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3',4',5,7-四(二乙基磷酰基)-木犀草素对碱性脂肪酶活性影响机制的研究

Study on the mechanism of alkaline lipase activity influenced by 3',4',5,7-four(2-ethyl-phosphoryl)-luteolin
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摘要 目的探讨黄酮类化合物3',4',5,7-四(二乙基磷酰基)-木犀草素对碱性脂肪酶活性的影响。方法采用3',4',5,7-四(二乙基磷酰基)-木犀草素作为抑制剂,以改进后的铜皂法测定脂肪酶活性,测定3',4',5,7-四(二乙基磷酰基)-木犀草素的浓度与脂肪酶活性的关系,得出该化合物对脂肪酶活性影响,并测定其IC50值。结果该化合物对碱性脂肪酶活性的抑制作用为非竞争性抑制,其IC50为3.17×10-7mol/L。米氏常数K m=100 mmol/L,抑制常数K i=2.7×10-7mol/L。结论 3',4',5,7-四(二乙基磷酰基)-木犀草素对碱性脂肪酶的抑制机制是其与酶的活性部位以外的基团作用而导致酶活性降低,呈非竞争性抑制。 Objective To study the effect of flavonoid compounds on alkaline lipase activity. Method The improved copper soap method was choosed to determine the activity of lipase with 3',4',5,7-four(2-ethyl-phosphoryl)-luteolin as inhibitors. It was used to measure the relationship between the concentration of 3',4',5,7-four(2-ethyl-phosphoryl)-luteolin and the lipase activity to work out the effect of the compound on lipase activity, and calculate its IC50. Result The inhibition effect of the compound on the activity of alkaline lipase was non-competitive inhibition, the IC50 = 3.17 × 10^-7mol/L, K m = 100 mmol/L, and K i = 2.7 × 10^-7 mol/L.Conclosion The inhibitory effect of the compounds on alkaline lipase is non-competitive, which results from interaction with the groups outside the activation site and leads to the decrease of enzyme activity.
出处 《中国医药生物技术》 2015年第2期144-148,共5页 Chinese Medicinal Biotechnology
关键词 3' 4' 5 7-四(二乙基磷酰基)-木犀草素 酶抑制剂 IC50 3' 4' 5 7-four(2-ethyl-phosphoryl)-luteolin Enzyme inhibitors IC50
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