Abstract
This research aimed to discover and identify new poly ADP-ribose polymerase-1 (PARP) inhibitors with potent anti-cervical carcinoma activity, and then explore their potential biological roles on cervical carcinoma cell. For this purpose, we identified a new PARP inhibitor from a high-throughput virtual screening method and found that the compound strongly inhibited cervical carcinoma HeLa cell. Cell proliferation was evaluated by an MTT assay, and the cell apoptosis was assessed by flow cytometry. Results showed that PARP1 is a poly ADP-ribose catalyzing enzyme in eukaryotic cells, which is activated during DNA damage and repair, and plays an important role in DNA repair and cell apoptosis. Herein we report the first discovery of a new PARP inhibitor from a high-throughput virtual screening method, then the compound was measured its anti-cervical carcinoma activity by using an MTT assay, which suggested that the compound strongly inhibited HeLa cell proliferation, the IC50 value is 0.65 µM. In addition, the compound induced HeLa cell apoptosis in a dose-response manner. All these data suggested that the compound is a promising lead compound, which deserves further investigation. It is concluded that the compound discover herein is a promising PARP-1 inhibitor with potent anti-cervical carcinoma activity, which deserves further investigation.
Highlights
Cervical cancer is the second-largest malignancy in women worldwide
Results showed that PARP1 is a poly ADP-ribose catalyzing enzyme in eukaryotic cells, which is activated during DNA damage and repair, and plays an important role in DNA repair and cell apoptosis
We report the first discovery of a new poly ADP-ribose polymerase-1 (PARP) inhibitor from a high-throughput virtual screening method, the compound was measured its anti-cervical carcinoma activity by using an MTT assay, which suggested that the compound strongly inhibited HeLa cell proliferation, the IC50 value is 0.65 μM
Summary
Cervical cancer is the second-largest malignancy in women worldwide. It is a relatively common cancer and in many cases has very dangerous complications for women. This type of cancer occurs in cells in the lower part of the uterus that attach to the vagina. One of the triggers for cervical cancer is exposure to the human papillomavirus, which causes mutations in cervical cells. This mutation causes normal cells to become abnormal cells. With the application of new molecular targeted drugs and immune checkpoint inhibitors, the quality of life of cervical cancer patients has been greatly improved [5]
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