The genus of Oplopanax, which belongs to the family Araliaceae, comprises only three species, i.e., Oplopanax elatus (Nakai) native to temperate regions of the Northern China [1] [2], O. horridus (Smith) Miq. exclusively originated and distributed in North America [3] [4], and O. japonicus (Nakai) Nakai only localized in Japan [5]. Among them, O. elatus has been used for treating neurasthenia, hypopiesis, schizophrenia, cardiovascular disorders, diabetes mellitus, and rheumatism by the local people in China [6] [7], while O. horridus, known as _Devil_s Club_, whose inner bark of aerial stems is probably the most important spiritual and medicinal herb for many indigenous tribes in North America [8 – 10]. In addition, these roots are also commonly used to treat arthritis, digestive tract ailments, fever, dandruff, respiratory ailments, headaches, and cancer by First Nations peoples and many cultural groups [11] [12]. It is nowadays being utilized and marketed as a ginseng-like herbal medicine [13]. O. japonicus was used for skin-care preparation for improving skin lineae atrophicae such as striae gravidarum [14]. Recently, increasing attention has been paid to the Oplopanax genus and its chemical constituents because of their diverse features, such as antioxidant, antimycobacterial, antifungal, antituberculosis, antibiotic, lineae atrophicae-relieving, antipsoriasis, and anticancer activities [9] [15 – 19]. In this review, we compile the phytochemical progress including all the compounds isolated from the genus Oplopanax over the past decades. The biological activities of these ingredients are also discussed.