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Rosmarinic acid is an ester of caffeic acid and 3, 4-dihydroxyphenyllactic acid, being found to have a multitude of biological activities such as anti-inflammation, antimutagen and antioxidant. In order to establish the relationship between antioxidants and matrix metalloproteinase (MMP) -inhibitory activity, rosmarinic acid and caffeic acid were evaluated for their potential in 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity and blocking of MMP activity. Gelatinase activity was measured using the gelatin degradation and/or gelatin-zymography assay. From comparison of the different levels of DPPH radical scavenging activity, it was deduced that a crucial role in inhibition for MMP activity might play by an antioxidant activity. This comparative study is proposed as a basis for designing the enhanced antiproteolytic activities, and no or reduced side effects for use in hindering inflammation, cancer invasion or metastasis and angiogenesis in lung.