Pharmacological Effects of Cinobufagin

Hao Zhang; Baiyu Jian; Haixue Kuang

doi:10.12659/MSM.940889

25 September 2023 : Review article

Pharmacological Effects of Cinobufagin

Hao Zhang^1E, Baiyu Jian^2G*, Haixue Kuang^1ADG

DOI: 10.12659/MSM.940889

Med Sci Monit 2023; 29:e940889

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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

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Table 1 Anticancer activities of CBF – in vitro and in vivo studies summary.

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

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