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      In vitro inhibition of fatty acid synthase by 1,2,3,4,6-penta-O-galloyl-β-D-glucose plays a vital role in anti-tumour activity.

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          Abstract

          1,2,3,4,6-Penta-O-galloyl-β-D-glucose (PGG) inhibits glioma cancer U251 cells, more strongly than MDA-MB-231 and U87 cells. In addition, PGG is transported across cancer cell membrane to further down-regulate FAS and activate caspase-3 in MDA-MB-231 cells. Compared with other FAS inhibitors, including catechin gallate and morin, PGG involves a higher reversible fast-binding inhibition with half-inhibitory concentration value (IC50) of 1.16 μM and an irreversible slow-binding inhibition, i.e. saturation kinetics with a dissociation constant of 0.59 μM and a limiting rate constant of 0.16 min(-l). The major reacting site of PGG is on the β-ketoacyl reduction domain of FAS. PGG exhibits different types of inhibitions against the three substrates in the FAS overall reaction. The higher concentrations of PGG tested (higher than 20 μM) clearly altered the secondary structure of FAS by increasing the α-helix and induced a redshift in the FAS spectra. In addition, only PGG concentrations higher than 20 μM resulted in FAS precipitation.

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          Author and article information

          Journal
          Biochem. Biophys. Res. Commun.
          Biochemical and biophysical research communications
          Elsevier BV
          1090-2104
          0006-291X
          Mar 07 2014
          : 445
          : 2
          Affiliations
          [1 ] Capital Medical University, 10 Xitoutiao, You An Men, Beijing 100069, PR China.
          [2 ] Capital Medical University, 10 Xitoutiao, You An Men, Beijing 100069, PR China. Electronic address: mingzhao@bjmu.edu.cn.
          [3 ] Capital Medical University, 10 Xitoutiao, You An Men, Beijing 100069, PR China. Electronic address: sqpeng@bjmu.edu.cn.
          Article
          S0006-291X(14)00237-X
          10.1016/j.bbrc.2014.01.191
          24508804
          02f7099d-c71c-4df2-9c45-9d6517cbdf7a
          History

          Fatty acid synthase (FAS),Anti-tumour,1,2,3,4,6-Penta-O-galloyl-β-d-glucose (PGG)

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