| CAS |
No.28643-80-3 |
| 中文名称 |
尼日利亚菌素钠盐 |
| 英文名称 |
Nigericin Sodium Salt |
| 分子式 |
C40H67NaO11 |
| 分子量 |
746.94 |
| 溶解性 |
Soluble in Ethanol ≥5mg/mL |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 608-231-4 |
| MDL |
MFCD27977549 |
| SMILES |
C[C@H]1[C@](O[C@@H]2C[C@](CC[C@@H]3C)([H])O[C@@]3([H])[C@@H](C)C([O-])=O)([C@@H]([C@H](OC)C2)C)O[C@](C)([C@]4([H])O[C@](C)([C@]5([H])O[C@]([C@@]([C@H](C[C@H]6C)C)([H])O[C@@]6(O)CO)([H])C[C@@H]5C)CC4)C1.[Na+] |
| InChIKey |
MOYOTUKECQMGHE-PDEFJWSRSA-M |
| InChI |
InChI=1S/C40H68O11.Na/c1-21-11-12-28(46-33(21)26(6)36(42)43)17-29-18-30(45-10)27(7)40(48-29)25(5)19-38(9,51-40)32-13-14-37(8,49-32)35-23(3)16-31(47-35)34-22(2)15-24(4)39(44,20-41)50-34;/h21-35,41,44H,11-20H2,1-10H3,(H,42,43);/q;+1/p-1/t21-,22-,23-,24+,25+,26+,27+,28+,29+,30+,31+,32+,33+,34-,35+,37-,38-,39-,40+;/m0./s1 |
| PubChem CID |
16760591 |
| 靶点 |
Antibiotic;NLRP3 |
| 通路 |
Immunology & Inflammation;Anti-infection |
| 背景说明 |
Nigericin Sodium Salt是一种抗生素,作为 H+,K+ 和 Pb2+ 离子载体起作用,是NLRP3 的激动剂。 |
| 生物活性 |
Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H+， K+， and Pb2+ ionophore， a NLRP3 activator.[1-4] |
| In Vitro |
Nigericin (0.1 μM) 以剂量依赖的方式降低抑制 H460 肺癌细胞的增殖和克隆形成。尼日利亚菌素抑制 H460 肺癌细胞迁移和侵袭[1]。Nigericin (0.1-10 nM) 显然对细胞体积有双重作用，即在较低的 Nigericin 浓度下有收缩作用，在较高浓度下有膨胀作用。Nigericin (0.1-1 nM) 显著降低细胞溶质 pH (pHi)，并在 5 和 10 nM 时略微增加 PHi[2]。Nigericin 对 S18 细胞的毒性高于 S26 细胞，IC50 分别为 2.03±0.55 μM 和 4.77±2.35 μM。Nigericin 可以在体外选择性地杀死 NPC 中的癌症干细胞。Nigericin 显著降低 S18 和 HONE-1 细胞的迁移能力[3]。Nigericin 对 HT29 和 SW116 细胞系表现出胎儿毒性，IC50 分别为 12.92±0.25 μMol 和 15.86±0.18 μMol。在标准软琼脂测定中，尼日利亚菌素还表现出在不依赖贴壁的条件下形成菌落的能力下降[4]。 |
| In Vivo |
Ngericin (4 mg/kg，ip) 显著减少肿瘤生长并与化疗剂 DDP 协同作用，如肿瘤体积所示。Nigericin 在体内显著降低 Bmi-1。Bmi-1 的过表达部分恢复了尼日利亚菌素处理下 NPC 细胞的 CSC 含量和转移能力。Bmi-1的下调可能与尼日利亚菌素对鼻咽癌干细胞的抑制作用有关[3]。 |
| 细胞实验 |
For RCCs， cells (appr 2000 cells/well) are plated in 96-well cell-culture microplates and incubated over nigericinht in complete media (CM)-RPMI 1640 supplemented with 5% FBS and 2 mM l-glutamine. Cells are then exposed to the appropriate concentration of drug or vehicle for 72 h. For PPSS， cells (appr 500 cells/well) are plated in 96-well cell-culture microplates incubated over Nigericinht in CM to allow them to adhere and then maintained in serum-free media for 7-8 days and then treated with the appropriate concentration of drug or vehicle for 72 h in SFM. Cell viability for cells growing under RCCs and PPSS are evaluated by the MTT assay. The absorbance of solubilized formazan is read at 570 nm using ELISA (enzyme-linked immunosorbent assay) reader. In all cases， the highest concentration of DMSO is used in the control and this concentration is maintained below 0.001% (v/v). This DMSO concentration does not show any significant antiproliferative effect on the cell line in a short-term assay. |
| 动物实验 |
Mice[3]The S18 cells are injected near the scapula of the nude mice. Nine days after injection， the mice are randomly divided into four groups with six animals each (control， DDP， Nigericin and DDP combined with Nigericin). DDP (2.5 mg/kg) is injected intraperitoneally for five continuous days and nigericin (4 mg/kg) is administrated intraperitoneally every two days. Tumor length and width are measured with a vernier caliper every other day. Tumor volume is calculated using the formula V=0.5×(length×width2). The body weights of the mice are recorded every two days. Mice are humanely euthanized when the tumor volume reach 2000 mm3. |
| 数据来源文献 |
[1]. Yakisich JS， et al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiac glycosides. Tumour Biol. 2017 Mar;39(3):1010428317694310
[2]. Bissinger R， et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9
[3]. Deng CC， et al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006
[4]. Zhou HM， et al. Suppression of colorectal cancer metastasis by nigericin through inhibition of epithelial-mesenchymal transition. World J Gastroenterol. 2012 Jun 7;18(21):2640-8 |
| 规格 |
5mg 10mg |
| 单位 |
瓶 |
中文
英语
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