Xanthine oxidase inhibitory peptides derived from tuna protein: virtual screening, inhibitory activity, and molecular mechanisms

2020 ◽  
Author(s):  
Zhipeng Yu ◽  
Ruotong Kan ◽  
Sijia Wu ◽  
Hui Guo ◽  
Wenzhu Zhao ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Molecular Mechanisms ◽  
Inhibitory Peptides

scholarly journals Purification and Identification of Novel Xanthine Oxidase Inhibitory Peptides Derived from Round Scad (Decapterus maruadsi) Protein Hydrolysates

Marine Drugs ◽  
2021 ◽  
Vol 19 (10) ◽  
pp. 538
Author(s):  
Xiao Hu ◽  
Ya Zhou ◽  
Shaobo Zhou ◽  
Shengjun Chen ◽  
Yanyan Wu ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
High Performance ◽  
Amino Acid Sequences ◽  
Inhibitory Effects ◽  
Small Peptides ◽  
Inhibitory Peptides ◽  
Metal Affinity ◽  
Fluorescence Quenching Mechanism ◽  
Decapterus Maruadsi

The objective of the present study was to investigate the xanthine oxidase (XO) inhibitory effects of peptides purified and identified from round scad (Decapterus maruadsi) hydrolysates (RSHs). In this study, RSHs were obtained by using three proteases (neutrase, protamex and alcalase). Among them, the RSHs of 6-h hydrolysis by neutrase displayed the strongest XO inhibitory activity and had an abundance of small peptides (<500 Da). Four novel peptides were purified by immobilized metal affinity chromatography and identified by nano-high-performance liquid chromatography mass/mass spectrometry. Their amino acid sequences were KGFP (447.53 Da), FPSV (448.51 Da), FPFP (506.59 Da) and WPDGR (629.66 Da), respectively. Then the peptides were synthesized to evaluate their XO inhibitory activity. The results indicated that the peptides of both FPSV (5 mM) and FPFP (5 mM) exhibited higher XO inhibitory activity (22.61 ± 1.81% and 20.09 ± 2.41% respectively). Fluorescence spectra assay demonstrated that the fluorescence quenching mechanism of XO by these inhibitors (FPSV and FPFP) was a static quenching procedure. The study of inhibition kinetics suggested that the inhibition of both FPSV and FPFP was reversible, and the type of their inhibition was a mixed one. Molecular docking revealed the importance of π-π stacking between Phe residue (contained in peptides) and Phe914 (contained in the XO) in the XO inhibitory activity of the peptides.

Screening of Hungarian mushrooms for xanthine-oxidase inhibitory activity

Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
A Ványolós ◽  
O Orbán-Gyapai ◽  
T Támadi ◽  
J Hohmann
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity

Polyphenols from Cyclopia genistoides and their xanthine oxidase inhibitory activity

Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
O Roza ◽  
A Martins ◽  
J Hohmann ◽  
WC Lai ◽  
FR Chang ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity

scholarly journals Evaluation of Enzyme Inhibitory Activity of Flavonoids by Polydopamine-Modified Hollow Fiber-Immobilized Xanthine Oxidase

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3931
Author(s):  
Cong-Peng Zhao ◽  
Guo-Ying Chen ◽  
Yuan Wang ◽  
Hua Chen ◽  
Jia-Wen Yu ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Hollow Fiber ◽  
Inhibitory Activity ◽  
Ph Value ◽  
Enzymatic Reaction ◽  
Amino Acid Residues ◽  
Reaction Conditions ◽  
Docking Analysis ◽  
Dopamine Concentration ◽  
Immobilization Time

