Monensin(protein transport inhibitor) is an ionophore, which can destroy the Golgi apparatus and inhibit intracellular protein transport. Monensin is commonly used as a protein transport inhibitor.
Monensin is also often used to inhibit the secretion of secreted proteins such as cytokines, and to enhance the staining of secreted proteins by inhibiting secretion during immunostaining. As an ionophore, Monensin can selectively bind monovalent cations into Li+,Na+,K+,Rb+,Ag+ and Ti+, and transport these cations to the cell membrane[3,4].
Monensin could significantly inhibit the proliferation of A549 cells in vitro.Monensin induced G phase arrest in A549 cells, and the proteins related to G phase arrest were changed.Monensin can promote autophagy in A549 cells.Monensin can induce apoptosis in A549 cells[1]. Monensin is a potent inducer of oxidative stress and inhibitor of androgen signaling leading to apoptosis in prostate cancer cells. Monensin as a potential well-tolerated, in vivo compatible drug with strong proapoptotic effects in prostate cancer cells, and synergistic effects with antiandrogens[5].Nanomolar concentrations of Monensin inhibit early stages of capillary network formation in glioblastoma endothelial cells Monensin inhibits multiple endothelial events, including migration, growth and survival, without affecting adhesion to Matrigel by inhibiting VEGFR and EGFR Mediated signaling pathways act on endothelial cells[2]. Monensin can inhibit the proliferation and migration and activate apoptosis of breast cancer cells via downregulating the expression of UBA2[7].
The findings from electron microscopy such as membrane disruption, swelling and disintegration of Golgi apparatus strongly suggest the interference of monensin with the functioning of Golgi apparatus in the spermatogenic cells. Data from the sperm number and motility as well as the fertility studies and the resulted litter size further points towards the antifertility effects of monensin in male rats[6].
References:
[1]:Guo RT. Preliminary study on the mechanism of monensin action on A549 cells.2018. Qufu Normal University,MA Thesis.
[2]: Wan W, Zhang X, et,al. Monensin inhibits glioblastoma angiogenesis via targeting multiple growth factor receptor signaling. Biochem Biophys Res Commun. 2020 Sep 17;530(2):479-484. doi: 10.1016/j.bbrc.2020.05.057. Epub 2020 Jun 25. PMID: 32595038.
[3]: Nachliel E, Finkelstein Y, et,al.The mechanism of monensin-mediated cation exchange based on real time measurements. Biochim Biophys Acta. 1996 Dec 4;1285(2):131-45. doi: 10.1016/s0005-2736(96)00149-6. PMID: 8972697.
[4]: Huczy¨?ski A, Klejborowska G, et,al. Anti-proliferative activity of Monensin and its tertiary amide derivatives. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4539-43. doi: 10.1016/j.bmcl.2015.08.067. Epub 2015 Aug 28. PMID: 26338363.
[5]: Ketola K, Vainio P, et,al. Monensin is a potent inducer of oxidative stress and inhibitor of androgen signaling leading to apoptosis in prostate cancer cells. Mol Cancer Ther. 2010 Dec;9(12):3175-85. doi: 10.1158/1535-7163.MCT-10-0368. PMID: 21159605.
[6]: Singh M, Kalla NR, et,al. Testicular effects of monensin, a golgi interfering agent in male rats. Drug Chem Toxicol. 2014 Oct;37(4):384-90. doi: 10.3109/01480545.2013.866955. Epub 2013 Dec 16. PMID: 24341700.
[7]: Gu J, Huang L, et,al. Monensin inhibits proliferation, migration, and promotes apoptosis of breast cancer cells via downregulating UBA2. Drug Dev Res. 2020 Sep;81(6):745-753. doi: 10.1002/ddr.21683. Epub 2020 May 27. PMID: 32462716.
莫能菌素（蛋白质转运抑制剂）是一种离子载体,可破坏高尔基体,抑制细胞内蛋白质转运。莫能菌素通常用作蛋白质转运抑制剂。
莫能菌素还常用于抑制细胞因子等分泌蛋白的分泌,在免疫染色时通过抑制分泌增强分泌蛋白的染色。作为离子载体,莫能菌素可选择性地结合单价阳离子形成Li+、Na+、K+、Rb+、Ag+和Ti+,并将这些阳离子转运至细胞膜[3,4]。
莫能菌素在体外可显着抑制A549细胞增殖。莫能菌素诱导A549细胞G期阻滞,G期阻滞相关蛋白发生改变。莫能菌素可促进A549细胞自噬。莫能菌素可诱导A549细胞凋亡。 [1]。 Monensin 是一种有效的氧化应激诱导剂和导致前列腺癌细胞凋亡的雄激素信号转导抑制剂。莫能菌素作为一种潜在的耐受性良好、体内相容的药物,在前列腺癌细胞中具有强促凋亡作用,并与抗雄激素药物具有协同作用[5]。纳摩尔浓度的莫能菌素可抑制胶质母细胞瘤早期毛细血管网络形成内皮细胞 Monensin 通过抑制 VEGFR 和 EGFR 介导的信号通路作用于内皮细胞,从而抑制多种内皮事件,包括迁移、生长和存活,而不影响与 Matrigel 的粘附[2]。莫能菌素通过下调UBA2[7]的表达抑制乳腺癌细胞的增殖和迁移并激活细胞凋亡。
高尔基体膜破裂、肿胀和解体等电镜观察结果强烈提示莫能菌素干扰生精细胞中高尔基体的功能。来自精子数量和活力的数据以及生育力研究和产仔数进一步表明了莫能菌素对雄性大鼠的抗生育作用[6]。