Evaluation of the intestinal permeability of rosemary (Rosmarinus officinalis L.) extract polyphenols and terpenoids in Caco-2 cell monolayers

Abstract

Rosemary (Rosmarinus officinalis) is grown throughout the world and is widely used as a medicinal herb and to season and preserve food. Rosemary polyphenols and terpenoids have attracted great interest due to their potential health benefits. However, complete information regarding their absorption and bioavailability in Caco-2 cell model is scarce. The permeation properties of the bioactive compounds (flavonoids, diterpenes, triterpenes and phenylpropanoids) of a rosemary extract (RE), obtained by supercritical fluid extraction, was studied in Caco-2 cell monolayer model, both in a free form or liposomed. Compounds were identified and quantitated by liquid chromatography coupled to quadrupole time-of-flight with electrospray ionization mass spectrometry analysis (HPLC-ESI-QTOF-MS), and the apparent permeability values (Papp) were determined, for the first time in the extract, for 24 compounds in both directions across cell monolayer. For some compounds, such as triterpenoids and some flavonoids, Papp values found were reported for the first time in Caco-2 cells.Our results indicate that most compounds are scarcely absorbed, and passive diffusion is suggested to be the primary mechanism of absorption. The use of liposomes to vehiculize the extract resulted in reduced permeability for most compounds. Finally, the biopharmaceutical classification (BCS) of all the compounds was achieved according to their permeability and solubility data for bioequivalence purposes. BCS study reveal that most of the RE compounds could be classified as classes III and IV (low permeability); therefore, RE itself should also be classified into this category.

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces fromPhysalis peruvianaL. on the biopharmaceutics classification of rutin

“…Most studies intended to apply BCS for botanical drugs and plant extracts have focused on the intrinsic characteristics of representative compounds of the mixture . As far as we know, this is the first time that both, solubility and permeability, are experimentally established for rutin from an herbal matrix and its BCS category is compared with that for pure compound.…”

Polyphenols bioaccessibility and bioavailability assessment in ipecac infusion using a combined assay of simulated in vitro digestion and Caco‐2 cell model

“…It has been reported that using this method to mimic the intestinal absorption is quite efficient since Caco‐2 cells express the typical morphological and functional properties as well as the enzymatic activities of small bowel enterocytes (Lea, ). According to literature, Caco‐2 cell line model has been extensively used to study the bioavailability of a large number of nutrients and bioactive compounds with antioxidant properties, such as polyphenols and terpenoids (Pérez‐Sánchez et al ., ; Achour et al ., ) or carotenoids (Liu et al ., ). Furthermore, a high correlation between the Caco‐2 permeability data and the human enterocytes absorption coefficients in vivo was demonstrated (Chopra et al ., ; Lea, ).…”

“…The assessment of polyphenols bioavailability can be conducted in vivo and/or in vitro . Although in vivo assays could offer more advantages in terms of accuracy, a wide number of researchers have used cell cultures, namely Caco‐2 cells, as a useful tool to study the intestinal absorption of phenolic acids and flavonoids (Konishi et al ., ; Pérez‐Sánchez et al ., ; Achour et al ., ). In fact, this colonic line has the ability of differentiating, under normal culture conditions, into a cellular monolayer resembling an intestinal epithelium mimicking a functional intestinal barrier (Lea, ).…”

A Comparison between dietary effects of Cuminum cyminum essential oil and Cuminum cyminum essential oil, loaded with iron nanoparticles, on growth performance, immunity and antioxidant indicators of white leg shrimp (Litopenaeus vannamei )

“…However, FCR improvement in the shrimps treated with CEO and CEO‐loaded NPs supplemented diets suggested that the increasing digestibility and in turn the energetic benefits could increase the growth performance, possibly due to its appetite characteristics. It also demonstrated an improvement in the digestive activity and the absorptive capacity of the intestine related to the anti‐inflammatory and antiproliferative effects of the medicinal plants (Pérez‐Sánchez, Borrás‐Linares, Barrajón‐Catalán, Arráez‐Román, González‐Álvarez, Ibáñez,Segura‐Carretero, Bermejo, Micol, ).…”