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首页> 外文期刊>Journal of Agricultural and Food Chemistry >Measuring Angiotensin-I Converting Enzyme Inhibitory Activity by Micro Plate Assays: Comparison Using Marine Cryptides and Tentative Threshold Determinations with Captopril and Losartan
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Measuring Angiotensin-I Converting Enzyme Inhibitory Activity by Micro Plate Assays: Comparison Using Marine Cryptides and Tentative Threshold Determinations with Captopril and Losartan

机译：通过微孔板测定法测量血管紧张素-I转换酶的抑制活性：使用海洋肽的比较以及卡托普利和氯沙坦的初步阈值测定

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To determine the angiotensin-I converting enzyme (ACE) inhibitory activity of marine cryptides, different methods were tested. ACE inhibition was measured using two synthetic substrates, (N-[3-(2-furyl) acryloyl]-Phe-Gly-Gly (FAPGG) and N-hippuryl-His-Leu hydrate salt (HHL)), and a natural one, angiotensin-I. The IC_(50) value (denned as the concentration of inhibitory molecule needed to inhibit 50% of the ACE activity) of the reference synthetic inhibitor captopril was in the nanomolar range (1.79—15.1 nM) when synthetic substrates were used, whereas it exhibited IC_(50) of micromolar range (16.71 μM) with angiotensin-I. We chose losartan, an antagonist of angiotensin-II receptor as negative control for the ACE inhibition. Losartan was also able to inhibit ACE whatever the substrate tested, with IC_(50) of micromolar range (17.13-146 μM). We denned this value as a limit above which molecules are not showing in vitro ACE inhibitory activity. Val-Trp (VW), Val-Tyr (VY), Lys-Tyr (ICY), Lys-Trp (KW), Ile-Tyr (IY), Ala-Pro (AP), Val-Ile-Tyr (VIY), Leu-Lys-Pro (LKP), Gly-Pro-Leu (GPL), Ala-Lys-Lys (AKK), and Val-Ala-Pro (VAP) were tested as inhibitors of ACE with synthetic and natural substrates. IC_(50) displayed were substrate-dependent. With FAPGG as substrate, IW, VAP, ICY, IY, AP, AKK, and VIY show IC_(50) values over the IC_(50) value of losartan and should not be considered as inhibitors of ACE. VY, VW, ICW, and LKP exhibited IC_(50) value lower than the IC_(50) value of losartan for all substrates tested and were thus considered as good candidates for effectively decreasing hypertension. It appears that the comparison of IC_(50) is not consistent when IC_(50) values are obtained with different substrates and different methods. In vitro ACE inhibitory activity assays should always include various ACE substrates and references such as captopril and a negative control to obtain data reliable to discriminate ACE inhibitory peptides.
机译：为了确定海洋隐蛋白的血管紧张素转换酶（ACE）抑制活性，测试了不同的方法。使用两种合成底物（N- [3-（2-呋喃基）丙烯酰基] -Phe-Gly-Gly（FAPGG）和N-乙酰基-His-Leu水合物盐（HHL））测量ACE抑制，血管紧张素I。当使用合成底物时，参考合成抑制剂卡托普利的IC_（50）值（定义为抑制50％ACE活性所需的抑制分子的浓度）在纳摩尔范围内（1.79-15.1 nM），但显示具有血管紧张素-I的微摩尔范围（16.71μM）的IC_（50）。我们选择血管紧张素II受体拮抗剂氯沙坦作为ACE抑制的阴性对照。氯沙坦还能够抑制ACE，无论所测试的底物如何，IC_（50）的微摩尔范围（17.13-146μM）。我们将此值定义为一个极限值，在该极限值之上，分子未显示出体外ACE抑制活性。 Val-Trp（VW），Val-Tyr（VY），Lys-Tyr（ICY），Lys-Trp（KW），Ile-Tyr（IY），Ala-Pro（AP），Val-Ile-Tyr（VIY）分别测试了Leu-Lys-Pro（LKP），Gly-Pro-Leu（GPL），Ala-Lys-Lys（AKK）和Val-Ala-Pro（VAP）作为具有合成和天然底物的ACE抑制剂。显示的IC_（50）取决于底物。以FAPGG为底物，IW，VAP，ICY，IY，AP，AKK和VIY显示的IC_（50）值超过氯沙坦的IC_（50）值，因此不应视为ACE抑制剂。对于所有测试的底物，VY，VW，ICW和LKP的IC_（50）值均低于氯沙坦的IC_（50）值，因此被认为是有效降低高血压的良好候选者。当使用不同的基板和不同的方法获得IC_（50）值时，IC_（50）的比较似乎不一致。体外ACE抑制活性测定应始终包括各种ACE底物和参考，例如卡托普利和阴性对照，以获得可靠的数据来区分ACE抑制肽。

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