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Evaluation of the Effects of a Series of 1,2,3-Triazole Derivatives on Lipopolysaccharide Induction of Interleukin 6 in a Human Macrophage Cell Line

Abstract Details

2014, Master of Science (MS), Ohio University, Biomedical Engineering (Engineering and Technology).
The endotoxin lipopolysaccharide (LPS), a major component of Gram negative bacterial outer membrane, is a well-known inducer of inflammatory responses such as the release of cytokines in various types of cells including monocytes and macrophages. LPS can be specifically recognized by Toll-like receptor 4 (TLR4), in association with its accessory protein – myeloid differentiation factor (MD2) [1]. TLR4 in conjunction with other TLRs, plays a critical role in innate immunity, mediates pro-inflammatory cytokine production, and induces adaptive immunity of the host upon bacterial and viral infection. Intensive research aimed at identifying TLR4 inhibitors has been performed to identify possible treatments for inflammatory diseases. In the thesis, we investigated the effects of a series of 1,4- and 1,5-disubstituted-1, 2, 3-triazole derivatives on LPS-induced expression of the pro-inflammatory cytokine Interleukin 6 (IL-6), by phorbol 12-myristate 13-acetate (PMA)-differentiated THP-1 macrophages. The effect of these compounds on THP-1 derived macrophage viability was also assessed. A subset of 1,2,3-triazole derivatives that are potent inhibitors of LPS-induced IL-6 expression was identified and a preliminary structure-activity relationship analysis (SAR) was performed. These studies represent an initial step toward identifying 1,2,3-triazole derivatives that have the potential to become therapeutics for pathological inflammation.
Douglas Goetz, PhD (Advisor)
Stephen Bergmeier, PhD (Committee Chair)
Fabian Benencia, PhD (Committee Member)
Monica Burdick, PhD (Committee Member)
60 p.

Recommended Citations

Citations

  • Qi, C. (2014). Evaluation of the Effects of a Series of 1,2,3-Triazole Derivatives on Lipopolysaccharide Induction of Interleukin 6 in a Human Macrophage Cell Line [Master's thesis, Ohio University]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=ohiou1389020204

    APA Style (7th edition)

  • Qi, Chunyan. Evaluation of the Effects of a Series of 1,2,3-Triazole Derivatives on Lipopolysaccharide Induction of Interleukin 6 in a Human Macrophage Cell Line. 2014. Ohio University, Master's thesis. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=ohiou1389020204.

    MLA Style (8th edition)

  • Qi, Chunyan. "Evaluation of the Effects of a Series of 1,2,3-Triazole Derivatives on Lipopolysaccharide Induction of Interleukin 6 in a Human Macrophage Cell Line." Master's thesis, Ohio University, 2014. http://rave.ohiolink.edu/etdc/view?acc_num=ohiou1389020204

    Chicago Manual of Style (17th edition)