Objective To study the effect of tiaoyuansan on autistic rat behavior as well as proinflammatory factors and GABA in brain tissue and its therapeutic effect. Methods Forty VPA-induced autistic rats were divided into a model control group and three dosage groups of tiaoyuansan (2. 5, 5 and 10 g/ kg). Ten normal rats were used as the normal control group. Tiaoyuansan at various concentrations or water were administered orally to the corresponding groups once a day for 30 days. The open field test and the three chamber social test were performed. The cerebral cortex and hippocampus were collected to determine the contents of GABA, IL-1β and IL-6. Results Compared with the findings in the normal control group, in the model control group, the percentage of distance and time in the central area were decreased(P=0. 026, P= 0. 044) and the percentage of distance and time in the perimeter area were increased (P= 0. 026, P=0. 044) in the open field test, the times of searching for unfamiliar rats were decreased (phase II: P=0. 011, phase III: P=0. 041) in the three chamber social test, GABA in the cerebral cortex was increased (P=0. 002), and IL-1β and IL-6 in the hippocampus were increased (P=0. 011, P=0. 003). Compared with the findings in the model control group, in the high dosage group, the percentage of distance and time in the central area were increased (P=0. 007, P=0. 021) and the percentage of distance and time in the perimeter area were decreased (P= 0. 007, P= 0. 021) in the open field test, the times of searching for unfamiliar rats were increased (phase II: P=0. 032, phase III: P=0. 000) in three chamber social test, GABA in the cerebral cortex was decreased (P=0. 006), and IL-1β and IL-6 in the hippocampus were decreased (P=0. 001, P=0. 002). Conclusions Tiaoyuansan reduces stereotypical behavior and increases the social times of VPA-induced autistic rats. Therefore, it has certain therapeutic effect on autism.