Haploscleridamine, a novel tryptamine-derived alkaloid from a sponge of the order Haploselerida: 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 hahtoxins, tryptamine, and a novel tryptamine-derived alkaloid, haploscleridamine (1). The tetrahy...

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Bibliographic Details
Published inJournal of natural products (Washington, D.C.) Vol. 65; no. 4; pp. 628 - 629
Main Authors Patil, AD, Freyer, AJ, Carte, B, Taylor, PB, Johnson, RK, Faulkner, DJ
Format Journal Article
LanguageEnglish
Published WASHINGTON Amer Chemical Soc 01.04.2002
Subjects
Chemistry, Medicinal
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Plant Sciences
Science & Technology
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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 hahtoxins, 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 IC50 of 26 muM.
ISSN:0163-3864
1520-6025
DOI:10.1021/np010500l