Biomolecules
·
2024
·Vol. 14
·期 5
·581
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IF 4.8
Jiaming Cao,Boyuan Xiang,Baojie Dou,Jingfei Hu,Lei Zhang,Xinxin Kang,Mingsheng Lyu,Shujun Wang
Peptides possessing antihypertensive attributes via inhibiting the angiotensin-converting enzyme (ACE) were derived through the enzymatic degradation ofTrichiurus lepturus(ribbonfish) using alkaline protease. The resulting mixture underwent filtration using centrifugation, ultrafiltration tubes, and Sephadex G-25 gels. Peptides exhibiting ACE-inhibitory properties and DPPH free-radical-scavenging abilities were isolated and subsequently purified via LC/MS-MS, leading to the identification of over 100 peptide components. In silico screening yielded five ACE inhibitory peptides: FAGDDAPR, QGPIGPR, IFPRNPP, AGFAGDDAPR, and GPTGPAGPR. Among these, IFPRNPP and AGFAGDDAPR were found to be allergenic, while FAGDDAPRR, QGPIGPR, and GPTGPAGP showed good ACE-inhibitory effects. IC50values for the latter peptides were obtained from HUVEC cells: FAGDDAPRR (IC50= 262.98 μM), QGPIGPR (IC50= 81.09 μM), and GPTGPAGP (IC50= 168.11 μM). Peptide constituents derived from ribbonfish proteins effectively modulated ACE activity, thus underscoring their therapeutic potential. Molecular docking and modeling corroborated these findings, emphasizing the utility of functional foods as a promising avenue for the treatment and prevention of hypertension, with potential ancillary health benefits and applications as substitutes for synthetic drugs.
研究领域:
食品科学
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生物化学
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药理学
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DOI
PubMed
高影响因子
Food & Function
·
2018
·Vol. 9
·期 4
·2270-2281
·
IF 3.289
Han Wu,Xin Rui,Wei Li,Yu Xiao,Jianzhong Zhou,Mingsheng Dong
This study explored a novel strategy to develop solid-state whole-grain oats as a novel carrier of lactic acid bacteria and a nutraceutical supplement rich in ACE inhibitory peptides. Oats were fermented by Lactobacillus plantarum B1-6, Rhizopus oryzae, or a combination of L. plantarum B1-6 and R. oryzae. L. plantarum showed a much better growth performance in oats when it was combined with R. oryzae than when it was cultured alone, as evidenced by an increase in viable cell count to 9.70 log cfu g−1 after 72 h of fermentation. The coinoculated fermented oats (CFO) and the R. oryzae-fermented oats (RFO) were then selected for investigations on protein hydrolysis and on the functional properties of the released bioactive peptides. The results showed that the soluble protein contents changed from 7.05 mg g−1 to 14.43 and 10.21 mg g−1 for CFO and RFO, respectively. However, the degree of hydrolysis and the content of peptides with molecular masses less than 10 000 Da indicated that the CFO proteins can be degraded to a greater degree. As analyzed by electrophoresis and reversed-phase high-performance liquid chromatography, the protein and peptide profiles of CFO and RFO demonstrated that the proteins from CFO were more obviously hydrolyzed and more small peptides were obtained. In addition, both CFO and RFO presented higher ACE inhibitory activities than unfermented oats, whereas the protein extracts from CFO exerted a lower IC50 value of 0.42 mg protein per mL compared with the protein extracts from the other samples. This research has broadened our knowledge on the development of whole-grain oat products as a probiotic carrier and on the difference between mixed solid-state fermentation (SSF) and fungi SSF in terms of protein degradation and the capacity to release ACE inhibitory peptides. Our approach could be used to obtain probiotic food products and probably to develop oats as a potential therapeutic ingredient targeting hypertension.
研究领域:
食品科学
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微生物学
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营养学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2021
·
IF 5.279
Ritian Jin,Jiaqi Shang,Xiangyu Teng,Ligang Zhang,Minhe Liao,Jiaxin Kang,Ran Meng,Dangfeng Wang,Haowei Ren,Ning Liu
Here, we characterize the activities of two depeptidyl peptidase-IV (DPP-IV) inhibitory peptides, VLATSGPG and LDKVFER, using the Caco-2 monolayer model for the intestine. VLATSGPG and LDKVFR inhibited the DPP-IV in the cells via a mixed-type inhibition mode, with in situ IC50 values of 207.3 and 148.5 μM, respectively. Furthermore, VLATSGPG and LDKVFR were transported intact across the cells, with Papp values of 2.41 ± 0.16 and 4.23 ± 0.29 × 10–7 cm/s, respectively. Fragmented peptides were identified in the basolateral side of the membrane. Two of these, GPG and VLA, exhibited high inhibitory activities of 83.6 ± 3.3 and 58.5 ± 2.5%, respectively, at 100 μM concentration. Although 3 mM VLATSGPG and LDKVFR were transported across the epithelium in a concentration-dependent manner, their transport did not damage the tight junction proteins, ZO-1 and occludin. This study demonstrates that the two peptides potentially regulate DPP-IV activity in the intestine.
