Hyperdioxanes, dibenzo-1,4-dioxane derivatives from the roots of Hypericum ascyron

AbstractSix dibenzo-1,4-dioxane derivatives (1–6) were isolated from the roots of a Hypericaceous plantHypericum ascyron. Spectroscopic analyses revealed2 and4–6 to be new compounds. The partial racemic natures of1–3 were concluded by chiral HPLC analyses, while5 was confirmed to be a racemate. The absolute configurations1–4 were deduced on the basis of ECD calculations. Biological activity evaluation of the dibenzo-1,4-dioxane derivatives along with two related compounds: hyperdioxanes A (7) and B (8), previously isolated from the same plant material by our group demonstrated that7 exhibit an anti-HIV activity (IC50 5.3  μM, TI 7.2) while8 showed an inhibitory effect on IL-1 β production (inhibition rate: 72.3% at 6.3 μM) from LPS-stimulated microglial cells.
Source: Journal of Natural Medicines - Category: Drugs & Pharmacology Source Type: research