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美洛昔康潜在抗癌活性的评估——无色素性和色素性黑色素瘤的体外研究

The Evaluation of Potential Anticancer Activity of Meloxicam-In Vitro Study on Amelanotic and Melanotic Melanoma.

作者信息

Karkoszka-Stanowska Marta, Rzepka Zuzanna, Wrześniok Dorota

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical, University of Silesia in Katowice, Jagiellońska 4, 41-200 Sosnowiec, Poland.

出版信息

Int J Mol Sci. 2025 Jun 22;26(13):5985. doi: 10.3390/ijms26135985.

DOI:10.3390/ijms26135985
PMID:40649764
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12250357/
Abstract

Meloxicam (MLX), a member of the non-steroidal anti-inflammatory drugs (NSAIDs), is a preferential inhibitor of cyclooxygenase-2 (COX-2) responsible for the synthesis of pro-inflammatory prostaglandins. MLX, due to its inhibition of the COX-2 enzyme, which is overexpressed in many cancers, including melanoma, leading to rapid growth, angiogenesis, and metastasis, represents a potentially important compound with anticancer activity. This study aimed to investigate the potential anticancer activity of meloxicam against amelanotic C32 and melanotic COLO 829 melanoma cell lines. The objective was achieved by assessing cell metabolic activity using the WST-1 assay and analyzing mitochondrial potential, levels of reduced thiols, annexin, and caspases 3/7, 8, and 9 by imaging cytometry, as well as assessing reactive oxygen species (ROS) levels using the HDCFDA probe. The amelanotic melanoma C32 was more sensitive to MLX exposure, thus exhibiting antiproliferative effects, a disruption of redox homeostasis, a reduction in mitochondrial potential, and an induction of apoptosis. The results provide robust molecular evidence supporting the pharmacological effects of MLX, highlighting its potential as a valuable agent for in vivo melanoma treatment.

摘要

美洛昔康(MLX)是一种非甾体抗炎药(NSAIDs),是环氧化酶-2(COX-2)的选择性抑制剂,COX-2负责促炎前列腺素的合成。由于MLX抑制了COX-2酶,该酶在包括黑色素瘤在内的许多癌症中过度表达,导致肿瘤快速生长、血管生成和转移,因此它是一种具有潜在重要抗癌活性的化合物。本研究旨在探讨美洛昔康对无黑色素的C32和有黑色素的COLO 829黑色素瘤细胞系的潜在抗癌活性。通过使用WST-1法评估细胞代谢活性,利用成像细胞术分析线粒体电位、还原型硫醇水平、膜联蛋白以及半胱天冬酶3/7、8和9,并使用HDCFDA探针评估活性氧(ROS)水平来实现这一目标。无黑色素的黑色素瘤C32对MLX暴露更为敏感,从而表现出抗增殖作用、氧化还原稳态破坏、线粒体电位降低以及细胞凋亡诱导。这些结果提供了有力的分子证据支持MLX的药理作用,突出了其作为体内黑色素瘤治疗有价值药物的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bbb0/12250357/eb51a1441ee5/ijms-26-05985-g008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bbb0/12250357/eb51a1441ee5/ijms-26-05985-g008.jpg
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