Hop cones (Humuli Strobili) are the female inflorescences of hop plants (Humulus lupulus L.) belonging to the family Cannabaceae. They have been used as herbal remedies to treat mood and sleep disturbances, and mainly to add as a bittering ingredient in brewing process. Considerable interests on pharmacological and biological activities of hop cones have been focused on their major constituents, namely, phloroglucinols (humulone, lupulone), terpenes (myrcene, humulene), and prenylated flavonoids (xanthohumol, isoxanthohumol, 6-prenylnaringenin, and 8-prenylnaringenin). The present review describes and discusses biological activity profiles of these major compounds in the hop cones.