aristolochic acid I

Aristolochic acid I is a **naturally occurring nitrophenanthrene carboxylic acid** and the most abundant member of the aristolochic acids found in herbs of the Aristolochiaceae family, such as Aristolochia and Asarum[1][4]. It is a **highly carcinogenic, mutagenic, and nephrotoxic phytochemical**, historically present in herbal remedies, especially traditional Chinese medicine[1]. AA-I is absorbed orally, distributed systemically, and primarily metabolized by phase I nitroreduction to aristolactam I, which forms **stable DNA adducts** leading to A→T transversion mutations and selective TP53 tumor suppressor gene mutations[1][3][5]. It acts as a **phospholipase A2 inhibitor** and is bioactivated to reactive N-acylnitrenium ions that alkylate DNA, driving its mutagenic and carcinogenic effects[3][5]. AA-I has been definitively linked to urothelial malignancy, kidney failure, and aristolochic acid nephropathy (AAN)[1][5]. It is not approved for any pharmaceutical indication and is considered a toxin, not a therapeutic drug.

Other names

8-methoxy-6-nitrophenanthrol(3,4-d)-1,3-dioxide-5-carboxylic acidAristolochic acid AAristolochic acid I methyl ester (used for the methylated derivative)Aristolochic acid-IAristolochic acids (occasionally, but refers to a mixture)Birthwort (traditional/herbal reference)