ReviewInflammation research : official journal of the European Histamine Research Society ... [et al.]2022
Japonicone A and related dimeric sesquiterpene lactones: molecular targets and mechanisms of anticancer activity.
Review in Inflammation research : official journal of the European Histamine Research Society ... [et al.], 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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3 citing papers in PubMed, 9 citations in OpenAlex.
- A Computational Investigation of Four Sesquiterpene [4+2] Trimers, Inubritantrimers A-D, and Their Synthetic Intermediates Isolated fromMolecules (Basel, Switzerland) · 2026Article
- Research progress on antitumor mechanisms and molecular targets of Inula sesquiterpene lactones.Chinese medicine · 2023Review
- Article
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2 authors at 2 institutions in 1 country.
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Abstract
OBJECTIVE AND
designJaponicone A (Jap-A) is a sesquiterpene lactone (SL) dimer isolated from the plant Inula japonica Thunb. and the leading compound in the japonicone series of SL dimers which comprises 25 members (Jap-A to Jap-Y). We have analyzed the anticancer properties of Jap-A and the associated molecular targets.
methodsAll literature data on japonicones and related SL dimers, including inulanolide A (Inu-A) and lineariifolianoid A (Lin-A) have been analyzed. Molecular models of the compound/target interactions were constructed to support our analysis.
resultsInulae Flos (Xuan Fu Hua) is used in traditional medicine in China and Korea to treat inflammatory diseases. The plant contains diverse japonicones and structurally related SL dimers. The interactions of Jap-A with the two main proteins, the pro-inflammatory cytokine TNF-α and the ubiquitin ligase MDM2, are at the origin of the anti-inflammatory and anticancer effects. Molecular docking analyses suggest that Inu-A is better adapted than Lin-A and Jap-A to form stable complexes with both TNF-α and MDM2. Jap-A exhibits marked capacities to inhibit cancer cell proliferation and dissemination and to trigger apoptosis, both in vitro and in vivo in several tumor models in mice. Its analogue Inu-A is more potent, functioning as a dual inhibitor of the MDM2-NFAT1 pathway.
conclusionThis review shed some new light on the molecular targets and potential therapeutic benefits of these SL dimers and should help the design of novel anticancer agents derived from these compounds.
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