30,191 results match your criteria a549 cells


Transforming Type II to Type I c-Met kinase inhibitors via combined scaffold hopping and structure-guided synthesis of new series of 1,3,4-thiadiazolo[2,3-c]-1,2,4-triazin-4-one derivatives.

Bioorg Chem 2021 Aug 25;116:105304. Epub 2021 Aug 25.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt.

Novel 1,3,4-thiadiazolo[2,3-c]-1,2,4-triazin-4-one derivatives 3a-e, 4a-f and 5a-f were designed as Type I c-Met kinase inhibitors based on scaffold hopping of our previous Type II c-Met kinase lead. Target compounds were then synthesized under the guidance of molecular docking analysis to identify the potential inhibitors that fit the binding pocket of c-Met kinase in the characteristic manner as the reported Type I c-Met kinase inhibitors. All synthesized derivatives were evaluated for their c-Met kinase inhibitory activity at 10 µM concentration, where 3d, 5d and 5f displayed >80% inhibition. Read More

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Mesoporous silica particles functionalized with newly extracted fish oil ([email protected]) inhibit lung cancer cell growth.

Nanomedicine (Lond) 2021 Sep 17. Epub 2021 Sep 17.

Istituto per la Ricerca e l'Innovazione Biomedica, CNR, Via U. La Malfa 153, Palermo, 90146, Italy.

To assess whether [email protected] microparticles - fish oil from anchovy fillet leftovers (AnchoisOil) encapsulated within mesoporous silica particles - are effective in promoting antitumor effects in lung cancer cells. Three human non-small-cell lung cancer cell lines (A549, Colo 699 and SK-MES-1) were used. Cells were treated with AnchoisOil dispersed in ethanol (10 and 15 μg/ml) or encapsulated in silica and further formulated in aqueous ethanol. Read More

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September 2021

New chromanone derivatives containing thiazoles: Synthesis and antitumor activity evaluation on A549 lung cancer cell line.

Drug Dev Res 2021 Sep 17. Epub 2021 Sep 17.

Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.

Novel 2-[2-(chroman-4-ylidene)hydrazinyl]-4/5-substituted thiazole derivatives (2a-i) were synthesized and investigated for their anticancer activity. Cytotoxic activity on A549 and NIH/3T3 cell lines was determined, most of the compounds exhibited high cytotoxic profile with selectivity. Selected compounds 2b, 2c, 2e, 2g, 2h, and 2i were tested to determine induction of apoptosis, mitochondrial membrane depolarization, and cell cycle arrest. Read More

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September 2021

Isorhamnetin inhibits amplification of influenza A H1N1 virus inflammation mediated by interferon via the RIG-I/JNK pathway.

Ann Transl Med 2021 Aug;9(16):1327

State Key Laboratory of Respiratory Disease, National Clinical Research Center for Respiratory Disease, Guangzhou Institute of Respiratory Health, First Affiliated Hospital of Guangzhou Medical University, Guangzhou, China.

Background: Interferon (IFN) amplifies the influenza virus-mediated inflammatory response by forming a paracrine signal feedback loop, which is considered an important cause of excessive inflammatory damage. Isorhamnetin has a wide spectrum of beneficial pharmacological properties, including anti-inflammatory and antiviral effects. The regulatory effect and mechanism of isorhamnetin on influenza virus-mediated inflammation have not yet been reported. Read More

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[CacyBP promotes the proliferation and invasion of non-small cell lung cancer].

Zhonghua Zhong Liu Za Zhi 2021 Sep;43(9):924-931

Department of Thoracic Surgery, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100021, China.

To investigate the effects and the mechanism of Calcyclin-binding protein (CacyBP) on the proliferation and invasion of non-small cell lung cancer (NSCLC) cells. Six lung cancer tissues and paired normal lung tissues were collected from NSCLC patients who underwent surgical treatment in Jinan Central Hospital during 2016. The expression of CacyBP in these tissues was examined by western blot. Read More

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September 2021

Red fluorescent zwitterionic naphthalenediimides with di/mono-benzimidazolium and a negatively-charged oxygen substituent.

