Table 3.
Antitumor activities and mechanism of usnic acid.
| Cell Lines | Mechanism | IC50 | Year | Reference |
|---|---|---|---|---|
| Human gastric carcinoma cell lines BGC823 | Suppress the proliferation of human gastric carcinoma cells by inducing cycle phase arrest, cell apoptosis, and autophagy. | 236.55 µM | 2018 | [81] |
| Human gastric carcinoma cell lines SGC7901 | 618.82 µM | 2018 | [81] | |
| Human lung carcinoma A549 cells | Inhibit cell growth involving G0/G1 phase cell-cycle arrest and induce cell death via mitochondrial membrane depolarization and induction of apoptosis in human lung carcinoma cells. | NA | 2013 | [20] |
| Human breast cancer cell line MCF7 | Selective cytotoxic effects on HDBC and HDPC cells without damaging normal cells and inducing apoptotic cell death and G0/G1 cell-cycle arrest. | 71.4 µM | 2018 | [82] |
| Human prostate cancer cell line LNCaP | 77.5 µM | 2018 | [82] | |
| Human colon carcinoma wild-type p53 HCT-116 p53+/+ cells | Effective anti-cancer against a wide range of various cell lines originating from different tissues. It can accumulate cells in S-phase at the expense of the G1/G0-phase. Promote apoptosis. | 157.2 µM | 2011 | [83] |
| Human colon carcinoma wild-type p53 HCT-116 p53−/− cells | 143.1 µM | 2011 | [83] | |
| Human leukemia cell line U937 | The proliferation can be inhibited in a dose-dependent and time-dependent feature. The apoptosis of U937 cell induced by usnic acid is related to Caspase-dependent mitochondrial pathway. | 90.90 μmol/L (24 h), 54.08 μmol/L (48 h) |
2020 | [84] |
| Human osteosarcoma cell line MG-63 | 103.00 μmol/L (24 h), 90.48 μmol/L (48 h) |
2020 | [84] | |
| Human melanoma cell line A375 | 139.48 μmol/L (24 h), 65.39 μmol/L (48 h) |
2020 | [84] | |
| Human prostate cancer cells PC-3M | Inhibition of DNA replication and RNA transcription of tumor cells, interfering with DNA synthesis, which eventually lead to the slowdown of proliferation rate of prostate cancer cells or accelerating the apoptosis of tumor cells. | NA | 2005 | [85] |
| Human lung carcinoma A549 cells | Inhibit PD-L1 protein synthesis by reducing STAT3 and RAS pathways cooperatively, induce MiT/TFE nuclear translocation through the suppression of mTOR signaling pathways, and promote the biogenesis of lysosomes and the translocation of PD-L1 to the lysosomes for proteolysis; Inhibit cell proliferation, angiogenesis, migration, and invasion, respectively, by downregulating PD-L1, thereby inhibiting tumor growth. | NA | 2021 | [86] |
| Human cervical cancer HeLa cells | NA | 2021 | [86] | |
| Human cervical cancer SiHa cells | NA | 2021 | [86] | |
| Human cervical cancer CaSKi cells | NA | 2021 | [86] | |
| Mouse hepatocellular carcinoma cell line H22 | Inhibitory effect on usnic acid on VEGF and bFGF. | NA | 2016 | [87] |
| Human umbilical vascular endothelial cells | Suppress Bcap-37 breast tumor growth and angiogenesis without affecting mice body weight in mouse xenograft tumor model; Inhibit endothelial cell proliferation, migration and tube formation. Induce morphological changes and apoptosis in endothelial cells in vitro; Block vascular endothelial growth factor receptor (VEGFR) 2 mediated extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) and AKT/P70S6K signaling pathways in endothelial cells. | NA | 2012 | [88] |
| Human breast tumor cell line Bcap-37 | NA | 2012 | [88] | |
| Lewis lung carcinoma cells | / | NA | 1975 | [89] |
| S180 Bearing Mice | / | Inhibition rate: 75.1% (50 mg/kg) 66.6% (80 mg/kg) 69.1% (120 mg/kg) |
1996 | [90] |
| Human colorectal cancer HT-29 cells | / | 55 µM | 2013 | [91] |
| Murine lymphocytic leukaemia L1210 (ATCC CCL 219) | The cytotoxic activity of usnic acid against cancer cell lines can be improved by its conjugation to a polyamine chain. The amine conjugation may not alter fundamentally the mode of action of usnic acid since both the parent compound and its derivative appeared to be apoptosis-inducing agents. | 26.4 µM | 2008 | [92] * |
| Murine lymphocytic leukaemia L1210 (ATCC CCL 219) | Usnic acid was the only compound to display a moderate cytotoxic activity on various cancer cell lines. It was shown to induce apoptosis of murine leukaemia L1210 cells in a dose-and time-dependent manner. | 6 μg/mL | 2004 | [93] |
| Lewis lung carcinoma | / | NA | 1979 | [94] |
| Murine leukemia P388 cells | NA | 1979 | [94] |
*: Usnic-acid–amine conjugates; NA: Not Available.