花生壳乙醇提取物的脲酶抑制活性研究

以花生壳为研究对象,探索其防治胃炎、胃溃疡的可能性和作用机制。用乙醇进行提取,所得提取物总黄酮含量为29. 5%,其中木犀草素占总黄酮的84. 6%。脲酶活性研究表明,花生壳提取物具有较好抑制作用,IC50达到48. 1±2. 7μg/m L,表面等离子体共振(SPR)动力学亲和分析显示花生壳与脲酶具有较强的亲和力(KD为0. 11±0. 02μg/m L)。与木犀草素的折合活性相比,花生壳提取物具有更高的脲酶抑制活性,表明提取物中还存在其他具有脲酶抑制活性物质,并与木犀草素存在协同增效作用。主要活性成分木犀草素与脲酶活性点的Ni离子和周围的氨基酸残基存在强的配位键和氢键相互作用,占住脲酶活性点而导致脲酶失活。

Evaluation of peanut hull ethanol extract as an agent against urease

This paper was aimed to address the possible treatment and therapeutic mechanism of infected gastrosis by the ethanol extract from peanut hull.The obtained extract had 29.5%of total flavonoids which contains 84.6%of luteolin.Urease inhibition determination indicated that the extract showed high potency with IC50 of 48.1±2.7μg/mL,and urease-ligand interaction analysis by surface plasmon resonance(SPR)disclosed a high affinity of the extract with KD of 0.11±0.02μg/mL.Synergistic effect must be have between luteolin and other constituents by comparison of their urease inhibition activities.The main active compound luteolin inactivated the urease by occupied the active site,and was firmly anchored by several coordinate bonds and hydrogen-bonding interactions.