Hong JangJa, Sasaki Hirokazu, Niikura Kazuaki, Yanai Maiko, Nakano Yasuhiro, Yokomakura Aya, Ishihara Kenji, Hirasawa Noriyasu, Kang Young-Sook, Oh Joa Sub, Kwak Jong Hwan, Zee OkPyo, Ohuchi Kazuo
Laboratory of Pathophysiological Biochemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Miyagi, Japan.
Planta Med. 2007 Feb;73(2):173-5. doi: 10.1055/s-2006-957069.
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.
阿皮拉霉素A和B是从粘细菌类的尖顶软骨霉JW184中分离出来的。阿皮拉霉素A比阿皮拉霉素B更有效地抑制巴弗洛霉素A1敏感的ATP依赖性质子转运到微粒体囊泡中。在人甲状旁腺激素（PTH）或白细胞介素-1β（IL-1β）诱导的小鼠颅骨培养物中的骨吸收在10和100 nM时被阿皮拉霉素A抑制，而阿皮拉霉素B没有作用。双膦酸盐因卡膦酸盐在100 nM时抑制骨吸收，其效果不如阿皮拉霉素A。我们的研究结果表明，阿皮拉霉素A比阿皮拉霉素B更有效地抑制由PTH或IL-1β诱导的骨吸收，这可能是由于对V-ATP酶的抑制作用。
