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 ◽  
...  
Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
A Ványolós ◽  
O Orbán-Gyapai ◽  
T Támadi ◽  
J Hohmann

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3931
Author(s):  
Cong-Peng Zhao ◽  
Guo-Ying Chen ◽  
Yuan Wang ◽  
Hua Chen ◽  
Jia-Wen Yu ◽  
...  

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.


2021 ◽  
Author(s):  
Syarifah Ramadhani Lubis ◽  
Subandi Subandi ◽  
Muntholib Muntholib ◽  
Jamilah Abbas ◽  
Tjandrawati Mozef

2019 ◽  
Vol 14 (12) ◽  
pp. 1934578X1988789
Author(s):  
Takahiro Deguchi ◽  
Yusuke Hata ◽  
Atsushi Tamai ◽  
Moe Yamamoto ◽  
Takanori Fujita ◽  
...  

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.


Molecules ◽  
2018 ◽  
Vol 23 (5) ◽  
pp. 1107 ◽  
Author(s):  
Chi-Ya Huang ◽  
Ting-Feng Yeh ◽  
Fu-Lan Hsu ◽  
Chun-Ya Lin ◽  
Shang-Tzen Chang ◽  
...  

2016 ◽  
Vol 3 ◽  
pp. 160-163
Author(s):  
Muhammad Amir Masruhim ◽  
Wisnu Cahyo Prabowo ◽  
Dita Paramitha

Hyperuricemia is a condition in which increased levels of uric acid in the blood. Xanthine oxidase role in the oxidation of hypoxanthine and xanthine to uric acid. One treatment of hyperuricemia is inhibiting xanthine oxidase in the process of formation of uric acid. The purpose of this study to determine the inhibitory activity of xanthine oxidase in the ethanol extract of black betel leaf (Piper sp). Xanthine oxidase inhibitory activity test using UV-Vis spectrophotometry in vitro with a concentration of 5 ppm, 10 ppm and 20 ppm. The data obtained were analyzed using one-way ANOVA. The result is the ethanol extract of black betel leaf has a different activity significantly and IC50 values obtained is 65.96 ppm.


Author(s):  
Emadeldin M. Kamel ◽  
Noha A. Ahmed ◽  
Ashraf A. El-Bassuony ◽  
Omnia E. Hussein ◽  
Barakat Alrashdi ◽  
...  

Background: Various phenolics show inhibitory activity towards xanthine oxidase (XO), an enzyme that generates reactive oxygen species which cause oxidative damage. Objective: This study investigated the XO inhibitory activity of Euphorbia peplus phenolics. Methods: The dried powdered aerial parts of E. peplus were extracted, fractioned and phenolics were isolated and identified. The XO inhibitory activity of E. peplus extract (EPE) and the isolated phenolics was investigated in vitro and in vivo. Results: Three phenolics were isolated from the ethyl acetate fraction of E. peplus. All isolated compounds and the EPE showed inhibitory activity towards XO in vitro. In hyperuricemic rats, EPE and the isolated phenolics decreased uric acid and XO activity. Molecular docking showed the binding modes of isolated phenolics with XO, depicting significant interactions with the active site amino acid residues. Molecular dynamics simulation trajectories confirmed the interaction of isolated phenolics with XO by forming hydrogen bonds with the active site residues. Also, the root mean square (RMS) deviations of XO and phenolics-XO complexes achieved equilibrium and fluctuated during the 10 ns MD simulations. The radius of gyration and solvent accessible surface area investigations showed that different systems were stabilized at ≈ 2500 ps. The RMS fluctuations profile depicted that the drug binding site exhibited a rigidity behavior during the simulation. Conclusion: In vitro, in vivo and computational investigations showed the XO inhibitory activity of E. peplus phenolics. These phenolics might represent promising candidates for the development of XO inhibitors.


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