Chem Commun (Camb) 2021 Sep 16;57(74):9422-9425. Epub 2021 Sep 16.

Key Laboratory of Green Chemistry and Technology of Ministry of Education, College of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, P. R. China.

The C-H/C-X cross-coupling of a benzimidazolium salt with 2Br-NDI afforded two unprecedented zwitterionic NDIs with di/mono-benzimidazolium and an extra negatively-charged oxygen substituent. They exhibited intensified red fluorescence in polar solvents and negative solvatochromism due to an intramolecular charge transfer process, and could specifically label lysosomes and the endoplasmic reticulum in living A549 cells, respectively. They represent a rare case of NDI-derived ionic fluorophores. Read More

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September 2021

Metformin-induced chemosensitization to cisplatin depends on P53 status and is inhibited by Jarid1b overexpression in non-small cell lung cancer cells.

Aging (Albany NY) 2021 Sep 16;13(undefined). Epub 2021 Sep 16.

Centro de Investigação Translacional em Oncologia (LIM24), Departamento de Radiologia e Oncologia, Faculdade de Medicina da Universidade de São Paulo and Instituto do Câncer do Estado de São Paulo, São Paulo, SP 01246-000, Brazil.

Metformin has been tested as an anti-cancer therapy with potential to improve conventional chemotherapy. However, in some cases, metformin fails to sensitize tumors to chemotherapy. Here we test if the presence of P53 could predict the activity of metformin as an adjuvant for cisplatin-based therapy in non-small cell lung cancer (NSCLC). Read More

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September 2021

Aluminium (III) phthalocyanine chloride tetrasulphonate is an effective photosensitizer for the eradication of lung cancer stem cells.

R Soc Open Sci 2021 Sep 8;8(9):210148. Epub 2021 Sep 8.

Laser Research Centre, Faculty of Health Sciences, University of Johannesburg, PO Box 17011, Johannesburg 2028, South Africa.

Cancer stem cells (CSCs) are considered to contribute to the recurrence of lung cancer due to their stem-like nature and the involvement of genetic markers associated with drug efflux, regeneration and metastases. Photodynamic therapy (PDT) is a cost-effective and non-invasive therapeutic application that can act as an alternative therapy for lung cancer when considering CSC involvement. Stem-like cells derived from the A549 lung cancer cell line, positive for CD133, CD56 and CD44 antigen markers, were characterized, intracellular localization of aluminium (III) phthalocyanine chloride tetrasulphonate (AlPcSCl) determined and its anti-cancer PDT effects were evaluated. Read More

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September 2021

Circular RNA La-related protein 4 inhibits cell proliferation, migration, and invasion and sponges microRNA-367 in non-small cell lung cancer.

Int J Clin Exp Pathol 2021 15;14(8):858-865. Epub 2021 Aug 15.

Department of Oncology, Jilin Province Cancer Hospital Changchun, Jilin, China.

This study aimed to investigate the effect of circular RNA (circRNA) La-related protein 4 (LARP4) on inhibiting the malignant progression of non-small cell lung cancer (NSCLC) cells. CircRNA LARP4 expression in a human normal lung epithelial cell line and NSCLC cell lines was detected by reverse transcription-quantitative polymerase chain reaction. CircRNA LARP4 overexpression and control overexpression plasmids were transfected into NCI-H1650 cells; circRNA LARP4 knockdown and control knockdown plasmids were transfected into A549 cells. Read More

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Concomitant and decoupled effects of cigarette smoke and SCAL1 upregulation on oncogenic phenotypes and ROS detoxification in lung adenocarcinoma cells.

Sci Rep 2021 Sep 15;11(1):18345. Epub 2021 Sep 15.

Disease Molecular Biology and Epigenetics Laboratory, National Institute of Molecular Biology and Biotechnology, University of the Philippines Diliman, 1101, Quezon City, Philippines.

Lung cancer is the leading cause of cancer deaths worldwide, with smoking as its primary predisposing factor. Although carcinogens in cigarettes are known to cause oncogenic DNA alterations, analyses of patient cohorts revealed heterogeneous genetic aberrations with no clear driver mutations. The contribution of noncoding RNAs (ncRNAs) in the pathogenesis of lung cancer has since been demonstrated. Read More

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September 2021

K channel blockers increase effectiveness of the EGF receptor TK inhibitor erlotinib in non-small cell lung cancer cells (A549).

