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安维鲁单抗是一种新型 JAK1 抑制剂,可抑制非小细胞肺癌生长。

Anwulignan is a novel JAK1 inhibitor that suppresses non-small cell lung cancer growth.

机构信息

Department of Pathophysiology, School of Basic Medical Sciences, Academy of Medical Science, College of Medicine, Zhengzhou University, Zhengzhou, HA, China.

China-US (Henan) Hormel Cancer Institute, Zhengzhou, HA, China.

出版信息

J Cell Mol Med. 2021 Mar;25(5):2645-2654. doi: 10.1111/jcmm.16289. Epub 2021 Feb 1.

Abstract

Anwulignan is a monomer compound derived from Schisandra sphenanthera lignans. It has been reported to possess a spectrum of pharmacological activities, including anti-bacterial, anti-inflammatory, anticancer and hepatoprotective properties. However, its anticancer capacity and molecular mechanism(s) against non-small cell lung cancer (NSCLC) have not been fully elucidated. Anwulignan significantly inhibited cell growth and increased G1-phase cell cycle arrest in NSCLC cells. Anwulignan strongly attenuates the JAK1/STAT3 signalling pathway by directly targeting JAK1 protein kinase activity in vitro. The anticancer activity by Anwulignan is dependent upon the JAK1 protein expression. Remarkably, Anwulignan strongly inhibited tumour growth in vivo. In conclusion, Anwulignan is a novel JAK1 inhibitor that may have therapeutic implications for NSCLC management.

摘要

安五灵脂素是一种从五味子木脂素衍生而来的单体化合物。据报道,它具有多种药理活性,包括抗菌、抗炎、抗癌和保肝作用。然而,其抗癌能力及其针对非小细胞肺癌(NSCLC)的分子机制尚不完全清楚。安五灵脂素显著抑制 NSCLC 细胞的生长并增加 G1 期细胞周期阻滞。安五灵脂素通过体外直接靶向 JAK1 蛋白激酶活性,强烈抑制 JAK1/STAT3 信号通路。安五灵脂素的抗癌活性依赖于 JAK1 蛋白的表达。值得注意的是,安五灵脂素强烈抑制体内肿瘤生长。总之,安五灵脂素是一种新型的 JAK1 抑制剂,可能对 NSCLC 的治疗具有重要意义。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c81/7933975/91fbc55fb99f/JCMM-25-2645-g001.jpg

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