Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. It has traditionally been used to treat disorders including arthritis, heart disease, cancer, and other inflammatory diseases. It is also present in the leaves of the tree Mitragyna speciosa, commonly known as kratom, herb which is traditionally used to treat withdrawal symptoms associated with opiate addiction. However, the specific role and the mechanism of action of mitraphylline is not clear. Current research is focusing on mitraphylline as a new promising anticancer and anti-inflammatory agent. Its antiproliferative and cytotoxic effects and in vivo efficacy to induce apoptosis has been studied in human breast cancer, sarcoma, bladder cancer as well as lymphoblastic leukaemia cell lines. As a new candidate for inflammatory disease therapies mitraphylline has been studied in vitro in LPS-activated human primary neutrophils and Its activity against cytokines involved in inflammation process was tested in a murine model in vivo. In mice mitraphylline inhibited around 50% of the release of interleukins 1α, 1β, 17, and TNF-α. It also reduced about 40% of the production of interleukin 4 (IL-4). Mitraphylline was stable in simulated gastric fluid but unstable in simulated intestinal fluid (13.6 % degradation) and was metabolized by human liver microsomes with half-live of 50 min.