Cyathocline purpurea has been traditionally used to treat various diseases including cancers for many years. However, these applications of C. purpurea have not been supported by pharmacological investigation. Santamarine is one of the active component isolated from C. purpurea. It was discovered that santamarin inhibited inducible nitric oxide synthase (iNOS) protein, reduced iNOS-derived nitric oxide (NO), suppressed COX-2 protein and reduced COX-derived PGE(2) production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and murine peritoneal macrophages. Similarly, santamarin reduced tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) production. In addition, santamarin suppressed the phosphorylation and degradation of IκB-α as well as the nuclear translocation of p65 in response to LPS in RAW264.7 cells. Furthermore, santamarin induced heme oxygenase (HO)-1 expression mRNA and protein level that plays a cytoprotective role against inflammation. Also was shown that santamarine inhibited the set of cancer cells. Recently was found, that santamarine possessed mycobactericidal activity against clinical Mycobacterium tuberculosis strains.