Saponin-enriched sea cucumber extracts exhibit an antiobesity effect through inhibition of pancreatic lipase activity and upregulation of LXR-β signaling

Pharm Biol. 2016 Aug;54(8):1312-25. doi: 10.3109/13880209.2015.1075047. Epub 2015 Oct 6.

Abstract

Context: Sea cucumbers have been consumed as tonic, food, and nutrition supplements for many years.

Objective: The objective of this study is to investigate the antiobesity and lipid-lowering effects of sea cucumber extracts in in vitro and in vivo models and elucidate the mechanism of action of the extracts on obesity and dyslipidemia.

Materials and methods: The 60% ethanol extracts from the body walls of 10 different sea cucumbers were investigated for the inhibition of pancreatic lipase (PL) activity in vitro. The optimal active extract (SC-3) was further chemically analyzed by LC-MS and UV. And 0.1% and 0.2% of SC-3 was mixed with a high-fat diet to treat C57/BL6 mice for 6 weeks or 2 weeks as preventive and therapeutic study. The body weight, serum, and liver lipid profile in the mice were investigated.

Results: The crude extract of Pearsonothuria graeffei Semper (Holothuriidae) inhibited the PL activity by 36.44% of control at 0.5 μg/mL. SC-3 and echinoside A inhibited PL with an IC50 value at 2.86 μg/mL and 0.76 μM. 0.1% of SC-3 reduced the body weight (23.0 ± 0.62 versus 26.3 ± 0.76 g), the serum TC (2.46 ± 0.04 versus 2.83 ± 0.12 mmol/L), TG (0.19 ± 0.08 versus 0.40 ± 0.03 mmo/L), and LDL-c (0.48 ± 0.02 versus 0.51 ± 0.02 mmol/L), and liver TC (1.19 ± 0.17 versus 1.85 ± 0.13 mmol/mg) and TG (6.18 ± 0.92 versus 10.87 ± 0.97 mmol/mg) contents of the obese C57BL/six mice on a high-fat diet.

Discussion and conclusion: Sea cucumber may be used for developing antiobesity and antihyperlipidemia drugs.

Keywords: ABCA1 nRNAs; C57/BL6 mice, Echinoside A; Pearsonothuria graeffei; antihyperlipidemia.

MeSH terms

  • Adipocytes, White / drug effects
  • Adipocytes, White / metabolism
  • Animals
  • Anti-Obesity Agents / isolation & purification
  • Anti-Obesity Agents / pharmacology*
  • Diet, High-Fat
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology*
  • Female
  • Hep G2 Cells
  • Holothurin / analogs & derivatives
  • Holothurin / pharmacology
  • Humans
  • Intestinal Absorption / drug effects
  • Lipase / antagonists & inhibitors*
  • Lipase / metabolism
  • Lipids / blood
  • Liver / drug effects*
  • Liver / metabolism
  • Liver X Receptors / drug effects*
  • Liver X Receptors / metabolism
  • Mice, Inbred C57BL
  • Obesity / blood
  • Obesity / etiology
  • Obesity / prevention & control*
  • Pancreas / enzymology*
  • Saponins / isolation & purification
  • Saponins / pharmacology*
  • Sea Cucumbers / metabolism*
  • Signal Transduction / drug effects*
  • Time Factors
  • Up-Regulation
  • Weight Gain / drug effects

Substances

  • Anti-Obesity Agents
  • Enzyme Inhibitors
  • Lipids
  • Liver X Receptors
  • NR1H2 protein, human
  • Nr1h2 protein, mouse
  • Saponins
  • Holothurin
  • echinoside A
  • Lipase