Plant species that occur in the major biomes of Mato Grosso do Sul state (Pantanal and Cerrado) have been chemically investigated by the research group on Natural Products Chemistry (PRONABio) at the Institute of Chemistry of the Federal University of Mato Grosso do Sul, Brazil. Extracts from approximately 120 species have been evaluated for their biological activities and many of them have been chemically studied. Several of these works were inspired by the medicinal use of these plants by the local population. The studies also involved investigation of plants with implications in one of the main economic activities of Mato Grosso do Sul, namely livestock-including investigation of toxic species for cattle and with acaricidal activity. Dengue, one of the major public health problems in Brazil, was also the subject of chemical investigation of active species against its vector, the mosquito Aedes aegypti. In this context, some of the results obtained from studies performed with members from the families Apocynaceae, Combretaceae, Cucurbitaceae, Erythroxylaceae, Fabaceae, Lamiaceae, Lauraceae, Malpighiaceae, Meliaceae and Rubiaceae, among others, are highlighted in the present article. Promising results were obtained for extracts, fractions and secondary metabolites isolated from members of these families with cytotoxic, genotoxic, recombinogenic, antimicrobial, and leishmanicidal properties, in addition to larvicidal activities against Aedes aegypti and toxicity against the cattle tick. Therefore, this review about the work performed by PRONABio, emphasizes the potential of the biomes of Mato Grosso do Sul as sources of substances of medicinal and veterinary interest, and also relevant to public health.