title: Inhibition of bone resorption in cultures of mouse calvariae by apicularen A.
abstract: 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.
authors.affiliation: Laboratory of Pathophysiological Biochemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Miyagi, Japan.
authors.forename: JangJa
authors.initials: J
authors.lastname: Hong
authors.forename: Hirokazu
authors.initials: H
authors.lastname: Sasaki
authors.forename: Kazuaki
authors.initials: K
authors.lastname: Niikura
authors.forename: Maiko
authors.initials: M
authors.lastname: Yanai
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Nakano
authors.forename: Aya
authors.initials: A
authors.lastname: Yokomakura
authors.forename: Kenji
authors.initials: K
authors.lastname: Ishihara
authors.forename: Noriyasu
authors.initials: N
authors.lastname: Hirasawa
authors.forename: Young-Sook
authors.initials: YS
authors.lastname: Kang
authors.forename: Joa Sub
authors.initials: JS
authors.lastname: Oh
authors.forename: Jong Hwan
authors.initials: JH
authors.lastname: Kwak
authors.forename: OkPyo
authors.initials: O
authors.lastname: Zee
authors.forename: Kazuo
authors.initials: K
authors.lastname: Ohuchi
mesh_terms: 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
chemical_list: 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