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Cytotoxic and anti-tumor activities of Inula sesquiterpenoids have been extensively studied since the 1970s. One promising compound, Japonicone A, a dimeric sesquiterpene lactone from traditional herb Inula japonica, has displayed potent in vitro and in vivo anti-tumor activity against Burkitt's lymphoma. Additionally, acetylbritannilactone is thought to be capable of suppressing the abnormal vascular smooth muscle cell proliferation, with the induction of apoptosis in vivo and in vitro. In this regard, it may be worthwhile further investigating acetylbritannilactone in patients with vascular restenosis. Furthermore, given the anti-inflammatory property of britanin, clinical studies on chronic bronchitis and asthma, using the ethanol extract of I. japonica, are currently underway in South Korea. However, despite demonstrating good therapeutic effects, additional pharmacological and toxicological studies are still needed.