Sci Rep 2021 Sep 15;11(1):18330. Epub 2021 Sep 15.

Institut für Physiologie II, Westfälische Wilhelms-Universität, Robert-Koch-Str. 27b, 48149, Münster, Germany.

Non-small cell lung cancer (NSCLC) has a poor prognosis with a 5 year survival rate of only ~ 10%. Important driver mutations underlying NSCLC affect the epidermal growth factor receptor (EGFR) causing the constitutive activation of its tyrosine kinase domain. There are efficient EGFR tyrosine kinase inhibitors (TKIs), but patients develop inevitably a resistance against these drugs. Read More

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September 2021

Discovery of facile amides-functionalized rhodanine-3-acetic acid derivatives as potential anticancer agents by disrupting microtubule dynamics.

J Enzyme Inhib Med Chem 2021 Dec;36(1):1996-2009

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guiyang, People's Republic of China.

Microtubule dynamics are crucial for multiple cell functions, and cancer cells are particularly sensitive to microtubule-modulating agents. Here, we describe the design and synthesis of a series of ()-2-(5-benzylidene-4-oxo-2-thioxothiazolidin-3-yl)--phenylacetamide derivatives and evaluation of their microtubule-modulating and anticancer activities . Proliferation assays identified as the most potent of the antiproliferative compounds, with 50% inhibitory concentrations ranging from 7. Read More

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December 2021

A cGAS-dependent response links DNA damage and senescence in alveolar epithelial cells: A potential drug target in IPF.

Am J Physiol Lung Cell Mol Physiol 2021 Sep 15. Epub 2021 Sep 15.

School of Biomedical Sciences and Pharmacy, grid.266842.cUniversity of Newcastle, Callaghan, NSW, Australia.

Alveolar epithelial cell (AEC) senescence is implicated in the pathogenesis of idiopathic pulmonary fibrosis (IPF). Mitochondrial dysfunction including release of mitochondrial DNA (mtDNA) is a feature of senescence, which led us to investigate the role of the DNA-sensing GMP-AMP synthase (cGAS) in IPF, with a focus on AEC senescence. cGAS expression in fibrotic tissue from lungs of IPF patients was detected within cells immunoreactive for epithelial cell adhesion molecule (EpCAM) and p21, epithelial and senescence markers respectively. Read More

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September 2021

Ratiometric Fluorescence Imaging of Intracellular MicroRNA with NIR-Assisted Signal Amplification by a [email protected] Nanoplatform.

ACS Appl Mater Interfaces 2021 Sep 15. Epub 2021 Sep 15.

Zhangdayu School of Chemistry, Dalian University of Technology, Dalian 116023, P. R. China.

Accurate and sensitive fluorescence imaging of intracellular miRNA is essential for understanding the mechanism underlying some physiological and pathological events, as well as the prevention and diagnosis of diseases. Herein, a highly sensitive ratiometric fluorescent nanoprobe for intracellular miRNA imaging was fabricated by integrating a [email protected] ([email protected]) nanoplatform with a near-infrared light (NIR)-assisted DNA strand displacement signal amplification strategy. The [email protected] spheres have excellent biosafety, high photothermal effect, and unique photophysical properties that can both emit a stable red fluorescence and well quench the fluorophores getting closer to them. Read More

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September 2021

Downregulation of miR-487a-3p suppresses the progression of non-small cell lung cancer via targeting Smad7.

Drug Dev Res 2021 Sep 15. Epub 2021 Sep 15.

Department of Thoracic Surgery, Ningbo Zhenhai People's Hospital, Ningbo, Zhejiang, China.

Non-small cell lung cancer (NSCLC) is the most prevalent type of lung cancer; however, the treatment efficacy of advanced NSCLC remains poor. MicroRNAs (miRNAs) are closely associated with the pathogenesis of lung cancer, while the detailed function of miR-487a-3p in NSCLC remains unclear. Bioinformatic analysis was performed to identify differentially expressed miRNAs (DEmiRNAs) between NSCLC and normal tissues. Read More

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September 2021

The petroleum ether extract of L. induces apoptosis of lung adenocarcinoma cells the mitochondria-dependent pathway.

