The objective of this paper is to review the natural products and the pharmacological functions of Ganodermataceae family. Presently, studies on the bioactive components of Lingzhi are focused on polysaccharides and triterpenes/triterpenoids compounds. New Ganoderma polysaccharides, including their molecular weights, glycosyl residue compositions, glycosyl linkage and branches, are summarized in this paper. Also presented are new types of triterpenes and their characteristics from Lingzhi. Taking Ganoderma lucidum as an example, we reviewed its pharmacological functions in anti-tumor and immune-modulating activities for treating hypoglycemosis, hepatoprotection, and the effect on blood vessel system. Based on the advances in Lingzhi research in the past few decades, both G. lucidum and G. sinense are considered as the representative species of medicinal mushroom Lingzhi in China. Until 2001, G. tsugae was only advised to be used as the materials of the health products. The biologically-active components related to pharmacological functions of these three species were studied more than other Ganodermataceae family species; however, which have been used in less modern folk medicine.