苏拉明钠
中文名称:
苏拉明钠
中文同义词:
苏拉明钠(SURAMIN);8,8-碳酰双亚氨-3,1-亚苯基碳酰亚氨-(4-甲基-3,1-亚苯基)碳酰亚氨双-1,3,5-萘三磺酸六钠;苏拉明钠;苏拉明钠盐;蘇拉明鈉;苏拉明;舒拉明钠;DNA拓扑异构酶II抑制剂(多磺化萘脲)
英文名称:
Suramin sodium
英文同义词:
naphuridesodium;nf060;reasodiumsalt;sodiumsuramin;suraminesodium;SURAMIN;SURAMIN SODIUM, 98+%;8,8-[Carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bis-1,3,5-naphthalenetrisulfoni
CAS号:
129-46-4
分子式:
C51H34N6Na6O23S6
分子量:
1429.17
EINECS号:
204-949-3
相关类别:
小分子抑制剂，天然产物;合成;小分子抑制剂;细胞生物学试剂;医药原料;陕西林奈主打产品;原料;Active Pharmaceutical Ingredients;Purinergics P2 receptor;EPIVIR;Inhibitors;化工原料
Mol文件:
129-46-4.mol
储存条件
0-6°C
溶解度
H2O: >10mg/mL
形态
Crystalline Powder
颜色
White
PH值
pH(10g/l, 25℃) : 5.0～8.0
水溶解性
soluble
BRN
3694087
背景
苏拉明钠(suramin),又名舒拉明钠、苏拉明等,是德国Bayer AG公司于1961年合成的一种抗锥虫类化合物，主要用于治疗非洲锥虫病和盘尾丝虫病。20世纪80年代，有学者发现苏拉明钠能够抑制肿瘤病毒有关的逆转录酶活性，将苏拉明钠应用于获得性免疫缺陷综合症(acquired immunodeficiency syndrome, AIDS)的治疗，表明苏拉明钠对人类免疫缺陷病毒(human immunodeficiency virus,HIV)有一定的抑制作用
简介
苏拉明钠是一种可逆的竞争性蛋白酪氨酸磷酸酶 (PTPases) 抑制剂。苏拉明钠是有效的 sirtuins 抑制剂：SirT1 (IC50=297 nM)，SirT2 (IC50=1.15 μM)，SirT5 (IC50=22 μM)。苏拉明钠是竞争性逆转录酶抑制剂 (DNA topoisomerase II: IC50=5 μM)。苏拉明钠有效抑制 IP5K，并且是抗寄生虫 (antiparasitic)，抗肿瘤和抗血管生成剂。
应用
苏拉明钠已经被证实具有抗锥虫病，抗肿瘤，防治眼部增殖性疾病，抗病毒，免疫调节剂的作用，并广泛应用于临床实践中。目前尚未有苏拉明钠具有抗鸡球虫作用的报导，通过苏拉明钠已知的性质无法推断其是否具有抗鸡球虫的作用。
生物活性
Suramin sodium salt (Suramin hexasodium salt) 是一种可逆的竞争性蛋白酪氨酸磷酸酶 (PTPases) 抑制剂。Suramin sodium salt 是有效的 sirtuins 抑制剂：SirT1 (IC50=297 nM)，SirT2 (IC50=1.15 μM)，SirT5 (IC50=22 μM)。Suramin sodium salt 是竞争性逆转录酶抑制剂 (DNA topoisomerase II: IC50=5 μM)。Suramin sodium salt 是一种有效的 SARS-CoV-2 RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。Suramin sodium salt 有效抑制 IP5K，并且是抗寄生虫 (antiparasitic)，抗肿瘤和抗血管生成剂。
靶点
SIRT1
297 nM (IC 50 )
SIRT2
1.15 μM (IC 50 )
SIRT5
22 μM (IC 50 )
SIRT1
297 nM (IC 50 )
SIRT2
1.15 μM (IC 50 )
体外研究
Suramin sodium salt (Suramin hexasodium salt; 50-600 μg/mL; for 24-96 hours) inhibits cells proliferation in a dose-dependent and time-dependent manner and decreases viability in cancer cells.
Suramin sodium salt (300 μg/mL; for 48 hours) induces cells apoptosis and down-regulates mRNA expression in HeLa cells.
Suramin sodium salt (1 mg/mL; 1 hour) significantly suppresses the phosphorylated ERK1/2.
The IC 50 values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively.
Suramin blocks viral replication in Vero E6 cells.
Cell Proliferation Assay
Cell Line: HO-8910 PM ovarian and Hela cervical cancer cells
Concentration: 50, 100, 200, 300, 400, 500 and 600 μg/mL
Incubation Time: For 24, 48, 72 and 96 hours
Result: Inhibited cells proliferation in a dose-dependent and time-dependent manner.
Apoptosis Analysis
Cell Line: HeLa cells
Concentration: 300 μg/mL
Incubation Time: For 48 hours
Result: Induced cells apoptosis.
Western Blot Analysis
Cell Line: PA-SMCs cells
Concentration: 1 mg/mL
Incubation Time: For 1 hour
Result: Significantly suppressed the phosphorylated ERK1/2.
Cell Line:
HO-8910 PM ovarian and Hela cervical cancer cells
Concentration:
50, 100, 200, 300, 400, 500 and 600 μg/mL
Incubation Time:
For 24, 48, 72 and 96 hours
Result:
Inhibited cells proliferation in a dose-dependent and time-dependent manner.
Cell Line:
HeLa cells
Concentration:
300 μg/mL
Incubation Time:
For 48 hours
Result:
Induced cells apoptosis.
Cell Line:
PA-SMCs cells
Concentration:
1 mg/mL
Incubation Time:
For 1 hour
Result:
Significantly suppressed the phosphorylated ERK1/2.
体内研究
Suramin sodium salt (Suramin hexasodium salt; 10 mg/kg; IV; twice weekly for 3 weeks) reverses established pulmonary hypertension (PH), thereby normalizing the pulmonary artery pressure values and vessel structure.
Animal Model: Adult male Wistar rats (200-225 g)
Dosage: 10 mg/kg
Administration: IV; twice weekly for 3 weeks
Result: Reversed established PH, thereby normalizing the pulmonary artery pressure values and vessel structure.
Animal Model:
Adult male Wistar rats (200-225 g)
Dosage:
10 mg/kg
Administration:
IV; twice weekly for 3 weeks
Result:
Reversed established PH, thereby normalizing the pulmonary artery pressure values and vessel structure.
安全说明
22-24/25
WGK Germany
3
RTECS号
QM7000000
F
3-10
海关编码
29242998
毒性
LD50 in mice (mg/kg): ~620 i.v. (Hawking)
