Helichrysum species (Asteraceae) are renowned for their diverse phytochemical profiles and traditional medicinal applications. Among their specialized metabolites, phloroglucinol-α-pyrone derivatives represent a structurally unique and pharmacologically significant class of compounds. This review consolidates over five decades of phytochemical research, documenting 52 distinct compounds isolated from 11 Helichrysum species across the Mediterranean, African, and Iranian regions. The compounds are organized into structural subclasses, including monopyrones, dipyrones, and various phloroglucinol derivatives distinguished by their molecular scaffolds. Isolation yields reported in the literature range from trace amounts to relatively abundant constituents (0.48% w / w ), with arzanol emerging as the most extensively studied compound. Bioactivity profiles reveal anti-inflammatory, antimicrobial, antioxidant, and antiparasitic properties, with arzanol demonstrating potent dual inhibition of mPGES-1 and 5-LOX. This review provides comprehensive reference data for future investigations into the chemistry and therapeutic potential of α-pyrone secondary metabolites from Helichrysum species.

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Background Natural extracts have played an important role in the prevention and treatment of diseases and are important sources for drug discovery. However, to be effectively used in these processes, natural extracts must be characterized through the identification of their active compounds and their modes of action. Methodology/principal findings From an initial set of 29,779 natural products that are annotated with their natural source and using a previously developed virtual screening procedure (carefully validated experimentally), we have predicted as potential peroxisome proliferators-activated receptor gamma (PPARγ) partial agonists 12 molecules from 11 extracts known to have antidiabetic activity. Six of these molecules are similar to molecules with described antidiabetic activity but whose mechanism of action is unknown. Therefore, it is plausible that these 12 molecules could be the bioactive molecules responsible, at least in part, for the antidiabetic activity of the extracts containing them. In addition, we have also identified as potential PPARγ partial agonists 10 molecules from 16 plants with undescribed antidiabetic activity but that are related (i.e., they are from the same genus) to plants with known antidiabetic properties. None of the 22 molecules that we predict as PPARγ partial agonists show chemical similarity with a group of 211 known PPARγ partial agonists obtained from the literature. Conclusions/significance Our results provide a new hypothesis about the active molecules of natural extracts with antidiabetic properties and their mode of action. We also suggest plants with undescribed antidiabetic activity that may contain PPARγ partial agonists. These plants represent a new source of potential antidiabetic extracts. Consequently, our work opens the door to the discovery of new antidiabetic extracts and molecules that can be of use, for instance, in the design of new antidiabetic drugs or functional foods focused towards the prevention/treatment of type 2 Diabetes Mellitus.

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