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Mar. Drugs 2016, 14(6), 114;

Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus

Marine Drug and Food Institute, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China
Author to whom correspondence should be addressed.
Academic Editor: Kirsten Benkendorff
Received: 14 March 2016 / Revised: 27 May 2016 / Accepted: 7 June 2016 / Published: 17 June 2016
(This article belongs to the Collection Bioactive Compounds from Marine Invertebrates)
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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. View Full-Text
Keywords: sea cucumber saponins; bioavailability; Caco-2 cells; intestinal perfusion; structure-effect sea cucumber saponins; bioavailability; Caco-2 cells; intestinal perfusion; structure-effect

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Li, S.; Wang, Y.; Jiang, T.; Wang, H.; Yang, S.; Lv, Z. Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus. Mar. Drugs 2016, 14, 114.

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