Haploscleridamine, a Novel Tryptamine-Derived Alkaloid from a Sponge of the Order Haplosclerida: an Inhibitor of Cathepsin K

As part of a search for novel inhibitors of cathepsin K, the MeOH extract of a Micronesian sponge of the order Haplosclerida was shown to be active. Bioassay-guided fractionation of the extract yielded halitoxins, tryptamine, and a novel tryptamine-derived alkaloid, haploscleridamine (1). The tetrah...

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Published inJournal of natural products (Washington, D.C.) Vol. 65; no. 4; pp. 628 - 629
Main Authors Patil, AD, Freyer, A J, Carte, B, Taylor, P B, Johnson, R K, Faulkner, D J
Format Journal Article
LanguageEnglish
Published 26.04.2002
Subjects
alkaloids
Haplosclerida
Haploscleridamine
Marine
natural products
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Summary:As part of a search for novel inhibitors of cathepsin K, the MeOH extract of a Micronesian sponge of the order Haplosclerida was shown to be active. Bioassay-guided fractionation of the extract yielded halitoxins, tryptamine, and a novel tryptamine-derived alkaloid, haploscleridamine (1). The tetrahydro- beta -carboline structure of haploscleridamine (1) was elucidated through spectral techniques. Haploscleridamine (1) was found to be an inhibitor of cathepsin K with an IC sub(50) of 26 mu M.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
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ISSN:0163-3864
DOI:10.1021/np0105001