Table 6.
Antiproliferative activity of citral.
| Compound/ Extract |
Doses | Effect | Ref. |
|---|---|---|---|
| Citral | 145.32 µg/mL 85.47 µg/mL 52.63 µg/mL |
Inhibition of HCT116 cell proliferation (IC50: 24, 48, and 72 h) | [89] |
| Citral | 181.21 µg/mL 143.61 µg/mL 91.5 µg/mL |
Inhibition of HT29 cell proliferation (IC50: 24, 48, and 72 h) | [89] |
| Citral | 3.125–200 µM | Inhibition of CCD841-CoN cell (IC50 not detected at 200 μM) | [89] |
| Citral | 3.7 µg/mL | Inhibition of Caco-2 cell proliferation (IC50: 72 h) | [90] |
| CIT-SNEDDS | 38.50 µg/mL 23.75 µg/mL 16.50 µg/mL |
Inhibition of SW620 cell proliferation (IC50: 24, 48, and 72 h) | [88] |
| CIT-SNEDDS | 44.10 µg/mL 36.60 µg/mL 34.10 µg/mL |
Inhibition of HT29 cell proliferation (IC50: 24, 48, and 72 h) | [88] |
| Citral | 31.25 µg/mL 23.30 µg/mL 22.50 µg/mL |
Inhibition of SW620 cell proliferation (IC50: 24, 48, and 72 h) | [88] |
| Citral | 28.33 µg/mL 22.00 µg/mL 21.77 µg/mL |
Inhibition of HT29 cell proliferation (IC50: 24, 48, and 72 h) | [88] |
| Citral | <25 µg/mL | Inhibition of AGS cell proliferation (IC50: 48 h) | [91] |
| Citral | >75 µg/mL | Inhibition of MRC-5 cell proliferation (IC50: 48 h) | |
| Citral | 1.04 µM | Inhibition of B16F10 cell proliferation (IC50: 24 h) | [92] |
| Citral | 11.7 µM | Inhibition of SK-MEL-147 cell proliferation (IC50: 24 h) | |
| Citral | 13.4 µM | Inhibition of UACC-257 cell proliferation (IC50: 24 h) | |
| Citral | 50.3 µM | Inhibition of HaCaT cell proliferation (IC50: 24 h) | |
| Citral | 2.5 µM | Inhibition of NIH-3T3 cell proliferation (IC50: 72 h) | |
| Citral | 7 µg/mL | Inhibition of HepG2 cell proliferation (IC50: 72 h) | [90] |
| Citral | 1.3 µg/mL | Inhibition of MCF-7 cell proliferation (IC50: 72 h) | |
| Citral | 71.90 µM 57.11 µM 50.20 µM |
Inhibition of KKU-M213 cell proliferation (IC50: 24, 48, and 72 h) | [93] |
| Citral | 94.43 µM 75.06 µM 58.92 µM |
Inhibition of HuCCA-1 cell proliferation (IC50: 24, 48, and 72 h) | [93] |
| Citral | 87.53 72.17 69.22 |
Inhibition of MMNK-1 cell proliferation (IC50: 24, 48, and 72 h) | [93] |
| Citral | 10 µg/mL | Inhibition of PC-3 cell proliferation (IC50: 72 h) | [94] |
| Citral | 12.5 µg/mL | Inhibition of PC-3M cell proliferation (IC50: 72 h) | [94] |
| Citral | >75 µg/mL | Inhibition of MRC-5 cell proliferation (IC50: 72 h) | [94] |
| Citral | 238 µM | Inhibition of PaCa-2 cell proliferation (IC50: 72 h) | [95] |
| Citral | 300 µM | Inhibition of DeFew cell proliferation (IC50: 72 h) | [95] |
| Citral | 5, 10, 20, 40 µg/mL | Inhibit colony formation and migration of AGS (96 h) | [91] |
| Citral | 5, 10, 20, 30, 40 µg/mL | Inhibit colony formation and migration PC-3 (96 h) | [94] |
| Citral | 17.5 and 35 µM | Increase the surviving fraction of KKU-M213 in 106.75 and 115.64% (168 h) | [93] |
| Citral | 23.5 and 47 µM | Decrease the surviving fraction of HU-CCA-1 in 76.35 and 57.71% (168 h) | [93] |
| Citral | 24 and 48 µM | Decrease the surviving fraction of MMNK-1 in 98.46 and 85.26% (168 h) | [93] |
| Citral | 0.25, 0.375, 0.50 mM 0.25, 0.375, 0.50 mM |
Decrease the clonogenicity of HaCaT in 0.3, 4, and 7% (3 h) Decrease the clonogenicity of HaCaT in 22, 28, and 30% (8 h) |
[96] |
| Citral | Decrease the clonogenicity of M624 in 20, 38, and 50% (3 h) | [96] | |
| Citral | 50 µM 100 µM 200 µM |
Early apoptosis (17.1%), late apoptosis (3.1%) in HCT116 (24 h) Early apoptosis (14.2%), late apoptosis (15.1%) in HCT116 (24 h) Early apoptosis (26.2%), late apoptosis (25.8%) in HCT116 (24 h) |
[89] |
| Citral | 50 µM 100 µM 200 µM |
Early apoptosis (22.3%), late apoptosis (16.1%) in HCT116 (48 h) Early apoptosis (26.2%), late apoptosis (24.6%) in HCT116 (48 h) Early apoptosis (32.1%), late apoptosis (37.5%) in HCT116 (48 h) |
