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Effect of Bisphosphonate on Osteoclast of Bone

机译:双膦酸盐对骨破骨细胞的影响

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Bisphosphonates are synthetic analogues of naturally occurring pyrophosphate molecule and are potent inhibitors of osteoclastic bone resorption. Bisphosphonates bind to hydroxyapatite crystals with high affinity and after incorporation by osteoclasts, the primary target cell, it inhibits osteoclastic bone resorption. The anti-resorptive effect has been shown to occur in organ culture as well as in-vivo, but the precise mechanism by which it exerts its bone resorbing effect is not yet fully understood. In vitro and in vivo studies have demonstrated that zoledronate is a more potent inhibitor of osteoclasts than earlier bisphosphonates. Bisphosphonates have now emerged as a leading therapeutic agent for the treatment of hypercalcaemia of malignancy, bone metabolic diseases, Paget’s disease and postmenopausal osteoporosis.
机译:双膦酸盐是天然存在的焦磷酸盐分子的合成类似物,是破骨细胞骨吸收的有效抑制剂。双膦酸盐以高亲和力与羟基磷灰石晶体结合,并通过破骨细胞(主要的靶细胞)掺入后,抑制破骨细胞的骨吸收。已经显示抗吸收作用在器官培养物中以及在体内都发生,但是还没有完全了解其发挥其骨吸收作用的确切机制。体外和体内研究表明,唑来膦酸盐是比早期双膦酸盐更有效的破骨细胞抑制剂。现在,双膦酸盐已成为治疗恶性肿瘤高钙血症,骨代谢疾病,佩吉特氏病和绝经后骨质疏松症的主要治疗剂。

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