The anticancer/cytotoxic effect of a novel gallic acid derivative in non-small cell lung carcinoma A549 cells and peripheral blood mononuclear cells from healthy individuals and lung cancer patients.

Gallic acid (GA) is a naturally occurring polyphenol with a strong antioxidant capacity. GA stimulates the apoptosis of cancer cells, thereby suppressing cancer cell invasion. However, the low oral permeability of GA limits its therapeutic use. In order to enhance the antioxidant capacity and oral permeability of GA, a series of compounds analogous to GA were synthesized: 4-methoxybenzenesulfonamide (MBS), 3,4-dimethoxybenzenesulfonamide (DMBS) and 3,4,5-trimethoxybenzenesulfonamide (TMBS). In the new compounds, hydroxyl groups were replaced with various numbers of methoxy groups (stronger electron-donating groups), to increase hydrophobicity and oral permeability compared to GA. In addition, the carboxylic group was replaced with a sulfonyl group (a stronger electron-withdrawing group), to increase the molecular polarity and antioxidative activities of the compounds. The cell counting kit-8 (CCK-8) assay was used to detect the effect of GA, MBS, DMBS, and TMBS on cell proliferation and apoptosis in peripheral blood mononuclear cells (PBMCs) from healthy individuals and non-small cell lung carcinoma A549 cells. Additionally, the comet assay was used to assess the genotoxicity of these compounds in PBMCs from healthy individuals, lung cancer patients, and A549 cells. Compared to untreated cells, TMBS reduced DNA damage more effectively than GA in PBMCs from lung cancer patients and healthy donors. Furthermore, in comparison to GA, TMBS was more cytotoxic in A549 cells. Moreover, TMBS was not cytotoxic in healthy PBMCs, suggesting that TMBS demonstrates therapeutic potential in cancer.

Interferon-γ liposome: a new system to improve drug delivery in the treatment of lung cancer.

Lung cancer is one of the main causes of death worldwide. Published data show the use of interferons (IFNs) in treating lung tumours. IFNs also have potential for their antiproliferative, antiangiogenic, immunoregulatory and proapoptotic effects. IFN-γ functions as an anticancer agent against various forms of cancer. This study aimed to investigate the effect of IFN-γ liposome (nano) on peripheral lymphocytes from 20 individuals in each group: lung cancer patients compared to healthy individuals. The effectiveness of IFN-γ liposome against oxidative stress was also evaluated in this study. A concentration of 100 U·mL-1 of IFN-γ liposome was used to treat the lymphocytes in the Comet and micronucleus assays based on the preliminary test for the optimal dose. The lymphocytes from lung cancer patients presented with higher DNA damage levels than those of healthy individuals. In healthy individuals, IFN-γ liposome did not cause any DNA damage in the lymphocytes. Also, it caused a significant reduction in DNA damage in the lymphocytes from lung cancer patients in both the Comet and micronucleus assays. The 100 U·mL-1 of IFN-γ liposome significantly reduced the oxidative stress caused by H2O2 and appeared to be effective in both groups using the Comet and micronucleus assays. Results from both Comet and micronucleus assays were consistent. The data obtained indicated that IFN-γ in both forms (IFN-γ bulk and IFN-γ nanoliposome) may potentially be effective for the treatment of lung cancer and showed the ability of IFN-γ liposome to reduce DNA damage more than the bulk form.