A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using the brine shrimp lethality test (BSLT) and the methyl thiazolyl tetrazolium assay against Vero, HeLa, and MCF7 cell lines. The structures of the synthesized compounds were confirmed by Fourier transform infrared spectrophotometry (FTIR), 1H-nuclear magnetic resonance (NMR), 13C-NMR, and mass spectral data. The results of the cytotoxicity evaluation showed that the synthesized compounds exhibited moderate to very high toxic activity in BSLT, requiring a concentration of 13.06–714.49 µg/mL to kill half the population. Most of the compound exhibited cytotoxic activity against HeLa cell lines, comparable to the activity of cisplatin with a concentration of the synthesized compounds required to inhibit 50% of the growth of the cell lines (IC50) value of 40.65–95.55 µM, and most of the compounds tested against MCF7 cell lines exhibited moderate to very high cytotoxic activity (IC50 value 7.86–35.88 µM). However, the selectivity index of the compounds was low, less than 1–1.96. Among the synthesized compounds, compound 1b showed the highest cytotoxicity and selectivity against MCF7 cell lines. Compound 1b could be considered for further development to obtain more active and selective chemotherapeutic agents against breast cancer.
A series of diethylamine Mannich base of asymmetrical mono-carbonyl analogs of 10 curcumin (AMACs) were synthesized and evaluated for cytotoxic activity against Hela Cell lines.
11The structures of the synthesized compounds were confirmed on the basis of FTIR, 1 H-NMR,
1213 C-NMR and mass spectral data. Preliminary cytotoxic test using BSLT showed that all the
Muscle tissues make up about 40-50% of the human bodies. Satellite cells, which present in between the basal lamina and myofiber, are the adult muscle stem cells or myoblasts which are important for the regeneration of muscle tissues. Anticancer agents generally possess high cytotoxicity to either cancer cells or normal cells. Their effects on muscle cells generate cachexia or the deterioration of muscle tissues. Chemopreventive agents which possess lower cyctotoxic effects are expected to show higher safety in normal cells. Therefore, we investigated the effects of chemopreventive agents curcumin, naringin, and epigallocathecin-3-gallate (EGCG), which show anticancer properties in cancer cells, in C2C12 myoblast cells. We observed the C2C12 cell viability by MTT and WST assays, cell migration by wound healing scratch assay, as well as differentiation assay after treatment with the chemopreventive agents. The results indicated that curcumin showed highest cytotoxicity compared to naringin and EGCG. In addition, naringin and EGCG exhibited lower cytotoxicity. Both naringin and EGCG inhibited C2C12 cell migration at cell density 150, 000 cells/ml. Whereas, at cell density 100, 000 cells/ml, there was no significant effects of naringin as well as EGCG. Altogether, the results suggest that naringin and EGCG possess lower cytotoxic effect on C2C12 myoblast cells whereas curcumin showed stronger cytotoxicity at concentration higher than 20 µM.
Doxorubicin is one of the first line chemotherapeutic agents used to treat different types of cancer. However, despite its efficacy, doxorubicin can be toxic to muscle tissue and worsen the prognosis of cancer patients. Previously, we investigated the effect of chemopreventive agents curcumin, naringin and epigallocathecin-3-gallate (EGCG), which show anticancer properties in cancer cells, in C2C12 myoblast cells. We found that naringin, a citrus flavonoid, showed no significant cytotoxic effect on C2C12 cells. In this study, we investigated doxorubicin cytotoxicity alone or in combination with naringin against C2C12 myoblast cells, which can be differentiated into multinucleated myotubes. Cell viability assays had been carried out by WST assay, whereas C2C12 differentiation was observed after incubation of C2C12 cells with 2% horse serum and stained with crystal violet. As a result, C2C12 cell viability decreased to 43.89% after treatment with 2 µM doxorubicin for 24 hours. Moreover, C2C12 differentiation is also inhibited by doxorubicin. In contrast, C2C12 cell viability was maintained at 90.45% after treatment with 500 µM naringin. Interestingly, naringin may alleviate doxorubicin cytotoxic effects on C2C12 cell myogenesis.
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