Departamento de Biotecnología de Alimentos, Instituto de Agroquímica y Tecnología de Alimentos, Consejo Superior de Investigaciones Científicas (IATA-CSIC), Avenida Agustín Escardino 7, 46980 Paterna, Valencia, Spain.
J Agric Food Chem. 2014 Feb 19;62(7):1609-16. doi: 10.1021/jf4053868. Epub 2014 Feb 6.
Novel antihypertensive peptides released by Kluyveromyces marxianus from bovine lactoferrin (LF) have been identified. K. marxianus LF permeate was fractionated by semipreparative high performance liquid chromatography and 35 peptides contained in the angiotensin I-converting enzyme (ACE)-inhibitory fractions were identified by using an ion trap mass spectrometer. On the basis of peptide abundance and common structural features, six peptides were chemically synthesized. Four of them (DPYKLRP, PYKLRP, YKLRP, and GILRP) exerted in vitro inhibitory effects on ACE activity and effectively decreased systolic blood pressure after oral administration to spontaneously hypertensive rats (SHRs). Stability against gastrointestinal enzymes suggested that the sequence LRP could contribute to the in vivo effects of parental peptides. Finally, there were reductions in circulating ACE activity and angiotensin II level in SHRs after either DPYKLRP or LRP intake, thus confirming ACE inhibition as the in vivo mechanism for their antihypertensive effect.
已鉴定出从牛乳铁蛋白（LF）中释放的新型枯草芽孢杆菌降压肽。使用离子阱质谱仪，通过半制备高效液相色谱法对枯草芽孢杆菌 LF 透液进行分级，并鉴定出血管紧张素转化酶（ACE）抑制肽中存在的 35 种肽。基于肽丰度和常见结构特征，化学合成了六种肽。其中四个（DPYKLRP、PYKLRP、YKLRP 和 GILRP）在体外对 ACE 活性具有抑制作用，并且在口服给予自发性高血压大鼠（SHR）后有效地降低了收缩压。对胃肠道酶的稳定性表明，LRP 序列可能有助于母体肽的体内作用。最后，无论是 DPYKLRP 还是 LRP 摄入后，SHR 中的循环 ACE 活性和血管紧张素 II 水平均降低，从而证实 ACE 抑制是其降压作用的体内机制。
