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首页> 外文期刊>Biological chemistry >Combination of quercetin and tannic acid in inhibiting 26S proteasome affects S5a and 20S expression, and accumulation of ubiquitin resulted in apoptosis in cancer chemoprevention
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Combination of quercetin and tannic acid in inhibiting 26S proteasome affects S5a and 20S expression, and accumulation of ubiquitin resulted in apoptosis in cancer chemoprevention

机译：槲皮素和单宁酸在抑制26s蛋白酶体中的组合影响S5a和20s表达，泛素的积累导致癌症化学预防凋亡

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摘要

To look for oral proteasome inhibitors, daily injested food is the best source for cancer chemoprevention. A combination of active components from vegetables, coffee, tea, and fruit could be more efficient to inhibit 26S proteasome activities for preventing cancer diseases. Tannic acid and quercetin have been shown to strongly inhibit 26S proteasome activity, but the molecular target involved remains unknown. Overlay assay, peptide assay, Western blot, and 2-D gels were used to assess the combination of quercetin and tannic acid as a potential inhibitor. Here, we demonstrated that the combination of quercetin and tannic acid (1) synergistically suppresses chymotrypsin-, caspase-, and trypsin-like proteolytic activities, (2) are tightly binding substrates, (3) do not perturb the proteasome structure, (4) inhibit the 26S proteasome affected by ubiquitin, ATP, or beta-casein, and (5) inhibit beta-casein degradation by the 26S proteasome in vitro. Finally, the inhibition of the proteasome by a combination of quercetin plus tannic acid in Hep-2 cells resulted in the induction of S5a at low dose, accumulation of ubiquitin, and the cleavage of pro-caspase-3, followed by the induction of apoptotic cell death. Evaluating the combination of quercetin and tannic acid as an oral drug to prevent cancer may provide a pharmacological rationale to pursue preclinical trials of this combination.
机译：为了寻找口服蛋白酶体抑制剂，每日注册食物是癌症化学预防的最佳来源。来自蔬菜，咖啡，茶和水果的活性成分的组合可能更有效地抑制26s的预防癌症疾病的蛋白质组活动。已显示单宁酸和槲皮素强烈抑制26s蛋白酶体活性，但涉及的分子靶标仍然未知。覆盖测定，肽测定，蛋白质印迹和2-D凝胶用于评估槲皮素和单宁酸作为潜在抑制剂的组合。在这里，我们证明了槲皮素和单宁酸（1）的组合协同抑制了胰凝乳蛋白酶，胰岛素 - 和胰蛋白酶样蛋白水解活性，（2）是紧密结合的基材，（3）不要扰乱蛋白酶体结构（4 ）抑制受泛素，ATP或β-酪蛋白影响的26s蛋白酶体，（5）抑制26s蛋白酶体体外抑制β-酪蛋白的降解。最后，通过Hep-2细胞中的槲皮素加单宁酸的组合抑制蛋白酶，导致S5A的诱导在低剂量，泛素的积累和Pro-Caspase-3的切割，然后诱导凋亡细胞死亡。评估槲皮素和单宁酸作为口服药物的组合，以预防癌症可以提供药理学理由，以追求这种组合的临床前试验。

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