依替膦酸（EHDP）抑制破骨细胞介导的骨吸收，促进凋亡并破坏分离的成熟破骨细胞中的肌动蛋白环。

Etidronate (EHDP) inhibits osteoclastic-bone resorption, promotes apoptosis and disrupts actin rings in isolate-mature osteoclasts.

作者信息

Hiroi-Furuya E, Kameda T, Hiura K, Mano H, Miyazawa K, Nakamaru Y, Watanabe-Mano M, Okuda N, Shimada J, Yamamoto Y, Hakeda Y, Kumegawa M

机构信息

Department of Oral Anatomy, Meikai University School of Dentistry, Sakado, Saitama 350-02, Japan.

出版信息

Calcif Tissue Int. 1999 Mar;64(3):219-23. doi: 10.1007/s002239900606.

DOI:10.1007/s002239900606

PMID:10024379

Abstract

Bisphosphonates, therapeutic reagents against tumoral bone diseases (Paget's disease or osteoporosis), are potent inhibitors of bone resorption. The mechanisms by which they directly act on mature osteoclasts remain unclear. Using a recently developed technique for isolation of highly purified mammalian mature osteoclasts, we demonstrated that etidronate [ethane-1-hydroxy-1,1-diphosphonate (EHDP), 1-hydroxy-1,1-ethylidenebisphosphonate], inhibited directly osteoclastic bone-resorbing activity by pit assay. In addition, EHDP also directly induced apoptosis and disrupted actin rings in osteoclasts. The data support previous data on non-purified osteoclasts and results in vivo.

摘要

双膦酸盐是治疗肿瘤性骨疾病（佩吉特氏病或骨质疏松症）的治疗试剂，是骨吸收的有效抑制剂。它们直接作用于成熟破骨细胞的机制尚不清楚。使用最近开发的用于分离高度纯化的哺乳动物成熟破骨细胞的技术，我们证明依替膦酸[乙烷-1-羟基-1,1-二膦酸（EHDP），1-羟基-1,1-亚乙基双膦酸]通过凹坑试验直接抑制破骨细胞的骨吸收活性。此外，EHDP还直接诱导破骨细胞凋亡并破坏肌动蛋白环。这些数据支持了之前关于未纯化破骨细胞的数据以及体内实验结果。