The objectives of the current study were to evaluate the quality and quantity of phenolic constituents (as biomarkers) in acclimatized Pelargonium sidoides plants using ultra performance liquid chromatography (UPLC-MS/MS) analysis and to compare their respective pharmacological activity with that of wild plants. In addition, the phytochemical and pharmacological properties of aerial parts were compared to the predominantly used underground tubers for both acclimatized and wild plants.