Pharmacokinetic properties of phytochemicals in Hypericum perforatum influence efficacy of regulating oxidative stress

Abstract

Background: Hypericum perforatum is used in ethnopharmacology and has recently become popular in conventional medicine for treatment of mild to moderate depression. The abundance of potentially functional phytochemicals and their broader utilizations in traditional medicine suggests that ingestion of H. perforatum may impart additional secondary health benefits.

Hypothesis/purpose: Considering that many phytochemicals are known to display antioxidant activity, it was hypothesized that H. perforatum ingestion may inhibit oxidative stress and inflammation (OSI) which occurs in transient cycles following exercise and consumption of meals. The aim of this study was to explore the pharmacokinetics of H. perforatum phytochemicals after ingestion to predict the absorption timing of putative medicinal phytochemicals.

Study design/methods: In silico analyses of previously published plant extract phytochemical profiles were performed, wherein the Phytochemical Absorption Prediction (PCAP) model was used to predict the pharmacokinetics of phytochemicals. The predicted times for phytochemicals to reach maximum plasma concentration (T_max), and associated antioxidant activities, were compared to prior clinical in vivo studies to assess the accuracy and applicability of predictions.

Results: The PCAP model identified that phytochemicals with antioxidant activity concurrently accumulate in plasma with T_max in the range of 1.6-2.3 h after ingestion. Comparison with previously published results identified that attenuation of OSI following H. perforatum ingestion aligns with the predicted T_max of antioxidant phytochemicals.

Conclusion: Based on these results it is therefore recommended that H. perforatum administration occurs 2 h before meals to provide optimal secondary health benefits associated with inhibition of postprandial stress. Additionally, these results highlight the use of in silico analyses to inform ingestion time and optimize the health benefits from ingestion of plant-based foods and medicines.

Keywords: Antioxidant fingerprint; Bio-matching; Functional fingerprint; Medicinal plants; PCAP model; St. John's Wort.