Antitumor Efficacy of Arylquin 1 through Dose-Dependent Cytotoxicity, Apoptosis Induction, and Synergy with Radiotherapy in Glioblastoma Models

Author:

Lieu Ann-Shung12,Pan Yu-Chi3,Lee Jia-Hau4,Hsieh Yuan-Chin5,Lin Chien-Ju6,Hsu Ya-Ling37,Chang Kung-Chao8ORCID,Kuo Shih-Hsun9,Tseng Tzu-Ting1,Tsai Hung-Pei1ORCID

Affiliation:

1. Division of Neurosurgery, Department of Surgery, Kaohsiung Medical University Hospital, Kaohsiung 80708, Taiwan

2. Department of Surgery, School of Medicine, College of Medicine, Kaohsiung Medical University, Kaohsiung 80756, Taiwan

3. Graduate Institute of Medicine, College of Medicine, Kaohsiung Medical University, Kaohsiung 80756, Taiwan

4. National Institute of Cancer Research, National Health Research Institutes, Tainan 70456, Taiwan

5. School of Medicine for International Students, I-Shou University, Kaoshiung 82445, Taiwan

6. School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 80756, Taiwan

7. Drug Development and Value Creation Research Center, Kaohsiung Medical University, Kaohsiung 80756, Taiwan

8. Department of Pathology, National Cheng Kung University Hospital, College of Medicine, National Cheng Kung University, Tainan 70101, Taiwan

9. Department of Radiation Oncology, Kaohsiung Medical University Hospital, Kaohsiung 80708, Taiwan

Abstract

Glioblastoma (GBM), the most aggressive form of brain cancer, is characterized by rapid growth and resistance to conventional therapies. Current treatments offer limited effectiveness, leading to poor survival rates and the need for novel therapeutic strategies. Arylquin 1 has emerged as a potential therapeutic candidate because of its unique mechanism of inducing apoptosis in cancer cells without affecting normal cells. This study investigated the efficacy of Arylquin 1 against GBM using the GBM8401 and A172 cells by assessing its dose-dependent cytotoxicity, apoptosis induction, and synergy with radiotherapy. In vitro assays demonstrated a significant reduction in cell viability and increased apoptosis, particularly at high concentrations of Arylquin 1. Migration and invasion analyses revealed notable inhibition of cellular motility. In vivo experiments on NU/NU nude mice with intracranially implanted GBM cells revealed that Arylquin 1 substantially reduced tumor growth, an effect magnified by concurrent radiotherapy. These findings indicate that by promoting apoptosis and enhancing radiosensitivity, Arylquin 1 is a potent therapeutic option for GBM treatment.

Funder

Kaohsiung Medical University Chung-Ho Memorial Hospital

Publisher

MDPI AG

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