scholarly journals In vitro and in vivo inhibition of xanthine oxidase by the flowers of Chrysanthemum morifolium Ramat.

2020 ◽  
Author(s):  
Teng Lit Ng ◽  
Khye Er Loh ◽  
Sheri-Ann Shu Wei Tan ◽  
Hui Yin Tan ◽  
Sze Ping Wee
Keyword(s):  
Gene Expression ◽  
Uric Acid ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Competitive Inhibition ◽  
Chrysanthemum Morifolium ◽  
Inhibitory Potential ◽  
Tof Ms

Abstract Background: Xanthine oxidase (XO) plays an important role in human’s purine degradation. Excessive uric acid formation results in hyperuricemia and gout. The study aimed to determine the XO inhibitory potential of Chrysanthemum morifolium Ramat. dried flower and its effect on XO gene expression in animal models.Methods: In vitro XO inhibitory assay was employed to investigate the XO inhibitory potential of C. morifolium flowers. The bioactive sub-fraction was investigated further to give additional insight on its uric acid lowering potential via animal study and XO gene expression analysis. HPLC-Q-TOF-MS/MS was utilized to identify the putative compounds in the sub-fraction.Results: Among the fractions, EtOAc fraction exhibited the highest in vitro XO inhibitory potency (51.77 ± 0.98%; IC50 = 10.64 ± 0.51 µg/mL) and it was further fractionated into 15 sub-fractions through open column chromatography. EtOAc F7, F8, F9, F10, and F11 possessed >75% XO inhibition. F9 and F10 exhibited high in vitro XO inhibitory activity, cellular pro-proliferative effect and intracellular antioxidant activity among the sub-fractions tested. These two sub-fractions were also non-cytotoxic at the concentration range of 0.1 – 10 µg/mL. F10 was shown to be very effective in both serum and urine uric acid lowering properties in rats model upon oral consumption. It was subjected to further fractionation and a total of 11 sub-fractions were obtained. F10-4, F10-8, F10-9, and F10-10 possessed >90% XO inhibition. These sub-fractions were subjected to HPLC-Q-TOF-MS/MS analysis. A total of nine known compounds have been identified and 26 unknown compounds were detected. Conclusions: The possible mechanisms contributed to the anti-hyperuricemic effect of F10 were suggested to be non-competitive inhibition of XO enzyme, XO gene expression down regulation, and enhancement of uric acid excretion. Structure elucidation of the unknown compounds and the evaluation of the XO inhibitory activity of a single or a mixture of these compounds are recommended to identify possible synergism between them.

Application of UHPLC/ESI-Q-TOF-MS/MS to Identify Constituents of Erding Granule and Anti-hyperuricemia Effect

2019 ◽  
Vol 15 (5) ◽  
pp. 465-486 ◽  
Author(s):  
Haifang Chen ◽  
Yun Yao ◽  
Yuan Zhan ◽  
Hui Jian ◽  
Yan Li ◽  
...  
Keyword(s):  
Uric Acid ◽  
Xanthine Oxidase ◽  
Chemical Constituents ◽  
Serum Urate ◽  
Chemical Information ◽  
Upper Respiratory Tract ◽  
Serum Urate Level ◽  
Tof Ms

Background: Erding granule (EDG) widely used as an agent with the effect of heat-clearing, detoxifying, eliminating dampness, relieving jaundice and upper respiratory tract disease in clinical application, but the systematic chemical information and anti-hyperuricemia effect of EDG was still unclear. Methods: An ultra-high performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC/ESI-Q-TOF-MS/MS) method was utilized to rapidly identify the chemical constituents of EDG. The anti-hyperuricemia effect of EDG was evaluated based on the effect on xanthine oxidase inhibitory activity (in vitro) and lowering uric acid (in vivo). Results: 198 compounds were tentatively separated and identified or characterized within 30 min by UHPLC/ESI-Q-TOF MS/MS. These compounds were categorized as 22 coumarins, 38 flavones, 67 alkaloids, 36 organic acids, 16 sesquiterpenes, 14 lignans and 5 the others constituents. Meanwhile, EDG significantly decreases the serum urate level of hyperuricemic mice induced by potassium oxonate, while EDG did not significantly decrease the serum urate level of hyperuricemic mice induced by hypoxanthine and activity of xanthine oxidase in vitro. Conclusion: The method developed was rapid and sensitive to characterize the chemical constituents of EDG, and provide a systematic view of chemical information for EDG. Furthermore, we first discovered the anti-hyperuricemia effect of EDG and it would further provide the reference for clarifying the mechanism of EDG on lowering uric acid.

