Table 1 Examples of autophagy inhibitors and activators for colitis/CRC therapy
From: The role of autophagy in colitis-associated colorectal cancer
Drugs | Mechanism | Effects | Ref. |
|---|---|---|---|
Autophagy inhibitors | Â | Â | Â |
 3-MA | Prevents autophagosome formation | Enhances the apoptosis effect of 5-FU (5-fluorouracil) in CRC | |
 CQ | Inhibits lysosomal acidification and prevents fusion with autophagosomes | 1. Enhances the apoptosis effect of 5-FU in CRC | |
| Â | Â | 2. Augments sunitinib-induced apoptosis and enhances the antiangiogenic capacity of sunitinib | Â |
| Â | Â | 3. Enhances trichostatin A-induced apoptosis in radiotherapy-treated colon cancer cells | Â |
| Â | Â | 4. Enhances sensitivity to oxaliplatin and bevacizumab | Â |
| Â | Â | 5. Triggers apoptosis of CSCs and decreases colonosphere formation ability combined with PDT (photodynamic therapy) in vitro and tumorigenicity in vivo | Â |
 Lys05 | Deacidifies the lysosome | Displays single-agent antitumor activity in vivo | |
 Bafilomycin-A1 | Inhibits fusion between autophagosomes and lysosomes | Enhances pyrrolo-1,5-benzoxazepine-6-induced apoptosis | |
 Vitexin | Downregulates ATG5, beclin-1, LC3-II | Induces apoptosis and suppresses tumor growth in an HCT116 xenograft model | |
Autophagy activators | Â | Â | Â |
 Andrographolide | Suppresses the PIK3CA-AKT1-MTOR-RPS6KB1 pathway | Attenuates colitis progression and tumor burden | |
 AZD-2014 | Inhibits mTOR | Inhibits the growth of HT-29 cell xenografts in SCID mice and improves mice survival | |
 Silibinin | Induces autophagic death mediated by endoplasmic reticulum stress | Induces autophagic death of colon cancer cells and CRC xenograft | |
 Temsirolimus | Inhibits mTOR | Inhibits cell growth via anti-angiogenesis activity and enhances apoptosis | |
 Resveratrol | Induces autophagy-mediated through ROS | Induces apoptosis | |
 Bufalin | Induces autophagy-mediated through ROS | Induces autophagic cell death | |
 BIX-01294 | Induces autophagy via EHMT2 (euchromatic histone-lysine N-methyltransferase 2) dysfunction and intracellular ROS accumulation | Induces autophagy cell death | |
 Celastrol | Suppresses the PI3K/Akt/mTOR signaling pathway | Ameliorates experimental colitis in IL-10-deficient mice | |
 BCG/CWS (Mycobacterium bovis Bacille Calmette–Guerin cell wall skeleton) | Induces autophagy-mediated through ROS | Enhances radiotherapy effect in colon cancer cells |
