Natural products, well known for unique chemical diversity and bioactivity, have continued to offer templates for the development of novel scaffolds of drugs. With the remarkable developments in the areas of separation science, spectroscopic techniques, microplate-based ultrasensitive in vitro assays and high-throughput screening (HTS) technologies, natural products research has gained momentum in recent years. The pre-isolation analyses of crude extracts or fraction from different natural matrices, isolation, online detection and dereplication of natural products, studies on chemotaxonomy and biosynthesis, chemical finger-printing, quality control of herbal products, and metabolomic studies have now become much easier than ever before because of the availability of a number of modern sophisticated hyphenated techniques, e.g., GC-MS, LC-PDA, LC-MS, LC-FTIR, LC-NMR, LC-NMR-MS, and CE-MS. This introductory chapter presents a general overview of the processes involved in natural products research, starting from extraction and isolation to elucidation of the structures of purified natural products and their bioactivity.