Alendronate sodium hydrate is a nitrogen-containing bisphosphonate that strongly inhibits bone resorption, it is often used in research on the prevention and treatment of osteoporosis [1]. Alendronate sodium hydrate has a strong affinity for circulating calcium and minerals on the bone surface, and inhibits the enzyme activity in osteoclasts, thereby hindering the dissolution of bone tissue and the degradation of collagen [2].
Alendronate sodium hydrate (10-4mol/L) incubated for 48 hours significantly reduced the collagen synthesis of osteoblasts. Alendronate sodium hydrate at a concentration of 10-12-10-5mol/L has no effect on calcium deposition in normal human osteoblasts [3].
Alendronate sodium hydrate (25mg/kg) treatment twice each week for 8 weeks, exhibited a reversal of mouse liver fibrosis to a significant extent, and the expression of α-SMA positive cells in the hepatic fibrosis area was significantly reduced in CCl4 induced liver fibrosis mouse model [4]. Alendronate sodium hydrate (0.01 to 0.25mg/kg, s.c., 11 days) preserves alveolar bone resorption and has anti-inflammatory and antibacterial activities in experimental periodontitis [5]. Alendronate sodium hydrate pretreated mice (0.1mg/kg twice a week or once a week) combined with paclitaxel administration (10-50mg/kg/day twice a week or once a week) statistically significantly blocked the growth of PC3 ML tumors in bone marrow and soft tissue. And significantly improve survival time [6].
References:
[1] Bell NH, Johnson RH. Bisphosphonates in the treatment of osteoporosis. Endocrine. 1997 Apr;6:203-6.
[2] Iwamoto J, Miyata A, Sato Y, Takeda T, Matsumoto H. Five-year alendronate treatment outcome in older postmenopausal Japanese women with osteoporosis or osteopenia and clinical risk factors for fractures. Therapeutics and Clinical Risk Management. 2009 Oct 12:773-9.
[3] Garcia-Moreno C, Serrano S, Nacher M, Farré M, Diez A, Marinoso ML, Carbonell J, Mellibovsky L, Nogués X, Ballester J, Aubía J. Effect of alendronate on cultured normal human osteoblasts. Bone. 1998 Mar 1;22(3):233-9.
[4] Bi WR, Jin CX, Xu GT, Yang CQ. Effect of alendronate sodium on the expression of mesenchymal-epithelial transition markers in mice with liver fibrosis. Experimental and Therapeutic Medicine. 2013 Jan;5(1):247-52.
[5] Menezes AM, Rocha FA, Chaves HV, Carvalho CB, Ribeiro RA, Brito GA. Effect of sodium alendronate on alveolar bone resorption in experimental periodontitis in rats. Journal of periodontology. 2005 Nov;76(11):1901-9.
[6] Stearns ME, Wang M. Effects of alendronate and taxol on PC-3 ML cell bone metastases in SCID mice. Invasion & Metastasis. 1996 Jan 1;16(3):116-31.
Alendronate sodium hydrate是含氮双膦酸盐，强力抑制骨吸收，常用于预防和治疗骨质疏松症的研究[1]。Alendronate sodium hydrate 对循环钙和骨表面的矿物质具有很强的亲和力，并抑制破骨细胞中的酶活性，从而阻碍骨组织的溶解和胶原蛋白的降解[2]。
Alendronate sodium hydrate(10-4mol/L)孵育48 h显著减少了成骨细胞的胶原合成。10-12-10-5mol/L浓度的Alendronate sodium hydrate对正常人成骨细胞的钙沉积无影响[3]。
每周两次给予Alendronate sodium hydrate（25mg/kg），持续 8 周，可显著逆转小鼠肝纤维化，CCl4 诱发的肝纤维化小鼠模型中肝纤维化区域 α-SMA 阳性细胞的表达显著降低 [4]。Alendronate sodium hydrate（0.01 to 0.25mg/kg, s.c., 11 days）可保持牙槽骨吸收，并在实验性牙周炎中具有抗炎和抗菌活性[5]。lendronate sodium hydrate预处理小鼠(0.1mg/kg，一周两次或一周一次)，并联合紫杉醇给药(10-50mg/kg/day，一周两次或一周一次)统计学上显著阻断骨髓和软组织中PC-3 ML肿瘤的生长，并显著提高生存时间 [6]。