25 September 2023: Review Articles
Pharmacological Effects of Cinobufagin
Hao Zhang 1E , Baiyu Jian 2G* , Haixue Kuang 1ADG*DOI: 10.12659/MSM.940889
Med Sci Monit 2023; 29:e940889
Background
Physicochemical Properties
Pharmacological Activities of CBF
Analgesic Effects of CBF
Cardiotonic Effects of CBF
Immunomodulatory Effects of CBF
Antifibrotic Effects of CBF
Antiviral Effects of CBF
Antiprotozoal Effects of CBF
The Pharmacokinetics of CBF
Future Directions
Conclusions
Reference
Table 1 Anticancer activities of CBF – in vitro and in vivo studies summary.
| Cancer | Cell lines/model | Activity | Mechanism(s) of action | Application | Reference |
|---|---|---|---|---|---|
| HepG2 | LD=170 ng/L(12 h)LD=78 ng/L (24 h)LD=40 ng/L (48 h) | Upregulates the p53 pathway and down-regulates the Akt and ERK pathways | In vitro | []16 | |
| HepG2 | IC=86.025 μM | Downregulation of prosurvival proteins (Bcl-2) and upregulation of the proapoptotic proteins (Fas and Bax) | In vitro | []11 | |
| Nude mice bearing HepG2 cells | 1.14 mg/kg CBF (intraperitoneal route every two day for 20 doses), tumors weight decreased | In vivo | []11 | ||
| Huh-7 | 1 μmol/L viability rate was 74.5±4.5% (12 h), 1 μmol/L viability rate was 53.7±3.8% (24 h), 1 μmol/L viability rate was 27.9±2.3% (36 h) | Triggers defects in spindle formation and cap-dependent translation by inhibiting the AURKA-mTOR-eIF4E Axis | In vitro | []17 | |
| Nude mice bearing Huh-7 cells | 10 mg/kg CBF (intratumorally injected for 21 days), tumors weight decreased | In vivo | []17 | ||
| U2OS | Inhibits the viability | Induces cell cycle arrest at G2/M phases and induces apoptosis via inhibition of the GSK-3β/NF-κB pathway. | In vitro | []18 | |
| MG63 | Inhibits the viability | In vitro | []18 | ||
| SaOS-2 | Inhibits the viability | In vitro | []18 | ||
| U2OS | Inhibits the viability | Downregulates the stem-like properties of osteosarcoma cells, thus inhibiting the process of tumorigenesis by inhibiting the IL-6-OPN-STAT3 pathway | In vitro | []19 | |
| MG63 | Inhibits the viability | In vitro | []19 | ||
| U2OS | IC=120 mg/L (24 h) | Triggers apoptosis and autophagic cell death via activation of the ROS/JNK/p-38 axis | In vitro | []20 | |
| A375 | IC=0.2 μg/mL (24 h) | Induces cell cycle arrest at the G2/M phase and induces apoptosis by inhibiting the PI3K/Akt pathway | In vitro | []21 | |
| B16 | Inhibits the viability | In vitro | []21 | ||
| OCM1 | IC=0.8023 μM (48 h) | CBF arrested the cell cycle in the G1 phase and induces apoptosis via intrinsic apoptosis pathway | In vitro | []22 | |
| Nude mice bearing OCM1 cells | 5 mg/kg CBF (injected once a day for 7 days), after 30 days, the mice were killed, the tumors weight decreased | In vivo | []22 | ||
| HCT116 | IC=0.7821uM (48 h) | Promotes cell apoptosis and inhibits the invasion and metastases via STAT3 signaling pathway | In vitro | []23 | |
| RKO | IC=0.3642uM (48 h) | In vitro | []23 | ||
| SW480 | IC=0.1822uM (48 h) | In vitro | []23 | ||
| Nude mice bearing HCT116 cells | 0.5 or 1.0 mg/kg CBF (intraperitoneal route every other day for 7 doses), the tumors weight decreased | In vivo | []23 | ||
| NB4 | Inhibits the viability | Induces cell apoptosis and PML-RARA degradation by inhibiting the β-catenin signaling pathway | In vitro | []26 | |
| NB4-R1 | Inhibits the viability | In vitro | []26 | ||
| HK-1 | IC=0.061 μg/ml | Induces cell cycle arrest at the S phase and induces apoptosis through the mitochondrial apoptosis pathway | In vitro | []27 | |
| 5–8F | 446.0 nM | Induces ENKUR to repress the β-catenin/c-Jun/MYH9 signal and thus decreased UBE3A-mediated p53 ubiquitination degradation, ultimately, epithelial-mesenchymal transition signal is inactivated to suppress nasopharyngeal carcinoma metastasis | In vitro | []28 | |
| HONE-1 | 627.6 nM | In vitro | []28 | ||
| U266 | Inhibits the viability | Inhibits ROS-mediated MAPKs signaling pathway and this led to the down-regulation of various gene products that mediate tumor cell survival, proliferation, metastasis and angiogenesis | In vitro | []29 | |
| SGC-7901 | 0.24 mM (24 h) | Induces cell apoptosis and inhibition of autophagy enhances CBF-induced apoptosis | In vitro | []30 | |
| MCF-7 | 0.94±0.08 μM (24 h)0.44±0.12 μM (48 h)0.22±0.03 μM (72 h) | Induces cell cycle arrest at the G1 phase and induces apoptosis through the mitochondrial apoptosis pathway | In vitro | []31 |