Table 2.
Some compounds that affect autophagy, with their respective mechanism of action.
| Compounds | Effect on Autophagy | Mechanism of Action * | FDA Approval | Reference |
|---|---|---|---|---|
| Chloroquine (CQ) and Hydroxychloroquine (HCQ) | Inhibitors | Interfere with autophagosome-lysosome fusion. | Yes | [220] |
| ARN5187 Lys05 |
Inhibitors | Block autophagosome maturation. | No Yes |
[184,185] |
| Eugenol | Inhibitor | A decline in oxidative stress and activation of ERK1/2, p38MAPK and IKK/NF-κB; downstream, lesser dissociation of the Beclin1-Bcl2 heterodimer and reduced autophagy. | No | [186] |
| Evodiamine | Inhibitor | A decreased formation of the Atg5-Atg12/Atg16 heterotrimer and expression of Atg5, Atg7 and Atg12. | No | [187] |
| Berberine derivatives | Inhibitors | Diminished activation of the MEK/ERK signaling pathway. | No | [221] |
| ULK-100 ULK-101 Compound 6 MRT67307 MRT68921 SBI-0206965 |
Inhibitors | Inhibition of the ULK complex. | No | [188,189,190,191] |
| 3-methyladenine Wortmannin LY294002 PT210 GSK-2126458 |
Inhibitors | Inhibition of PI3K. | No | [192,193,194,195] |
| VPS34-IN1 VVPS34-IN1 Spautin-1 SAR405 Compound 31 PIK-III |
Inhibitors | Inhibition of VPS34. | No | [103,104,196,197,198,199] |
| Spermidine | Activator | An increase in the expression of acetyltransferase EP300, known to bind to crucial autophagy proteins (Beclin1 and LC3) and stimulate autophagy. | Substance registration system |
[206] |
| Nonsteroidal anti-inflammatory drugs (NSAIDs): Celecoxib Sodium Salicylate Aspirin Sulfasalazine Piroxicam Indomethacin |
Activators | Modulation of autophagy through the signaling pathways of PI3K/Akt/mTOR, MAPK/ERK1/2, P53/DRAM, AMPK/mTOR, Bip/GRP78, CHOP/GADD153 and HGF/MET. | Yes | [222] |
| Rapamycin and derivative compounds (RAD001, CCI-779 and AP23573). AZD8055 Torin 1 Metformin |
Activators | Inhibition of mTOR. | Yes No Yes |
[223] |
| Vitamin D3 | Activator | Activation of autophagy, though the pathway is unclear. Stimulation of calcium signaling is a proposed mechanism. | No | [224] |
| Resveratrol | Activator | Activation of autophagy by triggering the cAMPPRKA- AMPK-SI RT1 signaling pathway. |
Clinical trial on animals (cancer therapy). |
[225] |
| Trehalose | Activator | Activity independent of mTOR. | A food additive. | [209] |
* Only mechanisms of action associated with autophagy are mentioned. Some compounds act on other cellular processes.