Etoposide (VP-16; VP-16-213) is an anticancer chemotherapeutic agent. It functions by inhibiting topoisomerase II, thereby halting DNA replication. Etoposide induces cell cycle arrest, apoptosis, and autophagy [1].
体内研究
Etoposide (50 μM) and Anti-Human VEGF-treated hypoxic cells, when injected intravenously into immunodeficient mice, demonstrate decreased ability to form lung colonies, which also occur after a prolonged latency period [2].
Etoposide (10 mg/kg/day, i.v.) in combination with NSC 109724 and NSC 241240, decreases tumor volume in NMRI nude mice injected with hepatoblastoma cells [3].
体外研究
Etoposide induces cytotoxicity in pancreatic β-cells by activating apoptosis through the JNK/ERK-mediated GSK-3 downstream signaling pathway in RIN-m5F cells [1].
Etoposide and Anti-Human VEGF effectively eliminate the P1 sphere-forming capacity, which is linked to apoptosis in this cell subset [2].
Etoposide phosphate (0-1μM; 72 hours) inhibits HCT116 cells with different genotypes (FBXW+/+, FBXW-/-, and p53-/-) in a dose-dependent manner, demonstrating IC50 values of 0.945 μM, 0.375 μM, and 1.437 μM, respectively [5].
Etoposide (25 μM; 6 hours) delays p53 recovery in FBXW7-deficient cells. Moreover, FBXW7 expression is absent in FBXW7-/- cells [5].
Etoposide/依托泊苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
H1299 cells
50 µM
24 hours
To evaluate the effect of Pin1 on p53NLS-induced transcription-independent apoptosis, results showed that Pin1 co-expression significantly increased apoptosis induced by p53NLS.
Cell Death Differ. 2013 Feb;20(2):198-208.
HeLa cells
50 µM
2 h
Induced TOP2-DNA crosslinks and monitored SPRTN autocleavage
Nat Commun. 2023 Jan 21;14(1):352.
MCF7/VP cells
5 μM
18 h
To evaluate the sensitivity of MCF7/VP cells to etoposide, results showed that CBLC4H10, CBLC4E10, and CBLC4E11 increased the sensitivity of cells to etoposide by 11.6-fold, 6.8-fold, and 7.7-fold, respectively
Cancer Res. 2009 Aug 15;69(16):6573-80.
U2OS cells
68 μM
24 h
To investigate the effect of RSF1 deficiency on etoposide-induced cell death, results showed that RSF1 deficiency significantly reduced cell death.
Cell Death Dis. 2018 Oct 22;9(11):1079.
H1048 and H69 cells
1 µM
To investigate the anticancer efficacy of Etoposide in combination with Silibinin and Cisplatin on small cell lung cancer (SCLC) cells
Signal Transduct Target Ther. 2022 Oct 5;7(1):346.
HeLa cells
100 µM
Etoposide was used to induce cell death, and the results showed that it could cause apoptosis.
J Exp Med. 2003 May 19;197(10):1323-34.
TC-32 cells
7.2 nM
2–8 h
To investigate the effect of Etoposide on MRP-1 expression in TC-32 cells, results showed that Etoposide increased MRP-1 expression in the plasma membrane and mitochondria.
Br J Cancer. 2012 Mar 13;106(6):1224-33.
TC-32MRP-1.Fb-neo cells
7–240 nM
48 h
To investigate the effect of Etoposide on the viability of TC-32MRP-1.Fb-neo cells, results showed that Etoposide significantly increased drug resistance in these cells.
Br J Cancer. 2012 Mar 13;106(6):1224-33.
Etoposide/依托泊苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
TKO mouse model
Intraperitoneal injection
15 mg/kg
On days 2 and 4
To evaluate the therapeutic effect of etoposide on tumors in TKO mice, results showed that etoposide increased tumor cell apoptosis and the proportion of Hes1-positive cells
Nature. 2017 May 18;545(7654):360-364
Mice
Neuroblastoma model
Intraperitoneal injection
6 mg/kg
Once daily for 5 consecutive days
To evaluate the efficacy of etoposide in the neuroblastoma model, results showed that the combination of Reversan with etoposide significantly prolonged the survival time of mice compared to etoposide alone
Cancer Res. 2009 Aug 15;69(16):6573-80.
Mice
4T1 breast cancer model
Intraperitoneal injection
5 mg/kg
Administered on day 7 and 12
To evaluate the effect of Etoposide on MDSC, results showed that Etoposide had limited effects on MDSC depletion
Cancer Res. 2014 Jan 1;74(1):104-18
Mice
Rsf1 conditional knockout mice
Intraperitoneal injection
4 mg/kg
Single dose, embryos treated at E15.0
To investigate the effect of Rsf1 deficiency on etoposide-induced DNA damage and apoptosis, results showed that Rsf1 deficiency significantly reduced apoptosis.
Cell Death Dis. 2018 Oct 22;9(11):1079.
BALB/c nude mice
Human small cell lung cancer (SCLC) xenograft model
Intraperitoneal injection
12 mg/kg
Once daily for 3 days
To investigate the anticancer efficacy of Etoposide in combination with Silibinin and Cisplatin on small cell lung cancer (SCLC) xenograft models
Signal Transduct Target Ther. 2022 Oct 5;7(1):346.
Nude mice
SCLC subcutaneous tumor model
Intraperitoneal injection
4 mg/kg
Once every 2 days
To evaluate the antitumor effect of Etoposide on the SCLC subcutaneous tumor model, the results showed that Etoposide significantly inhibited tumor growth
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