Ecology- and Bioassay-Guided Drug Discovery for Treatments of Tropical Parasitic Disease: 5α,8α-Epidioxycholest-6-en-3β-ol Isolated from the Mollusk Dolabrifera dolabrifera Shows Significant Activity against Leishmania donovani-Reference-Cited by-同舟云学术

Ecology- and Bioassay-Guided Drug Discovery for Treatments of Tropical Parasitic Disease: 5α,8α-Epidioxycholest-6-en-3β-ol Isolated from the Mollusk Dolabrifera dolabrifera Shows Significant Activity against Leishmania donovani

Published:2013-11 Issue:11 Volume:8 Page:1934578X1300801
ISSN:1934-578X
Container-title:Natural Product Communications
language:en
Short-container-title:Natural Product Communications

Author:

Clark Kathryn E.¹²³,Capper Angela⁴⁵,Togna Gina Della⁶⁷,Paul Valerie J.⁴,Romero Luz I.⁶,Johns Timothy²,Cubilla-Rios Luis⁸,Capson Todd L.¹²⁹

Affiliation:

1. Smithsonian Tropical Research Institute, Apartado 2072, Balboa Ancón, Republic of Panama

2. Department of Plant Science, McGill University, 21,111 Lakeshore, Ste. Anne de Bellevue, Quebec H9X 3V9, Canada

3. current address: Oxford University Centre for the Environment, South Parks Road, Oxford, OX1 3QY, UK

4. Smithsonian Marine Station at Fort Pierce, 701 Seaway Drive, Fort Pierce, Florida 34949, USA

5. current address: Centre for Sustainable Tropical Fisheries and Aquaculture & School of Marine and Tropical Biology, James Cook University, Townsville, QLD 4811, Australia

6. Instituto de Investigaciones Científicas Avanzadas y Servicios de Alta Tecnología, Clayton, Edificio 175, PO Box 7250, Panama City, Republic of Panama

7. current address: Center for Species Survival, Smithsonian Conservation Biology Institute, National Zoological Park, P.O. Box 37012, MRC 5502, Washington, DC 20013–7012, USA

8. Laboratorio de Bioorgánica Tropical, Departamento de Química Orgánica, Universidad de Panamá, Apartado 0824–10835, Panama City, Republic of Panama

9. current address: 1743 18th St. NW Washington DC, 20009 USA

Abstract

An 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, 5α,8α-epidioxycholest-6-en-3β-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.

Publisher

SAGE Publications

Subject

Complementary and alternative medicine,Plant Science,Drug Discovery,Pharmacology,General Medicine

Link

http://journals.sagepub.com/doi/pdf/10.1177/1934578X1300801109

Reference38 articles.

1. Clinical and Experimental Advances in Treatment of Visceral Leishmaniasis

2. Antileishmanial High-Throughput Drug Screening Reveals Drug Candidates with New Scaffolds

3. The Molecular Mechanism of Action of Artemisinin—The Debate Continues

4. A review of natural products with antileishmanial activity

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