The main active ingredients in lotus leaves were introduced in this review, including flavonoids, alkaloids, volatile oils, terpenoids, polysaccharides, and organic acids. The pharmacological functions of lotus leaves, such as lipid-lowering and anti-obesity activities, anti-oxidant, anti-bacterial, and blood-lowering activities, protective effects of the cardiovascular system, nervous system, and liver, and anti-tumor activity were also summarized. The relative research and application were prospected in order to provide references for the comprehensive utilization of lotus leaf resources.