Inhibition of HMG-CoA reductase activity and cholesterol permeation through Caco-2 cells by caffeoylquinic acids from Vernonia condensata leaves

Abstract

The aim of this study was to provide scientific knowledge to support the use of Vernonia condensata Baker,Asteraceae, beverages for their alleged hypocholesterolemic properties by testing their action as HMG-CoA reductase inhibitors and their capacity to lower dietary cholesterol permeation. Chlorogenic acid,and other caffeoylquinic acids derivatives were identified as the main components of these beveragesby LC–MS/MS. No changes in the composition were notice after the in vitro gastrointestinal digestionand no toxicity against Caco-2 and HepG2 cell lines was detected. Cholesterol permeation through Caco-2 monolayers was reduced in 37% in the presence of these herbal teas, and the caffeoylquinic acidspermeated the monolayers in 30–40% of their initial amount in 6 h. HMG-CoA reductase activity wasreduced with these beverages, showing an IC50of 217 μg ml−1. It was concluded that caffeoylquinicacids, the major components, justified 98% of the enzyme inhibition measured.