New Leukotriene B4 Receptor Antagonist: Leucettamine A and Related Imidazole Alkaloids from the Marine Sponge Leucetta microraphis

Three new imidazole alkaloids, leucettamines A [1] and B [2] and leucettamidine [3], have been isolated from the Palauan sponge Leucetta microraphis. Their structures were established on the basis of extensive spectral analyses. Leucettamine A showed potent leukotriene B4 receptor binding activity (...

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Bibliographic Details
Published in:Journal of natural products (Washington, D.C.) D.C.), 1993-01, Vol.56 (1), p.116-121
Main Authors: Chan, George W, Mong, Seymour, Hemling, Mark E, Freyer, Alan J, Offen, Priscilla H, DeBrosse, Charles W, Sarau, Henry M, Westley, John W
Format: Article
Language:English
Subjects:
Alkaloids - pharmacology
Animals
Biological and medical sciences
Cells, Cultured
Dioxoles - isolation & purification
Dioxoles - pharmacology
Gas Chromatography-Mass Spectrometry
General pharmacology
Imidazoles - isolation & purification
Imidazoles - pharmacology
Magnetic Resonance Spectroscopy
Medical sciences
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Porifera - chemistry
Receptors, Immunologic - antagonists & inhibitors
Receptors, Immunologic - metabolism
Receptors, Leukotriene B4
Spectrometry, Mass, Fast Atom Bombardment
Structure-Activity Relationship
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Summary:Three new imidazole alkaloids, leucettamines A [1] and B [2] and leucettamidine [3], have been isolated from the Palauan sponge Leucetta microraphis. Their structures were established on the basis of extensive spectral analyses. Leucettamine A showed potent leukotriene B4 receptor binding activity (K(i) = 1.3 microM), while leucettamine B was essentially inactive (K(i) = 100 microM) and leucettamidine showed significant activity (K(i) = 5.3 microM). With leucettamine A identified as a pure LTB4 receptor antagonist, a new structure lead is presented to inflammation therapy.
ISSN:0163-3864
1520-6025
DOI:10.1021/np50091a016