scholarly journals Aktivitas Penghambatan Xantin Oksidase pada Ekstrak Daun Sirih Hitam (Piper sp)

2016 ◽  
Vol 3 ◽  
pp. 160-163
Author(s):  
Muhammad Amir Masruhim ◽  
Wisnu Cahyo Prabowo ◽  
Dita Paramitha
Keyword(s):  
Uric Acid ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Ethanol Extract ◽  
Betel Leaf ◽  
Activity Test ◽  
Ic50 Values ◽  
One Way Anova

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.

Xanthine oxidase inhibitory activity of Euphorbia peplus L. phenolics

2021 ◽  
Vol 24 ◽  
Author(s):  
Emadeldin M. Kamel ◽  
Noha A. Ahmed ◽  
Ashraf A. El-Bassuony ◽  
Omnia E. Hussein ◽  
Barakat Alrashdi ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Active Site ◽  
Inhibitory Activity ◽  
Drug Binding ◽  
Dynamics Simulation ◽  
Solvent Accessible Surface Area ◽  
Radius Of Gyration ◽  
Euphorbia Peplus

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.

Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro , in silico to in vivo studies

2017 ◽  
Vol 25 (8) ◽  
pp. 2351-2371 ◽  
Author(s):  
Humaira Zafar ◽  
Muhammad Hayat ◽  
Sumayya Saied ◽  
Momin Khan ◽  
Uzma Salar ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
In Silico ◽  
Systematic Approach ◽  
In Vivo Studies

scholarly journals LOWERING URIC ACID EFFICACY TEST OF THE COMBINED EXTRACT OF UNCARIA GAMBIR (HUNTER) ROXB. AND CAESALPINIA SAPPAN L. IN VIVO AND IN VITRO

2018 ◽  
Vol 11 (8) ◽  
pp. 166
Author(s):  
Sri Ningsih ◽  
Fahri Fahrudin
Keyword(s):  
Antioxidant Activity ◽  
Uric Acid ◽  
Inhibitory Activity ◽  
Positive Control ◽  
Polyphenol Content ◽  
Caesalpinia Sappan ◽  
In Vivo Experiments ◽  
A Value

 Objective: Hyperuricemia (high uric acid levels) prevalence increased year by year. This study was aimed to elaborate the in vitro xanthine oxidase (XO) inhibitory activity and in vivo lowering hyperuricemic effect of Uncaria gambir (Hunter) Roxb) (gambir), Caesalpinia sappan L. (secang) and the combined extract of secang and gambir (formulae extract [FE]).Methods: Gambir and secang extracts were prepared by maceration with ethanol and FE was the proportioned combination of these two extracts. XO inhibitory activity was determined by measuring the formation of uric acid in the xanthine/XO system in vitro using allopurinol as a positive control at 100 ug/mL. Antioxidant activity was by 1,1-diphenyl-2-picrylhydrazyl radical reducing methods. The in vivo experiments were conducted in the oxonate-induced hyperuricemia rat model, in which FE was gavaged p.o. at the arrange dose of 75, 150, and 300 mg/kg bw for 2 weeks. Polyphenol content was measured using Folin–Ciocalteu reagent spectrophotometrically.Results: The XO inhibitory activity of FE was 80% of allopurinol, while secang and gambir were 98% and 50%, respectively. The strength was appropriate to the total polyphenol content, in which it decreased in the order of secang (99%) > FE (86%) > gambir (46%). Furthermore, FE at all tested doses was able to decrease uric acid levels. FE also demonstrated antioxidant activity with a value of 74% relative to Vitamin C at 4 ug/mL.Conclusion: These studies could be concluded that FE exhibited the ability to decrease uric acid level so that it was potential to be developed further as a uric acid-lowering agent.

