Abstract:[Background] Ganoderma lobatum is a species of Ganoderma spp., which and can be used as a medicinal herb in the folk. However, there is no scientific research on the chemical composition and pharmacological activity of Ganoderma lobatum. [Objective] To explore the medicinal value of Ganoderma lobatum, the antitumor and immunological activity of Ganoderma lobatum were studied, with the Ganoderma lingzhi as a reference. [Methods] Triterpenoids and polysaccharides in the two species of Ganoderma were analyzed by chemical and instrumental analysis, and their antitumor and immunological activity were studied. [Results] There were not significantly different in the contents of triterpenoids in Ganoderma lobatum and Ganoderma lingzhi, which were 1.14% and 1.21%, respectively. However, the kinds of triterpenoids in the two species of Ganoderma was distinctive. The content of polysaccharides in Ganoderma lobatum were slightly higher than that in Ganoderma lingzhi, which were 3.60% and 2.67%, respectively. Meanwhile, there was a difference in the molecular weight distribution of polysaccharides in the two fruiting bodies. Both of the ethanol extracts had inhibitory activity on K562 and SW620 cell. Among them, Ganoderma lobatum has a strong inhibitory activity on SW620 cells with IC50 of 52.5 μg/mL. Furthermore, both of them aqueous extracts could promote RAW 264.7 cells to release NO, which illustrated that both have certain immunological activity. [Conclusion] Ganoderma lobatum has good antitumor and immunological activity, which could be used as a source of raw material potential materials for medicinal development.