In this study, a polydopamine (PDA)-modified hollow fiber-immobilized xanthine oxidase (XOD) was prepared for screening potential XOD inhibitors from flavonoids. Several parameters for the preparation of PDA-modified hollow fiber-immobilized XOD, including the dopamine concentration, modification time, XOD concentration and immobilization time, were optimized. The results show that the optimal conditions for immobilized XOD activity were a dopamine concentration of 2.0 mg/mL in 10.0 mM Tris-HCl buffer (pH 8.5), a modification time of 3.0 h, an XOD concentration of 1000 μg/mL in 10.0 mM phosphate buffer (pH 7.5) and an immobilization time of 3.0 h. Subsequently, the enzymatic reaction conditions such as the pH value and temperature were investigated, and the enzyme kinetics and inhibition parameters were determined. The results indicate that the optimal pH value (7.5) and temperature (37 °C) of the PDA-modified hollow fiber-immobilized XOD were consistent with the free enzyme. Moreover, the PDA-modified hollow fiber-immobilized XOD could still maintain above 50% of its initial immobilized enzyme activity after seven consecutive cycles. The Michaelis–Menten constant (Km) and the half-maximal inhibitory concentration (IC50) of allopurinol on the immobilized XOD were determined as 0.25 mM and 23.2 μM, respectively. Furthermore, the PDA-modified hollow fiber-immobilized XOD was successfully applied to evaluate the inhibitory activity of eight flavonoids. Quercetin, apigenin, puerarin and epigallocatechin showed a good inhibition effect, and their percentages of inhibition were (79.86 ± 3.50)%, (80.98 ± 0.64)%, (61.15 ± 6.26)% and (54.92 ± 0.41)%, respectively. Finally, molecular docking analysis further verified that these four active compounds could bind to the amino acid residues in the XOD active site. In summary, the PDA-modified hollow fiber-immobilized XOD is an efficient method for the primary screening of XOD inhibitors from natural products.

scholarly journals Discovery of a Bradykinin B2 Partial Agonist Profile of Raloxifene in a Drug Repurposing Campaign

2020 ◽  
Vol 22 (1) ◽  
pp. 257
Author(s):  
Patricia Gomez-Gutierrez ◽  
Juan J. Perez
Keyword(s):  
Virtual Screening ◽  
Molecular Mechanisms ◽  
Partial Agonist ◽  
Drug Repurposing ◽  
Cytokine Storm ◽  
Bradykinin Receptors ◽  
Screening Process ◽  
Bradykinin Antagonists ◽  
Illness Progression

Covid-19 urges a deeper understanding of the underlying molecular mechanisms involved in illness progression to provide a prompt therapeutical response with an adequate use of available drugs, including drug repurposing. Recently, it was suggested that a dysregulated bradykinin signaling can trigger the cytokine storm observed in patients with severe Covid-19. In the scope of a drug repurposing campaign undertaken to identify bradykinin antagonists, raloxifene was identified as prospective compound in a virtual screening process. The pharmacodynamics profile of raloxifene towards bradykinin receptors is reported in the present work, showing a weak selective partial agonist profile at the B2 receptor. In view of this new profile, its possible use as a therapeutical agent for the treatment of severe Covid-19 is discussed.

scholarly journals Antioxidant activity, xanthine oxidase inhibitory activity, and compounds determination of Cipadessa baccifera leaf extract

2021 ◽  
Author(s):  
Syarifah Ramadhani Lubis ◽  
Subandi Subandi ◽  
Muntholib Muntholib ◽  
Jamilah Abbas ◽  
Tjandrawati Mozef
Keyword(s):  
Antioxidant Activity ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Leaf Extract

Inhibitory Activity of Asana, Heartwood of Pterocarpus marsupium, Against Xanthine Oxidase

2019 ◽  
Vol 14 (12) ◽  
pp. 1934578X1988789
Author(s):  
Takahiro Deguchi ◽  
Yusuke Hata ◽  
Atsushi Tamai ◽  
Moe Yamamoto ◽  
Takanori Fujita ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Soluble Fraction ◽  
Ethanolic Extract ◽  
Modern Medicine ◽  
Noncommunicable Disease ◽  
Promising Candidate ◽  
Pterocarpus Marsupium ◽  
Novel Agent

The heartwood of Pterocarpus marsupium is called as “Asana” in Ayurveda. Its aquatic infusion was used for treating “prameha,” which indicates a polyuria disease in modern medicine. In our research program to investigate a novel agent to improve hyperuricemia, we focused on the extract of Asana as a xanthine oxidase (XOD) inhibitor. Asana extract (50% ethanolic extract, PM-ext) showed 11%, 35%, and 38% inhibition at 50, 200, and 500 µg/mL, respectively. Subsequently, PM-ext was partitioned with ethyl acetate (AcOEt), butanol, and water. Among them, AcOEt-soluble fraction indicated the most potent XOD inhibitory activity and was consecutively fractionated using various liquid chromatography to obtain liquiritigenin (1), isoliquiritigenin (2), and marsupsin (3) as active principles. Compound 1 showed 16% inhibition at 200 µM while 2 showed 20%, 32%, and 46% inhibition at 50, 100, and 200 µM, respectively. Compound 3 showed 15% inhibition at 500 µM. This is the first report on the XOD inhibitory activity of 3. From these results, PM-ext is a promising candidate material for improvement of hyperuricemia. Here, Asana was recognized as an effective material against noncommunicable disease and is expected to be developed as a functional ingredient.

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