Morus is a plant genus of the family Moraceae, most of which is used as a decoction in traditional medicines for the treatment of cough, bronchitis, pulmonary diseases and reduces the plasma sugar level. Many studies in Morus phytochemistry have contributed to the discovery of Diels-Alder-type adducts, arylbenzofurans, and flavonoids with antioxidant, antihyperglycemic, antihypertensive, antihyperlipidemic, and anti-inflammatory activities. The purpose of this article was to offers an account of the updated knowledge on the phytochemicals and pharmacological activities of these compounds. This review will help to fully understanding the efficacy and pave the way for further explore the comprehensive use of Morus. We conclude that Morus needs further reports in the identification of bioactive constituents and strengthen the claim of folk medicines.