研究领域:
生物化学
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药理学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2017
·
IF 3.154
Long Liu,Yanan Wei,Qing Chang,Huaju Sun,Kungang Chai,Zuqiang Huang,Zhenxia Zhao,Zhongxing Zhao
A novel, moderately hydrophilic peptide (RYL) with high ACE-inhibitory activity was screened ultrafast via a concept of waste conversion using waste. This novel peptide was screened from silkworm pupa using an Fe-doped porous biocarbon (FL/Z-SE) derived from silkworm excrement. FL/Z-SE possessed magnetic properties and specific selection for peptides due to Fe’s dual functions. The selected RYL, which has moderate hydrophilicity (LogP = −0.22), exhibited a comparatively high ACE-inhibitory activity (IC50 = 3.31 ± 0.11 μM). The inhibitory kinetics and docking-simulation results show that, as a competitive ACE inhibitor, RYL formed five hydrogen bonds with the ACE residues in the S1 and S2 pockets. In this work, both the screening carbon material and the selected ACE-inhibitory peptide were derived from agricultural waste (silkworm excrement and pupa), which offers a new way of thinking about the development of advanced uses of the silkworm byproducts and wastes.
研究领域:
生物技术
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环境科学
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药学
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DOI
PubMed
高影响因子
Food Bioscience
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2025
·
IF 5.9
Xianjiang Ye,Ran Yang,Zhizhi Yang,Baote Huang,Talha Riaz,Chao Zhao,Jicheng Chen
Food-derived peptides with angiotensin-I-converting enzyme inhibitory (ACEI) activity have garnered significant research attention. This study focused on examining ACEI peptides from Porphyra haitanensis and investigating their potential inhibitory mechanisms through a combination of in silico and in vitro methods. Five novel potential ACEI peptides (ASF: Ala-Ser-Phe, EIIL: Glu-Ile-Ile-Leu, LCVPR: Leu-Cys-Val-Pro-Arg, LDVVN: Leu-Asp-Val-Val-Asn, and LSPSW: Leu-Ser-Pro-Ser-Trp) were identified through a combination of peptidomics and in silico bioinformatics analysis, of which LSPSW showed the highest activity (IC 50 : 5.27 ± 0.53 μM). After simulated gastrointestinal digestion (SGD), the activities of LCVPR and LSPSW remained almost unchanged. The results from inhibition kinetics and molecular docking demonstrated that ACEI peptides with differing inhibition mechanisms could successfully bind to ACE through hydrogen bonds. Based on network pharmacology analysis and cellular experiments, LSPSW exerted antihypertensive effects by regulating the expression levels of peroxisome proliferator activated receptor gamma (PPARG), prostaglandin-endoperoxide synthase 2 (PTGS2), and renin (REN). This research provided a novel theoretical foundation for the high-value application of P. haitanensis .
研究领域:
食品科学
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生物信息学
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药理学
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DOI
高影响因子
FOOD CHEMISTRY
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2025
·
IF 9.8
Weijing Wu,Ju Qiu,Libo Wang,Qianglai Tan,Ziyuan Zhuang,Yanling Wang,Lanlan Wu
This study analyzed dipeptidyl peptidase-IV (DPP-IV) inhibitory peptides from Tartary buckwheat ( Fagopyrum tataricum ) protein hydrolysates, known for managing chronic diseases. Simulated gastrointestinal digestion enhanced the inhibitory activity of DPP-IV. Using anion-exchange resin DEAE-52, reverse high-performance liquid chromatography, and LC-MS/MS, eight novel peptides were identified. Among them, the peptides LAGQS (LA5) and LREIDDADK (LR9) exhibited the strongest inhibition in both competitive and noncompetitive modes. Molecular docking revealed electrostatic, hydrogen bond, and hydrophobic interactions for both peptides, with LR9 also engaging in π-cation interactions. Based on the Caco-2 model, the in situ DPP-IV inhibitory effect of LR9 was superior to that of LA5, likely because of LR9's greater stability during hydrolysis. Moreover, LA5 could not be transported through the Caco-2 monolayer, and LR9 demonstrated moderate transportability. These findings highlight Tartary buckwheat protein's potential for application in high-value plant-based products, including functional foods and pharmaceuticals targeting blood glucose regulation using DPP-IV inhibitory peptides.
