Department of Pharmacology, Sri Ramachandra University, Chennai 600118, India.
Department of Biomedical Sciences, Sri Ramachandra University, Chennai 600118, India.
Cancer Biol Med. 2013 Sep;10(3):142-7. doi: 10.7497/j.issn.2095-3941.2013.03.004.
Flupirtine is a non-opioid analgesic without antipyretic or antiphlogistic properties but with favorable tolerability in humans. This analgesic also exhibits neuroprotective activities. Furthermore, flupirtine antagonizes glutamate- and NMDA-induced intracellular levels of Ca(2+) and counteracts the effects of focal cerebral ischemia. Although flupirtine has been used to relieve pain caused by different diseases and clinical procedures, information on the safety and efficacy of flupirtine is limited. The present study was conducted to investigate the neuroprotective effects of flupirtine on U373 malignant glioma (MG) cell lines.
Cell viability and cell cycle analysis was performed by MTT assay and flow cytometry, respectively.
Variations in the growth of U373 MG cells in 5 mM N-methyl-D-aspartate (NMDA), 1 mM flupirtine, and combined treatment indicated the antagonistic effects of NMDA and flupirtine on MG cell lines. The variation in the percentage of gated cell population in different cell cycle phases showed significant variations after 48 h of treatment.
Flupirtine has neuroprotective effect of on U373 MG cells, which limits its use in the pain management of brain tumors. This property warrants further studies using animal models and large-scale clinical trials.
氟吡汀是一种非阿片类镇痛药，没有解热或抗炎作用，但在人类中具有良好的耐受性。这种镇痛药还具有神经保护活性。此外，氟吡汀拮抗谷氨酸和 NMDA 诱导的细胞内 Ca(2+)水平，并抵消局灶性脑缺血的影响。尽管氟吡汀已被用于缓解不同疾病和临床操作引起的疼痛，但关于氟吡汀的安全性和疗效的信息有限。本研究旨在探讨氟吡汀对 U373 恶性神经胶质瘤（MG）细胞系的神经保护作用。
通过 MTT 法和流式细胞术分别进行细胞活力和细胞周期分析。
在 5 mM N-甲基-D-天冬氨酸（NMDA）、1 mM 氟吡汀和联合治疗中 U373 MG 细胞生长的变化表明 NMDA 和氟吡汀对 MG 细胞系具有拮抗作用。不同细胞周期阶段的门控细胞群体百分比的变化在 48 小时治疗后显示出显著变化。
氟吡汀对 U373 MG 细胞具有神经保护作用，这限制了其在脑肿瘤疼痛管理中的应用。该特性需要使用动物模型和大规模临床试验进一步研究。
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