Objective To investigate the pharmacological effects and mechanisms of natural medicine artemisinin and its derivatives. Methods The pertinent domestic and overseas literatures of recent years were reviewed and summarized. Results Artemisinin and its derivatives have unique structure, high efficiency with low toxicity. The pharmacological effects include anti-malaria, anti-tumor, immune function regulation, anti-bacterial, anti-fetation, anti-fibrosis, heat-clearing and detoxicating, etc. Conclusion Artemisinin and its derivatives play pharmacological effects in different ways, and have a good foreground in the application.