尼日利亚菌素钠盐

中文名称:

尼日利亚菌素钠盐

中文同义词:

尼日利亚菌素钠盐;尼日利亚菌素钠盐, 来源于吸水链霉菌;尼日利亚菌素钠盐,来源于链霉菌,吸湿性菌;NIGERICIN(钠盐形式);尼日利亚菌素钠;尼日利亚菌素钠 NIGERICIN SODIUM SALT;尼日利亚菌素,钠盐, 吸水链霉菌

英文名称:

Nigericin sodium salt

英文同义词:

Nigericin sodium salt;Polyetherin A, Azalomycin M, Helixin C, Antibiotic K178, Antibiotic X-464;Antibiotic K178, Antibiotic X464, Azalomycin M, Helexin C, Polyetherin A;Sodium (2R)-2-[(3S,6R)-6-[[(2S,4R,5R,7R,9R,10R)-2-[(5S)-5-[(2R,3S,5R)-5-[(2S,3S,5R,6R)-6-hydroxy-6-(hydroxymethyl)-3,5-dimethyloxan-2-yl]-3-methyloxolan-2-yl]-5-methyloxolan-2-yl]-9-methoxy-2,4,10-trimethyl-1,6-dioxaspiro[4.5]decan-7-yl]methyl]-3-methyloxan-2-yl]propanoate;Nigericin, monosodium salt;Nsc292567;Nigericin sodium salt,Antibiotic K178, Antibiotic X464, Azalomycin M, Helexin C, Polyetherin A;Nigericin sodiuM sa

CAS号:

28643-80-3

分子式:

C40H69NaO11

分子量:

748.97

EINECS号:

608-231-4

相关类别:

微生物代谢物;抗生素;聚醚类抗生素;抗生素及抗病毒;生化试剂;原料药;API

Mol文件:

28643-80-3.mol

熔点 

approximate 255℃

储存条件 

2-8°C

溶解度 

Soluble in chloroform, methanol or ethanol

形态

solution

Merck 

13,6569

BRN 

3892398

InChIKey

MOYOTUKECQMGHE-NTQCAYBPSA-M

CAS 数据库

28643-80-3

生物活性

Nigericin钠盐是从Streptomyces hygroscopicus衍生的抗生素，通过充当H+，K+和Pb2+的离子载体起作用。Nigericin可以激活NLRP3炎性体以诱导促炎和免疫刺激过程。

靶点

Target Value Potassium channel () Hydrogen channel () Pb 2+ () NLRP3 ()

Target

Value

Potassium channel ()

Hydrogen channel ()

Pb 2+ ()

NLRP3 ()

体外研究

Nigericin (0.1 µM) decreases inhibits proliferation and clonogenicity of H460 lung cancer cells in a dose dependent manner. Nigericin inhibits migration and invasion of H460 lung cancer cells. Nigericin (0.1-10 nM) has apparently a dual effect on cell volume, that is a shrinking effect at lower Nigericin concentrations and a swelling effect at higher concentrations. Nigericin (0.1-1 nM) significantly decreases cytosolic pH (pHi), and slightly increases the pHi at 5 and 10 nM. Nigericin exhibits higher toxicity on S18 cells than S26 cells, with IC 50 of 2.03±0.55 μM and 4.77±2.35 μM, respectively. Nigericin can selectively kill cancer stem cells in NPC in vitro. Nigericin dramatically reduces the migration ability of S18 and HONE-1 cells. Nigericin exhibits gteat toxicity for the HT29 and SW116 cell line with IC 50 of 12.92±0.25 μmol and 15.86±0.18 μmol. Nigericin also shows a decreased ability to form colonies under anchorage-independent conditions in a standard soft agar assay.

体内研究

Ngericin (4 mg/kg, i.p.) significantly reduces tumor growth and acts synergistically with the chemotherapeutic agent DDP, as shown by the tumor volumes. Nigericin markedly decreases Bmi-1 in vivo. Overexpression of Bmi-1 partially restores CSC content and metastatic ability of NPC cells under Nigericin treatment. The downregulation of Bmi-1 may be involved in the inhibitory effect of Nigericin on CSCs in NPC.

危险品标志 

T

危险类别码 

25-36/37/38

安全说明 

26-36/37/39-45

危险品运输编号 

UN 3462 6.1/PG 3

WGK Germany 

3

RTECS号

QT6840000

HazardClass 

6.1

海关编码 

29419090