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柿子单宁体外抑制胰脂肪酶活性及其作用机制。

Inhibitory Effect of Persimmon Tannin on Pancreatic Lipase and the Underlying Mechanism in Vitro.

机构信息

College of Food Science and Technology , Huazhong Agricultural University , Wuhan 430070 , China.

Key Laboratory of Environment Correlative Food Science , Huazhong Agricultural University, Ministry of Education , Wuhan 430070 , China.

出版信息

J Agric Food Chem. 2018 Jun 20;66(24):6013-6021. doi: 10.1021/acs.jafc.8b00850. Epub 2018 Jun 11.

Abstract

Pancreatic lipase (PL) is a critical enzyme associated with hyperlipidemia and obesity. A previous study of ours suggested that persimmon tannin (PT) was the main component accounting for the antihyperlipidemic effects of persimmon fruits, but the underlying mechanisms were unclear. In this present study, the inhibitory effect of PT on PL was studied and the possible mechanisms were evaluated by fluorescence spectroscopy, circular dichroism (CD) spectra, isothermal titration calorimetry (ITC), and molecular docking. PT had a high affinity to PL and inhibited the activity of PL with the half maximal inhibitory concertation (IC) value of 0.44 mg/mL in a noncompetitive way. Furthermore, molecular docking revealed that the hydrogen bonding and π-π stacking was mainly responsible for the interaction. The strong inhibition of PT on PL in the gastrointestinal tract might be one mechanism for its lipid-lowering effect.

摘要

胰脂肪酶(PL)是与高脂血症和肥胖症相关的关键酶。我们之前的研究表明,柿子单宁(PT)是柿子果实发挥降血脂作用的主要成分,但具体机制尚不清楚。在本研究中,通过荧光光谱法、圆二色性(CD)光谱法、等温热滴定(ITC)和分子对接研究了 PT 对 PL 的抑制作用,并评估了可能的机制。PT 与 PL 具有高亲和力,以非竞争性方式抑制 PL 的活性,其半最大抑制浓度(IC)值为 0.44mg/mL。此外,分子对接表明氢键和π-π堆积主要负责相互作用。PT 在胃肠道中对 PL 的强烈抑制可能是其降脂作用的机制之一。

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