The inhibitory effects of three dietary constituents, tea polyphenols, resveratrol, and diallyl trisulfide, on acrylamide-biomacromolecule (liver DNA, protamine, and hemoglobin) adduct formation at human exposure level were studied by accelerator mass spectrometry. The results demonstrated that the three dietary constituents all significantly inhibited the formation of acrylamide adducts with liver DNA, whereas tea polyphenols and diallyl trisulfide reduced protamine and hemoglobin adducts, respectively. Further biochemical studies showed that acrylamide could significantly inactivate creatine kinase and glutathione S-transferase and deplete glutathione. When the inhibitors were cotreated with acrylamide, all of them could effectively recover the activities of creatine kinase. In addition, tea polyphenols and diallyl trisulfide could increase glutathione S-transferase activity remarkably. On the basis of these results, mechanisms of the effects are discussed. This study might provide a beneficial guide to people's diet for the purpose of reducing the harmful effect of acrylamide.