Synthesis and biological evaluation of pseudolaric acid B derivatives as potential immunosuppressive agents

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

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was financially supported by the Special Financial Grant from China Postdoctoral Science Foundation [grant number 201104796]; Tianjin Municipal Science and Technology Commission [grant number 11JCYBJC14600]; and National Nature Science Foundation of China (NSFC) for Young Scientists Fund [grant number 81202843].