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guaiazulene
Frontiers in Pharmacology · 2021 · IF 5.811

Guaiazulene Triggers ROS-Induced Apoptosis and Protective Autophagy in Non-small Cell Lung Cancer

Ye Qin,Zhou Li,Jin Ping,Li Lei,Zheng Shuwen,Huang Zhao,Liu Jiayang,Qin Siyuan,Liu Hao,Zou Bingwen,Xie Ke

Non-small cell lung cancer (NSCLC) is one of the most frequent cancers worldwide, yet effective treatment remains a clinical challenge. Guaiazulene (GYZ), a cosmetic color additive, has previously been characterized as a potential antitumor agent due to observed anticancer effects. However, the efficacy of GYZ in the treatment of NSCLC and the involved molecular mechanisms remain largely unknown. Here, we indicated a role for GYZ in the suppression of NSCLC both in vitro and in vivo via triggering reactive oxygen species (ROS)-induced apoptosis. Concomitantly, GYZ induced complete autophagic flux in NSCLC cells via inhibiting the Akt/mTOR signaling pathway, which displayed cytoprotective effect against GYZ-induced growth suppression. Accompanied with autophagy inhibition obviously enhanced the effects of GYZ. Notably, GYZ acts synergistically with paclitaxel in the suppression of NSCLC in vitro. Together, our results for the first time reported that GYZ suppressed the proliferation of NSCLC and suggested a potential strategy for inhibiting NSCLC growth by combinational use of GYZ and autophagy inhibitors.

CAS / MDL: 489-84-9
研究领域: 肿瘤学 · 药理学 · 细胞生物学
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ORGANIC & BIOMOLECULAR CHEMISTRY · 2022 ·Vol. 20 ·期 7 ·1510-1517 · IF 3.89

Synthesis of C3-functionalized indole derivatives via Brønsted acid-catalyzed regioselective arylation of 2-indolylmethanols with guaiazulene

Yang Liu,Meng Cao,Shangxi Zhang,Zhenxi Wang,Xin Dai,Xinde Jiang,Yucheng Dong,Jie Fu

A Brønsted acid catalyzed method for the construction of guaiazulenyl C3-functionalized indole derivatives is reported for the first time. The reactions proceeded smoothly at ambient temperature by using (±)-10-camphorsulfonic acid (CSA) as a catalyst, 2-indolylmethanols and guaiazulene as substrates, and the desired products were obtained in high yields with excellent regioselectivities.

研究领域: 有机化学 · 药物化学
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