Aristolochic acid analogues (AAAs) are a class of nitrophenanthrene derivatives predominantly occurring in Aristolochiaceae plants. Over the past decades, academic research has mostly focused on its strong adverse reactions such as nephrotoxicity and carcinogenicity. In contrast, their potential pharmacological activities—including anti-inflammatory, analgesic, and antitumor effects—have remained relatively underexplored, resulting in an imbalanced understanding of this compound class. In the face of the dual characteristics of toxicity and efficacy of this type of component, how to balance its toxicity and medicinal value is the key. Methods such as processing, compatibility, and structural modification may reduce adverse reactions, which could provide guarantees for the safe use of such components and traditional Chinese medicine. This review integrates current global advances in AAAs research, with a particular focus on their pharmacological activities and detoxification strategies, to provide references for the clinical application of drugs containing AAAs.

aristolochic acids analogues  /  detoxification  /  anti-inflammatory  /  analgesic  /  antitumor