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**Isopetasin** is a bioactive sesquiterpene found principally in Petasites species, especially *Petasites hybridus* and *Petasites formosanus*, and is part of the terpenoid family[10]. It possesses notable anti-inflammatory, analgesic, and antispasmodic actions, and has been identified as an active component responsible for anti-migraine effects in butterbur extracts[2][4][10]. Mechanistically, isopetasin acts as a selective agonist of the TRPA1 ion channel (Transient receptor potential ankyrin 1), thus desensitizing peptidergic nociceptors[2][4]. It also exhibits cytotoxic activity toward multidrug-resistant cancer cell models by directly inhibiting the P-glycoprotein (ABCB1), resulting in increased drug accumulation, mitochondrial stress, reactive oxygen species (ROS) generation, and apoptosis[7]. The compound is primarily researched for migraine prevention, but also investigated in cancer models.
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