Abstract: Objective By combing pertinent literature and summarizing the current states of chemical composition of Bupleurum Chinense related with its efficacy and toxicity, to identify its effective and toxical composition, offer the accordance and research ideas for further research on the relationship between efficacy, toxicity and chemical composition of Bupleurum Chinense. Methods The related references in recent 20 years at home and abroad about Bupleurum Chinense were analyzed, collated and summarized. Results The main chemical composition of was saikosaponin, naphtha, flavonoids, polysaccharide and plant sterol, etc, and the saikosapoin and naphtha were the main chemical compositions; the pharmacological activity research was focused on saikosaponin, naphtha, flavonoids and polysaccharide; the toxicity research was focused on the extracts of , saikosaponin and naphtha, and the toxical target organ was liver. Conclusion The saikosaponin and naphtha were not only effective compositions that protected the liver, but also the toxical composition that injured of the liver. How to maximize the "shuganjieyu" efficacy and limit the hepatotoxicity of "Chinense robbing hepatic yin" were the key that restricted the chemical composition research. The efficacy and toxicity research of should be put on the background of traditional Chinese medicine syndrome to make the comprehensive evaluation and scientific cognitive, to explore the "effective treatment window " and "drug safety window", and to insure the safety and effectiveness of clinical medication.

Key words: chemical composition, efficacy, toxicity