体外研究
(In Vitro) | APE1-IN-2 (compound AP1) can strongly inhibit the growth of malignant cells, including Cisplatin-resistant cancer cells, with up to 18.11 times inhibition compared withCisplatin(HY-17394)[1].
APE1-IN-2 (500 nM, 24 h) arrests the cell cycle in A549 and MCF7 cells[1].
APE1-IN-2 (10 μM, 24 h) induces p53-dependent apoptosis in A549 cells[1].
APE1-IN-2 (0-250 μM, 72 h) inhibits AP-cutting activity with an IC50of 45.14 ± 17.37 μM[1].
APE1-IN-2 can directly inhibit the AP endonuclease activity of APE1, leading to an interruption of miRNA processing and upregulation of the tumor suppressor PTEN[1].
Cell Proliferation Assay[1] | Cell Line: | A549 (non-small cell lung cancer), MCF7 (breast cancer), U251 (glioblastoma), A375 (melanoma), PC3 (prostate cancer), and HEP-G2 (hepatocarcinoma) cell lines | | Concentration: | | | Incubation Time: | 72 h | | Result: | Demonstrated more potent antiproliferation effects thanCisplatin(HY-17394), with IC50of 0.45 ± 0.03, 0.43 ± 0.03, 4.70 ± 0.14, 0.39 ± 0.03, 5.65 ± 0.21, and 3.53 ± 0.31 μM in A549, MCF7, U251, A375, PC3, and HEP-G2 cell lines, respectively. |
Cell Cycle Analysis[1] | Cell Line: | A549 and MCF7 cells | | Concentration: | 500 nM | | Incubation Time: | 24 h | | Result: | Induced the most severe S-phase arrest in A549 and MCF7 cells. |
Cell Proliferation Assay[1] | Cell Line: | A549 cells | | Concentration: | 10 μM | | Incubation Time: | 24 h | | Result: | Caused apoptosis in approximately 38.7% (22.9% early apoptosis and 15.8% late apoptosis) of cancer cells. |
Western Blot Analysis[1] | Cell Line: | A549 and HEK-293T cell lines | | Concentration: | 0, 16, 40, 100, 250 μM | | Incubation Time: | 72 h | | Result: | Significantly increased the level of p53 by 2.09 ± 0.51-fold. Slightly raised the levels
of p53, γH2A.X, and cl.PARP in HEK-293T. Inhibited AP-cutting activity with an IC50value of 45.14 ± 17.37 μM. |
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体内研究
(In Vivo) | APE1-IN-2 (compound AP1) (2 mg/kg, IP, once every 3 days for 15 days) exhibits an antitumor effect on the A549 xenograft model[1].
| Animal Model: | BALB/c nude mice (5 week-old, female, 16 ± 2 g of body weight bearing A549 xenograft tumors)[1] | | Dosage: | 2 mg/kg | | Administration: | IP, once every 3 days for 15 days | | Result: | Exhibited a 3.86-fold xenograft tumor inhibitory activity compared to Cisplatin. Did not significantly alter the body weight of mice, improving its sufficient safety. |
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