scholarly journals EVALUASI AKTIVITAS INHIBISI XANTIN OKSIDASE DAN KANDUNGAN SENYAWA POLIFENOL DARI EKSTRAK SAPPAN

2018 ◽  
Vol 5 (2) ◽  
pp. 157
Author(s):  
Sri Ningsih ◽  
. Churiyah
Keyword(s):  
Uric Acid ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Ethanolic Extract ◽  
Polyphenol Content ◽  
Total Polyphenol ◽  
Caesalpinia Sappan ◽  
Total Polyphenol Content

Evaluation of xanthine oxidase inhibitory activity and polyphenolic content of sappan extractABSTRACTHyperuricemia is a disease that is characterized by a high uric acid level, in which the number of patients tends to increase every year. This research was intended to evaluate the xanthine oxidase (XO) inhibitory activity and determinate the total polyphenol content of heartwood sappan (Caesalpinia sappan L.) extract. The extract was prepared by macerating the dry powder wood using 70% ethanol at room temperature. The quality of ethanolic extract obtained was evaluated based on BPOM guideline. XO inhibitory power was determined by measuring uric acid produced in the xanthine/XO system in vitro. The polyphenol content of the extract was measured using Folin-Ciocalteu reagent spectrophotometrically. The results showed that the quality of sappan semisolid extract fulfilled the required standard. Sappan extract inhibited XO activity by 98% relative to the positive control, allopurinol, at the final extract concentration of 100 µg/mL. The total polyphenol content was 26% of the crude extract. It could be concluded that sappan ethanolic extract has the potential to be developed as an ingredient for hyperuricemia treatment.Keywords: hyperuricemia, sappan, total polyphenol, xanthine, xanthine oxidase ABSTRAKHiperurisemia adalah penyakit yang dicirikan dengan kadar asam urat tinggi dimana prevalensi penderita cenderung meningkat. Penelitian ini bertujuan untuk mempelajari aktivitas esktrak kayu sappan (Caesalpinia sappan L.) dalam menginhibisi enzim XO (xantin oksidase) secara in vitro dan penentuan kadar senyawa polifenol total yang terkandung di dalamnya. Ekstrak dibuat dengan cara maserasi serbuk kayu menggunakan pelarut etanol 70% pada suhu kamar. Kualitas ekstrak dievaluasi mengacu pada parameter karakterisasi ekstrak yang ditetapkan oleh BPOM. Aktivitas inhibisi XO ditetapkan dengan mengukur kadar asam urat yang terbentuk pada sistem xantin/XO in vitro. Kadar polifenol ekstrak diukur menggunakan pereaksi Folin-Ciocalteu secara spektrofotometri. Hasil analisis menyatakan bahwa kualitas ekstrak kental sappan memenuhi persyaratan yang ada. Pengujian inhibisi XO dengan pembanding positif allopurinol pada konsentrasi akhir ekstrak sebesar 100 µg/mL menunjukkan bahwa ekstrak mempunyai kekuatan menginhibisi XO sebesar 98% relatif terhadap pembanding positif allopurinol. Kadar senyawa polifenol total dalam ekstrak sappan sebesar 26% dari ekstrak kasar. Dari penelitian ini dapat disimpulkan bahwa ekstrak sappan mempunyai potensi untuk dikembangkan sebagai bahan untuk mengatasi hiperurisemia.Kata Kunci: hiperurisemia, polifenol total, sappan, xantin, xantin oksidase

