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Alisiaquinones and Alisiaquinol, Dual Inhibitors of Plasmodium falciparum Enzyme Targets from a New Caledonian Deep Water Sponge

Year: 2008

Type: article

Abstract: Four new meroterpenes, alisiaquinones A-C (1-3) and alisiaquinol (4), were isolated from a New Caledonian deep water sponge. Their structures and relative stereochemistry were elucidated by spectroscopic data analysis. They are related to xestoquinone, but showed unusual substitution on a tetrahydrofuran junction. They displayed micromolar range activity on two enzymatic targets of importance for the control of malaria, the plasmodial kinase Pfnek-1 and a protein farnesyl transferase, as well as on different chloroquine-sensitive and -resistant strains of Plasmodium falciparum. Alisiaquinone C displayed a submicromolar activity on P. falciparum and a competitive selectivity index on the different plasmodial strains.

Source: Journal of Natural Products

DOI: 10.1021/np8000909

Authors: Denis Desoubzdanne, Laurence Marcourt, Roselyne Raux, Séverine Chevalley, Dominique Dorin, Christian Doerig, Alexis Valentin, Frédéric Ausseil, Cécile Debitus

Institutions: Centre National de la Recherche Scientifique, Université Toulouse III - Paul Sabatier, Inserm, Wellcome Centre for Molecular Parasitology, Pharmacochimie et Biologie pour le Développement, Institut de Recherche pour le Développement

Language: English

Topic: Marine Sponges and Natural Products

Subfield: Biotechnology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

OpenAlex ID: W2005164409

FWCI: 5.273

Cites: 18

Cited by: 76

Related to: 10