Andrographolide is a labdane diterpenoid isolated from Andrographis paniculata and traditionally used in Chinese and Indian medicine. Reported effects include anti-bacterial, anti-inflammatory and anti-cancer functions. Most of the studies support the hypothesis that andrographolide supplementation stimulates immune system, so the observed effects migh in fact be secondary to the stimulation of defense reactions. As andrographolide is involved in regulation of inflammation, it is not surprising that it is also evaluated in inflammation-mediated diseases such as ulcerative colitis. Anticancer effects of the andrographolide have been tested on various cancer panels. Colon cancer, breast cancer, and head and neck carcinomas were the most investigated, followed by prostate cancer and glioblastoma. The results looked promising. However, problems with solubility and low level of active substance in natural extract leads to preparation of chemical analogs. Objective of this short review is to summarize current knowledge of the biological effects of andragrapholide. We conclude that despite documented effects and some partly characterized mechanisms of action, more research is clearly needed. At present, the doses, types of treatment and possible negative side effects are not yet established. In addition, various isolations and compound formulas have been used for treatment of various diseases, making final conclusions problematic.