Short Lecture "Metabolisation of Hypericum perforatum extract by human gut microbiota"

Hypericum perforatum L. is widely used for mild depression. Several clinical studies have been performed [1], and oral bioavailability of its key constituents is known [2] [3]. With an aim to investigate microbiome- mediated metabolisation, we subjected H. perforatum ethanolic extract to fermentation with human gut microbiota. As a first step, digestion in the upper GI tract was mimicked by successively incubating the extract with the respective enzyme and buffer mixes according to the Infogest protocol [4]. The Infogest intestinal phase was subsequently incubated with fecal samples from ten healthy donors (24h, anoxic, 37°C) [5]. An UHPLC-HRMS method was optimised for the analysis and annotation of the constituents present in the preparation, in digestive phases, and after fermentation. Analysis indicated that the levels of most annotated constituents, including flavonoids, phenylpropanoids, procyanidins, xanthones, and phloroglucinols, with the exception of hypericins, are stable towards the three Infogest digestive phases. However, subsequent fermentation with gut microbiota led to an intensive metabolisation of the constituents. Donors presented differences regarding the degree and velocity of metabolisation, however the majority of the annotated constituents have been metabolised by gut microbiota similarly in most donor samples, and several intermediate and final metabolites were formed. The newly formed metabolites, potentially possessing different pharmacokinetics and pharmacodynamics than the progenitor compounds, may provide new insights into the observed therapeutic effects of Hypericum extracts.

Publication History

Article published online:
16 November 2023

• References

• 1 www.ema.europa.eu/en/medicines/herba/hyperici-herba
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