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The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness.
- Source :
-
Journal of natural products [J Nat Prod] 2009 Feb 27; Vol. 72 (2), pp. 218-22. - Publication Year :
- 2009
-
Abstract
- Human African trypanosomiasis, also known as African sleeping sickness, is a neglected tropical disease with inadequate therapeutic options. We have launched a collaborative new lead discovery venture using our repository of extracts and natural product compounds as input into our growth inhibition primary screen against Trypanosoma brucei. Careful evaluation of the spectral data of the natural products and derivatives allowed for the elucidation of the absolute configuration (using the modified Mosher's method) of two new peroxiterpenes: (+)-muqubilone B (1a) and (-)-ent-muqubilone (3a). Five known compounds were also isolated: (+)-sigmosceptrellin A (4a), (+)-sigmosceptrellin A methyl ester (4b), (-)-sigmosceptrellin B (5), (+)-epi-muqubillin A (6), and (-)-epi-nuapapuin B methyl ester (7). The isolated peroxiterpenes demonstrated activities in the range IC(50) = 0.2-2 mug/mL.
- Subjects :
- Animals
Humans
Marine Biology
Molecular Structure
Parasitic Sensitivity Tests
Peroxides chemistry
Stereoisomerism
Terpenes chemistry
Trypanosomiasis, African etiology
Peroxides isolation & purification
Peroxides pharmacology
Porifera chemistry
Terpenes isolation & purification
Terpenes pharmacology
Trypanosoma brucei brucei drug effects
Trypanosomiasis, African drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1520-6025
- Volume :
- 72
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Journal of natural products
- Publication Type :
- Academic Journal
- Accession number :
- 19159277
- Full Text :
- https://doi.org/10.1021/np800711a