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Wang W.,Guangzhou University | Zheng J.-P.,Guangzhou University | Zhu S.-X.,Guangzhou BaiYunShan Pharmaceutical General Factory | Guan W.-J.,Guangzhou University | And 2 more authors.
International Immunopharmacology | Year: 2015

Carbocisteine is a mucolytic drug with anti-oxidative effect, we had previously proved that carbocisteine remarkably reduced the rate of acute exacerbations and improved the quality of life in patients with chronic obstructive pulmonary disease (COPD), however, very little is known about its mechanisms. In this study, we aimed to investigate the anti-inflammatory effects of carbocisteine against hydrogen peroxide (H2O2). A549 cells were cultured in vitro and treated with H2O2 as damaged cell models, carbocisteine was administered 24 h prior to or after H2O2 exposure, and the protective effects of carbocisteine were determined by MTT, qRT-PCR, ELISA, western blot and immunofluorescence assays. The results showed that carbocisteine could increase cell viability and decrease LDH, IL-6 and IL-8 levels in the supernatant. Additionally, carbocisteine decreased IL-6, IL-8, TNF-α, IP-10 and MIP-1β mRNA in a dose-dependent manner. Moreover, carbocisteine could attenuate phosphorylation of NF-κB p65 and ERK1/2 and inhibit the nuclear translocation of pNF-κB p65 induced by H2O2. In conclusion, carbocisteine inhibited H2O2-induced inflammatory injury in A549 cells, NF-κB and ERK1/2 MAPK were the target pathways. © 2014 Elsevier B.V. All rights reserved.


PubMed | Guangzhou BaiYunShan Pharmaceutical General Factory, Guangzhou University and First Affiliated Hospital of Guangzhou Medical University
Type: Journal Article | Journal: Acta pharmacologica Sinica | Year: 2016

We previously proven that carbocisteine, a conventional mucolytic drug, remarkably reduced the rate of acute exacerbations and improved the quality of life in the patients with chronic obstructive pulmonary disease. In this study we investigated the mechanisms underlying the anti-inflammatory effects of carbocisteine in human alveolar epithelial cells in vitro.Human lung adenocarcinoma cell line A549 was treated with TNF- (10 ng/mL). Carbocisteine was administered either 24 h prior to or after TNF- exposure. The cytokine release and expression were measured using ELISA and qRT-PCR. Activation of NF-B was analyzed with Western blotting, immunofluorescence assay and luciferase reporter gene assay. The expression of ERK1/2 MAPK signaling proteins was assessed with Western blotting.Carbocisteine (10, 100, 1000 mol/L), administered either before or after TNF- exposure, dose-dependently suppressed TNF--induced inflammation in A549 cells, as evidenced by diminished release of IL-6 and IL-8, and diminished mRNA expression of IL-6, IL-8, TNF-, MCP-1 and MIP-1. Furthermore, pretreatment with carbocisteine significantly decreased TNF--induced phosphorylation of NF-B p65 and ERK1/2 MAPK, and inhibited the nuclear translocation of p65 subunit in A549 cells. In an NF-B luciferase reporter system, pretreatment with carbocisteine dose-dependently inhibited TNF--induced transcriptional activity of NF-B.Carbocisteine effectively suppresses TNF--induced inflammation in A549 cells via suppressing NF-B and ERK1/2 MAPK signaling pathways.


Huang X.,Guangzhou Baiyunshan Pharmaceutical General Factory | Bao Y.,Guangzhou Baiyunshan Pharmaceutical General Factory | Zhu S.,Guangzhou Baiyunshan Pharmaceutical General Factory | Zhang X.,Guangzhou Baiyunshan Pharmaceutical General Factory | And 2 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

Abstract A series of C10 non-basic building block-substituted, levofloxacin core-based derivatives were synthesized in 43-86% yield. The antibacterial activity of these new fluoroquinolones was evaluated using a standard broth microdilution technique. The quinolone (S)-9-fluoro-10-(4-hydroxypiperidin-1-yl)-3-methyl-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid l-arginine tetrahydrate exhibited superior antibacterial activity against quinolone-susceptible and resistant strains compared with the clinically used fluoroquinolones ciprofloxacin, levofloxacin, moxifloxacin, penicillin, and vancomycin, especially to the methicillin-resistant Staphylococcus aureus clinical isolates, penicillin-resistant Streptococcus pneumoniae clinical isolates, and Streptococcus pyogenes. © 2015 Elsevier Ltd.


PubMed | Guangzhou Baiyunshan Pharmaceutical General Factory
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2015

A series of C10 non-basic building block-substituted, levofloxacin core-based derivatives were synthesized in 43-86% yield. The antibacterial activity of these new fluoroquinolones was evaluated using a standard broth microdilution technique. The quinolone (S)-9-fluoro-10-(4-hydroxypiperidin-1-yl)-3-methyl-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid L-arginine tetrahydrate exhibited superior antibacterial activity against quinolone-susceptible and resistant strains compared with the clinically used fluoroquinolones ciprofloxacin, levofloxacin, moxifloxacin, penicillin, and vancomycin, especially to the methicillin-resistant Staphylococcus aureus clinical isolates, penicillin-resistant Streptococcus pneumoniae clinical isolates, and Streptococcus pyogenes.

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