粉蝶霉素A

用途生物活性体外研究体内研究粉蝶霉素A 试剂级价格

粉蝶霉素A

CAS号:2738-64-9
英文名:PIERICIDIN A
中文名:粉蝶霉素A
CBNumber:CB9758229
分子式:C25H37NO4
分子量:415.57
MOL File:2738-64-9.mol

粉蝶霉素A化学性质

沸点 :614.9±55.0 °C(Predicted)
密度 :1.044±0.06 g/cm3(Predicted)
闪点 :85 °C
储存条件 :2-8°C
溶解度 :Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 20 mg/ml).
酸度系数(pKa) :5.21±0.33(Predicted)
形态 :liquid
颜色 :green-yellow
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or Ethanol may be stored at -20°C for up to 1 month.

安全信息

危险品标志 :T+,Xn
危险类别码 :26/27/28-20/21/22
安全说明 :28-36/37-45
危险品运输编号 :UN 3382 6.1/PG 1
WGK Germany :3
RTECS号 :YD4588000
F :3-10
海关编码 :2933399990

粉蝶霉素A性质、用途与生产工艺

用途粉蝶霉素A源自链霉菌属的Streptomyces mobaraensis，可用作抗生素。
生物活性 Piericidin A (AR-054) 是一种天然线粒体 NADH-泛醌氧化还原酶 (复合物 I; complex I) 抑制剂。Piericidin A 是一种有效的神经毒素，通过其对 NADH-泛醌还原酶 (NADH-ubiquinone reductase) 的作用破坏电子传输系统，从而抑制线粒体呼吸。Piericidin A 还是一种潜在的群体感应抑制剂，可抑制胡萝卜欧文氏菌亚种 atroseptica (Eca) 的毒力基因的表达。Piericidin A 是一种 ADC 细胞毒素，具有抗菌，抗癌，杀虫活性。
体外研究

In a cell free assay, the potency of Piericidin A to inhibit mitochondrial complex I is ∼2 fold smaller than the one of annonacin. In cultured neurons, Piericidin A potently induces the redistribution of phosphorylated tau from the dendrites into the cell soma and induces cell death.
The viability of Tn5B1-4 cells is inhibited by Piericidin A in a time- and concentration-dependent manner with IC ₅₀ value of 0.061 μM, whilst Piericidin A shows slight inhibitory effect on the viability of HepG2 and Hek293 cells with IC ₅₀ value of 233.97 μM and 228.96 μM, respectively. Piericidin A induces apoptosis of Tn5B1-4 cells coincides with a decrease in the mitochondrial membrane potential.
体内研究

Piericidin A (0.5 mg/kg/d; for 28 days via osmotic minipumps) significantly increases the number of phospho-tau immunoreactive cells in the cerebral cortex in P301S ^+/+ mice. Piericidin A leads to increased levels of pathologically phosphorylated tau only in P301S ^+/+ mice. The synaptic density is reduced by Piericidin A treatment in P301S ^+/+ mice. Exposure to Piericidin A aggravates the course of genetically determined tau pathology.