Inhibition of bone resorption in cultures of mouse calvariae by apicularen A.
Apicularens A and B were isolated from the myxobacterial genus Chondromyces apiculatus JW184. Apicularen A inhibited bafilomycin A1-sensitive ATP-dependent proton transport into microsome vesicles more potently than apicularen B. Bone resorption in cultures of mouse calvariae induced by human parathyroid hormone (PTH) or interleukin-1beta (IL-1beta) was inhibited by apicularen A at 10 and 100 nM, while apicularen B had no effect. The bisphosphonate incadronate inhibited bone resorption at 100 nM, being less effective than apicularen A. Our findings indicate that apicularen A inhibits bone resorption induced by PTH or IL-1beta more potently than apicularen B, probably due to inhibition of the V-ATPase.
Hong
JangJa
J
Laboratory of Pathophysiological Biochemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Miyagi, Japan.
Sasaki
Hirokazu
H
Niikura
Kazuaki
K
Yanai
Maiko
M
Nakano
Yasuhiro
Y
Yokomakura
Aya
A
Ishihara
Kenji
K
Hirasawa
Noriyasu
N
Kang
Young-Sook
YS
Oh
Joa Sub
JS
Kwak
Jong Hwan
JH
Zee
OkPyo
O
Ohuchi
Kazuo
K
D000818:Animals; D001862:Bone Resorption; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004164:Diphosphonates / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D018942:Macrolides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D051379:Mice; D009231:Myxococcales / Q000737:chemistry*; D010281:Parathyroid Hormone / Q000494:pharmacology; D012886:Skull / Q000187:drug effects; D025262:Vacuolar Proton-Translocating ATPases / Q000037:antagonists & inhibitors
D019086:Bridged Bicyclo Compounds, Heterocyclic; D004164:Diphosphonates; D018942:Macrolides; D010281:Parathyroid Hormone; C117813:apicularen A; C117814:apicularen B; C071542:cimadronate; C040929:bafilomycin A1; D025262:Vacuolar Proton-Translocating ATPases