Magnolol is a conventional polyphenolic bioactive substance extracted and isolated from the stem bark of the Magnoliaceae plant Magnolia officinalis Rehd.et Wils. It exhibited a wide range of biological effects, such as pesticidal, antiinflammatory, anticancer, antimicrobial, antioxidant, and neuroprotective activities. Additionally, since magnolol has many modification sites, its derivatives are also varied. In order to pave the way for continued development of magnolol and its analogs, it is necessary to summarize their current research advances by combination of the most recent and existing data. Herein recent advances on magnolol and its derivatives on extraction, purification, chemical synthesis, biosynthesis, structural modification, and biological activities were reviewed. The goal is to serve as a reference for future high value–added applications of magnolol and its derivatives in the pharmaceutical and agricultural fields.