Since ancient times, coffee has been one of the widely consumed beverages all over the world. It is renowned for its refreshing, body stimulating effect and unique taste. It belongs to the genus Coffea, class Dicotyledoneae, order Rubiales and family Rubiaceae. Coffee is a natural complex chemical mixture constituted of several compounds. It is accountable for numerous bioactivities and a number of compounds exhibit these effects. Some of the significant bioactivities documented are anti-oxidant, anti-mutagenic, anti-carcinogenic and anti-obesity properties. The varying constituents of coffee responsible for the chemo-protective effects are mainly polyphenols including chlorogenic acids and their degradation products. Others include caffeine, diterpenoid alcohols such as kahweol, cafestol and other phenolics. Coffee has been reported to exhibit both protective and adverse effects on various body systems such as skeletal (bone), reproductive, nervous and cardiovascular systems; homocysteine and cholesterol levels and so on. The present review provides an overview of the coffee and its constituents; and their relationship with various diseases. Recent investigations on its health benefits, with focus on their anti-cancer, anti-obesity properties and effect on cardiovascular diseases have also been discussed.