研究领域:
食品科学
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生物化学
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DOI
PubMed
高影响因子
Nutrients
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2025
·Vol. 17
·期 10
·1693
·
IF 5
Binsong Han,Yuhui Ye,Cunzheng Zhang,Lina Zhang,Peng Zhou
Background: Camel milk is considered to be an important source of bioactive peptides with potential anti-diabetic effects. However, the mechanism by which these active peptides exert their anti-diabetic effects is not clear. The aim of this study was to systematically evaluate the in vivo anti-diabetic effects of Leucine-Leucine-Proline-Lysine (LLPK), a novel dipeptidyl peptidase-4 (DPP-4) inhibitory peptide identified from the in vitro gastrointestinal digestion product of camel milk.Methods: Adb/dbdiabetic mouse model was used, and LLPK was administered to mice at doses of 50 mg/kg BW and 100 mg/kg BW as a daily oral gavage for 30 days. The effects of LLPK on fasting blood glucose (FBG), oral glucose tolerance test (OGTT), insulin tolerance test (ITT), and serum lipid levels were monitored, and possible mechanisms of action were elucidated using proteomics.Results: The results demonstrated that LLPK significantly improved diabetic symptoms, including FBG, OGTT, ITT, and serum lipid levels indb/dbdiabetic mice. Furthermore, significantly increased levels of serum glucagon-like peptide 1 (GLP-1) and reduced serum DPP-4 activity were observed in the LLPK-treated group compared to the control group. Hepatic proteomics indicated that LLPK improved glucose and lipid metabolism via the PPAR signaling pathway, where the key targets were Scd1, Acox1, Acaa1b, Slc27a1, Acsl1, and Ehhadh.Conclusions: In summary, this study provided new insights into the anti-diabetic mechanisms of camel milk and supported the development of camel milk-based anti-diabetic functional foods or nutraceuticals.
研究领域:
营养学
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分子生物学
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代谢研究
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DOI
PubMed
高影响因子
JOURNAL OF FOOD COMPOSITION AND ANALYSIS
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2025
·
IF 4.6
Ying Sun,Dong Wei,Ziming Huang,Jinyao Song,Yiyang Zhang,Yueting Zhou,Bingbing Wang,Can Wang,Jing Wang,Hao Zhang
The inhibitory activity of different ultrafiltration fractions derived from the water-soluble extract of Zhenjiang aromatic vinegar (ZAV) on angiotensin-converting enzyme (ACE) was evaluated, and endogenous peptides with potential ACE inhibition were screened through ultrafiltration and reversed-phase high-performance liquid chromatography (RP–HPLC) coupled with ACE inhibition detection. Several novel ACE inhibitory peptides were identified using a peptidomic approach based on nanoLC-MS/MS. A total of 710 peptides were identified in the RP–HPLC fractions. Additionally, four novel peptides with potential ACE inhibitory activity were identified: FPEQPP, VVPPGHPV, FPPQQP, and YGRGPIE, with IC 50 values of 3.7 ± 0.1 μM, 3.3 ± 0.4 μM, 1.6 ± 0.2 μM, and 5.9 ± 0.2 μM, respectively. Of these novel peptides, FPPQQP was the peptide with the most potent antihypertensive activity, which acted as a strong inhibitor of ACE through molecular docking. These findings suggest that integrating peptidomics and molecular docking provides an efficient strategy for the rapid investigation of ACE inhibitory peptides in food matrices.
研究领域:
食品科学
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生物化学
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药理学
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DOI
高影响因子
ACS Applied Materials & Interfaces
·
2019
·
IF 8.456
Long Liu,Zhiwei Qiao,Xinfang Cui,Chunjiao Pang,Hong Liang,Peng Xie,Xuan Luo,Zuqiang Huang,Yanjuan Zhang,Zhongxing Zhao
Introduction of targeted defects into microporous UiO-66s for manipulating their three-dimensional size and surface properties can endow them with adsorption and separation areas involving angiotensin-converting-enzyme-inhibitory (ACE-inhibitory) peptides. Three hydrophobic amino acids (AAs) (i.e., proline (Pro), phenylalanine (Phe), and tryptophan (Trp)) having different physical/chemical properties were applied to in situ tailor defects in UiO-66 through targeted incoordination of missing linkers or missing nodes. Characterization results revealed a uniform oval shape of the developed defects with lengths ranging from 1.8 to 3.1 nm, which was also highly consistent with our molecular simulation. Among these three defective UiO-66s, Phe and Trp imprinted UiO-66s significantly promoted the adsorption affinity of small ACE-inhibitory peptides (uptake: 1.25 mmol g–1 for DDFF and 1.37 mmol g–1 for DDWW) and ultrahigh selectivity for DDFF (249) or DDWW (279) from inactive KKKK solution based on a lock-and-key mechanism. As a result, the imprinted UiO-66 showed an enrichment capacity for ACE-inhibitory peptides about eight times higher than that of pristine UiO-66. Therefore, the amino acid imprinting strategy endorsed by its facile and discerning ability can be envisioned to be of great value for small functional peptide separation and oriented enrichment in biomedicines.
