Given that psoralens have been shown to be potent inhibitors of
several enzymes from the cytochrome P450 superfamily, in the
current work molecular docking methodologies were used to
predict the binding pose between each of these ligands and the
enzyme CYP2A6. The enzyme CYP2A6 was chosen since it is one of
the 57 CYP isoenzymes found in humans [21] and it is involved in
the metabolism of several pharmaceuticals, carcinogens, and
a number of coumarin-type alkaloids [22,23]. As previously
mentioned, psoralens, such as xanthotoxin and Bergapten, have
been shown to efficiently inhibit this enzyme, and contribute to the
programmed cancer cell death and increased sensitivity to
chemotherapy. Several studies demonstrated the anti-proliferative
effect of xanthotoxin and Bergapten on cancer cell lines, including
B16F10 (melanoma cells), gastric adenocarcinoma (MK-1), breast
cancer (MCF-7 and T47D), and hepatocellular carcinoma [24e27].
The cytotoxic effect of these psoralens was also demonstrated
against HeLa [25,28e30] and MDA MB 231 [26,31], which are the
cell lines under study in the current work. Moreover, xanthotoxin
was evaluated against the bladder carcinoma cell line EJ but the
preliminary results were not very promising [32]. No data on TCCSUP
cells has been reported in the literature regarding the effect of
xanthotoxin and Bergapten.
Given that psoralens have been shown to be potent inhibitors of
several enzymes from the cytochrome P450 superfamily, in the
current work molecular docking methodologies were used to
predict the binding pose between each of these ligands and the
enzyme CYP2A6. The enzyme CYP2A6 was chosen since it is one of
the 57 CYP isoenzymes found in humans [21] and it is involved in
the metabolism of several pharmaceuticals, carcinogens, and
a number of coumarin-type alkaloids [22,23]. As previously
mentioned, psoralens, such as xanthotoxin and Bergapten, have
been shown to efficiently inhibit this enzyme, and contribute to the
programmed cancer cell death and increased sensitivity to
chemotherapy. Several studies demonstrated the anti-proliferative
effect of xanthotoxin and Bergapten on cancer cell lines, including
B16F10 (melanoma cells), gastric adenocarcinoma (MK-1), breast
cancer (MCF-7 and T47D), and hepatocellular carcinoma [24e27].
The cytotoxic effect of these psoralens was also demonstrated
against HeLa [25,28e30] and MDA MB 231 [26,31], which are the
cell lines under study in the current work. Moreover, xanthotoxin
was evaluated against the bladder carcinoma cell line EJ but the
preliminary results were not very promising [32]. No data on TCCSUP
cells has been reported in the literature regarding the effect of
xanthotoxin and Bergapten.
การแปล กรุณารอสักครู่..
