Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus.
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 A₁; the findings indicated that the bioavailability of Holotoxin A₁ 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 A₁, 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 A₁, 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.
Marine Drug and Food Institute, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China. lishuai890126@126.com.
Shuai
S
Li
Marine Drug and Food Institute, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China. yhwang@ouc.edu.cn.
Yuanhong
Y
Wang
Marine Drug and Food Institute, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China. jiangtingfu@ouc.edu.cn.
Tingfu
T
Jiang
Marine Drug and Food Institute, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China. wanghan0812@sina.com.
Han
H
Wang
Marine Drug and Food Institute, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China. yangshuang@ouc.edu.cn.
Shuang
S
Yang
Marine Drug and Food Institute, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China. lvzhihua@ouc.edu.cn.
Zhihua
Z
Lv
D000818:Animals; D001682:Biological Availability; D001692:Biological Transport / Q000502:physiology; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D006027:Glycosides / Q000378:metabolism; D006697:Holothurin / Q000031:analogs & derivatives / Q000378:metabolism; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology*; D007413:Intestinal Mucosa / Q000378:metabolism; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012503:Saponins / Q000378:metabolism* / Q000493:pharmacokinetics; D012616:Sea Cucumbers / Q000378:metabolism*; D047528:Stichopus / Q000378:metabolism*; D014315:Triterpenes / Q000378:metabolism
D006027:Glycosides; D012503:Saponins; D014315:Triterpenes; D006697:Holothurin; C001883:stichoposide; C043973:echinoside A
Caco-2 cells; bioavailability; intestinal perfusion; sea cucumber saponins; structure-effect