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Background: The popular drink, coffee (Coffea arabica) is under the great attention of late because of its promising pharmacological potential. Caffeine (the major constituent of coffee) is known for its prominent psychoactive impact. This review aims at highlighting the therapeutic potentials of caffeine and other five coffee components viz. caffeic acid, chlorogenic acids, cafestol, ferulic acid and kahweol and their mechanisms of action., Methods: An up-to-date search was made with selected keywords in PubMed, Science Direct, Web of Science, Scopus, The American Chemical Society and miscellaneous databases (e.g., Google Scholar) for the published literature on the selected topic., Results: A number of pharmacological activities are attributed to these components that include anti-oxidant, antiinflammatory, immunomodulatory, anti-microbial, anti-cancer, cardioprotective and neuroprotective effects. In addition, osteogenesis (kahweol), anti-diabetic (caffeine, chlorogenic acid and ferulic acid) and hepatoprotective (chlorogenic acid) activities have also been reported by some of these components in the scientific literature. Caffeine has also been noted for adverse effect on the development of the brain at early stages and reproductive systems., Conclusion: A more advanced pre-clinical and clinical trials are recommended to investigate the safety profiles of these coffee components before their use as possible therapeutics., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)