Inhibitory activity of flavonols towards the xanthine oxidase enzyme

1992 ◽  
Vol 86 (1) ◽  
pp. 17-23 ◽  
Author(s):  
L. Costantino ◽  
G. Rastelli ◽  
A. Albasini
Author(s):  
Rini Hendriani ◽  
Nursamsiar Nursamsiar ◽  
Ami Tjitraresmi

Objective: The aim of the present study was to examine the inhibiting effects of quercetin contained in Sonchusarvensis leaf extract on the activity of xanthine oxidase, an essential enzyme for uric acid synthesis.Methods: Activity test was conducted in vitro by measuring the activity of xanthine oxidase using UV spectrophotometry and in silico by determining the interaction of quercetin and allopurinol (as comparation drug) with xanthine oxidase enzyme in terms of hydrogen bonds and binding free energy. Docking simulations were performed by Autodock4.2 package.Results: The active fraction, using the solvent n-hexane, ethyl acetate and water, tested the inhibitory activity of the xanthine oxidase enzyme in vitro obtained respectively IC50 of 263.19, 16.20 and 141.80 μg/ml. Isolates with highest activity identified as quercetin. The xanthine oxidase enzyme inhibitory activity insilico by molecular docking showed quercetin has free energy binding ˗7.71 kcal/mol, more negative than that of allopurinol ˗5.63 kcal/mol.Conclusion: This shows the affinity of quercetin stronger than that of allopurinol; so that it can be predicted that quercetin was more potential to inhibit xanthine oxidase enzyme activity. Thus the extract of the S. arvensis leaves containing the active compound quercetin was a potential use as antihyperuricemia.  


2018 ◽  
Vol 67 ◽  
pp. 03011 ◽  
Author(s):  
Abdullah ◽  
Angelina ◽  
Mauhibah Yumna ◽  
Rita Arbianti ◽  
Tania Surya Utami ◽  
...  

Hyperuricemia is a disease that is characterized by high uric acid levels, in which the number of victim increase year by year in the worldwide. Flavonoid is an active compound with inhibitory activity towards Xanthine Oxidase Enzyme which is a compound that plays a role in the formation of uric acid in the body. Sansevieria trifasciata is an ornamental plant which is also useful as a source of antibacterial and antioxidant agent. Studies of S. trifasciata as Xanthine Oxidase Enzyme inhibitor have not been reported. This research isolate flavonoid compounds using open column chromatography from crude extract of S. trifasciata leaves that extracted by sonication method. There are six eluent used to isolate flavonoid which are methanol : ethyl acetate, chloroform : ethyl acetate, chloroform : ethyl acetate : methanol. Wilstater test is used to select the fraction that rich of flavonoid. The best result from isolation step that contains flavonoid is assessed the inhibitory activity of xanthine oxidase. It is analyzed qualitative using Liquid Chromatography Mass Spectrometry (LCMS). The inhibition percentage showed that fraction 3 was potential to inhibit XO by 85.48 %. LC-MS chromatogram can show that crude extract and positive fraction of isolation were containing falvonoid.


2011 ◽  
Vol 6 (10) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Shivraj H. Nile ◽  
Chandrahasy N. Khobragade

The methanolic extract of Tephrosia purpurea (Leguminosae) shoots was evaluated in-vitro for its anti-inflammatory and xanthine oxidase inhibitory activity. Anti-inflammatory activity was measured by the Diene-conjugate, HET-CAM and β-glucuronidase methods. The enzyme inhibitory activity was tested against isolated cow milk xanthine oxidase. The average anti-inflammatory activity of T. purpurea shoot extract in the concentration range of 1-2 μg/mL in the reacting system revealed significant anti-inflammatory activities, which, as recorded by the Diene-conjugate, HET-CAM and β-glucuronidase assay methods, were 45.4, 10.5, and 70.5%, respectively. Screening of the xanthine oxidase inhibitory activity of the extract in terms of kinetic parameters revealed a mixed type of inhibition, wherein the Km and Vmax values in the presence of 25 to 100 μg/mL shoot extract was 0.20 mM/mL and 0.035, 0.026, 0.023 and 0.020 μg/min, while, for the positive control, the Km and Vmax values were 0.21 mM/mL and 0.043 μg/min, respectively. These findings suggest that T. purpurea shoot extract may possess constituents with good medicinal properties that could be exploited to treat the diseases associated with oxidative stress, xanthine oxidase enzyme activity and inflammation.


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

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

2015 ◽  
Vol 11 (2) ◽  
pp. 108-115 ◽  
Author(s):  
Bijo Mathew ◽  
Jerad Suresh ◽  
Githa Mathew ◽  
Sherin Rasheed ◽  
Jobin Vilapurathu ◽  
...  

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.


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