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3,3'-((3,4,5-trifluoropHenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) inhibit lung cancer cell proliferation and
Wenhui Luo1,2, Guoxin Chang3, Dingmei Lin3
1School of Medicine, Foshan University, Foshan, Guangdong Province, PR China.
Abstract:
Lung cancer is a major public health challenge and, despite therapeutic improvements, is the first leading cause of cancer worldwide. The current cure rate from advanced cancer treatment is excessively low. Therefore, it is of great importance to identify novel, potent and less toxic anticancer agents for the treatment of lung cancer. The aim of our research is to synthesize a new biscoumarin 3,3'-((3,4,5-trifluorop -phenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) (C35) as an anticancer agent. C35 was simply prepared by 4-hydroxycoumarin and 3,4,5-trifluorobenzaldehyde under ethanol and its structure was analyzed by spectroscopic analyses. The anti-proliferation effect of C35 was detected using CCK-8 assay. Migration abilities were measured by Transwell assay. The expression of correlated proteins was determined by Western blot. The results showed that C35 displayed strong cytostatic effects on lung cancer cell proliferation. In addition, C35 possessed a significant inhibition of migration by reducing the expression of matrix metalloproteinases-2 (MMP-2) and MMP-9 in lung cancer cells. Furthermore, C35 treatment suppressed the phosphorylation of p38 in lung cancer cells. Moreover, in vivo experiments were carried out, in which we treated Lewis tumor-bearing C57 mice via intraperitoneal injection of C35. Results showed that C35 inhibited tumor growth in vivo. In conclusion, our study demonstrated the anticancer activity of C35 via suppression of lung cancer cell proliferation and migration, which is possibly involved with the inhibition of the p38 pathway.
Insights
A novel biscoumarin compound, C35, effectively inhibits lung cancer cell proliferation and migration. In vivo studies confirmed C35
Area of Science:
- Oncology
- Medicinal Chemistry
Background:
- Lung cancer remains a leading cause of cancer mortality worldwide, with low cure rates for advanced stages.
- There is a critical need for novel, potent, and less toxic anticancer agents to improve lung cancer treatment outcomes.
Purpose of the Study:
- To synthesize and evaluate a new biscoumarin derivative, 3,3'-((3,4,5-trifluorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) (C35), as a potential anticancer agent for lung cancer.
Main Methods:
- C35 was synthesized from 4-hydroxycoumarin and 3,4,5-trifluorobenzaldehyde and characterized using spectroscopic analyses.
- In vitro assays (CCK-8, Transwell) assessed C35's anti-proliferation and anti-migration effects on lung cancer cells.
- Western blot analysis determined protein expression changes, and in vivo studies utilized Lewis lung tumor-bearing mice.
Main Results:
- C35 demonstrated significant cytostatic effects, inhibiting lung cancer cell proliferation.
- C35 markedly reduced cancer cell migration by downregulating matrix metalloproteinases-2 (MMP-2) and MMP-9 expression.
- C35 suppressed p38 mitogen-activated protein kinase (MAPK) phosphorylation and inhibited tumor growth in vivo.
Conclusions:
- The novel biscoumarin C35 exhibits potent anticancer activity against lung cancer by suppressing cell proliferation and migration.
- The anticancer effects of C35 are potentially mediated through the inhibition of the p38 MAPK signaling pathway.
- C35 represents a promising candidate for further development as a lung cancer therapeutic agent.
