Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus

被引:17
|
作者
Li, Shuai [1 ]
Wang, Yuanhong [1 ]
Jiang, Tingfu [1 ]
Wang, Han [1 ]
Yang, Shuang [1 ]
Lv, Zhihua [1 ]
机构
[1] Ocean Univ China, Marine Drug & Food Inst, Sch Med & Pharm, Qingdao 266003, Peoples R China
来源
MARINE DRUGS | 2016年 / 14卷 / 06期
基金
中国国家自然科学基金;
关键词
sea cucumber saponins; bioavailability; Caco-2; cells; intestinal perfusion; structure-effect; PASS INTESTINAL-PERFUSION; EPITHELIAL CACO-2 CELLS; IN-VITRO; TRITERPENE GLYCOSIDES; BIOLOGICAL-ACTIVITIES; HOLOTHURIA-SCABRA; DRUG ABSORPTION; PERMEABILITY; RAT; VIVO;
D O I
10.3390/md14060114
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The present study is focused on the intestinal absorption of sea cucumber saponins. We determined the pharmacokinetic characteristics and bioavailability of Echinoside A and Holotoxin A(1); the findings indicated that the bioavailability of Holotoxin A(1) was lower than Echinoside A. We inferred that the differences in chemical structure between compounds was a factor that explained their different characteristics of transport across the intestine. In order to confirm the absorption characteristics of Echinoside A and Holotoxin A(1), we examined their transport across Caco-2 cell monolayer and effective permeability by single-pass intestinal perfusion. The results of Caco-2 cell model indicate that Echinoside A is transported by passive diffusion, and not influenced by the exocytosis of P-glycoprotein (P-gp, expressed in the apical side of Caco-2 monolayers as the classic inhibitor). The intestinal perfusion also demonstrated well the absorption of Echinoside A and poor absorption of Holotoxin A(1), which matched up with the result of the Caco-2 cell model. The results demonstrated our conjecture and provides fundamental information on the relationship between the chemical structure of these sea cucumber saponins and their absorption characteristics, and we believe that our findings build a foundation for the further metabolism study of sea cucumber saponins and contribute to the further clinical research of saponins.
引用
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页数:16
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