Gossypol, a natural polyphenolic compound, possesses antivirus activity and induces cell death of different types of tumors. However, the efficacy of gossypol on lung carcinoma metastases and epithelial to mesenchymal transition remains unknown. The aim of the present work was to determine the cellular and molecular mechanism of the anti‐cancer and anti‐metastatic efficacies of gossypol on human lung carcinoma cells. Gossypol showed a marked suppression of the viability, motility, and invasion in H1299 and A549 cells. Zymography assay showed that gossypol was sufficient to suppress the activities of urokinase‐type plasminogen activator and matrix metalloproteinase‐2. Gossypol reversed TGF‐β‐induced epithelial to mesenchymal transition. Gossypol reduced vimentin, p‐FAK, p‐Src and p‐paxillin. In vivo studies of gossypol were performed using subcutaneous inoculation and tail vein injection of A549 into immunodeficient BALB/c nude mice and severe combined immunodeficient mice.

中文翻译：

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Gossypol 通过逆转上皮细胞向间充质转化和抑制蛋白酶活性来抑制肺细胞癌的转移


Gossypol 是一种天然多酚化合物，具有抗病毒活性并诱导不同类型肿瘤的细胞死亡。然而，棉酚对肺癌转移和上皮间质转化的疗效仍然未知。本研究的目的是确定棉酚对人肺癌细胞的抗癌和抗转移功效的细胞和分子机制。棉酚对 H1299 和 A549 细胞的活力、运动和侵袭表现出显著抑制。酶谱测定显示棉酚足以抑制尿激酶型纤溶酶原激活剂和基质金属蛋白酶-2 的活性。棉酚逆转 TGF β诱导的上皮间质转化。棉酚降低波形蛋白、p-FAK、p-Src 和 p-桩蛋白。使用皮下接种和尾静脉注射 A549 对免疫缺陷的 BALB/c 裸鼠和严重联合免疫缺陷小鼠进行棉酚的体内研究。