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毛药黄檀酮C,一种天然的呫吨酮,通过调节信号转导和转录激活因子3(STAT3)及黏着斑激酶(FAK)信号通路来抑制肺癌的增殖和转移。

Cratoxylumxanthone C, a natural xanthone, inhibits lung cancer proliferation and metastasis by regulating STAT3 and FAK signal pathways.

作者信息

Li Yeling, Wang Huimei, Liu Wenhui, Hou Jiantong, Xu Jing, Guo Yuanqiang, Hu Ping

机构信息

State Key Laboratory of Medicinal Chemistry Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, China.

Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education, Hainan Normal University, Haikou, China.

出版信息

Front Pharmacol. 2022 Aug 9;13:920422. doi: 10.3389/fphar.2022.920422. eCollection 2022.

Abstract

To discover phytochemicals as lead compounds for cancer treatment, cratoxylumxanthone C, a natural xanthone, was obtained from (Lour.) Bl., for which there have been no reports on the biological effects against cancer Our study revealed that cratoxylumxanthone C had significant anti-tumor activity by inducing apoptosis, augmenting cellular reactive oxygen species (ROS), and arresting cell circle. The mechanistic examination showed the inhibition of A549 cell proliferation and metastasis by cratoxylumxanthone C was coupled with the signal transducer and activator of transcription 3 (STAT3) and focal adhesion kinase (FAK) signaling pathways. Furthermore, the zebrafish models confirmed its significant anti-tumor activity, in which cratoxylumxanthone C inhibited tumor proliferation and metastasis and suppressed the angiogenesis. Comprehensively, these cellular and zebrafish experiments implied that cratoxylumxanthone C may have the potential to become an anti-tumor agent for lung cancer, especially non-small cell lung cancer (NSCLC).

摘要

为了发现可作为癌症治疗先导化合物的植物化学物质,从黄牛木(Cratoxylum cochinchinense (Lour.) Bl.)中获得了一种天然呫吨酮——黄牛木呫吨酮C,此前尚无关于其抗癌生物学效应的报道。我们的研究表明,黄牛木呫吨酮C通过诱导细胞凋亡、增加细胞活性氧(ROS)和阻滞细胞周期具有显著的抗肿瘤活性。机制研究表明,黄牛木呫吨酮C对A549细胞增殖和转移的抑制作用与信号转导和转录激活因子3(STAT3)及粘着斑激酶(FAK)信号通路有关。此外,斑马鱼模型证实了其显著的抗肿瘤活性,其中黄牛木呫吨酮C抑制肿瘤增殖和转移并抑制血管生成。综合来看,这些细胞和斑马鱼实验表明,黄牛木呫吨酮C可能有潜力成为一种治疗肺癌尤其是非小细胞肺癌(NSCLC)的抗肿瘤药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2e23/9396379/946d992484f4/fphar-13-920422-g001.jpg

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