Escin 通过凋亡机制诱导人类皮肤黑色素瘤细胞死亡。

IF 2.2 4区 医学 Q3 TOXICOLOGY Toxicology Research Pub Date : 2024-08-05 eCollection Date: 2024-08-01 DOI:10.1093/toxres/tfae124
Canan Vejselova Sezer
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引用次数: 0

摘要

天然产品具有显著的抗癌功效,已被用于癌症治疗。从七叶树(Aesculus hippocastanum L.)中提取的一种三萜类皂苷天然混合物的主要活性成分逸辛已被用于各种疾病的研究。在此,我们研究了 escin 对人类皮肤黑色素瘤(CHL-1)细胞的潜在抗增殖、促凋亡和细胞毒性活性。细胞毒性采用 MTT 法测定。共聚焦显微镜检测了细胞的形态变化,透射电子显微镜研究了细胞的超微结构变化。磷脂酰丝氨酸转位检测、Bcl-2 激活评估和氧化应激分析用于确定细胞的死亡模式。结果表明,在暴露 24 小时内,埃辛以剂量依赖的方式降低了细胞活力,在较低浓度下具有很强的细胞毒性(IC50 值为 6 μg/mL)。埃辛能使 Bcl-2 信号失活,并通过增加活性氧以及引起形态学和超微结构的变化引发细胞凋亡,这些变化都与促凋亡活性有关。经过进一步的体外和体内研究发现,Escin 具有很高的抗癌潜力。
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Escin induces cell death in human skin melanoma cells through apoptotic mechanisms.

Natural products based on their significant anti-cancer potencies have been used in cancer treatment. A natural blend of triterpenoid saponins derived from the horse chestnut (Aesculus hippocastanum L.), has been investigated in various diseases based on its main active ingredient escin. Herein, we examined the potential antiproliferative, proapoptotic, and cytotoxic activities of escin on human skin melanoma (CHL-1) cells. Cytotoxicity of escin was determined by MTT assay. Morphological changes were detected by confocal microscopy and ultrastructural changes by transmission electron microscopy studies. Phosphatidylserine translocation assay, Bcl-2 activation assessment, and oxidative stress analysis were used to determine the cell death mode of the cells. The results showed that escin reduced cell viability in a dose-dependent manner within 24 h of exposure and was highly cytotoxic at lower concentrations (IC50 value 6 μg/mL). Escin inactivated Bcl-2 signaling and triggered apoptosis by increasing the reactive oxygen species and by causing morphological and ultrastructural changes that implicate to the proapoptotic activity. Escin has been found to exert high potential for an anti-cancer drug following further in vitro and in vivo investigations.

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来源期刊
Toxicology Research
Toxicology Research TOXICOLOGY-
CiteScore
3.60
自引率
0.00%
发文量
82
期刊介绍: A multi-disciplinary journal covering the best research in both fundamental and applied aspects of toxicology
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