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一种新型化合物 Trichomicin 通过抑制 STAT3 信号通路发挥抗肿瘤活性。

A new compound Trichomicin exerts antitumor activity through STAT3 signaling inhibition.

机构信息

NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 100050, China; Chinese Pharmaceutical Association, Beijing, 100050, China.

NHC Key Laboratory of Biotechnology of Antibiotics, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 100050, China.

出版信息

Biomed Pharmacother. 2020 Jan;121:109608. doi: 10.1016/j.biopha.2019.109608. Epub 2019 Nov 7.

Abstract

Trichomicin, a novel small-molecule compound isolated from the fungus Trichoderma harzianum and identified as new structure compound, exhibited antitumor activities in various human cancer cell lines and reversed drug resistance activity in the multidrug-resistant cancer cell line KBV. The underlying cellular and molecular mechanism was illuminated. Trichomicin can significantly induce cancer cell apoptosis and reduced IL-6 expression and phosphorylation of STAT3 were found in response to Trichomicin treatment. The blockade of IL-6 mediated JAK-STAT3 signaling pathway by Trichomicin was confirmed using reporter gene system. As a promising antitumor-activity compound, Trichomicin is presented in this study.

摘要

曲古抑菌素,一种从哈茨木霉中分离得到的新型小分子化合物,被鉴定为新结构化合物,在多种人癌细胞系中表现出抗肿瘤活性,并逆转多药耐药癌细胞系 KBV 的耐药活性。阐明了潜在的细胞和分子机制。曲古抑菌素能显著诱导癌细胞凋亡,且在曲古抑菌素处理后发现 IL-6 表达降低,STAT3 磷酸化。利用报告基因系统证实了曲古抑菌素通过阻断 IL-6 介导的 JAK-STAT3 信号通路。曲古抑菌素作为一种有前途的抗肿瘤活性化合物,在本研究中被提出。

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