3-(4-氯苯基)-5-(4-甲氧基苄基)- 4h -1,2,4-三唑衍生物对人黑色素瘤细胞的细胞毒作用

IF 0.3 Q4 BIOLOGY
E. Demir, A. Colak, Selcen Çelik Uzuner, O. Bekircan
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引用次数: 1

摘要

黑色素瘤是癌症中致死率最高的一种。尽管化疗已被广泛用于治疗黑色素瘤,但常规化疗药物的耐药性和副作用会对治疗的连续性和成功率产生负面影响。1,2.4三唑衍生物是近年来流行的化合物,具有抗微生物、抗炎、镇痛、抗病毒、抗增殖和与新冠肺炎相关的抗真菌活性。然而,揭示1,2.4三唑化合物对黑色素瘤细胞影响的研究是有限的。本研究的目的是用MTT法和流式细胞仪分别研究3-(4-氯苯)-5-(4-甲氧基苯)-4H-1,4-三唑衍生物(B9)化合物对细胞毒性和细胞周期的影响,并用黑色素含量比色法研究其对人黑色素瘤(VMM917)细胞酪氨酸酶的抑制作用。与正常细胞相比,化合物B9对VMM917细胞表现出选择性细胞毒性作用(4.9倍)。B9诱导细胞周期停滞在S期,也降低了细胞中黑色素的含量。研究结果提示了一种新的治疗黑色素瘤的候选药物。对这种选择性细胞毒性作用的分子机制的详细研究将有助于了解B9作为黑色素瘤替代化疗剂的可用性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Cytotoxic effect of a 3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazole derivative compound in human melanoma cells
Melanoma represents the most forceful derm cancer with a high rate of mortality. Although chemotherapy has been commonly used in the treatment of melanoma, drug resistance and side effects of conventional chemotheurapeutics negatively affect the continuity and success the treatment. 1,2.4 triazole derivatives are popular compounds of recent years with anti-microbial, anti-inflammatory, analgesic, antiviral, anti-proliferative and COVID-19 associated anti-fungal activities. However, studies that revealed the effects of 1,2.4 triazole compounds on melanoma cells are limited. The aim of this study was to investigate the effects of a 3-(4-chloropheny1)-5-(4-methoxybenzy1)-4H-1,2.4-triazole derivative (B9) compound on cytotoxicity and cell cycle using MTT and flow cytometrv, respectively and the inhibitory' effect on tyrosinase in human melanoma (VMM917) cells using colorimetric assay for melanin content. The compound B9 exhibited a selective cytotoxic effect (4.9-fold) on VMM917 cells compared to normal cells. B9 induced cell cycle arrest at the S phase and also decreased the amount of melanin in the cells. The results suggest a novel candidate drug in melanoma therapy. The detailed investigation of the molecular mechanism of this selective cytotoxic effect will provide understanding on the usability of B9 as an alternative chemotherapeutic agent in melanoma.
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