| RRC ID |
41630
|
| 著者 |
Tanigaki K, Sato T, Tanaka Y, Ochi T, Nishikawa A, Nagai K, Kawashima H, Ohkuma S.
|
| タイトル |
BE-18591 as a new H(+)/Cl(-) symport ionophore that inhibits immunoproliferation and gastritis.
|
| ジャーナル |
FEBS Lett
|
| Abstract |
In our previous papers [e.g. Sato et al., J. Biol. Chem. 273 (1998) 21455-21462], we have shown that prodigiosins can uncouple various H(+)-ATPases through their H(+)/Cl(-) symport activity. BE-18591 is an enamine of 4-methoxy-2,2'-bipyrrole-5-carboxyaldehyde (tambjamine group antibiotics) which resembles the prodigiosins. We found that BE-18591 was a new group of antibiotics that uncouples various H(+)-ATPases: it inhibited proton pump activities with IC(50)s of about 1-2 nM (about 20 pmol/mg protein) for submitochondrial particles as well as gastric vesicles and of 230 nM (about 230 pmol/mg protein) for lysosomes, but it had little effect on their ATP hydrolyses (up to 10 microM), a property of H(+)/Cl(-) symport activity. At low concentrations (<1 microM), BE-18591 inhibited immunoproliferation, the IC(50) of lipopolysaccharide-stimulated mouse splenocytes was 38 nM, that of Concanavalin A-stimulated cells was 230 nM. Gastritis of rabbits was also inhibited. At higher concentrations (>1 microM), BE-18591 induced neurite outgrowth (15% induction in 48 h at 4 microM), inhibited bone resorption (approximately 35% in 48 h at 10 microM) and caused cell death (approximately 30% in 48 h at 4 microM) but with little apoptosis.
|
| 巻・号 |
524(1-3)
|
| ページ |
37-42
|
| 公開日 |
2002-7-31
|
| DOI |
10.1016/s0014-5793(02)02996-4
|
| PII |
S0014579302029964
|
| PMID |
12135738
|
| MeSH |
Adenosine Triphosphatases / metabolism
Animals
Antiporters / drug effects*
Bone Resorption / prevention & control
CHO Cells
Cell Division / drug effects*
Cricetinae
Gastric Acid / metabolism
Gastritis / prevention & control*
Guinea Pigs
Male
PC12 Cells
Pyrroles / pharmacology*
Rats
Rats, Wistar
Spleen / cytology
Spleen / drug effects
|
| IF |
3.057
|
| 引用数 |
26
|
|
WOS 分野
|
BIOPHYSICS
BIOCHEMISTRY & MOLECULAR BIOLOGY
CELL BIOLOGY
|
| リソース情報 |
| ヒト・動物細胞 |
PC-12(RCB0009) |
