title: A Novel Antihypertensive Derived from Adlay (Coix larchryma-jobi L. var. ma-yuen Stapf) Glutelin.
abstract: Our previous studies have shown thatCoixglutelin 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 fromCoixglutelin. TheCoixglutelin 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 fromCoixglutelin has a significant antihypertensive effect, and it could be a good natural ingredient for pharmaceuticals against hypertension and the related diseases.
authors.affiliation: Beijing University of Chinese Medicine, 6 South Zhonghuan Road, Wangjing, Chaoyang District, Beijing 100102, China. libinzyy@163.com.
authors.forename: Bin
authors.initials: B
authors.lastname: Li
authors.affiliation: Beijing University of Chinese Medicine, 6 South Zhonghuan Road, Wangjing, Chaoyang District, Beijing 100102, China. b20100222012@163.com.
authors.forename: Liansheng
authors.initials: L
authors.lastname: Qiao
authors.affiliation: Beijing University of Chinese Medicine, 6 South Zhonghuan Road, Wangjing, Chaoyang District, Beijing 100102, China. lilingling@126.com.
authors.forename: Lingling
authors.initials: L
authors.lastname: Li
authors.affiliation: Beijing University of Chinese Medicine, 6 South Zhonghuan Road, Wangjing, Chaoyang District, Beijing 100102, China. collean_zhang@163.com.
authors.forename: Yanling
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Beijing University of Chinese Medicine, 6 South Zhonghuan Road, Wangjing, Chaoyang District, Beijing 100102, China. lk20162016@163.com.
authors.forename: Kai
authors.initials: K
authors.lastname: Li
authors.affiliation: Beijing University of Chinese Medicine, 6 South Zhonghuan Road, Wangjing, Chaoyang District, Beijing 100102, China. wanglz@bucm.edu.cn.
authors.forename: Lingzhi
authors.initials: L
authors.lastname: Wang
authors.affiliation: Beijing University of Chinese Medicine, 6 South Zhonghuan Road, Wangjing, Chaoyang District, Beijing 100102, China. yjqiao@263.net.
authors.forename: Yanjiang
authors.initials: Y
authors.lastname: Qiao
mesh_terms: D000595:Amino Acid Sequence; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000959:Antihypertensive Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D031742:Coix / Q000737:chemistry*; D015870:Gene Expression; D005983:Glutens / Q000737:chemistry*; D006868:Hydrolysis; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D008297:Male; D062105:Molecular Docking Simulation; D056004:Molecular Dynamics Simulation; D010434:Pepsin A / Q000737:chemistry; D010455:Peptides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007703:Peptidyl-Dipeptidase A / Q000378:metabolism*; D010936:Plant Extracts / Q000737:chemistry; D051381:Rats; D011918:Rats, Inbred SHR; D012639:Seeds / Q000737:chemistry; D014462:Ultrafiltration
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D010455:Peptides; D010936:Plant Extracts; D005983:Glutens; C488034:ACE protein, human; D007703:Peptidyl-Dipeptidase A; D010434:Pepsin A
keywords: Coix larchryma-jobi L. var. ma-yuen Stapf; angiotensin I-converting enzyme; antihypertensive peptide; glutelin; molecular simulation