Artemisinin and its derivatives are the first-line antimalarial drugs, and have saved millions of lives across the globe, especially in developing world. The discovery of artemisinin by Youyou Tu was awarded the 2015 Nobel Prize in Physiology or Medicine. In addition to treating malaria, accumulating evidences suggest that artemisinin and its derivatives also possess potent anti-inflammatory and immunoregulatory properties. We recently showed that artesunate, an artemisinin analog, dramatically ameliorated autoimmune arthritis by selectively diminishing germinal center B cells. Herein, we review the immunosuppressive properties of artemisinin family drugs and the potential underlying mechanisms.