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Synthesis and biological evaluation of pseudolaric acid B derivatives as potential immunosuppressive agents
Authors:Shou-Qiang Chen  Jie Wang  Chuan Zhao  Qiang-Wen Sun  Yi-Teng Wang  Ting Ai
Affiliation:1. Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin 300070, China;2. Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazard, Logistics University of Chinese People's Armed Police Forces, Tianjin 300162, China;3. Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazard, Logistics University of Chinese People's Armed Police Forces, Tianjin 300162, China
Abstract:Pseudolaric acid B (PB) derivatives with immunosuppressive activity were found by our group. In order to find potential immunosuppressive agents with high efficacy and low toxicity, a series of novel PB derivatives were synthesized and evaluated on their immunosuppressive activities. Most of the synthesized compounds were tested in vitro on murine T and B proliferation. In particular, compound 11 exhibited excellent inhibitory activity toward murine T cells (up to 19-fold enhancement compared to that of mycophenolatemofetil) and little cytotoxicity toward normal murine spleen cells. These experimental data demonstrated that some of these PB derivatives have great potential for future immunosuppressive studies.
Keywords:pseudolaric acid B derivatives  immunosuppressive activity  cytotoxicity
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