Abstract: Objective To collate the ancient and modern toxicity reduction methods of Dichroa Radix, explore the regularities and effective strategies for toxicity reduction, thereby providing a reference for establishing a toxicity-reduction and control process for Dichroa Radix based on its unique “toxicity-efficacy”characteristics. Method By collating the toxicity-reducing methods for Dichroa Radix recorded in ancient medical classics, including processing, compatibility, and syndrome-based medication, as well as, combining them with modern processing techniques, studies on the toxicity efficacy relationship, and combination drug toxicity reduction research, the relevant data were analyzed. Results The toxicity-reducing methods recorded in ancient texts primarily involved processing and compatibility. The processing methods gradually evolved from wine-processing to the combined use of multiple excipients. Modern studies have clearly indicated that quinazolinone alkaloids are not only the active components responsible for the antimalarial and other therapeutic effects of Dichroa Radix, but also the main toxic substrates, exhibiting a typical characteristic of “integration of toxicity and efficacy.” Experimental evidence has confirmed that processing can reduce the content of febrifugine, while compatibility can alleviate adverse reactions such as vomiting, and the related toxicity-reducing mechanisms have been elucidated. Conclusion The methods for reducing the toxicity of Dichroa Radix have a long history and diverse forms. The integration of traditional experience with modern research has laid a foundation for its safe clinical application. A thorough elucidation of the molecular basis and target underlying the reduction of toxicity and enhancement of efficacy in active ingredients characterized by the “integration of toxicity and efficacy”, combined with modern formulation technologies to optimize manufacturing processes, is helpful for advancing the modern development and precise application of Dichroa Radix.

Key words: Dichroae Radix, Quinazolinone, Alkaloids, Antimalarial, Processing, Compatibility, Toxicity Reduction, Efficacy Enhancement