holothurin and Obesity

Sea cucumbers have been consumed as tonic, food, and nutrition supplements for many years.. 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.. 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.. 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.. Sea cucumber may be used for developing antiobesity and antihyperlipidemia drugs.

Topics: Adipocytes, White; Animals; Anti-Obesity Agents; Diet, High-Fat; Disease Models, Animal; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Hep G2 Cells; Holothurin; Humans; Intestinal Absorption; Lipase; Lipids; Liver; Liver X Receptors; Mice, Inbred C57BL; Obesity; Pancreas; Saponins; Sea Cucumbers; Signal Transduction; Time Factors; Up-Regulation; Weight Gain

Two similarly sulfated triterpene saponins from Pearsonothuria graeffei were prepared to investigate the anti-obesity effects of echinoside A (EA) and holothurin A (HA). The in vitro inhibitory activities of EA and HA toward pancreatic lipase were investigated, and two in vivo studies were performed: (i) Male Wistar rats were orally administered the lipid emulsion with or without a saponin (HA or EA). The serum's total triglyceride concentration was measured at various times. (ii) C57BL/6 mice were assigned to four groups, high fat (HF), EA (0.03%), HA (0.04%), and orlistat (0.01%), and the weight of adipose tissue and level of fatty acids excreted in the feces were determined. Both EA and HA repressed the pancreatic lipase activity and increased fatty acid excretion in the feces. Treatment with EA and HA significantly decreased the adipose tissue accumulation in mice. EA and HA manifested different inhibitory activities in vitro, but each of them dramatically inhibited lipid absorption in vivo and showed strong anti-obesity activity.

Topics: Absorption, Physicochemical; Animals; Body Weight; Dietary Fats; Eating; Holothurin; Lipase; Liver; Male; Mice; Molecular Docking Simulation; Obesity; Organ Size; Pancreas; Protein Conformation; Rats