Background: Hibiscus sabdariffa, Lippia citriodora, Rosmarinus officinalis and Olea europaea, are rich
in bioactive compounds that represent most of the phenolic compounds’ families and have exhibited potential benefits
in human health. These plants have been used in folk medicine for their potential therapeutic properties in human
chronic diseases. Recent evidence leads to postulate that polyphenols may account for such effects. Nevertheless, the
compounds or metabolites that are responsible for reaching the molecular targets are unknown.
Objective: data based on studies directly using complex extracts on cellular models, without considering metabolic
aspects, have limited applicability. In contrast, studies exploring the absorption process, metabolites in the blood
circulation and tissues have become essential to identify the intracellular final effectors that are responsible for extracts
bioactivity. Once the cellular metabolites are identified using high-resolution mass spectrometry, docking
techniques suppose a unique tool for virtually screening a large number of compounds on selected targets in order to
elucidate their potential mechanisms.
Results: we provide an updated overview of the in vitro and in vivo studies on the toxicity, absorption, permeability,
pharmacokinetics and cellular metabolism of bioactive compounds derived from the abovementioned plants to identify
the potential compounds that are responsible for the observed health effects.
Conclusion: we propose the use of targeted metabolomics followed by in silico studies to virtually screen identified
metabolites on selected protein targets, in combination with the use of the candidate metabolites in cellular models,
as the methods of choice for elucidating the molecular mechanisms of these compounds.