Background and Introduction: Sesquiterpene lactones are a class of secondary metabolite
that contains sesquiterpenoids and lactone ring as pharmacophore moiety. A large group of bioactive
secondary metabolites such as phytopharmaceuticals belong to this category. From the Asteraceae
family-based medicinal plants, more than 5,000 sesquiterpene lactones have been reported so
far. Sesquiterpene lactone-based pharmacophore moieties hold promise for broad-spectrum biological
activities against cancer, inflammation, parasitic, bacterial, fungal, viral infection and other functional
disorders. Moreover, these moiety based phytocompounds have been highlighted with a new
dimension in the natural drug discovery program worldwide after the 2015 Medicine Nobel Prize
achieved by the Artemisinin researchers.
Objective: These bitter substances often contain an α, β-unsaturated-γ-lactone as a major structural
backbone, which in recent studies has been explored to be associated with anti-tumor, cytotoxic, and
anti-inflammatory action. Recently, the use of sesquiterpene lactones as phytomedicine has been
increased. This study will review the prospect of sesquiterpene lactones against inflammation and
Methods: Hence, we emphasized on the different features of this moiety by incorporating its structural
diversity on biological activities to explore structure-activity relationships (SAR) against inflammation
Results: How the dual mode of action such as anti-inflammatory and anti-cancer has been exhibitedby
these phytopharmaceuticals will be forecasted in this study. Furthermore, the correlation of
anti-inflammatory and anti-cancer activity executed by the sesquiterpene lactones for fruitful phytotherapy
will also be revealed in the present review in the milieu of pharmacophore activity relation
and pharmacodynamics study as well.
Conclusion: So, these metabolites are paramount in phytopharmacological aspects. The present discussion
on the future prospect of this moiety based on the reported literature could be a guide for
anti-inflammatory and anti-cancer drug discovery programs for the upcoming researchers.