1,3,7-Trihydroxyxanthone is a compound isolated from Polygalae Radix, a medicinal herb frequently applied for treatment of psychiatric disordres with symptoms of forgetfulness and depression in ancient China. In current research, this compound was applied onto rat astrocyte primary cultures in exploring the action mechanisms of 1,3,7-trihydroxyxanthone on regulating synthesis of neurotrophic factors. It was found that 1,3,7-trihydroxyxanthone could significantly stimulate the expression of NGF and BDNF in dose-dependent manners: the stimulation was both in mRNA and protein levels. Furthermore, 1,3,7-trihydroxyxanthone might fulfill this effect by regulating critical enzymes, such as plasminogen, tissue plasminogen activator, neuroserpin and tissue inhibitor of metalloproteinases in metabolic pathway of neurotrophic factors. Besides, inhibitors of cAMP- and ERK-dependent pathways, which implied the possible signaling pathway, could reverse this inducing effect. These results might support the potentiality of 1,3,7-trihydroxyxanthone in drug development in treating psychiatric disorders.