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Piericidin A

CAS No. : 2738-64-9

MCE 站：Piericidin A

产品活性：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-ubiqui 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。

研究领域：Anti-infection  |  Antibody-drug Conjugate/ADC Related  |  Metabolic Enzyme/Protease

作用靶点：Bacterial  |  ADC Cytotoxin  |  Antibiotic  |  Mitochondrial Metabolism

In Vitro: 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 IC₅₀ value of 0.061 μM, whilst Piericidin A shows slight inhibitory effect on the viability of HepG2 and Hek293 cells with IC₅₀ 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.

In Vivo: 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.

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