In vitro assays in natural products research – a matter of concentration and relevance to in vivo administration using resveratrol, α-mangostin/γ-mangostin and xanthohumol as examples

Abstract

Herbal or botanical dietary supplements are an ever increasingly popular category of products in the United States and around the world. In vitro data can provide meaningful insight into the potential target and mechanism of action for a proposed active compound but may also be misused to promote a supplement to consumers with unverified health claims. In vitro data need to be considered alongside pharmacokinetic and pharmacodynamic data in preclinical animal and clinical human trials. While considerable activity of compounds and extracts in vitro may lead to further testing in vivo, in many instances, concentrations tested in cell lines or isolated targets are not achievable at the target site in vivo. Thus, whether the in vitro data are relevant to humans after oral administration is questionable. This review will discuss this discrepancy using in vitro and in vivo data of resveratrol, xanthones (α-mangostin and γ-mangostin) and xanthohumol.

Keywords:

• In vitro assay
• in vitro–in vivo correlation
• pharmacodynamics
• pharmacokinetics
• natural products