首页> 外文期刊>International Dairy Journal >Screening milk-derived antihypertensive peptides using quantitative structure activity relationship (QSAR) modelling and in vitro/in vivo studies on their bioactivity.
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Screening milk-derived antihypertensive peptides using quantitative structure activity relationship (QSAR) modelling and in vitro/in vivo studies on their bioactivity.

机译:使用定量结构活性关系(QSAR)建模及其生物活性的体外/体内研究筛选牛奶来源的降压肽。

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In this study, we constructed a quantitative structure activity relationship (QSAR) model of angiotensin I-converting enzyme (ACE) inhibitory tripeptides from published data (R 2 = 0.8437; Q 2 = 0.649) and applied the model to screen 27 tripeptides derived from cow milk protein sequences. Potential ACE inhibitory tripeptides were synthesised and evaluated in in vitro/in vivo studies. Results showed that ACE inhibitory activities of tripeptides followed the order (p< 0.05): isoleucine-proline-proline (IPP, commercial) > valine-isoleucine-proline (VIP) > isoleucine-valine-proline (IVP) based on concentrations (7.57-49.72 muM) that decreased 50% of ACE activity. Lowering systolic blood pressure (SBP) effect of tripeptides in rats (1.5 mg kg-1 body weight dosage) followed the order according to relative lowering SBP rates: IVP (24%) > IPP (17%) > VIP (12%), consistent with results on mRNA levels of sarcoplasmic reticulum Ca2+, Mg2+ -ATPase gene in rat hearts (p< 0.05). IPP and IVP showed no negative effects on blood glycometabolism
机译:在这项研究中,我们根据已发表的数据(R 2 = 0.8437; Q 2 = 0.649),然后将该模型应用于筛选来自牛奶蛋白序列的27个三肽。合成了潜在的ACE抑制三肽,并在体外/体内研究中进行了评估。结果显示三肽的ACE抑制活性遵循以下顺序(p <0.05):异亮氨酸-脯氨酸-脯氨酸(IPP,商业)>缬氨酸-异亮氨酸-脯氨酸(VIP)>异亮氨酸-缬氨酸-脯氨酸(IVP)基于浓度(7.57) -49.72μM)降低了ACE活性的50%。按照相对降低SBP的比率,降低三肽在大鼠(1.5 mg kg -1 体重剂量)的收缩压(SBP)效应的顺序为:IVP(24%)> IPP(17%) > VIP(12%),与大鼠心脏肌浆网Ca 2 + ,Mg 2 + -ATPase基因mRNA水平的结果一致(p <0.05)。 IPP和IVP对血糖代谢没有负面影响

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