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尼日利亚菌素钠

尼日利亚菌素钠用途

Nigericin sodium salt 是从吸水链霉菌中得到的一种抗生素,作为 H+,K+ 和 Pb2+ 离子载体起作用。

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尼日利亚菌素钠名称

[ CAS 号 ]:
28643-80-3

[ 中文名 ]:
尼日利亚菌素钠

[ 英文名 ]:
Nigericin sodium salt

[英文别名 ]:

Nigericin,Natrium-Salz
nigericin.Na
nigericin monosodium salt
Leelamine hydrochloride
nigericin sodium
Nigericinsodiumsalt
sodium nigericin
Nigericin sodium salt
Nigericin (sodium salt)

尼日利亚菌素钠生物活性

[ 描述 ]:

Nigericin sodium salt 是从吸水链霉菌中得到的一种抗生素,作为 H+,K+ 和 Pb2+ 离子载体起作用。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 癌症

[体外研究]

Nigericin(0.1μM)以剂量依赖性方式降低H460肺癌细胞的增殖和克隆形成。 Nigericin抑制H460肺癌细胞的迁移和侵袭[1]。尼日利亚(0.1-10 nM)显然对细胞体积具有双重作用,即在较低的Nigericin浓度下具有收缩效应,在较高浓度下具有溶胀效应。尼日利亚(0.1-1 nM)显着降低细胞溶质pH(pHi),并在5和10 nM时略微增加pHi [2]。与S26细胞相比,尼日利亚对S18细胞的毒性更高,IC50分别为2.03±0.55μM和4.77±2.35μM。 Nigericin可以在体外选择性地杀死NPC中的癌症干细胞。尼日利亚显着降低了S18和HONE-1细胞的迁移能力[3]。 Nigericin对HT29和SW116细胞系具有gteat毒性,IC50为12.92±0.25μmol和15.86±0.18μmol。在标准软琼脂试验中,Nigericin还显示在锚定非依赖性条件下形成菌落的能力降低[4]。

[体内研究]

Ngericin(4mg/kg,ip)显着降低肿瘤生长并与化学治疗剂DDP协同作用,如肿瘤体积所示。 Nigericin在体内显着降低Bmi-1。在Nigericin处理下,Bmi-1的过表达部分恢复了NPC细胞的CSC含量和转移能力。 Bmi-1的下调可能参与了Ngericin对NPC中CSCs的抑制作用[3]。

[细胞实验]

对于RCC，将细胞（约2000细胞/孔）接种于96孔细胞培养微孔板中，并在补充有5％FBS，2mM L-谷氨酰胺，100U / mL的完全培养基（CM）-RPMI 1640中通过尼日利亚培养物孵育。青霉素和100 mg / mL链霉素使它们粘附。然后将细胞暴露于适当浓度的药物或载体72小时。对于PPSS，将细胞（约500细胞/孔）接种于96孔细胞培养微孔板中，在CM中用Nigericinh孵育，使其粘附，然后在无血清培养基中维持7-8天，然后用适当的处理。在SFM中药物或载体的浓度为72小时。通过MTT测定评估在RCC和PPSS下生长的细胞的细胞活力。使用ELISA（酶联免疫吸附测定）读数器在570nm处读取溶解的甲amount的吸光度。在所有情况下，在对照中使用最高浓度的DMSO，并且该浓度保持低于0.001％（v / v）。在短期测定中，该DMSO浓度未显示对细胞系的任何显着的抗增殖作用。

[动物实验]

小鼠[3]将S18细胞注射到裸鼠的肩胛骨附近。注射后9天，将小鼠随机分成4组，每组6只动物（对照组，DDP，Nigericin和DDP与Nigericin组合）。腹膜内注射DDP（2.5mg / kg）连续5天，并且每两天腹膜内注射尼日利亚（4mg / kg）。每隔一天用游标卡尺测量肿瘤长度和宽度。使用公式V = 0.5×（长度×宽度2）计算肿瘤体积。每两天记录小鼠的体重。当肿瘤体积达到2000mm 3时，小鼠被人道地安乐死。

[参考文献]

[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

[相关活性小分子]

尼日利亚菌素钠物理化学性质

[ 密度 ]:
1.19g/cm3

[ 沸点 ]:
779.9ºC at 760mmHg

[ 分子式 ]:
C₄₀H₆₇NaO₁₁

[ 分子量 ]:
746.943

[ 闪点 ]:
226.9ºC

[ 精确质量 ]:
746.458130

[ PSA ]:
145.20000

[ LogP ]:
4.37090

[ 蒸汽压 ]:
4.26E-28mmHg at 25°C

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
Soluble in chloroform, methanol or ethanol

尼日利亚菌素钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QT6840000

CHEMICAL NAME :: Nigericin, monosodium salt

CAS REGISTRY NUMBER :: 28643-80-3

LAST UPDATED :: 198910

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C40-H68-O11.Na

MOLECULAR WEIGHT :: 748.07

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 48 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 30,77-5,1977 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 5 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 27,81A,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 5 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 27,81A,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 5 mg/kg

SEX/DURATION :: female 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 27,81A,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 5 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 33,47,1986

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尼日利亚菌素钠安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H315-H319-H335

[ 警示性声明 ]:
P261-P301 + P310-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R25;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36/37/39-S45

[ 危险品运输编码 ]:
UN 3462

[ WGK德国 ]:
3

[ RTECS号 ]:
QT6840000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
29419090

尼日利亚菌素钠文献

Caspase-dependent cell death-associated release of nucleosome and damage-associated molecular patterns.

Cell Death Dis. 5 , e1494, (2014)

Apoptosis, which is anti-inflammatory, and necrosis, which is pro-inflammatory, represent the extremes of the cell death spectrum. Cell death is complex and both apoptosis and necrosis can be observed...

In Vitro Assessment of Uptake and Lysosomal Sequestration of Respiratory Drugs in Alveolar Macrophage Cell Line NR8383.

Pharm. Res. 32 , 3937-51, (2015)

To assess accumulation and lysosomal sequestration of 9 drugs used in respiratory indications (plus imipramine as positive control) in the alveolar macrophage (AM) cell line NR8383.For all drugs, upta...

Caspase-8 as an Effector and Regulator of NLRP3 Inflammasome Signaling.

J. Biol. Chem. 290 , 20167-84, (2015)

We recently described the induction of noncanonical IL-1β processing via caspase-8 recruited to ripoptosome signaling platforms in myeloid leukocytes. Here, we demonstrate that activated NLRP3·ASC inf...

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