Food Funct 2021 Sep 13. Epub 2021 Sep 13.

Xinjiang Key Laboratory of Biological Resources and Genetic Engineering, College of Life Science and Technology, Xinjiang University, Urumqi, Xinjiang, China.

L. is one of the most popular traditional foods with a variety of biological activities. In this study, the petroleum ether extract of was separated by silica gel column chromatography, and named BRPS, which was identified by LC-MS. Read More

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September 2021

Identification of circ_0058357 as a regulator in non-small cell lung cancer cells resistant to cisplatin by miR-361-3p/ABCC1 axis.

Thorac Cancer 2021 Sep 14. Epub 2021 Sep 14.

Department of Respiratory Medicine, the First Affiliated Hospital of Zhengzhou University, Zhengzhou, China.

Background: Drug resistance is a major clinical drawback behind the failure of chemotherapy in non-small cell lung cancer (NSCLC). In this study, we undertook to identify the precise role of circular RNA (circRNA) circ_0058357 in the functional properties of DDP-resistant NSCLC cells.

Methods: Circ_0058357, miR-361-3p and ATP-binding cassette (ABC) subfamily C member 1 (ABCC1) were quantified by qRT-PCR and western blot. Read More

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September 2021

Targeted nanostructured lipid carrier containing galangin as a promising adjuvant for improving cytotoxic effects of chemotherapeutic agents.

Naunyn Schmiedebergs Arch Pharmacol 2021 Sep 15. Epub 2021 Sep 15.

Nanobiotechnology Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran.

Resistance to chemotherapeutic drugs is the main limitation of cancer therapy. The combination use of chemotherapeutic agents and galangin (a naturally active flavonoid) amplifies the effectiveness of cancer treatment. This study aimed to prepare arginyl-glycyl-aspartic acid (RGD) containing nanostructured lipid carrier (NLC-RGD) to improve the bioavailability of galangin and explore its ability in improving the cytotoxic effects of doxorubicin (DOX). Read More

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September 2021

3'untranslated regions (3'UTR) of mRNA displays anticancer effects in non-small cell lung cancer (NSCLC) cells.

Am J Cancer Res 2021 15;11(8):3857-3876. Epub 2021 Aug 15.

Key Laboratory of Functional Protein Research of Guangdong Higher Education Institutes and MOE Key Laboratory of Tumor Molecular Biology, Institute of Life and Health Engineering, Jinan University Guangzhou 510632, China.

RNA-based therapeutics has attracted substantial interest from both academics and pharmaceutical companies. In this study, we investigated the function and the underlying mechanism of 3'UTR in NSCLC H1299 and A549 cells. We found that transfected plasmids significantly increased the proliferation, migration and invasion of NSCLC cells, whereas 3'UTR could suppress the promotional effect of GSN protein on the development of NSCLC . Read More

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Identifying the lungs as a susceptible site for allele-specific regulatory changes associated with type 1 diabetes risk.

Commun Biol 2021 Sep 14;4(1):1072. Epub 2021 Sep 14.

Liggins Institute, The University of Auckland, Auckland, New Zealand.

Type 1 diabetes (T1D) etiology is complex. We developed a machine learning approach that ranked the tissue-specific transcription regulatory effects for T1D SNPs and estimated their relative contributions to conversion to T1D by integrating case and control genotypes (Wellcome Trust Case Control Consortium and UK Biobank) with tissue-specific expression quantitative trait loci (eQTL) data. Here we show an eQTL (rs6679677) associated with changes to AP4B1-AS1 transcript levels in lung tissue makes the largest gene regulatory contribution to the risk of T1D development. Read More

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September 2021

Engineered exosomes loaded with miR-449a selectively inhibit the growth of homologous non-small cell lung cancer.

Cancer Cell Int 2021 Sep 14;21(1):485. Epub 2021 Sep 14.

Department of Cardiothoracic Surgery, Affiliated Hospital of Nantong University, No. 20, Xisi Road, Nantong, 226021, Jiangsu, China.

