tailieunhanh - Báo cáo khoa học: Novel synthetic gluco-disaccharide RSCL-0409 – a lipopolysaccharide-induced Toll-like receptor-mediated signalling antagonist

The regulation of cytokines and pro-inflammatory genes is an absolute essentiality to combat inflammatory diseases. The present study investigated the effects of 4-O-chloroacetyl-2,3-di-O-acetyl-6-O-levulinoyl-b-d-glucopyr-anosyl]-(1-3)-1-O-(p-methoxyphenyl)-2-deoxy-2-N-trichloroacetyl-4,6-O-ben-zylidene-a-d-glucopyranoside (RSCL-0409), a novel small molecule Toll-like receptor (TLR) signalling antagonist, and its mechanism of action in human monocytic (THP-1) cells stimulated with lipopolysaccharide (LPS) | Novel synthetic gluco-disaccharide RSCL-0409 -a lipopolysaccharide-induced Toll-like receptor-mediated signalling antagonist o n I n lốo 1111 t i 1 p I a I riatl a2 Ạ lzọh owo Rpl Io ft 1 l h a Is nrliit Racha1 A Ọ li A o ft ĩ RKĩỉrmĩỉ1 IVI al 11 LA ixa Iiui I I lai Icci L atia Mxoiiaya Deidiy 1X1 laiaiiviei LJdsid Aoiivvaiii wiiaiiiia Anuradha Sharma1 Shiva Singh1 Shakti Upadhyay2 and Vikram Rajagopal1 1 Drug Discovery and Development Group Reliance Life Sciences Pvt. Ltd Navi Mumbai India 2 EID Parry India Ltd Chennai India Keywords inflammation lipopolysaccharide monocytes NF-kB TLR signalling tumour necrosis factor-a Correspondence V. Rajagopal Drug Discovery and Development Group Reliance Life Sciences Pvt. Ltd Dhirubhai Ambani Life Sciences Center Rabale Navi Mumbai-400701 India Fax 91 22 67678099 Tel 91 22 67678854 E-mail vikram_rajagopal@ These authors contributed equally to this work Received 9 December 2009 revised 16 January 2010 accepted 21 January 2010 doi The regulation of cytokines and pro-inflammatory genes is an absolute essentiality to combat inflammatory diseases. The present study investigated the effects of 4-ơ-chloroacetyl-2 3-di-ơ-acetyl-6-ơ-levulinoyl-P-D-glucopyr-anosyl - 1-3 -1-ơ- p-methoxyphenyl -2-deoxy-2-N-trichloroacetyl-4 6-ơ-ben-zylidene-a-D-glucopyranoside RSCL-0409 a novel small molecule Toll-like receptor TLR signalling antagonist and its mechanism of action in human monocytic THP-1 cells stimulated with lipopolysaccharide LPS . In THP-1 and cells RSCL-0409 suppressed LPS-induced production of tumour necrosis factor-a TNF-a with a 50 inhibitory concentration of pM and mRNA expression of ICAM-1 Cox-2 and interleukin-8 with no evidence of cytotoxicity. RSCL-0409 also suppressed TNF-a production from LPS-stimulated human peripheral blood mononuclear cells. Similar results were obtained in vivo in a murine model of LPS-induced inflammation where pretreatment with RSCL-0409 .

TỪ KHÓA LIÊN QUAN
crossorigin="anonymous">
Đã phát hiện trình chặn quảng cáo AdBlock
Trang web này phụ thuộc vào doanh thu từ số lần hiển thị quảng cáo để tồn tại. Vui lòng tắt trình chặn quảng cáo của bạn hoặc tạm dừng tính năng chặn quảng cáo cho trang web này.