Intestinal Permeability of Sesquiterpenes in the Caco-2 Cell Monolayer Model

Abstract

The intestinal permeability of eight sesquiterpenes which are active constituents of some traditional Chinese medicines, were studied by using the Caco-2 cell monolayer; they include tanacetin, artesin, magnolialide, crossostephin, atractylon, isocalamenediol (ICL), bisabolangelone (BSE) and (3 R)-des- O-methyllasiodiplodin (DML). The bidirectional permeability of the eight sesquiterpenes was studied from the apical (AP) side to the basolateral (BL) side or from the BL side to the AP side. The eight compounds were assayed by HPLC. Transport parameters and apparent permeability coefficients ( P(app)) were then calculated. The bidirectional P(app) values of the eight compounds were compared with those of propranolol, a marker of high permeability and transcellular transport. The transport of the eight sesquiterpenes was concentration-dependent in the range of 10-200 microM. Lower recoveries of ICL, BSE and DML than other sesquiterpenes were found during transport. The results indicated that all the sesquiterpenes are well absorbed mainly by the passive diffusion via the transcellular pathway and metabolism may be involved during the absorption of ICL, BSE and DML.

Assessing the Intestinal Permeability and Anti-Inflammatory Potential of Sesquiterpene Lactones from Chicory

“…No cysteine conjugates for parthenolide or other SLs were reported in previous absorption studies in Caco-2 cells using HPLC [47,48]. However, this may reflect the targeted nature of the previous HPLC-based studies and highlights the advantages of the LC-MS method developed here.…”

“…Overall, we observed differential in vitro absorption and evidence of bioconversion of the main chicory SLs and to the best of our knowledge, there are still no reports about their in vivo bioavailability. Indeed, little is known about the ADME of chicory SLs and SLs in general, with the few published studies with Caco-2 cells suggesting that sesquiterpene lactones are well absorbed by diffusion [47][48][49] and undergo carrier mediated efflux and influx [38].…”

Intestinal absorption and bioavailability of traditional Chinese medicines: a review of recent experimental progress and implication for quality control

“…Many herbal-derived compounds are the substrates of P-gp, such as sesquiterpenes, glabridin, tanshinone IIA, berberine, palmatine, jateorhizine, and coptisine. [45][46][47][48] Proved by experimental and clinical trials, when administered with ciclosporin as a P-gp inhibitor, the bioavailability of paclitaxel derived from Taxus chinensis (Pilg.) Rehder.…”

Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment

“…The enterocytes constitute a lipid barrier to the drug absorption in the gastrointestinal tract, and hydrophobic bioactive compounds can cross it more easily [ 22 ]. Thus, due to its chemical composition, CO contains some substances that can permeate, but are poorly soluble in the gastrointestinal tract environment, leading to low bioavailability [ 22 , 23 , 24 , 25 ].…”