Antitumor effects of the novel quinazolinone holu-12: Induction of mitotic arrest and apoptosis in human oral squamous cell carcinoma CAL27 cells

KUO CHU LAI, YI TING CHIA, LING HUEI YIH, YI LIANG LU, SHIH TING CHANG, ZI XUAN HONG, TAI LIN CHEN*, MANN JEN HOUR*

*此作品的通信作者

研究成果: 期刊稿件文章同行評審

4 引文 斯高帕斯(Scopus)

摘要

Background/Aim: Quinazolinone is a privileged chemical structure employed for targeting various types of cancer. This study aimed to demonstrate the antitumor activity of synthesized 6,7-disubstituted-2-(3-fluorophenyl) quinazolines (HoLu-11 to HoLu-14). Materials and Methods: The cytotoxicity was assessed by the sulforhodamine B (SRB) assay. The cell cycle was examined by flow cytometry. The expression levels of cell cycle- and apoptosis-related proteins were estimated by western blotting. A xenograft animal model was used to explore the antitumor effects of HoLu-12. Results: Among four synthetic quinazolinone derivatives, HoLu-12 significantly reduced the viability of oral squamous cell carcinoma (OSCC) cells. HoLu-12 induced G2/M arrest and increased the expression of cyclin B, histone H3 (Ser10) phosphorylation, and cleaved PARP, indicating that HoLu- 12 could induce mitotic arrest and then apoptosis. Moreover, the combination of HoLu-12 and 5-fluorouracil (5-FU) displayed synergistic toxic effect on OSCC cells. HoLu-12 significantly inhibited tumor growth in vivo. Conclusion: HoLu-12 induces mitotic arrest and leads to apoptosis of OSCC cells. Furthermore, HoLu-12 alone or in combination with 5-FU is a potential therapeutic agent for OSCC.

原文英語
頁(從 - 到)259-268
頁數10
期刊Anticancer Research
41
發行號1
DOIs
出版狀態已出版 - 01 2021

文獻附註

Publisher Copyright:
© 2021 International Institute of Anticancer Research. All rights reserved.

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