Aristolochic acid is a group of chemical constituents with both toxicity and efficacy found in traditional herbal plants in the family of Aristolochaceae. Chinese traditional herbal medications containing aristolochic acid have been widely used in the treatment of many common diseases, but there has been a lot of controversy in clinical application because of its carcinogenic effect and toxic side-effects such as aristolochic acid nephropathy. Recently, aristolochic acid has been considered as an important factor in the high incidence of liver cancer. In order to understand the pharmacology and toxicology effect of aristolochic acid, this review summarized research status on the physical and chemical properties, toxic side-effects, pharmacological effects, and carcinogenic mechanism as well as in aspects of regulation of Chinese traditional herbal medications containing aristolochic acid at home and abroad, which would provide the pharmacological knowledge and Clinical effect for further researches on pharmacology and toxicology of aristolochic acid and its safe application.