Monensin
(Synonyms: 莫能菌素) 目录号 : GC61079
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。
Cas No.:17090-79-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
A549 cells |
|
Preparation Method |
Different experimental groups were added with different concentrations of monensin medium, and the concentrations were set as 1umol/L and 2 jmol/L. |
|
Reaction Conditions |
1 uM and 2uM monensin for 24h and 48h |
|
Applications |
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. |
| Animal experiment [2]: | |
|
Animal models |
Male Wistar rats |
|
Preparation Method |
Male Wistar rats were administered monensin at the dose levels of 2.5, 5, and 10 mg/kg. Animals were sacrificed after 67 days of the treatment. The activities of lactate dehydrogenase (LDH), ATPase, acid phosphatase and thiamine pyrophosphatase (TPPase) were measured in the testis. |
|
Dosage form |
2.5, 5, and 10 mg/kg monensin for 67 days |
|
Applications |
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. |
|
References: [1]: Guo RT. Preliminary study on the mechanism of monensin action on A549 cells.2018. Qufu Normal University,MA Thesis. | |
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]。
| Cas No. | 17090-79-8 | SDF | |
| 别名 | 莫能菌素 | ||
| Canonical SMILES | C[C@]1([C@]2([H])O[C@@](CC2)([C@]3([H])O[C@]([C@@]4([H])O[C@](O)([C@@H](C[C@@H]4C)C)CO)([H])C[C@@H]3C)CC)O[C@@]5(CC1)O[C@]([C@@H]([C@H](C5)O)C)([H])[C@@H](C)[C@@H](OC)[C@H](C)C(O)=O | ||
| 分子式 | C36H62O11 | 分子量 | 670.87 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4906 mL | 7.453 mL | 14.906 mL |
| 5 mM | 0.2981 mL | 1.4906 mL | 2.9812 mL |
| 10 mM | 0.1491 mL | 0.7453 mL | 1.4906 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Doxycycline, salinomycin, Monensin and ivermectin repositioned as cancer drugs
Bioorg Med Chem Lett 2019 Jul 1;29(13):1549-1554.PMID:31054863DOI:10.1016/j.bmcl.2019.04.045.
Chemotherapy is one of the standard methods for the treatment of malignant tumors. It aims to cause lethal damage to cellular structures, mainly DNA. Noteworthy, in recent years discoveries of novel anticancer agents from well-known antibiotics have opened up new treatment pathways for several cancer diseases. The aim of this review article is to describe new applications for the following antibiotics: doxycycline (DOX), salinomycin (SAL), Monensin (MON) and ivermectin (IVR) as they are known to show anti-tumor activity, but have not yet been introduced into standard oncological therapy. To date, these agents have been used for the treatment of a broad-spectrum of bacterial and parasitic infectious diseases and are widely available, which is why they were selected. The data presented here clearly show that the antibiotics mentioned above should be recognised in the near future as novel agents able to eradicate cancer cells and cancer stem cells (CSCs) across several cancer types.
Monensin toxicity in cattle
J Anim Sci 1984 Jun;58(6):1499-511.PMID:6378866DOI:10.2527/jas1984.5861499x.
Monensin has been tested to determine its toxicity and safety in cattle. Single dose acute toxicity and signs associated with toxicity were determined by oral gavage, 7-d oral gavage and feeding experiments with high concentrations of Monensin in feed. Oral feeding studies indicated a near complete anorexia resulting from intake of sublethal amounts of Monensin. In these cases, cattle recovered from the insulting dose and resumed growth and feed intake. In long-term chronic feedlot, pasture supplement, and reproduction safety studies conducted with Monensin administered in the feed, the high concentrations caused cattle to show signs of mild Monensin intoxication. Mortality resulted from feeding groups of cattle large quantities of Monensin in small quantities of feed. Furthermore, these studies have demonstrated no detrimental effects upon reproduction. Collectively, these studies indicate that the greatest risk of intoxication occurs when cattle first receive a feed containing Monensin. Mixing errors and misuse situations under actual use conditions have resulted in cases of cattle mortality. In most cases the mortality was predictable based upon the exposure in controlled studies.
