Abstract

Purpose

Melanoma is the most lethal form of skin cancer with the incidence drastically increasing over the past several decades. (S)-(-)-N-[2-(3-Hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)-ethyl]-acetamide (SA) was a new compound isolated from the leaves of Selaginella pulvinata, with potent activities to inhibit the proliferation of SK-mel-110 cells. This study was to further investigate effects of SA against melanoma and explore its underlying mechanisms.

Methods

B16 cells were treated with different concentrations of SA. Tumour model was established by injecting B16 cells into C57 mice subcutaneously. MTT and LDH assays were used to detect effects of SA on cell viability. ELISA assay, Annexin V/PI staining and TUNEL assay were used to detect apoptosis. RT-qPCR and western blot were used to detect the expression of genes and proteins, respectively.

Results

SA significantly inhibited the proliferation of melanoma cells and induced the apoptosis as well as autophagy, which may be associated with PI3K/Akt and MAPK signal pathways. Moreover, SA treatment significantly slowed melanoma tumour growth, evidenced by decreased tumour volume and tumour weight.

Conclusions

Our data suggested that SA could be developed as a potential anti-tumour drug against melanoma.

中文翻译：

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(S)-(-)-N-[2-(3-Hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)-ethyl]-acetamide 通过诱导细胞凋亡和自噬抑制黑色素瘤细胞生长

摘要

目的

黑色素瘤是最致命的皮肤癌形式，其发病率在过去几十年中急剧增加。( S )-(-)-N-[2-(3-Hydroxy-2-oxo-2,3-dihydro-1 H -indol-3-yl)-ethyl]-乙酰胺 (SA) 是一种分离的新化合物来自Selaginella pulvinata的叶子，具有抑制 SK-mel-110 细胞增殖的有效活性。本研究旨在进一步研究 SA 对黑色素瘤的作用并探索其潜在机制。

方法

B16 细胞用不同浓度的 SA 处理。通过将B16细胞皮下注射到C57小鼠体内建立肿瘤模型。MTT和LDH测定用于检测SA对细胞活力的影响。ELISA法、Annexin V/PI染色法和TUNEL法检测细胞凋亡。RT-qPCR和蛋白质印迹分别用于检测基因和蛋白质的表达。

结果

SA显着抑制黑色素瘤细胞的增殖并诱导细胞凋亡和自噬，这可能与PI3K/Akt和MAPK信号通路有关。此外，SA 治疗显着减缓了黑色素瘤肿瘤的生长，这可以通过减少肿瘤体积和肿瘤重量来证明。

结论

我们的数据表明，SA 可以被开发为一种潜在的抗黑色素瘤抗肿瘤药物。