Obi-wan
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- Mar 16, 2017
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"Fenbendazole, FZ], a benzimidazole compound, is a safe and inexpensive anthelmintic drug possessing an efficient anti-proliferative activity. In our earlier work, we reported a potent growth-inhibitory activity of FZ caused partially by impairment of proteasomal function. Here, we show that FZ demonstrates moderate affinity for mammalian tubulin and exerts cytotoxicity to human cancer cells at micromolar concentrations. Simultaneously, it caused mitochondrial translocation of p53 and effectively inhibited glucose uptake, expression of GLUT transporters as well as hexokinase (HK II) - a key glycolytic enzyme that most cancer cells thrive on"
The inhibition of glucose uptake really caught my eye...
Inhibition of glucose uptake by FZ sensitizes cancer cells to undergo apoptosis
In studies with parasites, the anthelmintic effects of the benzimidazoles have been related to inhibition of glucose uptake with resultant alterations in glucose metabolism41. We tested the effect of FZ on glucose uptake in human cancer cells. H460 and A549 cells were treated with 1 uM FZ for 4 h and uptake of fluorescent glucose analogue 2-NBDG was observed. FZ treatment resulted in inhibition in glucose uptake in both the cell lines (Fig. 8a). Similar results were obtained when a glucose oxidation assay was performed using culture supernatants from cells treated with increasing concentrations of FZ (Fig. 8b). Expectedly, FZ treatment also resulted in reduced lactate levels (Fig. 8c). Hence, FZ induced cell death appeared to be related to inhibition of glucose uptake.
The inhibition of glucose uptake really caught my eye...
Inhibition of glucose uptake by FZ sensitizes cancer cells to undergo apoptosis
In studies with parasites, the anthelmintic effects of the benzimidazoles have been related to inhibition of glucose uptake with resultant alterations in glucose metabolism41. We tested the effect of FZ on glucose uptake in human cancer cells. H460 and A549 cells were treated with 1 uM FZ for 4 h and uptake of fluorescent glucose analogue 2-NBDG was observed. FZ treatment resulted in inhibition in glucose uptake in both the cell lines (Fig. 8a). Similar results were obtained when a glucose oxidation assay was performed using culture supernatants from cells treated with increasing concentrations of FZ (Fig. 8b). Expectedly, FZ treatment also resulted in reduced lactate levels (Fig. 8c). Hence, FZ induced cell death appeared to be related to inhibition of glucose uptake.
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