Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco-2 Cell Model

Joint Authors

Xu, Renjie
Yuan, Yichu
Qi, Jia
Zhou, Jia
Guo, Xiaowen
Zhang, Jian
Zhan, Ruanjuan

Source

Evidence-Based Complementary and Alternative Medicine

Issue

Vol. 2018, Issue 2018 (31 Dec. 2018), pp.1-8, 8 p.

Publisher

Hindawi Publishing Corporation

Publication Date

2018-12-23

Country of Publication

Egypt

No. of Pages

8

Main Subjects

Medicine

Abstract EN

Loganin, iridoid glycosides, is the main bioactive ingredients in the plant Strychnos nux-vomica L.

and demonstrates various pharmacological effects, though poor oral bioavailability in rats.

In this study, the intestinal absorption mechanism of loganin was investigated using the human intestinal Caco-2 cell monolayer model in both the apical-to-basolateral (A-B) and the basolateral-to-apical (B-A) direction; additionally, transport characteristics were systematically investigated at different concentrations, pHs, temperatures, and potential transporters.

The absorption permeability (PappAB) of loganin, which ranged from 12.17 to 14.78 × 10−6cm/s, was high at four tested concentrations (5, 20, 40, and 80μM), while the major permeation mechanism of loganin was found to be passive diffusion with active efflux mediated by multidrug resistance-associated protein (MRP) and breast cancer resistance protein (BCRP).

In addition, it was found that loganin was not the substrate of efflux transporter P-glycoprotein (P-gp) since the selective inhibitor (verapamil) of the efflux transporter exhibited little effects on the transport of loganin in the human intestinal Caco-2 cells.

Meanwhile, transport from the apical to the basolateral side increased 2.09-fold after addition of a MRP inhibitor and 2.32-fold after addition of a BCRP inhibitor.

In summary, our results clearly demonstrate, for the first time, a good permeability of loganin in the human intestinal Caco-2 cell model and elucidate, in detail, the intestinal absorption mechanism and the effects of transporters on iridoid glycosides compounds.

American Psychological Association (APA)

Xu, Renjie& Yuan, Yichu& Qi, Jia& Zhou, Jia& Guo, Xiaowen& Zhang, Jian…[et al.]. 2018. Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco-2 Cell Model. Evidence-Based Complementary and Alternative Medicine،Vol. 2018, no. 2018, pp.1-8.
https://search.emarefa.net/detail/BIM-1156512

Modern Language Association (MLA)

Xu, Renjie…[et al.]. Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco-2 Cell Model. Evidence-Based Complementary and Alternative Medicine No. 2018 (2018), pp.1-8.
https://search.emarefa.net/detail/BIM-1156512

American Medical Association (AMA)

Xu, Renjie& Yuan, Yichu& Qi, Jia& Zhou, Jia& Guo, Xiaowen& Zhang, Jian…[et al.]. Elucidation of the Intestinal Absorption Mechanism of Loganin in the Human Intestinal Caco-2 Cell Model. Evidence-Based Complementary and Alternative Medicine. 2018. Vol. 2018, no. 2018, pp.1-8.
https://search.emarefa.net/detail/BIM-1156512

Data Type

Journal Articles

Language

English

Notes

Includes bibliographical references

Record ID

BIM-1156512