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Ecology- and bioassay-guided drug discovery for treatments of tropical parasitic disease: 5a,8a-epidioxycholest-6-en-3β-isolated from the mollusk dolabrifera dolabrifera shows significant activity against leishmania donovani
journal contribution
posted on 2021-07-28, 01:23 authored by Kathryn E Clark, Angela CapperAngela Capper, Gina D Togna, Valerie J Paul, Luz I Romero, Timothy Johns, Luis Cubilla-Rios, Todd L CapsonAn ecology- and bioassay-guided search employed to discover compounds with activity against tropical parasitic diseases and cancer from the opisthobranch mollusk, Dolabrifera dolabrifera, led to the discovery of antileishmanial properties in the known compound, 5a,8a-epidioxycholest-6- en-3ß-ol (1). Compound 1 was identified through nuclear magnetic resonance spectroscopy (1H, 13C) and mass spectrometry. The compound was concentrated in the digestive gland of D. dolabrifera, but was not detected in other body parts, fecal matter or mucus. Compound 1 showed an IC50 of 4.9 μM towards the amastigote form of Leishmania donovani compared with an IC50 of 281 μM towards the control Vero cell line, a 57.3-fold difference, and demonstrated no measurable activity against Plasmodium falciparum, Trypanosoma cruzi, and the breast cancer cell line, MCF-7.
History
Volume
8Issue
11Start Page
1537End Page
1540Number of Pages
4eISSN
1555-9475ISSN
1934-578XLocation
United StatesPublisher
Sage PublicationsPublisher DOI
Language
engPeer Reviewed
- Yes
Open Access
- No
Acceptance Date
2013-08-20External Author Affiliations
Smithsonian Marine Station at Fort Pierce, USA; McGill University, Canada; Universidad de Panamá, Instituto de Investigaciones Científicas Avanzadas y Servicios de Alta Tecnología, Smithsonian Tropical Research Institute, Republic of Panama;Era Eligible
- Yes