Zoledronic Acid
中文名:唑来膦酸
CAS:118072-93-8
品牌:MedChemExpress (MCE)
存储条件:Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性:Zoledronic Acid (Zoledronate) 是第三代双膦酸盐 (BP),具有强大的抗再吸收活性。 Zoledronic Acid 抑制破骨细胞的分化和凋亡。唑来膦酸还具有抗癌作用[1]。
体外:Zoledronic Acid(0.1-1 µM;48 小时)增加骨细胞样 MLO-Y4 细胞中核因子 kB 配体 (RANKL) 和硬化蛋白 mRNA 表达的受体激活剂[2]。
Zoledronic酸增加MLO-Y4细胞破骨细胞生成支持因子的表达[2]。
唑来膦酸通过IL-6/JAK2/STAT3通路增强MLO-Y4细胞中RANKL的表达[2].
唑来膦酸通过调控NF-κB和JNK信号通路抑制破骨细胞分化和功能[3].
唑来膦酸(10 -100 µM;1-7 天)显着降低 MC3T3-E1 细胞的活力[4]。
唑来膦酸(10-100 µM;1-7 天)诱导 MC3T3 细胞凋亡-E1 细胞[4]。
Zoledronic Acid(10-100 µM;4 天)因诱导细胞凋亡而抑制细胞活力[4]。唑来膦酸在浓度 µM[4].
体内:唑来膦酸(0.05 毫克/千克;腹腔注射;每周;持续 3 周)增加骨矿物质密度和含量[5]。
唑来膦酸(0.5-1 毫克/千克;腹腔注射;每周; 持续 3 周)抑制破骨细胞和成骨细胞的功能以及体内骨重塑,干扰骨力学性能[5]。
参考文献:
[1]. Lianwei Wang, et al. Various pathways of zoledronic acid against osteoclasts and bone cancer metastasis: a brief review. BMC Cancer. 2020; 20: 1059.
[2]. Hyung Joon Kim, et al. Zoledronate Enhances Osteocyte-Mediated Osteoclast Differentiation by IL-6/RANKL Axis. Int J Mol Sci. 2019 Mar; 20(6): 1467.
[3]. Xiao-Lin Huang, et al. Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways. Int J Mol Med. 2019 Aug;44(2):582-592.
[4]. XIN HUANG, et al. Dose-dependent inhibitory effects of zoledronic acid on osteoblast viability and function in vitro. Mol Med Rep. 2016 Jan; 13(1): 613-622.
[5]. Samantha Pozzi, et al. High-dose zoledronic acid impacts bone remodeling with effects on osteoblastic lineage and bone mechanical properties. Clin Cancer Res. 2009 Sep 15;15(18):5829-39.
[6]. Shea GKH, et al. Oral Zoledronic acid bisphosphonate for the treatment of chronic low back pain with associated Modic changes: A pilot randomized controlled trial. J Orthop Res. 2022 Feb 23.