Abstract
Lung cancer is the leading cause of death in the world, and the most common type of lung cancer is non-small-cell lung cancer (NSCLC), accounting for 85% of lung cancer. Patients with NSCLC, when detected, are mostly in a metastatic stage, and over half of patients diagnosed with NSCLC die within one year after diagnosis; the 5-year survival rate is 24%. However, in patients with metastatic NSCLC, the 5-year survival rate is 6%. Therefore, development of a new therapeutic agent or strategy is urgent for NSCLCs. Berberine has been illustrated to be a therapeutic agent of NSCLC. In the present study, we synthesized six derivatives of berberine, and the anti-NSCLC activity of these agents was examined. Some of them exert increasing proliferation inhibition comparing with berberine. Further studies demonstrated that two of the most effective agents, 9-O-decylberberrubine bromide (B6) and 9-O-dodecylberberrubine bromide (B7), performed cell cycle regulation, in-vitro tumorigenesis inhibition and autophagic flux blocking, but not induction of cellular apoptosis in NSCLC cells. Moreover, B6 and B7 were determined to be green fluorescent and could be penetrated and localized in cellular mitochondria. Herein, B6 and B7, the berberine derivatives we synthesized, revealed better anti-NSCLC activity with berberine and may be used as therapeutic candidates for the treatment of NSCLCs.
Highlights
Lung cancer is the second-most common cancer and the leading cause of cancer-associated deaths for both men and women
A549 and H1435 cells were sensitive to B6 and B7 treatment (Table 1) compared with H23 cells
B6 and B7 show the most inhibition of non-small-cell lung cancer (NSCLC) cells
Summary
Lung cancer is the second-most common cancer and the leading cause of cancer-associated deaths for both men and women. The 5-year survival is around 17.8%, and, when people are diagnosed with lung cancer, over half of them die within one year [1]. Small-cell lung cancer and non-small-cell lung cancer (NSCLC) are two main subtypes of lung cancer. Around 85% of lung patients are diagnosed with NSCLC [1]. Patients with NSCLC are recommended to remove the tumor with surgery. Patients with stage II and IIIA NSCLC usually receive adjuvant therapies, including radiation, chemotherapy, or targeted therapy. There are lots of chemotherapeutic agents and targeted agents to guide therapy. The need to constantly pursue novel therapeutic agents or new treatment strategies to improve overall survival for NSCLC is pressing
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