An ethnobotanical survey for a better knowledge of lactogenic plants has been conducted in Cascades region of Burkina Faso. Biological activities of the two most used plants were evaluated. The survey concerned 25 species classified into 22 genera and 19 families. The most represented families were Moraceae, Apocynaceae, Fabaceae-Caesalpinioideae and Malvaceae. The most used species were Euphorbia hirta, Calotropis procera and Ficus sycomorus with respectively 16.98%, 13.21% and 13.21% followed by Ficus platyphylla (9.43%) and Carica papaya, Holarrhena floribunda, Scoparia dulcis, Sorghum bicolor, each with 3.77% of frequency use. Plants organs mostly used for medicinal preparation were leaves, whole plant for herbaceous species, fruits and seeds. The main mode of medicinal preparation was decoction with 60.42% of frequency use. The most route of administration was oral (68.75%). Biological activities evaluation concerned Euphorbia hirta and Calotropis procera which were the most used plants. The acute toxicity of aqueous extracts of Calotropis procera (AECP) and Euphorbia hirta (AEEH) showed a LD50 of 2063 and 603 mg/kg body weight (b.w), respectively. These LD50 values permitted to classify these plants as slightly toxic herbal drugs. The uterotrophic test showed that the AECP and AEEH exhibited estrogenic activity. In conclusion, important medicinal plants in the Cascades region of Burkina Faso were used to stimulate or ameliorate lactation. However further studies must be conducted to confirm the traditional use of these plants.