Retro-2 acts as a specific inhibitor, blocking retrograde protein transport at the interface between the endosome and the trans-Golgi network. It also serves as an inhibitor against ebolavirus (EBOV) infection, demonstrating an effective concentration (EC50) of 12.2 µM in HeLa cells. Furthermore, Retro-2 triggers autophagy in cells[1][2][3].
体内研究
Treatment with Retro-2 (2-200 mg/kg; i.p; daily; for 21 days) significantly safeguards mice against lethal nasal exposure to ricin. A dose of 200 mg/kg of Retro-2 completely protects mice from the effects of a ricin challenge[1].
体外研究
Retro-2 (1 μM; 1-4 hours) triggers the process of autophagy in HeLa cells that express GFP-LC3, leading to the significant accumulation of large autophagosomes in the cytoplasm[2].
Treatment with Retro-2 (1 μM; 0.5-4 hours) results in a time-dependent increase in the levels of the LC3-II protein within cells[2].
Retro-2 disrupts the transport process between autophagosomes and lysosomes, leading to the inhibition of autolysosome formation[2].
Pretreatment with Retro-2 (20 μM; 30 minutes) prevents intoxication of HeLa cells by ricin, as well as Shiga-like toxins 1 (Stx1) and 2 (Stx2)[1].
Retro-2 inhibits the cellular invasion by the intracellular parasite Leishmania, and also hampers the replication of non-enveloped viruses such as polyoma-, papilloma-, and adeno-associated viruses[3].
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