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DPP-IV抑制肽
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2021 · IF 5.279

Characterization of DPP-IV Inhibitory Peptides Using an In Vitro Cell Culture Model of the Intestine

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 · 药理学
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Journal of Functional Foods · 2023 · IF 5.6

The bioactive peptide VLATSGPG regulates the abnormal lipid accumulation and inflammation induced by free fatty acids in HepG2 cells via the PERK signaling pathway

Ritian Jin,Jude Juventus Aweya,Rong Lin,Wuyin Weng,Jiaqi Shang,Dangfeng Wang,Yiling Fan,Shen Yang

VLATSGPG (VLA) was a DPP-IV inhibitory peptide isolated from salmon ( Salmo Salar ) skin. Here, we demonstrated that VLA inhibited the activation of PERK through the AKT signaling pathway. Furthermore, we investigated the effect of VLA on free fatty acid (FFA)-induced lipid accumulation disorder and inflammation in HepG2 cells, elucidating the potential regulatory mechanism in this nonalcoholic fatty liver disease cell model. VLA reduced the mRNA expression of adipogenic factors FAS, ACC, and SCD-1 through the PERK/eIF2α pathway and the level of apolipoprotein B-100 secretion. These may contribute to the reducing FFA-induced lipid accumulation in cells and reducing intracellular lipid levels. In addition, VLA increased IκBα mRNA expression via the PERK/IκBα pathway, inhibited the NF-κB p65 activation, and thus inhibited cell inflammation.

CAS / MDL: 64-17-5 67-63-0
研究领域: 分子生物学 · 细胞生物学 · 药理学 · 生物化学
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JOURNAL OF FOOD SCIENCE · 2024 · IF 3.2

Exploring dipeptidyl peptidase-IV inhibitory peptides from Tartary Buckwheat protein: A study of hydrolysis, fractionation, and molecular interactions

Weijing Wu,Libo Wang,Ju Qiu,Ziyuan Zhuang,Fei Qin,Qianglai Tan,Yanling Wang,Lanlan Wu

Tartary buckwheat, a protein-rich pseudocereal with anti-diabetic effects, has not yet been fully explored as a source of dipeptidyl peptidase-IV (DPP-IV) inhibitory peptides. This study aims to discover novel DPP-IV inhibitory peptides from tartary buckwheat protein (TBP). Five hydrolysis methods were employed, with simulated gastrointestinal digestion (SGID) releasing the most active DPP-IV inhibitory hydrolysates, showing both the highest degree of hydrolysis (22.66 ± 1.12%) and inhibition activity (41.81 ± 1.52% at 1.25 mg/mL). In addition, ultrafiltration enriched the <3 kDa fraction with the highest inhibitory rate, and further purification using reverse-phase high-performance liquid chromatography concentrated the DPP-IV inhibitory peptides in the first fraction (F1). Nano liquid chromatography-tandem mass spectrometry analysis identified 10 new peptides in F1, among which the peptide Leu-His-Ile-Val-Gly-Pro-Asp-Lys (LHIVGPDK) exhibited the strongest inhibitory effect, with an IC 50 value of 1.61 mM. Kinetic studies revealed that LHIVGPDK acts as a mixed-type inhibitor, and molecular docking indicated that it inhibits DPP-IV by forming stable complexes through five types of interactions, with hydrogen bonds playing a key role. This study underscores TBP's DPP-IV inhibitory potential and anti-diabetic properties, reinforcing the value of tartary buckwheat as a beneficial food for diabetes management. Practical Application This research identified new peptides from Tartary buckwheat protein that effectively inhibit DPP-IV, an enzyme associated with diabetes management. These findings suggest potential applications in developing functional foods to help control hypoglycemia.

研究领域: 食品科学 · 营养学 · 生物化学 · 药理学 · 糖尿病管理
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