Peptides from Harpadon nehereus Bone Ameliorate Angiotensin II-Induced HUVEC Injury and Dysfunction through Activation of the AKT/eNOS and Nrf2 Pathway

Article

作者: Shen, Kai ; Shao, Manfen ; Zhao, Wei ; Jin, Huoxi

Angiotensin II (Ang II)-induced vascular endothelial cell injury and dysfunction are important pathophysiological factors in the occurrence and development of hypertension. In this study, the amelioration effects of two peptides KA-8 (KLHDEEVA) and PG-7 (PSRILYG) from Harpadon nehereus bone on Ang II-induced damage and dysfunction in human umbilical vein endothelial cells (HUVECs) were investigated. The results showed that they could significantly decrease the reactive oxygen species (ROS) level and increase the activity of antioxidant enzymes in Ang II-induced HUVEC. Two peptides, especially PG-7, significantly upregulated the expression of nuclear factor erythroid 2-related factor 2 (Nrf2). In addition, PG-7 significantly reduced the level of expression of endothelin-1(ET-1) and increased the phosphorylation level of phosphoinositide 3-kinase (PI3K), serine/threonine kinase (AKT), and nitric oxide synthase (eNOS). These results indicated that the two peptides, especially PG-7, can ameliorate angiotensin II-induced HUVEC injury and dysfunction through activation of the AKT/eNOS and Nrf2 pathway. Furthermore, PG-7 showed a stronger affinity with angiotensin-converting enzyme (ACE) and ACE inhibitory than KA-8. In conclusion, peptide PG-7 reveals potential in the prevention and treatment of hypertension.

2014-02-01·European Journal of Medicinal Chemistry1区 · 医学

Design, structural and biological characterization of a VEGF inhibitor β-hairpin-constrained peptide

1区 · 医学

Article

作者: Basile, Anna ; D'Andrea, Luca Domenico ; De Rosa, Lucia ; Fattorusso, Roberto ; Turco, Maria Caterina ; Isernia, Carla ; Russomanno, Anna ; Diana, Donatella

The design, structural and biological characterization of a novel VEGF inhibitor peptide is described. The peptide was designed on the β5-β6 hairpin region of Placenta Growth Factor. NMR studies showed that the peptide assumes in solution a β-hairpin conformation similarly to the corresponding region of the natural ligand. In vitro experiments on endothelial cells demonstrated that the peptide is able to inhibit VEGF biological activity. This molecule represents a novel molecular entity to modulate VEGF activity and with potential application in therapy and diagnosis of angiogenesis-dependent diseases.

2008-07-01·Journal of Dairy Science1区 · 农林科学

Short Communication: Pregnancy Rates to Timed Artificial Insemination in Holstein Heifers Given Prostaglandin F2α Twenty-Four Hours Before or Concurrent with Removal of an Intravaginal Progesterone-Releasing Insert

1区 · 农林科学

Article

作者: Emmanuel, D. G. V. ; Ambrose, D. J. ; Kastelic, J. P. ; Colazo, M. G.

The objective was to compare pregnancy rates in nulliparous Holstein heifers given PGF(2alpha) 24 h before, or concurrent with, removal of an intravaginal progesterone-releasing (CIDR) insert in 3 timed artificial insemination (TAI) protocols. Heifers (from 2 herds) were assigned randomly, over 11 mo, to 1 of 3 modified Ovsynch protocols. On d 0 (without reference to the stage of the estrous cycle), all heifers were given 100 microg of GnRH i.m. and a CIDR insert (containing 1.9 g of progesterone). In the PG-7/P4-8 protocol (n = 99), PGF(2alpha) was given on d 7, and CIDR inserts were removed on d 8. In the PG-7/P4-7 (n = 98) and PG-8/P4-8 (n = 102) protocols, PGF(2alpha) administration and CIDR removal occurred concurrently, on d 7 or 8, respectively. In all 3 protocols, a second GnRH treatment (100 microg) was given 48 h after PGF(2alpha) with TAI 16 to 20 h later. Blood samples were collected (subset of 124 heifers) on d 0, 7, 10 or 11 (i.e., at TAI), and 17. Pregnancy rates (32 d after TAI) for protocols PG-7/P4-8, PG-7/P4-7, and PG-8/P4-8 were 61.8, 55.6, and 54.1%, respectively. Pregnancy rate was higher when synchronization was initiated during diestrus than when initiated at other stages (57.0 versus 34.8%). Although pregnancy rates were not affected by season, there was an interaction between protocol and season; pregnancy rates were significantly lower in summer in heifers subjected to PG-7/P4-7 and PG-8/P4-8, but season did not affect pregnancy rates in heifers subjected to PG-7/P4-8. In summary, giving PGF(2alpha) 24 h before CIDR removal, followed by TAI (PG-7/P4-8 protocol), resulted in consistent pregnancy rates, regardless of season, relative to protocols involving PGF(2alpha) treatment concurrent with CIDR removal.

100 项与 PG-007 相关的药物交易

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