Schisandra henryi(Schisandraceae) is a plant species endemic to Yunnan Province in China and is little known in Europe and America. To date, few studies, mainly performed by Chinese researchers, have been conducted onS. henryi. The chemical composition of this plant is dominated by lignans (dibenzocyclooctadiene, aryltetralin, dibenzylbutane), polyphenols (phenolic acids, flavonoids), triterpenoids, and nortriterpenoids. The research on the chemical profile ofS. henryishowed a similar chemical composition toS. chinensis—a globally known pharmacopoeial species with valuable medicinal properties whichis the best-known species of the genus Schisandra. The whole genus is characterized by the presence of the aforementioned specific dibenzocyclooctadiene lignans, known as “Schisandra lignans”. This paper was intended to provide a comprehensive review of the scientific literature published on the research conducted onS. henryi, with particular emphasis on the chemical composition and biological properties. Recently, a phytochemical, biological, and biotechnological study conducted by our team highlighted the great potential ofS. henryiin in vitro cultures. The biotechnological research revealed the possibilities of the use of biomass fromS. henryias an alternative to raw material that cannot be easily obtained from natural sites. Moreover, the characterization of dibenzocyclooctadiene lignans specific to the Schisandraceae family was provided. Except for several scientific studies which have confirmed the most valuable pharmacological properties of these lignans, hepatoprotective and hepatoregenerative, this article also reviews studies that have confirmed the anti-inflammatory, neuroprotective, anticancer, antiviral, antioxidant, cardioprotective, and anti-osteoporotic effects and their application for treating intestinal dysfunction.