sialic acid, it can be synthesized by a range of mammals except chickens and healthy human. After entering human body, Neu5Gc in foods such as red meat and milk can cause chronic inflammation, thus promoting the development of cancer and related diseases. In this study, we identified a gene sequence of Neu5Gc-specific single-chain variable fragment (ScFv) by phage display from a primary chicken antibodies library. Read More

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Long-QT founder variant T309I-Kv7.1 with dominant negative pattern may predispose delayed afterdepolarizations under β-adrenergic stimulation.

Sci Rep 2021 Feb 11;11(1):3573. Epub 2021 Feb 11.

Department of Internal Medicine and Cardiology, University Hospital Brno and Faculty of Medicine, Masaryk University, Jihlavská 20, 625 00, Brno, Czech Republic.

The variant c.926C > T (p.T309I) in KCNQ1 gene was identified in 10 putatively unrelated Czech families with long QT syndrome (LQTS). Read More

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February 2021

Inhibition of miR-96-5p in the mouse brain increases glutathione levels by altering NOVA1 expression.

Commun Biol 2021 Feb 10;4(1):182. Epub 2021 Feb 10.

Department of Pharmacology, Teikyo University School of Medicine, Tokyo, Japan.

Glutathione (GSH) is an important antioxidant that plays a critical role in neuroprotection. GSH depletion in neurons induces oxidative stress and thereby promotes neuronal damage, which in turn is regarded as a hallmark of the early stage of neurodegenerative diseases. The neuronal GSH level is mainly regulated by cysteine transporter EAAC1 and its inhibitor, GTRAP3-18. Read More

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February 2021

Propofol suppresses non-small cell lung cancer tumorigenesis by regulation of circ-RHOT1/miR-326/FOXM1 axis.

Life Sci 2021 Jan 27:119042. Epub 2021 Jan 27.

Department of Anesthesiology, The First People's Hospital of Lianyungang, 182 Tongguan Road, Lianyungang 222000, Jiangsu, China.

Background: Lung cancer is a common malignant tumor around the world. Propofol has been found to play an anti-tumor role. Therefore, the purpose of this study is to clarify the role and underlying molecular mechanisms of Propofol in non-small cell lung cancer (NSCLC). Read More

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January 2021

LncRNA CHRF aggravates myocardial ischemia/reperfusion injury by enhancing autophagy via modulation of the miR-182-5p/ATG7 pathway.

J Biochem Mol Toxicol 2021 Apr 24;35(4):e22709. Epub 2021 Jan 24.

Department of Cardiovascular Medicine, Lianyungang TCM Hospital Affiliated to Nanjing University of Chinese Medicine, Lianyungang, Jiangsu Province, China.

Myocardial ischemia/reperfusion (I/R) injury is a very frequent cardiovascular disease and one of the leading causes of death. Abundant evidence has shown that long noncoding RNAs (lncRNAs) are crucial players in myocardial I/R injury. LncRNA cardiac hypertrophy-related factor (CHRF) has been revealed as an important modulator in cardiac disease. Read More

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[Correlations of diurnal brain functional variations with serum biomarkers and objective sleep quality in patients with chronic insomnia disorder].

Zhonghua Yi Xue Za Zhi 2021 Jan;101(4):249-253

Department of Sleep Disorders, Affiliated Chaohu Hospital of Anhui Medical University, Chaohu 238000, China.

To investigate the correlations of diurnal brain functional variations with serum biomarkers and objective sleep quality in patients with chronic insomnia disorder (CID). A total of 60 CID patients and 30 healthy sleep volunteers who visited Department of Sleep Disorders of Chaohu Hospital affiliated to Anhui Medical University from March 2018 to June 2019 were collected. Diurnal brain function state was evaluated by Quantitative Measurement System of Brain Functional Status, and serum concentrations of corticotropin-releasing hormone (CRH) and glial fibrous acidic protein (GFAP) were detected using enzyme-linked immunosorbent assay (ELISA). Read More

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January 2021

Fenhexamid induces cancer growth and survival via estrogen receptor-dependent and PI3K-dependent pathways in breast cancer models.

Food Chem Toxicol 2021 Mar 20;149:112000. Epub 2021 Jan 20.

Laboratory of Biochemistry and Immunology, College of Veterinary Medicine, Chungbuk National University, Cheongju, Chungbuk, Republic of Korea. Electronic address:

Fenhexamid (Fen), a fungicide used to treat gray mold of fruits and vegetables, is reported to function as an endocrine disrupting chemical via the estrogen receptors (ER), despite low-toxicity of the pesticide. In this study, we elucidated that the disrupting effects of Fen are exerted via the ER and phosphatidylinositol 3-kinase (PI3K) pathways in breast cancer models. The WST assay, live cell monitoring, cell cycle analysis, colony formation assay, apoptotic analysis by JC-1 dyeing, and Western blot analysis were applied in ER positive MCF-7 and ER negative MDA-MB-231 breast cancer cells, after exposure to 17β-estradiol (E2), Fen, ICI 182,780 (ICI; an ER antagonist) and/or Pictilisib (Pic; a PI3K inhibitor). Read More

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