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In this review, an effort towards the presentation of an all-around account of the recent progress on the natural product, aloperine is made, and the antivirus structure-activity relationship of its derivatives is also summarized comprehensively. In addition, the principal pharmacological effects and corresponding molecular mechanisms of aloperine are discussed. Some new modification directions of aloperine are given in the end, which might be brief guidance for further investigations on the natural product aloperine.