scholarly journals Evaluation of Anti-glycation Activities of Phlorotannins in Human and Bovine Serum Albumin-methylglyoxal Models

2017 ◽  
Vol 12 (11) ◽  
pp. 1934578X1701201 ◽  
Author(s):  
Shingo Sugiura ◽  
Yuya Minami ◽  
Ryosuke Taniguchi ◽  
Reiji Tanaka ◽  
Hideo Miyake ◽  
...  

In this study, the anti-glycation activities of phlorotannins contained in the Japanese Lessoniaceae ( Ecklonia cava, Eck. kurome, Eck. stolonifera, Eisenia arborea, and Eis. bicyclis) were tested using serum albumin-methlglyoxal (MGO) models. In the human serum albumin (HSA)-MGO model and the bovine serum albumin (BSA)-MGO model, the concentrations of crude phlorotannins at 50% inhibition (IC50) of fluorescent advanced glycation end products (AGEs) formation was in the range of 0.45 to 0.53 mg/mL and 0.43 to 0.53 mg/mL, respectively. Among the purified phlorotannins, phlorofucofuroeckol A with the benzobisbenzofuran skeleton had the highest inhibitory activities (IC50: 4.8 × 102 μM in HSA-MGO model and 4.1 × 102 μM in BSA-MGO model) against fluorescent AGEs formation, and showed about 13 times the inhibition in the HSA-MGO model, and about 20 times the inhibition in the BSA-MGO model, with respect to aminoguanidine hydrochloride, which was used as a positive control. In the test on MGO-scavenging activity using HPLC analysis, it showed that eckol and its simple dimers (dieckol and 8,8′-bieckol) had higher scavenging rate than aminoguanidine hydrochloride. In addition, it was revealed by liquid chromatography-electrospray ionization-mass spectrometry that eckol reacted with MGO and formed two adducts with it. These results strongly suggest that phlorotannins are novel and effective anti-glycation substances derived from natural plants.

2018 ◽  
Vol 13 (8) ◽  
pp. 1934578X1801300
Author(s):  
Shingo Sugiura ◽  
Ryosuke Taniguchi ◽  
Yoshihiko Nishioka ◽  
Ryota Iwase ◽  
Reiji Tanaka ◽  
...  

The anti-glycation activities of phlorotannins contained in the Japanese Lessoniaceae ( Ecklonia cava, Eck. kurome, Eck. stolonifera, Eisenia arborea, and Eis. bicyclis) were tested using serum albumin-glyceraldehyde (GA) models. In the human serum albumin (HSA)-GA model and the bovine serum albumin (BSA)-GA model, the concentrations of crude phlorotannins at 50% inhibition (IC50) of fluorescent advanced glycation end products (AGEs) formation was in the range of 0.48 to 0.70 mg/mL and 0.52 to 0.75 mg/mL, respectively. In tests using phloroglucinol and purified phlorotannins (eckol, fucofuroeckol A, phlorofucofuroeckol A, dieckol, and 8,8'-bieckol), dieckol had the highest inhibitory activity (IC50: 5.5 × 102 μM) against fluorescent AGEs formation in HSA-GA model and showed about 18 times inhibition compared with aminoguanidine hydrochloride of positive control. In the BSA albumin model, 8,8'-bieckol had about 27 times AGEs formation inhibitory activity (IC50: 6.2 × 102 μM) against aminoguanidine hydrochloride. In tests on GA scavenging activity, it was shown that compounds with phloroglucinol tetramer or higher had a scavenging rate of 70%, or more, with a reaction time of 120 minutes. These results suggest that among the phlorotannins, in particular the dimers of eckol (dieckol and 8,8'-bieckol), there are effective compounds for inhibiting the formation of AGEs derived from GA.


2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Jing Liu ◽  
Liping Yan ◽  
Ruilan Niu ◽  
Limin Tian ◽  
Qi Zhang ◽  
...  

Endomorphins (EMs) have a very important bridge-function in cardiovascular, endocrinological, and neurological systems. This study is to investigate the effects of EMs on the synthesis and secretion of vasoactive substances induced by advanced glycation end products in primary cultured human umbilical vein endothelial cells (HUVECs). Firstly, HUVECs were stimulated with AGEs-bovine serum albumin (AGEs-BSA), bovine serum albumin (BSA), or both AGEs-BSA and EMs together, respectively. Then, HUVEC survival rate was calculated by MTT assay, the levels of NO, endothelial nitric oxide synthase (eNOS), and inducible nitric oxide synthase (iNOS) were detected by colorimetric analysis, and the contents of endothelin-1 (ET-1) were detected by ELISA. The mRNA levels of eNOS and ET-1 were measured by RT-PCR. The expression of p38 mitogen-activated protein kinase (p38 MAPK) was detected by immunofluorescence assay. The results showed that the mRNA expression and secretion of eNOS were significantly enhanced after incubation with EMs compared to those with AGEs-BSA, while the secretion of NO and iNOS, mRNA expression, and secretion of ET-1 had opposite changes. The fluorescence intensity of p38MAPK in nuclear was decreased after pretreatment with EMs compared to incubation with AGEs-BSA.Conclusion. The present study suggests that EMs have certain protection effect on AGEs-BSA-induced injury in HUVEC.


2019 ◽  
Vol 3 (Supplement_1) ◽  
Author(s):  
Christian Konopka ◽  
Annaliese Paton ◽  
Aleksandra Skokowska ◽  
Joe Rowles ◽  
John Erdman ◽  
...  

Abstract Objectives The Receptor for Advanced Glycation End Products (RAGE) and its ligands have been shown to be both over expressed and critical to prostate cancer (PCa) development. Importantly, the overexpression of both RAGE and its ligands is associated with poor PCa patient survival, suggesting its promise as a molecular target. Additionally, one of the largest sources of ligands for RAGE, advanced glycation end products (AGEs), come from one's diet and their concentrations are directly related to disease. We hypothesized that dietary AGEs (dAGEs) significantly contribute to the progression of PCa through interactions with RAGE. In this study we explore the use of a novel imaging strategy targeted at RAGE in combination with conventional imaging and histological techniques to assess the role of dAGEs on RAGE expression and PCa progression in murine xenografts. Methods To examine the impact of AGEs on PCa cell function, experiments were performed in two PCa cell lines. Cells were grown in growth media enriched with carboxymethyl-lysine-modified human serum albumin (CML) (the most common AGE) or a control protein, bovine serum albumin (BSA). Western blot, confocal microscopy, clonogenic assays, and proliferations assays were performed. To study the effects of an enhanced consumption of dAGEs on PCa growth and progression in vivo, NU/J mice were fed a modified Ain-93 G diet, which was either CML or BSA enriched. PCa tumors were then initiated. Their growth was monitored, their perfusion measured using Speckle Contrast Imaging, and their metabolic rate and RAGE content quantified using 18FDG and a novel RAGE-targeted tracer using PET-CT. Finally, the tissues were excised for histological analysis. Results CML significantly enhanced in vitro expression of both RAGE and proliferation marker KI-67. Cell doubling time was also significantly quickened, (1.5 vs 2.4 days) in the CML vs control. In vivo data demonstrated significant differences in tumor growth (CML group up to 2-fold increase) and successful tumor implantation rate (30% vs 60%). Perfusion, metabolism, and RAGE imaging demonstrated unique patterns which varied over the course of PCa progression. Conclusions These studies indicate that dAGEs may play a significant role in the progression of PCa. The data suggests that RAGE and its ligands are promising targets for further therapeutic investigations. Funding Sources University of Illinois at Chicago Cancer Center Pilot Grant. Supporting Tables, Images and/or Graphs


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