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CAS号:23256-30-6
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英文名称:nifurtimox
分子式
C10H13N3O5S
分子量
287
EINECS号
245-531-0
MDL
MFCD00869254
Smiles
InChIKey
乙二醇化学百科
基本信息
物化性质
安全信息
生产及用途
硝呋替莫是现在几乎唯一的对这些病原体具有活性的化合物。该活性可能是基于对酶Trypanothione还原酶(一种特殊的锥虫酶)的抑制。这种酶在其他原生动物病原体中是不存在的。硝呋替莫(nifurtimox)是自20世纪70年代以来治疗南美锥虫病(Chagasdisease)的主要药物,为一种硝基杂环类化合物,在细胞内被还原成硝基阴离子自由基、过氧化氢和超氧化物自由基等活性氧(reactiveoxygenspecies,ROS)。硝呋替莫和其他硝基呋喃化合物能够用于治疗癌症和由血管发生所介导或引起的疾病或病症。Nifurtimox (BAY-2502) 是一种抗原虫剂。
Trypanosoma cruzi
Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH). To differentiate if this effect is a result of a reduced LDH activity or a shift in pyruvate metabolism due to activation of PDH, the enzyme activity of LDH is determined after 4 h treatment with 50 µg/mL Nifurtimox. Compared to the untreated control, the LDH activity is significantly reduced for LA-N-1 (P=0.005), IMR-32 (P=0.009), LS (P=0.0035) and SK-N-SH (P=0.0065). Nifurtimox reduces cell viability and induces cell cycle arrest and apoptosis in neuroblastoma cells. To characterize the cytotoxic impacts of Nifurtimox on neuroblastoma, 4 cell lines are subjected to several experiments. Cell viability is reduced for all 4 neuroblastoma cell lines after 24 h incubation with 50 µg/mL to an average of 66%, 63%, 62% and 75% (LA-N-1, IMR-32 LS and SK-N-SH, respectively). The reduction is significant compared to the untreated control (P<0.01) and the vehicle control with DMSO (P<0.05) for all cell lines.
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