Holothurin

Pharmacology

Effects on nerves

Holothurin is shown to have a blocking effect on nerves in desheathed bullfrog sciatic nerve and rat phrenic nerve preparations, and its potency can be compared to that of cocaine, procaine, and physostigmine. Unlike the other mentioned blocking agents, the disrupting effect of holothurin appears to be quite irreversible upon washing.

In another experiment on frog sciatic nerve, holothurin A is shown to be capable of destroying electrical excitability of a node of Ranvier along with basophilic macromolecular material found in and near the cytoplasm of the node. In another experiment on rat phrenic nerve, the nerve-disrupting effect of holothurin A is found to be preventable when specific concentrations of physostigmine are present.

Other effects

Holothurin A and holothurin A1, along with other sea cucumber saponins, are found to reduce weight gain in mice. They improve glucose tolerance, reduce levels of lipids in blood and liver, and inhibit the absorption of lipids in the intestine. They also inhibit the activity of pancreatic lipase, decrease the growth of white adipocytes, a factor which contributes to obesity, and stimulate the production of LXR-β nuclear receptor and ABCA1 protein. These findings suggest a possibility of the holothurins and other sea cucumber saponins being used in the development of anti-obesity drug.

The holothurins are shown to have anti-melanogenic and anti-wrinkling effects on human skin by inhibiting melanin production in Melan-A cells and promoting collagen production in human dermal fibroblasts via the ERK pathway.

References

References

1. "Holothurin". [[National Center for Biotechnology Information]].
2. "Holothurin A". [[National Center for Biotechnology Information]].
3. "Holothurin B". [[National Center for Biotechnology Information]].
4. (1959). "Holothurin. I. Isolation, properties, and sugar components of holothurin A". Journal of the American Chemical Society.
5. (2004). "Invertebrate Zoology, 7th edition". Cengage Learning.
6. (1979). "Structure of holothurin A a biologically active triterpene-oligoglycoside from the sea cucumber holothuria leucospilota brandt". Tetrahedron Letters.
7. "Holothurin". [[National Center for Biotechnology Information]].
8. (August 1959). "Some pharmacologic properties of holothurin, an active neurotoxin from the sea cucumber.". The Journal of Pharmacology and Experimental Therapeutics.
9. (March 1964). "Neuromuscular and cytotoxic effects of holothurin A and related saponins at low concentration levels. III". Toxicology and Applied Pharmacology.
10. (6 October 2015). "Saponin-enriched sea cucumber extracts exhibit an antiobesity effect through inhibition of pancreatic lipase activity and upregulation of LXR-β signaling". Pharmaceutical Biology.
11. (November 2018). "Effects on skin of Stichopus japonicus viscera extracts detected with saponin including Holothurin A: Down-regulation of melanin synthesis and up-regulation of neocollagenesis mediated by ERK signaling pathway". Journal of Ethnopharmacology.