RRC ID 42629
著者 Hong J, Yokomakura A, Nakano Y, Ishihara K, Kaneda M, Onodera M, Nakahama K, Morita I, Niikura K, Ahn JW, Zee O, Ohuchi K.
タイトル Inhibition of vacuolar-type (H+)-ATPase by the cytostatic macrolide apicularen A and its role in apicularen A-induced apoptosis in RAW 264.7 cells.
ジャーナル FEBS Lett
Abstract Apicularen A and the known vacuolar-type (H(+))-ATPase (V-ATPase) inhibitor bafilomycin A(1) induced apoptosis of RAW 264.7 cells, while apicularen B, an N-acetyl-glucosamine glycoside of apicularen A, was far less effective. Apicularen A inhibited vital staining with acridine orange of the intracellular organelles of RAW 264.7 cells, inhibited the ATP-dependent proton transport into inside-out microsome vesicles, and inhibited the bafilomycin A(1)-sensitive ATP hydrolysis. The IC(50) values of the proton transport were 0.58 nM for apicularen A, 13 nM for apicularen B, and 0.95 nM for bafilomycin A(1). Furthermore, apicularen A inhibited the bafilomycin A(1)-sensitive ATP hydrolysis more potently than apicularen B. F-ATPase and P-ATPase were not inhibited by apicularen A. We concluded that apicularen A inhibits V-ATPase, and thus induces apoptosis in RAW 264.7 cells.
巻・号 580(11)
ページ 2723-30
公開日 2006-5-15
DOI 10.1016/j.febslet.2006.04.031
PII S0014-5793(06)00466-2
PMID 16647709
MeSH Adenosine Triphosphate / metabolism Adenosine Triphosphate / pharmacology Animals Apoptosis / drug effects* Bridged Bicyclo Compounds, Heterocyclic / chemistry Bridged Bicyclo Compounds, Heterocyclic / pharmacology* Cell Line Cell Nucleus / drug effects Cell Shape / drug effects Enzyme Inhibitors / chemistry Enzyme Inhibitors / pharmacology* Macrolides / chemistry Macrolides / pharmacology Membrane Potentials / drug effects Mice Mitochondrial Membranes / drug effects Proton-Translocating ATPases / antagonists & inhibitors* Proton-Translocating ATPases / metabolism
IF 3.057
引用数 16
WOS 分野 BIOPHYSICS BIOCHEMISTRY & MOLECULAR BIOLOGY CELL BIOLOGY
リソース情報
ヒト・動物細胞 A431