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. 2022 Jan 14;12:745683. doi: 10.3389/fphar.2021.745683

TABLE 3.

Anti-cancer effect of crocetin.

Pharmacologic action Subjects Doses Mechanism of action References
Breast cancer Breast cancer rats Reduces the number of tumors Maysam et al. (2011)
Breast tumor BALB/c mice Crocetin (100 mg/kg) Overexpresses EcSOD and increases antioxidant activity Sah et al. (2020)
MCF-7 cells Crocetin (200 μmol/L) Inhibits SOD activity by affecting copper binding sites Sah et al. (2020)
MCF-7 cells Crocetin glucosyl ester IC50 from 31.25 to 1,000 μg/ml Inhibits estrogen receptor α and HDAC2 mediated signaling cascade Mam et al. (2020)
Esophageal cancer KYSE-150 cells Crocetin (0, 12.5, 25, 50, 100, 200 μmol/L) S-phase cell arrest Li et al. (2015)
KYSE-150 cells Crocetin (200 μmol/L) Upregulates the p53/p21 pathway Li et al. (2017)
Gastric cancer AGS cells Crocetin (50–240 μmol/L) Decreases the Bcl-2/Bax ratio of AGS cells Bathaie et al. (2013a)
Gastric cancer rats Reverses changes in serum antioxidant activity and LDH in rats Bathaie et al. (2013b)
SGC7901 cells Crocetin (12.5, 25, 50 μmol/L) Upregulates Bax proteins expression and downregulates Bcl-2 protein expression Zhang (2020)
Colon cancer HCT116 cells Crocetin (30 µM) Downregulates inflammation-related genes, HMGB1, IL-6, and IL-8 Zhuang et al. (2018)
SW480 cells Crocetin (0.8 mM/L) Activates p21 in a P53- independent manner Li et al. (2012)
P53 damage cancer cells Exploits P73 (P53 paralog) through the FAS-associated death domain to induce apoptosis of colon cancer Ray et al. (2016)
Pancreatic cancer Cancer stem cells (CSC) Inhibits the expression of Sonic hedgehog (SHH) Parthasarathy et al. (2015)
MIA-PaCa-2 cells Crocetin (50, 100, 200 μmol/L) Enhances Cdc-2 phosphorylation and inhibits Cyclin B1 Dhar et al. (2009)
Mice without thymus are injected with MIA-PaCa-2 cells Crocetin (4 mg/kg/day) Increases the Bax/Bcl-2 ratio Dhar et al. (2009)
Cervical cancer HeLa cells (240 μmol/L) Inhibits the proliferation of cancer cells by inducing cell cycle arrest at the G1 phase (Zhong et al., 2011)
Cervical cancer model in mice Attenuates the serum levels of IL-1β, TNF-α, PMN, and nitrates Chen et al. (2015)
HeLa cells Upregulates COX-2 expression Chen et al. (2015)
Lung cancer Lung cancer animal Crocetin (20 mg/kg) Increases the activities of glutathione metabolic enzymes and antioxidant enzymes Magesh et al. (2006)
Lung cancer mice Crocetin (50 mg/kg) Inhibits polyamine synthesis and glycoprotein changes Magesh et al. (2010)
A549 cell Crocetin disodium salt Inhibits LDH Granchi et al. (2017)
Prostate cancer Two invasive PCa cell lines (PC3 and 22rv1) in male nude mice Crocetin (30 mg/kg) Interferes with topoisomerase II to induce DNA damage and apoptosis, inhibits the migration and invasion of PCa cells Claudio et al. (2014)
Ovarian cancer A2780 cells Crocetin (25, 50, 100, 200 μmol/L) Reduces the gene expression and efflux function of MRP2 transporters Neyshaburinezhad et al. (2019)
Leukemia HL-60 cells Inhibit cells proliferation and differentiation Tarantilis et al. (1994)
APL cells, NB4 and HL60 cells Crocetin (100 μmol/L) Reduces the expression of prosurvival genes and multidrug resistance proteins and inhibits tyrosyl DNA phosphodiesterase 1 Maliheh et al. (2019)
Skin cancer Female CD-I mice Crocetin (0.2 or 1.0 μmol/L) Inhibits the production of myeloperoxidase and hydrogen peroxide Wang et al. (1995)
B16F10 murine melanoma cells Reduces protein levels of tyrosinase and microphthalmia-associated transcription factor Hashemi et al. (2018)