[89] |
| Citral | 50 µM 100 µM 200 µM |
Early apoptosis (6.5%), late apoptosis (3.9%) in HT29 (24 h) Early apoptosis (8.5%), late apoptosis (14.2%) in HT29 (24 h) Early apoptosis (8.4%), late apoptosis (24.9%) in HT29 (24 h) |
[89] |
| Citral | 50 µM 100 µM 200 µM |
Early apoptosis (14.5%), late apoptosis (7.1%) in HT29 (48 h) Early apoptosis (22.7%), late apoptosis (17.8%) in HT29 (48 h) Early apoptosis (30.5%), late apoptosis (23.5%) in HT29 (48 h) |
[89] |
| Citral | 10 and 20 µg/mL | Induce early and late apoptosis in AGS | [91] |
| Citral | 1 µM | Apoptosis induction by annexin V-FITC/PI staining in B16F10 (24 h) |
[92] |
| Citral | 0.5, 1, and 2 µM | Apoptosis induction by TUNEL assay in B16F10 (24 h) | [92] |
| Citral | 10 µg/mL 20 µg/mL |
Early apoptosis (44.1%), late apoptosis (52.6%) in PC-3 (48 h) Early apoptosis (62.2%), late apoptosis (38.4%) in PC-3 (48 h) |
[94] |
| Citral | 50, 100, and 200 µM | Disruption of MMP (19.5, 38.8 and 60.9%) in HCT116 (24 h) | [89] |
| Citral | 50, 100, and 200 µM | Disruption of MMP (34.9, 56.4 and 77.3%) in HCT116 (48 h) | [89] |
| Citral | 50, 100, and 200 µM | Disruption of MMP (20.4, 28.2 and 41.9%) in HT29 (24 h) | [89] |
| Citral | 50, 100, and 200 µM | Disruption of MMP (24.5, 43.9 and 59.9%) in HT29 (24 h) | [89] |
| Citral | 50, 100, and 200 µM | Increase intracellular ROS level (1.26, 2.07, and 3.19 folds) in HCT116 (4 h) | [89] |
| Citral | 50, 100, and 200 µM | Increase intracellular ROS level (1.21, 1.39, and 2.25 folds) in HC29 (4 h) | [89] |
| Citral | 50, 100, and 200 µM | Decrease intracellular GSH level in HCT116 (4 h) | [89] |
| Citral | 50, 100, and 200 µM | Decrease intracellular GSH level in HT29 (4 h) | [89] |
| Citral | 1 µM | Autophagic vacuole induction formation in B16F10 (24 h) | [89] |
| Citral | 0.5, 1, and 2 µM | DNA damage in B16F10 (24 h) | [92] |
| Citral | 2.5 µM | Reduction of malondialdehyde level in B16F10 (24 h) | [92] |
| Citral | 10 and 20 µg/mL | Inhibition of lipid droplet accumulation in PC-3 (48 h) | [94] |
| Citral | 50, 100, and 200 µM | Down-expression of Bcl-2 and Bcl-xL proteins in HCT116 (24 h) High expression of Bax, p53, and caspase-3 proteins in HCT116 (24 h) |
[89] |
| Citral | 50, 100, and 200 µM | Down-expression of Bcl-2 and Bcl-xL proteins in HT29 (24 h) High expression of Bax, p53, and caspase-3 proteins in HT29 (24 h) |
[89] |
| Citral | 0.5 and 1 µM | Down-expression of ERK1/2, PI3K, AkT in HCT116 (24 h) High expression of p53 in HCT116 (24 h) |
[92] |
| Citral | 1 µM | Increase cytoplasmatic NF-κB in B16F10 (24 h) | [92] |
| Citral | 1 µM | Decrease nuclear translocation of NF-κB in B16F10 (24 h) | [92] |
| Citral | 0.25, 0.375, 0.5 mM | Caspase-3 activation in M624 (3 h) | [96] |
| Citral | 0.25, 0.375, 0.5 mM | Caspase-3 activation in HaCaT (3 h) | [96] |
| Citral | 20 µg/mL | Down-expression of HMGR, SREPB1, and ACC proteins in PC-3 (48 h) Up-expression of AMPαK in PC-3 (48 h) |
[96] |
| Citral | 5, 10, and 20 µg/mL | Down-expression of BCl-2 in PC-3 (48 h) and high expression of BAX proteins in PC-3 (48 h) |
[96] |
| Citral | Not reported | mRNA upregulate in AGS (48 h): MAPK, Nf-κB, PI3K-Akt, p53, and other signaling pathways. Spliceosoma, apoptosis, and prostate cancer, among others. | [91] |
| Not reported | mRNA downregulate in AGS: NF-κB, PI3K-Akt, p53, PPAR, among other signaling pathways. Cell cycle, fatty acid metabolism, and proteoglycans in cancer, among others. | [91] | |
| Citral | 5, 10, and 20 µg/mL | Down-expression of HMCR, ACC, FASN, and SREPB1 mRNAs in PC-3 (48 h) | [94] |
CIT-SNEDDS: Nano-emulsifying drug delivery system loading with citral. IC50: half-maximal inhibitory concentration.