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. 2017 Jan 13;22(1):123.
doi: 10.3390/molecules22010123.

A Novel Antihypertensive Derived from Adlay (Coix larchryma-jobi L. var. ma-yuen Stapf) Glutelin

Bin Li  1 , Liansheng Qiao  2 , Lingling Li  3 , Yanling Zhang  4 , Kai Li  5 , Lingzhi Wang  6 , Yanjiang Qiao  7
Affiliations

A Novel Antihypertensive Derived from Adlay (Coix larchryma-jobi L. var. ma-yuen Stapf) Glutelin

Bin Li et al. Molecules. .

Erratum in

Abstract

Our previous studies have shown that Coix glutelin pepsin hydrolysate can effectively inhibit angiotensin converting enzyme (ACE) activity in vitro. The main purpose of this study was to obtain potent anti-hypertensive peptides from Coix glutelin. The Coix glutelin hydrolysates (CGH) were prepared by pepsin catalysis and further separated by an ultrafitration (UF) system, gel filtration chromatography (GFC) and reversed-phase high performance liquid chromatography (RP-HPLC). As a result, the sub-fraction F5-3 had the highest ACE-inhibitory activity. Six ACE inhibitory peptides were identifiedusing nano-liquid chromatography coupled to tandem mass spectrometry. The most potent peptide GAAGGAF (IC50 = 14.19 μmol·L-1) was finally obtained by further molecular simulation screening and a series of division and optimization. Single oral administration of synthesized GAAGGAF at 15 mg/kg body weight (BW) in spontaneously hypertensively rats (SHR) could reduce the systolic blood pressure (SBP) around 27.50 mmHg and blood pressure-lowering effect lasted for at least 8 h. The study demonstrated for the first time that the ACE inhibitory peptide GAAGGAF from Coix glutelin has a significant antihypertensive effect, and it could be a good natural ingredient for pharmaceuticals against hypertension and the related diseases.

Keywords: Coix larchryma-jobi L. var. ma-yuen Stapf; angiotensin I-converting enzyme; antihypertensive peptide; glutelin; molecular simulation.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Gel filtration chromatography of the ultrafiltrate obtained under 0.1 Mpa pressure.
Figure 2
Figure 2
Purification profile of the fraction F5 by the reversed phase high performance liquid chromatography (RP-HPLC).
Figure 3
Figure 3
Representation of the angiotensin converting enzyme (ACE) pharmacophore model and molecular interactions between PDB 1O86 and the ligands. Purple sphere indicated hydrogen bond donor, green sphere indicated hydrogen bond acceptor, light blue sphere indicated hydrophobic aromatic features, and dark blue sphere indicated negative ionizable. (A) The best pharmacophore model of ACE; (B) The ACE pharmacophore model mapped with GAAGGAF; Molecular interactions between PDB 1O86 and the ligands: (C) Molecular interaction between 1O86 and lisinopril; and (D) Molecular interaction between 1O86 and GAAGGAF.
Figure 4
Figure 4
Change of systolic blood pressure (SBP) after oral administration of GAAGGAF in spontaneously hypertensive rats (SHR). Each point on the figure represented mean SBP of six animals and the vertical bars indicated the standard errors. Significant different from control group: * p < 0.05.
See this image and copyright information in PMC

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