Salvia plebeia Extract Inhibits Xanthine Oxidase Activity In Vitro and Reduces Serum Uric Acid in an Animal Model of Hyperuricemia

Planta Medica ◽  
2017 ◽  
Vol 83 (17) ◽  
pp. 1335-1341 ◽  
Author(s):  
Jin Kim ◽  
Woo Kim ◽  
Jung Hyun ◽  
Jong Lee ◽  
Jin Kwon ◽  
...  
Keyword(s):  
Animal Model ◽  
Enzyme Activity ◽  
Uric Acid ◽  
Xanthine Oxidase ◽  
Serum Uric Acid ◽  
Serum Urate ◽  
Key Enzyme ◽  
Ic50 Values

AbstractHyperuricemia is a clinical condition characterized by an elevated level of serum uric acid and is a key risk factor for the development of gout and metabolic disorders. The existing urate-lowering therapies are often impractical for certain patient populations, providing a rationale to explore new agents with improved safety and efficacy. Here, we discovered that Salvia plebeia extract inhibited the enzyme activity of xanthine oxidase, which is a key enzyme generating uric acid in the liver. In an animal model of hyperuricemia, S. plebeia extract reduced serum urate to the levels observed in control animals. The urate-lowering effect of S. plebeia extract in vivo was supported by the identification of compounds that inhibit xanthine oxidase enzyme activity in vitro. Nepetin, scutellarein, and luteolin contributed significantly to S. plebeia bioactivity in vitro. These compounds showed the highest potency against xanthine oxidase with IC50 values of 2.35, 1.74, and 1.90 µM, respectively, and were present at moderate quantities. These observations serve as a basis for further elaboration of the S. plebeia extracts for the development of new therapeutics for hyperuricemia and related diseases.

Anti-hyperuricemic peptides derived from bonito hydrolysates based on in vivo hyperuricemic model and in vitro xanthine oxidase inhibitory activity

Peptides ◽  
2018 ◽  
Vol 107 ◽  
pp. 45-53 ◽  
Author(s):  
Yujuan Li ◽  
Xiaoyan Kang ◽  
Qingyong Li ◽  
Chuanchao Shi ◽  
Yingyi Lian ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity

scholarly journals In Vitro and In Vivo Studies on Quercus acuta Thunb. (Fagaceae) Extract: Active Constituents, Serum Uric Acid Suppression, and Xanthine Oxidase Inhibitory Activity

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
In-Soo Yoon ◽  
Dae-Hun Park ◽  
Min-Suk Bae ◽  
Deuk-Sil Oh ◽  
Nan-Hui Kwon ◽  
...  
Keyword(s):  
South Korea ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
In Vivo Studies ◽  
Gas Chromatography Mass Spectrometry ◽  
Similar Extent ◽  
Active Constituents ◽  
Quercus Acuta

Quercus acuta Thunb. (Fagaceae) (QA) is cultivated as a dietary and ornamental plant in China, Japan, South Korea, and Taiwan. It has been widely used as the main ingredient of acorn tofu, a traditional food in China and South Korea. The aim of this study was to determine in vitro and in vivo xanthine oxidase (XO) inhibitory and antihyperuricemic activities of an ethyl acetate extract of QA leaf (QALE) and identify its active phytochemicals using gas chromatography-mass spectrometry (GC-MS) and liquid chromatography (LC) systems. The QALE was found to possess potent in vitro antioxidant and XO inhibitory activities. In vivo study using hyperuricemic mice induced with potassium oxonate demonstrated that the QALE could inhibit hepatic XO activity at a relatively low oral dose (50 mg/kg) and significantly alleviate hyperuricemia to a similar extent as allopurinol. Several active compounds including vitamin E known to possess XO inhibitory activity were identified from the QALE. To the best of our knowledge, this is the first study that reports the active constituents and antihyperuricemic effect of QA, suggesting that it is feasible to use QALE as a food therapy or alternative medicine for alleviating hyperuricemia and gout.

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