As an efficient drug carrier, exosome has been widely used in the delivery of genetic drugs, chemotherapeutic drugs, and anti-inflammatory drugs. As a genetic drug carrier, exosomes are beneficial to improve transfection efficiency and weaken side effects at the same time. Here, we use genetic engineering to prepare engineered exosomes (miR-449a Exo) that can actively deliver miR-449a. Read More

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September 2021

Antitumor activity, DNA and BSA interactions of novel copper(II) complexes with 3,4-dihydro-2(1H)-quinoxalinones.

Chem Biol Interact 2021 Sep 11;348:109647. Epub 2021 Sep 11.

University of Kragujevac, Institute for Information Technologies Kragujevac, Department of Sciences, Jovana Cvijića bb, 34000, Kragujevac, Serbia.

In order to discover new therapeutically active agents a series of novel copper(II) complexes with 3,4-dihydro-2(1H)-quinoxalinones were synthesized. All complexes were characterized by IR and EPR spectroscopic techniques and examined for their cytotoxic effect on human cancer cell lines HeLa, LS174, A549 and normal fibroblasts (MRC-5). For further examination of the cytotoxic mechanisms of novel complexes, three of them were chosen for analysing their effects on the distribution of HeLa cells in the cell cycle phases. Read More

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September 2021

Thalidomide suppresses angiogenesis and immune evasion via lncRNA FGD5-AS1/miR-454-3p/ZEB1 axis-mediated VEGFA expression and PD-1/PD-L1 checkpoint in NSCLC.

Chem Biol Interact 2021 Sep 11:109652. Epub 2021 Sep 11.

Department of Radiotherapy, The First Affiliated Hospital of Nanjing Medical University, Nanjing, 210029, Jiangsu Province, China. Electronic address:

Background: Non-small cell lung cancer (NSCLC) accounts for about 80-85% of total lung cancer cases. Identifying the molecular mechanisms of anti-tumor drugs is essential for improving therapeutic effects. Herein, we aim to investigate the role of thalidomide in the tumorigenicity of NSCLC. Read More

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September 2021

Antileishmanial and lung adenocarcinoma cell toxicity of (Linn.) dunal root and fruit extracts.

Nat Prod Res 2021 Sep 14:1-7. Epub 2021 Sep 14.

Department of Pharmacognosy, Graduate School of Biomedical and Health Sciences, Hiroshima University, Minami-ku, Hiroshima, Japan.

This study aims to evaluate the anti- and the lung adenocarcinoma (A549) cytotoxicity of root and fruit. The total extracts were obtained by homogenisation in aqueous MeOH, and the sub-extracts [-hexane, ethyl acetate (EtOAc), -butanol (-BuOH), and methanol (MeOH)] were obtained by flash chromatography. The activity evaluation showed that -BuOH sub-extracts from root and fruit exhibited noticeable antileishmanial promastigote properties. Read More

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September 2021

MiR-9-1 Suppresses Cell Proliferation and Promotes Apoptosis by Targeting UHRF1 in Lung Cancer.

Technol Cancer Res Treat 2021 Jan-Dec;20:15330338211041191

Shanghai Tenth People's Hospital, 278245Tongji University School of Medicine, Shanghai, China.

Lung cancer is listed as the most common reason for cancer-related death all over the world despite diagnostic improvements and the development of chemotherapy and targeted therapies. MicroRNAs control both physiological and pathological processes including development and cancer. A microRNA-9 to 1 (miR-9 to 1) overexpression model in lung cancer cell lines was established and miR-9 to 1 was found to significantly suppress the proliferation rate in lung cancer cell lines, colony formation in vitro, and tumorigenicity in nude mice of A549 cells. Read More

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September 2021

Influenza A Virus (H1N1) Infection Induces Glycolysis to Facilitate Viral Replication.

Virol Sin 2021 Sep 14. Epub 2021 Sep 14.

Department of Emergency and Critical Care Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 201620, China.

