Hops are a well-known source of resins, essential oils and polyphenolic substances, such as proanthocyanidins or prenylflavonoids with significant representatives of xanthohumol, isoxanthohumol, and 8-prenylnaringenine, and represent an essential ingredient in beer production. Recently, however, many additional bioactive effects of hop compounds have been investigated. A systematic review of the structure-function relationship between the individual hop-derived compounds and their bio-activity has been lacking. In this review we summarize some recent findings in this area from reports from our as well as other studies. It shows multiple bio-medical effects of the individual hop derived compounds, which can act individually, or in a synergistic manner. The hops can serve as a source of bio-active compounds in phyto-medicine and as such, more attention and detailed studies are warranted to utilize the broad spectrum of effects of individual compounds in future treatments.