A new patent regarding the discovery of natural compounds with antifungal properties has come out of a research collaboration between the Department of Physics of the University of Trento (UniTrento) and the Food Quality and Nutrition Department of the Edmund Mach Foundation (FEM). The research group coordinated by the writer and the group coordinated by Dr Fulvio Mattivi (FEM) have recently isolated new metabolites belonging to the class of acylphloroglucinols from the plant Hypericum mexicanum, belonging to the family of Hypericaceae.
Through extensive use of modern chromatographic and spectroscopic methods (Nuclear Magnetic Resonance and Mass Spectrometry) we succeeded in first purifying these natural organic compounds and then in establishing their molecular structure. We have also demonstrated that these compounds have a high enough level of biological activity to make them of interest for pharmaceutical applications. The biological tests showed strong antifungal activity and weak, if not absent, cytotoxicity. These products are active against important pathogenic fungi (such as Candida sp.), in particular against strains that are resistant to treatment with the powerful antifungal fluconazole, while being substantially innocuous for the cells of our organism.
Use of extracts from plants of the genus Hypericum has historically been widespread in the medicine of many countries for the treatment of various pathologies. The multiple pharmacological properties associated with treatments containing Hypericum extracts can be explained by the great biological diversity of the species belonging to this genus, and especially by the enormous chemical diversity of the secondary metabolites biosynthesised by these plant species. However, it is extremely difficult to associate a particular biological response to a precise class of compounds when biological testing uses crude organic extracts. The added value of our discovery is that we have assigned a precise chemical structure to the compounds responsible for this biological activity. This knowledge now allows us to be independent of the availability of the plant itself and to consider large scale preparation through the methodologies of total organic synthesis. This approach would also enable the creation of a library of synthetic analogues with greater biological activity or greater ease of administration.
The molecules described in this patent and the pharmaceutical formulations including acylphloroglucinols isolated from Hypericum mexicanum or other sources, or obtained through synthesis, are therefore a new and effective therapeutic tool for the treatment of fungal infections resistant to drugs already on the market. Among the advantages are its lack of cytotoxicity, strong antifungal activity and effectiveness against strains resistant to fluconazole.