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Synephrine, a natural product also known as deoxyepinephrine, exists in Rutaceae plants and is widely distributed in China. In addition to natural sources, synephrine may also be obtained by means of chemical synthesis and genetic engineering methods. In recent years, extensive studies on the biological activity of synephrine have shown that this compound has significant anti-cancer, anti-depressant, anti-Parkinson and other effects. In addition, synephrine exhibits good metabolic regulatory activity and thereby is widely used in weight loss. As a foodborne compound, synephrine has the outstanding features of low toxicity and side effects. In this review, we will elaborate the pharmacological activity and toxic side effects of synephrine, as well as its new applications in the field of biomedicine.