研究领域:
生物化学
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材料科学
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药物开发
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DOI
PubMed
高影响因子
LWT-FOOD SCIENCE AND TECHNOLOGY
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2021
·
IF 4.952
Peng Zhang,Chang Chang,Haijie Liu,Qiaojuan Yan,Zhengqiang Jiang
Three protein-rich materials were pretreated with a self-designed alkaline electrolyzed water (AEW) pretreatment equipment to promote the release of angiotensin I-converting enzyme (ACE) inhibitory peptides by improving hydrolysis efficiency. According to degree of hydrolysis (DH) and ACE inhibitory activity, defatted walnut meal (DWM) was selected to study antihypertensive activity by hydrolysis in assistance of AEW pretreatment. It was found DWM pretreated with AEW at pH 11.5 followed by Alcalase hydrolysis exhibited the highest DH (21.96%), protein recovery rate (94.76%), and ACE inhibitory activity (IC 50 of 0.137 mg/mL), in which AEW pretreatment resulted in the transformation of α-helix and β-turn to random coil and the destruction of hydrogen bonds to expose more cleavage sites to enhance hydrolysis efficiency. Thereafter, ACE inhibitory peptides GIENYRVV (IC 50 of 0.102 mg/mL) and AGRISTVNSHTLPVL (IC 50 of 0.20 mg/mL) were identified from the hydrolysate. Overall, AEW pretreatment was an innovative strategy to promote the release of antihypertensive peptides during hydrolysis.
研究领域:
食品科学
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生物化学
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DOI
高影响因子
INTERNATIONAL DAIRY JOURNAL
·
2025
·
IF 3.4
Ruikai Zhu,Hong Zhang,Yulong Wu,Huanhuan Li,Honggang Tang,Xianrong Xu,Ke Zhao
Hypertension poses a significant threat to human health, and the efficient exploration of food-derived ACEI peptides as milder and safer alternatives to ACEI drugs has garnered increasing attention. Therefore, a combined in silico and in vitro study was performed to investigate novel ACEI peptides from goat milk proteins. First, the papain plus proteinase K was identified as the best enzymatic combination for generating ACEI peptides using BIOPEP. Then the enzymatic conditions of the papain/proteinase, the input order of the enzymes, and the molecular weight (MW) of the hydrolysate were further optimized to obtain the hydrolysate with the highest ACEI activity. Under the optimized condition described, 698 peptides (<25 AA) were successfully identified from the milk hydrolysate of goat (MW < 3 KDa). Among them, six potential novel ACEI peptides were efficiently screened virtually. Verification studies using synthesized peptides partially confirmed the in silico results, with four out of the six selected peptides (FKF, FRY, RWL, and WKP) exhibiting ACEI activity. Additionally, the blood pressure-lowering effects of the top two ACEI peptides (FRY and FKF) were further validated in spontaneously hypertensive rats (SHRs), and FRY treatment significantly lowered the blood pressure of SHRs. To summarize, this study established a rapid enzymatic hydrolysis system for screening novel ACEI peptides and identified a novel antihypertensive peptide, FRY, which provides a new method for research on bioactive peptides research and high-value utilization of goat milk.
研究领域:
食品科学
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分子生物学
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医学
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DOI
高影响因子
Foods
·
2019
·Vol. 8
·期 9
·390
·
IF 3.011
Dong Wei,Wenlai Fan,Yan Xu
Distilled spent grain (DSG), the biggest by-product of the Chinese liquor industry, is rich in protein (167.8 g/kg DSG dry weight (DW)). Accounting for 60% of the total protein, prolamins are isolated from dried DSG (DDSG). In this study, angiotensin-converting enzyme (ACE) inhibitory peptides were screened from the prolamin hydrolysates of DDSG using two independent active-directed separations, ultrafiltration and reversed phase high performance liquid chromatography (RP-HPLC) coupled with ACE inhibitory activity evaluation. Six novel ACE inhibitory peptides, AVQ, YPQ, NQL, AYLQ, VLPVLS, and VLPSLN, were successfully identified and quantified from the active RP-HPLC fractions. AVQ and YPQ exhibited the highest activity, having the concentration inducing 50% inhibition (IC50) values for ACE of 181.0 and 220.0 μM, respectively. It was observed that VLPVLS was the most abundant peptide (16.96 mg/g DW) in prolamins. The results indicated that prolamin hydrolysates from DDSG could be served as a source of ACE inhibitory peptides.Keywords:distilled spent grain (DSG);baijiu (Chinese liquor);ACE inhibitory peptides;Prolamin isolate hydrolysates;RP-HPLC;AVQ;YPQ
研究领域:
食品科学
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生物化学
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药学
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）