Viruses depend on host cellular metabolism to provide the energy and biosynthetic building blocks required for their replication. In this study, we observed that influenza A virus (H1N1), a single-stranded, negative-sense RNA virus with an eight-segmented genome, enhanced glycolysis both in mouse lung tissues and in human lung epithelial (A549) cells. In detail, the expression of hexokinase 2 (HK2), the first enzyme in glycolysis, was upregulated in H1N1-infected A549 cells, and the expression of pyruvate kinase M2 (PKM2) and pyruvate dehydrogenase kinase 3 (PDK3) was upregulated in H1N1-infected mouse lung tissues. Read More

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September 2021

Histone Deacetylase as a Valuable Predictive Biomarker and Therapeutic Target in Immunotherapy for Non-Small Cell Lung Cancer.

Cancer Res Treat 2021 Sep 10. Epub 2021 Sep 10.

Division of Pulmonary, Allergy, and Critical Care Medicine, Department of Internal Medicine, Korea University Guro Hospital, Seoul, Korea.

Purpose: Histone deacetylase inhibitors (HDACis) are epigenetic regulators and used clinically for hematopoietic malignancies. Recently, HDACis have received attention as a factor that modulates the immune system. In this study, the role of HDAC expression as a predictive marker in lung cancer patients who were treated with immune checkpoint inhibitors (ICIs) and the role of HDACi and ICI combination treatment in the mouse tumor model were analyzed. Read More

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September 2021

Air-liquid interphase culture confers SARS-CoV-2 susceptibility to A549 alveolar epithelial cells.

Biochem Biophys Res Commun 2021 Sep 10;577:146-151. Epub 2021 Sep 10.

Division of Molecular Pathobiology, International Institute for Zoonosis Control, Hokkaido University, Sapporo, 001-0020, Japan; International Collaboration Unit, International Institute for Zoonosis Control, Hokkaido University, Sapporo, 001-0020, Japan; Global Virus Network, Baltimore, MD, 21201, USA; One Health Research Center, Hokkaido University, Sapporo, 060-0818, Japan.

The human lung cell A549 is susceptible to infection with a number of respiratory viruses. However, A549 cells are resistant to Severe Acute Respiratory Syndrome-Coronavirus-2 (SARS-CoV-2) infection in conventional submerged culture, and this would appear to be due to low expression levels of the SARS-CoV-2 entry receptor: angiotensin-converting enzyme-2 (ACE2). Here, we examined SARS-CoV-2 susceptibility to A549 cells after adaptation to air-liquid interface (ALI) culture. Read More

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September 2021

Radiosensitizing effect of gold nanoparticle loaded with small interfering RNA-SP1 on lung cancer: AuNPs-si-SP1 regulates GZMB for radiosensitivity.

Transl Oncol 2021 Sep 10;14(12):101210. Epub 2021 Sep 10.

Department of Radiation Oncology, Harbin Medical University Tumor Hospital, No. 150, Haping Road, Nangang District, Harbin 150001, Heilongjiang Province, China. Electronic address:

Radioresistance is a major challenge that largely limits the efficacy of radiotherapy in lung cancer. Gold nanoparticles (AuNPs) are emerging as novel radiosensitizers for cancer patients. Therefore, this study was designed to explore the radiosensitizing effect and mechanism of AuNPs loaded with small interfering RNA (siRNA)-SP1 (AuNPs-si-SP1) on lung cancer. Read More

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September 2021

Long non-coding RNA MALAT1 enhances the protective effect of dexmedetomidine on acute lung injury by sponging miR-135a-5p to downregulate the ratio of X-box binding proteins XBP-1S/XBP-1U.

Bioengineered 2021 Dec;12(1):6377-6389

Department of Anesthesiology, Jiangsu Cancer Hospital & Jiangsu Institute of Cancer Research & the Affiliated Cancer Hospital of Nanjing Medical University, Nanjing, Jiangsu, China.

Acute lung injury (ALI) is the common and clinically severe complication. Dexmedetomidine (DEX) can protect against lipopolysaccharide (LPS)-induced ALI through anti-apoptosis, anti-inflammatory and immune regulatory actions. It is well documented that major causes of LPS-induced ALI are endoplasmic reticulum stress (ERS) and abnormally elevated CHOP. Read More

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December 2021