Chapter 15 Phytochemicals in drug discovery

Abstract

Here, we summarize phytochemicals, their health benefits, pharmacokinetics and pharmacodynamic characteristics, toxicity, and their application in the development of lead compounds and related drug analogs. Natural products and their structural analogues have significant contributions to pharmacotherapy, especially for the treatment of cancer, malaria, diabetes, and infectious diseases. Drug discovery employing phytochemicals obtained from different plant sources is the basis of new drug discovery and lead compound development. The process of drug discovery involves the identification, isolation, and purification of phytochemicals from the selected plant species, biochemical characterization, and pharmacological investigation followed by preclinical and clinical trials. Drug discovery also requires bioinformatics computational tools and structure elucidation by cutting-edge analytical techniques such as high-performance liquid chromatography, gas chromatography, and mass spectrometry. The phytochemicals sometimes require modification in the native structure for the enhancement of biological activity and stability. Consequently, lead identification and new drug discovery is an important toolbox for tackling antimicrobial resistance. At present, phytochemicals are the main pillar in new drug discovery and the pharmaceutical industry revolution. Therefore, new opportunities would be expected in the new drug discovery using phytochemicals in near future.