Chemotherapeutic Potential of Monensin as an Anti-microbial Agent
Curr Top Med Chem 2018;18(22):1976-1986.PMID:30499391DOI:10.2174/1568026619666181129141151.
Monensin is a lipid-soluble naturally occurring bioactive ionophore produced by Streptomyces spp. Its antimicrobial activity is mediated by its ability to exchange Na+ and K+ ions across the cell membrane thereby disrupting ionic gradients and altering cellular physiology. It is approved by Food and Drug Administration as a veterinary antibiotic to treat coccidiosis. Besides veterinary applications, Monensin exhibits a broad spectrum activity against opportunistic pathogens of humans such as bacteria, virus, fungi and parasites in both drug sensitive and resistant strains. This ionophore can selectively kill pathogens with negligible toxic effect on mammalian cells. In this review, we discuss the therapeutic potential of Monensin as a new broad-spectrum anti-microbial agent that warrants further studies for clinical use.
Co-exposure of Monensin Increased the Risks of Atrazine to Earthworms
Environ Sci Technol 2022 Jun 21;56(12):7883-7894.PMID:35593893DOI:10.1021/acs.est.2c00226.
Antibiotics could enter farmlands through sewage irrigation or manure application, causing combined pollution with pesticides. Antibiotics may affect the environmental fate of pesticides and even increase their bioavailability. In this study, the influence of Monensin on the degradation, toxicity, and availability of atrazine in soil-earthworm microcosms was investigated. Monensin inhibited the degradation of atrazine, changed the metabolite patterns in soil, and increased the bioavailability of atrazine in earthworms. Atrazine and Monensin had a significant synergistic effect on earthworms in the acute toxic test. In long-term toxicity tests, co-exposure of atrazine and Monensin also led to worse effects on earthworms including oxidative stress, energy metabolism disruption, and cocoon production compared to single exposure. The expression of tight junction proteins was down-regulated significantly by Monensin, indicating that the intestinal barrier of earthworms was weakened, possibly causing the increased bioavailability of atrazine. The expressions of heat shock protein 70 (Hsp70) and reproductive and ontogenetic factors (ANN, TCTP) were all downregulated in binary exposure, indicating that the resilience and cocoon production of earthworms were further weakened under combined pollution. Monensin disturbed the energy metabolism and weakened the intestinal barrier of earthworms. These results showed that Monensin increased the risks of atrazine in agricultural areas.
Influence of Monensin on the performance of cattle
J Anim Sci 1984 Jun;58(6):1484-98.PMID:6378865DOI:10.2527/jas1984.5861484x.
Performance data on nearly 16,000 head of cattle that were used in trials to document effects of Monensin on feedlot cattle were summarized. Cattle fed monensin-containing diets gained 1.6% faster, consumed 6.4% less feed and required 7.5% less feed/100 kg gain than cattle fed control diets. Monensin resulted in the greatest improvement in feed/gain at 2.9 Mcal metabolizable energy (ME)/kg diet dry matter (DM). Within the range of Monensin concentrations used in the trials that were summarized (31.8 +/- 7.5 mg/kg DM), high Monensin concentrations did not improve feed/gain over that obtained with lower concentrations. Carcass characteristics were not significantly influenced by Monensin. Responses of cattle to Monensin and implants were additive. Energy metabolism data suggested that Monensin improved digestibility of DM, reduced fasting heat production and increased dietary net energy maintenance (NEm) values more than it increased net energy gain (NEg) values. Data showing the response of cattle to Monensin when fed various dietary protein concentrations or sources of supplemental N suggested that Monensin had a protein sparing effect. Monensin has also been shown to reduce lactic acid production, aid in the control of coccidia and bloat and to be toxic to face and horn fly larva in feces of monensin-fed cattle. In pasture trials, Monensin improved daily gains. When fed to beef cows, Monensin reduced amounts of feed required to maintain cow weight.