Our findings provide useful baseline and regional speciality information on the biodiversity of the Wedelia genus plants. Specific plant secondary metabolites that may confer potent RGD bioactivities in both mammalian and plant systems are discussed. The possible application of our findings to systematic exploration of plant secondary metabolites as phytomedicines present in reputed, traditional medicinal plants is contemplated. In this study, we used a combined technological approach to authenticate, validate or profile the various species/varieties and bio diversities of plants that grow naturally in Taiwan, and further investigated their reputed bioactivities in vivo in a clinically-relevant animal/disease model as an example of a systematic exploration of plant secondary metabolites found in traditional medicinal plants. Among various medicinal plants from the genus commonly found in Taiwan, as compared to the untreated mice, only the phytoextract from species exhibited statistically significant anti-inflammatory bioactivity on DSS-induced murine colitis. This result may be connected to two groups of secondary plant metabolites, caffeic acid derivatives and chlorogenic acid, present in W. chinensis extracts. Further study is needed however to verify whether these index compound-like phytochemicals are indeed the active ingredient of the detected bioactivities. Caffeic acid and derivatives are efficacious phytochemicals that may help defend plants against abiotic and/or biotic stresses. They were reported to help protect plants against plant pathogens, MNS including fungi, bacteria and insects. They have also been shown to contribute or be associated with the control of physical or chemical stresses including drought, salinity and heat. On the other hand, the anti-oxidant, anti-carcinogenic, anti inflammatory, immune modulatory and even anti-colitis activities of caffeic acid and some of its derivatives have also been previously reported by our own group and others. Chlorogenic acid has also been reported to exhibit various bioactivities in mammalian systems, including anti-inflammatory and cytokine-modulatory activities.