Tsubaki Masanobu, Takeda Tomoya, Sakamoto Kotaro, Shimaoka Hirotaka, Fujita Arisa, Itoh Tatsuki, Imano Motohiro, Mashimo Kenji, Fujiwara Daiichiro, Sakaguchi Katsuhiko, Satou Takao, Nishida Shozo
Division of Pharmacotherapy, Kinki University School of Pharmacy Kowakae, Higashi-Osaka, Japan.
Department of Food Science and Nutrition, Kinki University School of Agriculture Nara, Nara, Japan.
Am J Cancer Res. 2014 Dec 15;5(1):168-79. eCollection 2015.
Osteolytic bone disease in multiple myeloma (MM) is associated with upregulated osteoclast activity. Macrophage inflammatory protein-1α (MIP-1α) is crucially involved in the development of osteolytic bone lesions in MM. We previously reported that minodronate inhibited lipopolysaccharide-induced MIP-1α secretion in mouse myeloma cells. However, it remains unknown whether bisphosphonates and statins inhibit MIP-1α secretion by human MM cells. In present study, we investigated whether bisphosphonates and statins had any inhibitory effect on MIP-1α secretion by human myeloma cells and the mechanism underlying this effect. In this study, we found that bisphosphonates and statins inhibited MIP-1α mRNA and MIP-1α secretion and suppressed extracellular signal-regulated kinase 1/2 (ERK1/2) and Akt phosphorylation by inhibiting Ras prenylation. Moreover, bisphosphonates and statins suppressed the expression of acute myeloid leukemia-1A (AML-1A) mRNA, a MIP-1α transcription factor. These results indicate that bisphosphonates and statins suppress the Ras/mitogen-activated protein kinase kinase/ERK/AML-1A and Ras/phosphatidylinositol-3 kinase/Akt/AML-1A pathways, thereby inhibiting MIP-1α secretion by MM cells. Therefore, use of MIP-1α expression inhibitors such as bisphosphonates and statins may provide a new therapeutic approach to inhibiting tumour progression and bone destruction in MM patients.
多发性骨髓瘤(MM)中的溶骨性骨病与破骨细胞活性上调有关。巨噬细胞炎性蛋白-1α(MIP-1α)在MM溶骨性骨病变的发展中起关键作用。我们之前报道过米诺膦酸盐可抑制小鼠骨髓瘤细胞中脂多糖诱导的MIP-1α分泌。然而,双膦酸盐和他汀类药物是否能抑制人骨髓瘤细胞分泌MIP-1α仍不清楚。在本研究中,我们调查了双膦酸盐和他汀类药物对人骨髓瘤细胞分泌MIP-1α是否有抑制作用以及该作用的潜在机制。在本研究中,我们发现双膦酸盐和他汀类药物通过抑制Ras异戊二烯化来抑制MIP-1α mRNA和MIP-1α分泌,并抑制细胞外信号调节激酶1/2(ERK1/2)和Akt磷酸化。此外,双膦酸盐和他汀类药物抑制了MIP-1α转录因子急性髓系白血病-1A(AML-1A)mRNA的表达。这些结果表明,双膦酸盐和他汀类药物抑制Ras/丝裂原活化蛋白激酶激酶/ERK/AML-1A和Ras/磷脂酰肌醇-3激酶/Akt/AML-1A信号通路,从而抑制骨髓瘤细胞分泌MIP-1α。因此,使用双膦酸盐和他汀类药物等MIP-1α表达抑制剂可能为抑制MM患者的肿瘤进展和骨破坏提供一种新的治疗方法。