Objective:To discuss the synergistic effects and mechanism of channel ushering drug Chaihu (Bupleuri Radix) on tissue inhibitor of metalloproteinases-1 (TIMP-1) and transforming growth factor-β1 (TGF-β1) in rats with pancreatic fibrosis. Methods50 SD rats were randomly divided into the model group, sham operation group, Chaihu group, Dahuang (Rhei Radix et Rhizoma)-Danshen (Salviae Miltiorrhizae Radix et Rhizoma) group and Chaihu-Dahuang-Danshen group. In sham operation group, the rats were performed laparotomy and then the abdominal cavities was closed without any operation, while in the model group and three drug treatment groups, the rat model of pancreatic fibrosis was established by pancreatic duct ligation combined with cerulein by intraperitoneal injection. Before and after operation, three drug treatment groups were treated with Chaihu, Dahuang-Danshen and Chaihu-Dahuang-Danshen by intragastric administration at doses of 1.38g·kg-1d-1, 3.04 g·kg-1d-1 and 4.11 g·kg-1d-1, respectively, with a course of 3 days. Rats were sacrificed and the samples were collected on the 4th day after operation. The expression of serum TIMP-1 was measured by ELISA and the expression of TGF-β1 in pancreas was measured by immunohistochemistry. The mRNA and protein expression levels of TGF-β1 in pancreas were detected by Real-time PCR and Western blot, respectively.  Results:Compared with the model group, the level of serum TIMP-1 was decreased in three drug treatment groups (P<0.01). Compared with Chaihu group, the level of TIMP-1 was decreased in Chaihu-Danhuang-Dansheng group (P<0.01). Compared with Dahuang-Danshen group, the level of TIMP-1 was decreased in Chaihu-Danhuang-Dansheng group (P<0.01). Compared with the model group, the mRNA and protein expressions of TGF-β1 were decreased in three drug treatment groups (P<0.01). Compared with Chaihu group, the mRNA and protein expressions of TGF-β1 were decreased in Chaihu-Dahuang-Danshen group (P<0.01), and the protein expression of TGF-β1 was decreased in Dahuang-Danshen group (P<0.01). The protein expression of TGF-β1 was decreased in Chaihu-Dahuang-Danshen group compared with Dahuang-Danshen group (P<0.01).  Conclusion:“Down-regulating TGF-β1 expression- inhibiting PSC activation-reducing ECM synthesis” and “down-regulating TGF-β1 expression- inhibiting TIMP secretion-promoting ECM degradation” may be two main lines in anti-pancreatic fibrosis effects of Chaihu, Dahuang-Danshen and Chaihu-Dahuang-Danshen. The regulation effects of these three drugs on TGF-β1 play a dual role in ECM synthesis and degradation. Chaihu shows some synergism on the anti-pancreatic fibrosis effects of Dahuang-Danshen, which mainly displays in inhibiting TIMP-1 secretion and down-regulating protein expression of TGF-β1.