Herbal medicines are a great deal of attention to investigate emphasizing on health benefits. Alpha-hederin (α-HN) is a plant-derived saponin having a number of important biological activities. However, the studies on this component are not enough. This revision aims at summarizing the biological roles of α-HN including possible mechanism of actions. This study is made on the basis of evidence observed in electronic databases, Pubmed, Science Direct, Scopus, Web of Science and miscellaneous. A number of pharmacological actions of α-HN have been investigated, including antioxidant, anti-inflammatory, antiarthritic, bronchiolytic, antifungal, and antiparasitic activities. It also has anti-histaminic and antitumor activities. In addition, desmutagenic and hepatoprotective potentials also have been shown. Physiological zinc depletion and calcium influx are the two observed toxic events in α-HN treated rodents. However, it has synergistic effects with other chemicals, while antagonistic to a number of toxicants. The α-HN may be an interesting phytochemical, therefore, more researches are necessary for it.