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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.
AuthorsJangJa Hong, Hirokazu Sasaki, Kazuaki Niikura, Maiko Yanai, Yasuhiro Nakano, Aya Yokomakura, Kenji Ishihara, Noriyasu Hirasawa, Young-Sook Kang, Joa Sub Oh, Jong Hwan Kwak, OkPyo Zee, Kazuo Ohuchi
JournalPlanta medica (Planta Med) Vol. 73 Issue 2 Pg. 173-5 (Feb 2007) ISSN: 0032-0943 [Print] Germany
PMID17415879 (Publication Type: Journal Article)
Chemical References
  • Bridged Bicyclo Compounds, Heterocyclic
  • Diphosphonates
  • Macrolides
  • Parathyroid Hormone
  • apicularen A
  • apicularen B
  • cimadronate
  • bafilomycin A1
  • Vacuolar Proton-Translocating ATPases
Topics
  • Animals
  • Bone Resorption
  • Bridged Bicyclo Compounds, Heterocyclic (chemistry, isolation & purification, pharmacology)
  • Diphosphonates (chemistry, pharmacology)
  • Humans
  • Macrolides (chemistry, isolation & purification, pharmacology)
  • Mice
  • Myxococcales (chemistry)
  • Parathyroid Hormone (pharmacology)
  • Skull (drug effects)
  • Vacuolar Proton-Translocating ATPases (antagonists & inhibitors)

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