Nemoto R, Satou S, Miyagawa I, Koiso K
Department of Urology, Tottori University School of Medicine, Yonago, Japan.
Cancer. 1991 Feb 1;67(3):643-8. doi: 10.1002/1097-0142(19910201)67:3<643::aid-cncr2820670320>3.0.co;2-w.
A new bisphosphonate, 4-amino-1-hydroxybuthylidene-1,1-bisphosphonate (AHBuBP), was compared with 3-amino-1-hydroxypropylidene-1,1-bisphosphonate (AHPrBP) and 1-hydroxyethylidene-1,1-bisphosphonate (HEBP) in terms of its effect on tumor-induced osteolysis using a bladder tumor in mice (MBT-2). Tumor cells were inoculated subcutaneously (SC) over the calvaria in mice, resulting in a local tumor causing fragmentation of the bone. The tumor-induced osteolysis associated with osteoclasts proliferation was accompanied with reactive new bone formation. This osteolysis was evaluated by measuring the increased area of bone resorption in reduced opacity to radiograph and histologic study. The results showed the following sequence of potency: AHBuBP greater than AHPrBP = HEBP. This inhibition was obtained with no apparent effect on the growth of the MBT-2 tumor. The authors conclude that AHBuBP appears to be an interesting new bisphosphonate with possible clinical application.
使用小鼠膀胱肿瘤（MBT - 2）模型，就新型双膦酸盐4 - 氨基 - 1 - 羟基丁叉 - 1,1 - 双膦酸盐（AHBuBP）对肿瘤诱导的骨溶解的影响，将其与3 - 氨基 - 1 - 羟基丙叉 - 1,1 - 双膦酸盐（AHPrBP）和1 - 羟基乙叉 - 1,1 - 双膦酸盐（HEBP）进行了比较。将肿瘤细胞皮下接种于小鼠颅骨上，导致局部肿瘤并引起骨碎裂。与破骨细胞增殖相关的肿瘤诱导的骨溶解伴随着反应性新骨形成。通过测量X线片透明度降低区域的骨吸收增加面积以及组织学研究来评估这种骨溶解。结果显示效力顺序如下：AHBuBP大于AHPrBP = HEBP。这种抑制作用在对MBT - 2肿瘤生长无明显影响的情况下获得。作者得出结论，AHBuBP似乎是一种有潜在临床应用价值的新型双膦酸盐。
