Table 2 Summarized data of the most representative results from preclinical studies regarding inhibitory effects of phenolic compounds on Nrf2 signaling pathways
From: Phenolic compounds as Nrf2 inhibitors: potential applications in cancer therapy
Tested extracts/ polyphenolic compounds | Experimental Model | Main results | Ref |
|---|---|---|---|
Cinnamomi Cortex extract | A549 human lung cancer cells | ↓Nrf2 overexpression ↓IGF-1R ↓anticancer drug resistance | |
Chrysanthemum naktongense Nakai licorice Glycyrrhiza uralensis Fisch | HT-29 human colon cancer cells HepG C8 human hepatoma cells | antioxidant ↑detoxifying enzymes induction mediated by ↓Nrf2 ↓NF-κB, ↓pro-inflammatory markers ↑NQO1, ↑Nrf2, ↑UGT1A1, ↑Nrf2-ARE | [104] |
Castanea crenata Siebold & Zucc extract | MCF-7 breast cancer stem cells | ↓Nrf2 ↑susceptibility of cancerc cells to anticancer drugs | [105] |
rosemary extract | HT-29 human colon cancer cells | ↓Nrf2, ↑ ROS ↑apoptosis, ↑cytotoxicity | [106] |
strawberry tree honey | HT-29 human colon cancer cells | ↓NF-kB, ↓P-IkBa, ↓Nrf2 | [107] |
B Bergenia pacumbis (Buch.-Ham. ex D.Don) C.Y.Wu & J.T.Pan extract | PC3 prostate cancer cells PC3 tumor xenograft mice | ↓Nrf2 ↑ apoptosis, ↓MAO-A, ↑ROS ↓tumor growth | [108] |
Rhododendron luteum Sweet extract | HeLa human cervical cancer cells | ↓Nrf2, ↓ mRNA ↑antiproliferative effect | [109] |
Luteolin | NHBE normal human bronchial epithelial NHBE cells exposed to cigarette smoke | IC50 = 5–40 μM ↓toxic effects of cigarette smoke ↑cell viability, ↓oxidative stress, ↓apoptosis ↓Nrf2, ↓NADPH, ↓NQO1, ↓HO-1 | [110] |
Wedelolactone isolated from Eclipta prostrate Lour | IC50 = 2.5–20 μM ↑ NHBE cell viability ↓COX-2, ↓ICAM-1 ↓NQO1, ↓HO-1 | [111] | |
Procyanidins Isolated from Cinnamomi cortex | PC3 prostate cancer cells | IC50 = 2.5 μg/ml ↓Nrf2 ↑antiproliferative effect | |
neferine isolated from Nelumbo nucifera Gaertn. leaves | KYSE30, KYSE150 and KYSE510 esophageal squamous cells carcinoma | IC50 = 0–20 μM ↓Nrf2, ↑ ROS, ↑JNK ↑antiproliferative effect | [113] |
schisantherin A isolated from Fructus schisandrae | MKN45, SGC-7901 gastric cancer cell lines | IC50 = 2.5 μM ↓cell viability, ↓Nrf2 ↑cell cycle arrest, ↑apoptosis ↓migration, ↑ ROS/JNK | [114] |
galloyl glucoses—1,2,3,4,6-penta-O-galloyl-β-D-glucose 1,3,6 -tri-O-galloyl-β-d-glucose isolated from Excoecaria formosana | Huh7 cancer liver cells | ↓Nrf2 ↑antiproliferative effect | [115] |
agrimoniin isolated from Agrimonia pilosa Aitch | PANC-1, CFPAC-1 pancreatic cancer cells | IC50 = 100, 200, 300 μM ↓Nrf2, ↑ ROS ↑apoptosis | [116] |
pterostilbene a natural dimethoxylated analog of resveratrol | Tumour xenograft mice with human melanomas | ↓Nrf2 ↓tumor growth of melanomas | [117] |