TOPSENTINS

Molecular Weight (Topsentin B1): 342.351 g/mol
Molecular Formula (Topsentin B1): C₂₀H₁₄N₄O₂

Source: The sponges Topsentia genitrix, Hexadella sp., and Spongosorites ruetzleri (PORIFERA)
Activity: anti-inflammatory agent
Status:Preclinical

The Topsentins are a class of natural products that have been extracted from several sponge species subsequent to their initial isolation from the sponge Spongosorites ruetzleri.

These compounds have been shown to have significant anti-inflammatory properties. Although the precise mode of action is not known, the compound has been reported capable of suppressing immunogenic as well as neurogenic (originating in nerve tissue) inflammation. The topsentins may hold promise as an arthritis medication or as additives in anti-inflammatory creams for the treatment of skin irritations. Early research suggests the compounds may also one day prove useful as treatments against colon cancer, Alzheimer's disease, and inflammatory bowel disease.

Isolation of the topsentins from a number of unrelated sponge species strongly suggests that the target compounds may actually be produced by bacteria or other microorganisms living within the tissues of the sponges.

Some success has been reported in preparing synthetic topsentin analogs that retain good bioactivity. Such efforts will hopefully obviate the need for large-scale collection of topsentin-containing deepwater sponges as a source of natural product if and when clinical trials are commenced.

At the 9th International Symposium on Marine Natural Products (Townsville, July 1998), the researchers recently reported success in preparing a relatively simple synthetic bis-indole derivative that has good anti-inflammatory activity, thereby circumventing the difficult and expensive task of collecting the deep-water sponge.

NCBI PubChem compound summary page - [ LINK ]

NCBI PubMed biomedical literature citations and abstracts - [ LINK ]

References

Faulkner, D.J. 2000. Marine Pharmacology. Antonie van Leeuwenhoek 77: 135-145,

Marine Biotechnology in the Twenty-First Century: Problems, Promise, and Products. Committee on Marine Biotechnology: Biomedical Applications of Marine natural Products. National Research Council. 2002.

@Sea web site Overview of Marine Drug Discovery: http://www.at-sea.org/missions/floridafrontiers/feature.html