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芝麻酚抑制脂氧合酶作用佐证其潜在抗炎活性。

Inhibition of lipoxygenase by sesamol corroborates its potential anti-inflammatory activity.

机构信息

Department of Protein Chemistry & Technology, CSIR-Central Food Technological Research Institute, Mysuru, 570020, India.

Department of Protein Chemistry & Technology, CSIR-Central Food Technological Research Institute, Mysuru, 570020, India.

出版信息

Int J Biol Macromol. 2017 Jan;94(Pt B):781-787. doi: 10.1016/j.ijbiomac.2016.06.048. Epub 2016 Jun 15.

DOI:10.1016/j.ijbiomac.2016.06.048
PMID:27316769
Abstract

Reactive oxygen species, the byproducts of oxygenases reaction, when in excess, promote degenerative diseases like cardiovascular, cancer and arthritis. Sesame lignans- sesamin, sesamolin and the phenolic degradation product of sesamolin, sesamol, are empirically known for their health promoting properties like antioxidant, antimutagenic, antiaging and antiinflammatory activities. In the current study, the effect of sesamol on the inflammatory oxygenase - lipoxygenase (LOX) was investigated. Enzyme kinetics and spectroscopic techniques were used to understand the inhibition mechanism. Sesamol was a potent inhibitor of soy LOX-1. It inhibited soy LOX-1 in a dose dependent manner with IC value of 51.84μM and K of 4.9μM. Binding studies using circular dichroism and corroborated by surface plasmon resonance, revealed that sesamol does not bind or change the conformation of LOX. Further, sesamol prevented the conversion of inactive LOX (Fe) to active LOX (Fe) by arresting the oxidation state of iron and prolonging the lag phase by virtue of its ability to scavenge hydroperoxides. Understanding the mechanism of action of such molecules will help in their application and promotion as nutraceuticals.

摘要

活性氧物种是加氧酶反应的副产物,当其过量时,会促进心血管疾病、癌症和关节炎等退行性疾病的发生。芝麻木脂素-芝麻素、芝麻林素和芝麻林素的酚类降解产物芝麻酚,已被经验证具有促进健康的特性,如抗氧化、抗突变、抗衰老和抗炎活性。在本研究中,研究了芝麻酚对炎症加氧酶-脂氧合酶(LOX)的影响。酶动力学和光谱技术用于了解抑制机制。芝麻酚是大豆 LOX-1 的有效抑制剂。它以剂量依赖的方式抑制大豆 LOX-1,IC 值为 51.84μM,K 值为 4.9μM。圆二色性和表面等离子体共振的结合研究表明,芝麻酚不结合或改变 LOX 的构象。此外,芝麻酚通过阻止铁的氧化状态并通过清除过氧化物延长迟滞期,从而阻止无活性 LOX(Fe)向活性 LOX(Fe)的转化。了解此类分子的作用机制将有助于将它们作为营养保健品进行应用和推广。

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