Table 1.
Mitochondrial CI inhibitors with anti-cancer proprieties.
| Inhibitor | Mechanism of Action | Cellular Model | References |
|---|---|---|---|
| Rotenone | Induces cell death under starvation in vitro Increases ROS production in vitro |
Breast cancer cells, bovine heart mitochondria | [87,88] |
| Piericidin A | Induces cell death under starvation in vitro Increases ROS production in vitro |
Breast, pancreatic and lung cancer cells, bovine heart mitochondria | [87] |
| Capsaicin | Induces cell death under starvation in vitro | Breast cancer cells | [87] |
| Metformin | Induces cell death under starvation in vitro Promotes AMPK phosphorylation Induces HIF1α destabilization under hypoxic conditions |
Colon, lung, breast, cervical, osteosarcoma, oral carcinoma cancer cells | [94,96,100,101,102] |
| Phenformin | Induces cell death under starvation in vitro Promotes AMPK phosphorylation Induces HIF1α destabilization under hypoxic conditions |
Colon and breast cancer cells and xenografts | [94,103,104,105] |
| BAY 87-2243 | Induces cell death under starvation in vitro Decreases tumor growth in vivo Promotes AMPK phosphorylation Induces HIF1α destabilization under hypoxic conditionsIncreases intracellular ROS levels |
Lung cancer and melanoma cells and xenografts | [92,95] |
| AG311 | Induces cell death under starvation in vitro Decreases tumor growth in vivo Promotes AMPK phosphorylation Induces HIF1α destabilization under hypoxic conditions Induces mitochondrial superoxide production |
Breast cancer cells and xenografts | [93,106] |
| Fenofibrate | Induces cell death in vitro | Glioblastoma cells | [99] |
| JCI-20679 | Induces cell death in vitro | A panel of 39 human cancer cell lines | [107] |
| Celastrol | Promotes ROS production and apoptosis in vitro | Lung cancer and hepatocellular carcinoma cells | [108] |
| Kalkitoxin | Induces cell death in vitro Induces HIF1α destabilization under hypoxic conditions |
Neuroblastoma, breast and colon cancer cells | [109] |
| Lehualide B | Induces cell death in vitro | Multiple myeloma cells | [110] |
AMPK: Adenosine monophosphate (AMP)-activated kinase; HIF1α: Hypoxia-inducible factor 1α; ROS: Reactive oxygen species.