Piericidin A (AR-054) is a natural mitochondrialNADH-ubiquinone oxidoreductase (complex I)inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action onNADH-ubiquinone reductase. Piericidin A is also a potentialquorum-sensinginhibitor that suppresses the expression of the virulence genes ofErwinia carotovora subsp. atroseptica(Eca). Piericidin A is anADC cytotoxinand has anti-bacterial, anticancer, insecticidal activity^[1][2][2].

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^[1].
The viability of Tn5B1-4 cells is inhibited by Piericidin A in a time- and concentration-dependent manner with IC₅₀value of 0.061 μM, whilst Piericidin A shows slight inhibitory effect on the viability of HepG2 and Hek293 cells with IC₅₀value 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^[3].

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^[1].

415.57

Liquid

C₂₅H₃₇NO₄

2738-64-9

粉蝶霉素A

• Antibiotics
• Other Antibiotics

Streptomyces sp. BCC24731

Room temperature in continental US; may vary elsewhere.

Solution, -20°C, 2 years