9-O-Terpenyl-Substituted Berberrubine Derivatives Suppress Tumor Migration and Increase Anti-Human Non-Small-Cell Lung Cancer Activity

Lung cancer is one of the most common cancers and the leading cause of death in humans worldwide. Non-small-cell lung cancer (NSCLC) accounts for approximately 85% of lung cancer cases and is often diagnosed at a late stage. Among patients with NSCLC, 50% die within 1 year after diagnosis. Even with...

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Published inInternational journal of molecular sciences Vol. 22; no. 18; p. 9864
Main Authors Chang, Jia-Ming, Wu, Jin-Yi, Chen, Shu-Hsin, Chao, Wen-Ying, Chuang, Hsiang-Hao, Kam, Kam-Hong, Zhao, Pei-Wen, Li, Yi-Zhen, Yen, Yu-Pei, Lee, Ying-Ray
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 13.09.2021
MDPI
Subjects
Apoptosis
Autophagy
Cancer therapies
Cell growth
Immunotherapy
Investigations
Lung cancer
Medical prognosis
Metastasis
Tumorigenesis
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Summary:Lung cancer is one of the most common cancers and the leading cause of death in humans worldwide. Non-small-cell lung cancer (NSCLC) accounts for approximately 85% of lung cancer cases and is often diagnosed at a late stage. Among patients with NSCLC, 50% die within 1 year after diagnosis. Even with clinical intervention, the 5-year survival rate is only approximately 20%. Therefore, the development of an advanced therapeutic strategy or novel agent is urgently required for treating NSCLC. Berberine exerts therapeutic activity toward NSCLC; therefore, its activity as an antitumor agent needs to be explored further. In this study, three terpenylated-bromide derivatives of berberrubine were synthesized and their anti-NSCLC activities were evaluated. Each derivative had higher anti-NSCLCs activity than berberrubine and berberine. Among them, 9-O-gernylberberrubine bromide (B4) and 9-O-farnesylberberrubine bromide (B5) showed greater growth inhibition, cell-cycle regulation, in vitro tumorigenesis suppression, and tumor migration reduction. In addition, some degree of apoptosis and autophagic flux blocking was noted in the cells under B4 and B5 treatments. Our study demonstrates that the berberrubine derivatives, B4 and B5, exhibit impressive anti-NSCLC activities and have potential for use as chemotherapeutic agents against NSCLC.
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ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms22189864