摘要:Background: Herbs might affect the homeostasis of bile acids through influence of multiple metabolic pathways of bile acids. Aim: The present study aims to investigate the inhibition of cryptotanshinone towards the glucuronidation of LCA, trying to indicate the possible influence of cryptotanshinone-containing herbs towards the homeostasis of bile acids. Methods: The LCA-3-glucuronidation and LCA-24-glucuronidation reaction was monitored by LC-MS. Results: Initial screening showed that 100 μM of cryptotanshinone inhibited LCA-24-glucuronidation and LCA-3-glucuronidation reaction activity by 82.6% and 79.1%, respectively. This kind of inhibition behaviour exerted cryptotanshinone concentrations-dependent and LCA concentrations-independent inhibition behaviour. Conclusion: All these data indicated the possibility of cryptotanshinone’s influence towards the bile acids metabolism and homeostasis of bile acids.