A novel series of bis(furan-based chalcone) derivatives linked to aliphatic linkers, with the furan units at the A-or B-rings, were synthesized and evaluated as anticancer agents. Chalcones 5 ac in which the furan ring designed to be a B-ring were obtained from the Knoevenagel condensation reactions of the appropriate bis(acetyl) compounds 3 a-c with two equivalents of furan-2-aldehyde. Likewise, the condensation of bis(aldehydes) 7 a-c with two equivalents of 2-acetylfuran afforded the corresponding chalcones 9 a-c, in which the furan rings represent the A-rings of the chalcones, in excellent yields. The synthesized compounds have been fully characterized by 1 H-NMR, 13 C-NMR, and elemental analysis. The in vitro anticancer activity of the prepared compounds was tested against A549, HCT116, HePG2, PC3, A431 and BJ1 cell lines using MTT assay, gene expression analysis of skin and lung cancer related genes, comet assay, and DNA fragmentation assy. Compounds 9 a and 9 c were found to be the most promising, with IC 50 (24.9 and 13.7 μg/ml, respectively) against A549 compared with doxorubicin (IC 50 , 28.3 μg/ml) and IC 50 (26.1 and 14.4 μg/ml, respectively) against A431 in comparison to doxorubicin (IC 50 , 24.9 μg/ml). Comapred with neagtive control cell lines, the gene expression levels of hBD-2 and hBD-3 genes were decreased singnificantly (P < 0.05) in positive control and skin cancer cell lines (A431) treated with compounds 9 a and 9 c. The expression levels of FOSB and IL-8 genes were increased singnificantly (P < 0.05) in positive control and lung cancer cell lines (A549 and A541) treated with compounds 9 a and 9 c, respectively, comapred with neagtive control cell lines. The DNA damage was increased significantly (P < 0.001) in treated skin and lung cell lines samples compared with negative control. The negative control skin and lung cancer cell lines showed a significant decrease (P < 0.05) in DNA fragmentation rate compared with positive control. On the other hand, the DNA fragmentation rates were increased significantly (P < 0.001) in treated skin and lung cell lines samples compared with negative control. In summary, the synthesized compounds 9 a and 9 c showed a significant anticancer activity against lung and skin cancer cell lines compared with known chemotherapeutic drug (doxorubicin).
Since the development of cold atmospheric plasma (CAP), substantial and significant usage of CAP applications was introduced in medicine. Here, we developed two combined sources of plasma to produce in situ plasma‐activated air‐driven water mist (PAAWM). The first is generated using air as a feed gas, while the second is plasma‐activated water generated by the ignition of plasma within the air‐driven water mist. Both contribute to the plasma jet generation of PAAWM. The antitumor efficacy of PAAWM was evaluated against two hepatocellular carcinoma cell lines (SNU‐449 and SNU‐475). The generated PAAWM was efficient in the treatment of both chemosensitive and chemoresistant hepatocellular carcinoma cells. These results may support using PAAWM alone or in combination with other treatment modalities.
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