title: Bastadins, brominated-tyrosine derivatives, suppress accumulation of cholesterol ester in macrophages.
abstract: The formation of foam cells in macrophages has been suggested to play an essential role in the progression of early atherosclerotic lesions in vivo and, thus, its suppression is considered to be one of the major approaches for the treatment of atherosclerosis. We isolated eight brominated-tyrosine derivatives, bastadins, from the EtOH extract of the marine sponge Ianthella vasta as inhibitors of the formation of foam cells induced by acetylated low-density lipoproteins in human monocyte-derived macrophages. Bastadin 6 was the strongest inhibitor of foam cell formation due to its suppression of acyl-coenzyme A:cholesterol acyltransferase.
authors.affiliation: Department of Natural Medicines, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-honmachi 5-1, Kumamoto 862-0973, Kumamoto, Japan.
authors.forename: Keisuke
authors.initials: K
authors.lastname: Eguchi
authors.affiliation: Department of Natural Medicines, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-honmachi 5-1, Kumamoto 862-0973, Kumamoto, Japan.
authors.forename: Hikaru
authors.initials: H
authors.lastname: Kato
authors.affiliation: Department of Cell Pathology, Graduate School of Medical Sciences, Kumamoto University, Honjo 1-1-1, Kumamoto 860-8556, Kumamoto, Japan.
authors.forename: Yukio
authors.initials: Y
authors.lastname: Fujiwara
authors.affiliation: Faculty of Fisheries and Marine Science, Sam Ratulangi University, Kampus Bahu, Manado 95115, Indonesia.
authors.forename: Fitje
authors.initials: F
authors.lastname: Losung
authors.affiliation: Faculty of Fisheries and Marine Science, Sam Ratulangi University, Kampus Bahu, Manado 95115, Indonesia.
authors.forename: Remy E P
authors.initials: RE
authors.lastname: Mangindaan
authors.affiliation: Naturalis Biodiversity Centre, PO Box 9517, 2300 RA Leiden, The Netherlands.
authors.forename: Nicole J
authors.initials: NJ
authors.lastname: de Voogd
authors.affiliation: Department of Cell Pathology, Graduate School of Medical Sciences, Kumamoto University, Honjo 1-1-1, Kumamoto 860-8556, Kumamoto, Japan.
authors.forename: Motohiro
authors.initials: M
authors.lastname: Takeya
authors.affiliation: Department of Natural Medicines, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-honmachi 5-1, Kumamoto 862-0973, Kumamoto, Japan. Electronic address: sachiko@kumamoto-u.ac.jp.
authors.forename: Sachiko
authors.initials: S
authors.lastname: Tsukamoto
mesh_terms: D000818:Animals; D050197:Atherosclerosis / Q000188:drug therapy; D016466:CHO Cells; D002788:Cholesterol Esters / Q000378:metabolism*; D003412:Cricetulus; D004789:Enzyme Activation / Q000187:drug effects; D000431:Ethanol / Q000737:chemistry; D005487:Foam Cells / Q000187:drug effects* / Q000201:enzymology; D055768:Halogenated Diphenyl Ethers / Q000494:pharmacology*; D054879:Halogenation; D006801:Humans; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors; D014443:Tyrosine / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D002788:Cholesterol Esters; D055768:Halogenated Diphenyl Ethers; C515158:bastadin 6; D000431:Ethanol; D014443:Tyrosine; D002785:Sterol O-Acyltransferase
keywords: Atherosclerosis; Bastadin; Brominated-tyrosine derivatives; Cholesterol ester