Uptake and transport of Laportea bulbifera extract in Caco-2 cell model.
10.19540/j.cnki.cjcmm.20220623.201
- Author:
Jing HUANG
1
;
Hong-Qin XIAO
1
;
Ying LI
1
;
Yi CHEN
1
;
Si-Ying CHEN
1
;
Yue-Ting LI
1
;
Yong HUANG
1
;
Lin ZHENG
1
;
Yong-Lin WANG
1
;
Zi-Peng GONG
1
Author Information
1. Provincial Key Laboratory of Pharmaceutics in Guizhou, Guizhou Provincial Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine, School of Pharmaceutical Sciences, Guizhou Medical University Guiyang 550004, China.
- Publication Type:Journal Article
- Keywords:
Caco-2 cell model;
Laportea bulbifera;
efflux transporter;
transport;
uptake
- MeSH:
Humans;
Rats;
Animals;
Caco-2 Cells;
ATP Binding Cassette Transporter, Subfamily G, Member 2/genetics*;
Intestinal Absorption;
Neoplasm Proteins/metabolism*;
Urticaceae;
Biological Transport;
Plant Extracts/pharmacology*
- From:
China Journal of Chinese Materia Medica
2022;47(20):5617-5626
- CountryChina
- Language:Chinese
-
Abstract:
Laportea bulbifera extract is effective in resisting inflammation and shows a good therapeutic effect on rheumatoid arthritis in rats. However, the absorption characteristics of active components in L. bulbifera extract in Caco-2 cells are still unclear, which limits the in-depth development of L. bulbifera resources. The purpose of this study was to investigate the absorption and transport mechanism of the active components of L. bulbifera extract in the Caco-2 cell model and explore the effects of different factors(concentration, time, pH value, temperature, and efflux transporter inhibitor) on its uptake and transport. The results showed that L. bulbifera extract at the concentration of 2.0-8.0 mg·mL~(-1) showed no toxicity to Caco-2 cells. The uptake and transport of L. bulbifera extract in the Caco-2 cell model were concentration-dependent and time-dependent. The main absorption mechanism was passive diffusion, and acidic condition(pH 5.0-6.0) and 37 ℃ were more favorable for drug absorption. P_(app)>1.0×10~(-6 )cm·s~(-1) of each component indicated that L. bulbifera was a moderately absorbed drug. P-gp, MRP2, and BCRP were not involved in its uptake and transport.
