There is a consensus that plants are great sources of metabolites with a broad variety of functions. This is particularly important because plants cannot run away from environmental conditions that can threat their existence. The numerous biological activities exhibited by plant natural products prompted humanity to use such substances or their derivatives for the treatment and/or prevention of diseases. The more we know the flora around the world the higher is the chance to find new lead compounds for the design of more potent drugs or nutraceuticals. This review first deals with Brazilian flora, contextualizing the most studied medicinal species and related patents. It also describes a compilation of relevant works based on the use of stress conditions to enhance the biosynthesis of valuable metabolites in cell cultures, tissue cultures (hairy roots) and whole plants by using native or crop plants around the world.