Inhibition mechanism of baicalein and baicalin on xanthine oxidase and their synergistic effect with allopurinol

Zeng, Ni; Zhang, Guowen; Hu, Xiaofeng; Pan, Junhui; Zhou, Zhongwu; Gong, Deming

doi:10.1016/j.jff.2018.10.005

Cited by 63 publications

(30 citation statements)

References 41 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The slope of the line decreased with increasing inhibitor concentration, indicating that the inhibition of FPSV and FPFP on XO was reversible. This suggested that tetrapeptides could reversibly inhibit the XO activity rather than reducing the effective amount of the enzyme [31], and this implied that interaction between the peptide and XO is mainly a non-covalent intermolecular interaction [29]. The XO inhibitory types of FPSV and FPFP were determined from Lineweaver-Burk double reciprocal plots.…”

Section: Reversibility and The Type Of Inhibitionmentioning

confidence: 99%

See 1 more Smart Citation

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

Zhou

et al. 2021

Marine Drugs

View full text Add to dashboard Cite

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.

show abstract

Section: Reversibility and The Type Of Inhibitionmentioning

confidence: 99%

“…Then, the dynamic changes of the absorbance at 290 nm were recorded, and ν was calculated using the same method above. K m and V max values, as corresponding kinetic parameters, were obtained from the Lineweaver and Burk double reciprocal plots [31].…”

Section: Determination Of Reversibility and The Type Of Inhibitionmentioning

confidence: 99%

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

Zhou

et al. 2021

Marine Drugs

View full text Add to dashboard Cite

show abstract

“…A simple additive effect or a very slight antagonism was observed for the isobole of the 30% inhibition effect level as the convex curve was almost above the additive isobole, and CI values were 0.96, 1.14, and 1.04. At the 50% inhibition effect level, all dose points were below the additive isobole and the top of the convex curve was very close to the isobole, suggesting a weak synergistic effect of CRA with myricetin . In the case of the 70% inhibition effect level, the additive effect was dominant based on the CI values (0.89, 1.01, 0.98) because the convex curve had two intersection points with the additive isobole.…”

Section: Resultsmentioning

confidence: 94%

“…At the 50% inhibition effect level, all dose points were below the additive isobole and the top of the convex curve was very close to the isobole, suggesting a weak synergistic effect of CRA with myricetin. 35 In the case of the 70% inhibition effect level, the additive effect was dominant based on the CI values (0.89, 1.01, 0.98) because the convex curve had two intersection points with the additive isobole. In short, the combination of myricetin and CRA mainly showed a weak synergistic effect.…”

Section: Isobolographic Analysis Of Combined Inhibitionmentioning

confidence: 99%

Inhibitory effect of corosolic acid on α‐glucosidase: kinetics, interaction mechanism, and molecular simulation

Pan

et al. 2019

J Sci Food Agric

Self Cite

View full text Add to dashboard Cite

BACKGROUND The suppression of α‐glucosidase activity to retard glucose absorption is an important therapy for type‐2 diabetes. Corosolic acid (CRA) is a potential antidiabetic component in many plant‐based foods and herbs. In this study, the interplay mechanism between α‐glucosidase and corosolic acid was investigated by several methods, including three‐dimensional fluorescence spectra, circular dichroism spectra, and molecular simulation. RESULTS Corosolic acid significantly inhibited α‐glucosidase reversibly in an uncompetitive manner and its IC50 value was 1.35 × 10−5 mol L−1. A combination of CRA with myricetin exerted a weak synergy against α‐glucosidase. The intrinsic fluorescence of α‐glucosidase was quenched via a static quenching course and the binding constant was 3.47 × 103 L mol−1 at 298 K. The binding of CRA to α‐glucosidase was mainly driven by hydrophobic forces and resulted in a partial extension of the protein polypeptide chain with a loss of α‐helix content. The molecular simulation illustrated that CRA bound to the entrance part of the active center of α‐glucosidase and interacted with the amino acid residues Ser157, Arg442, Phe303, Arg315, Tyr158, and Gln353, which could hinder the release of substrate and catalytic reaction product, eventually suppressing the catalytic activity of α‐glucosidase. CONCLUSIONS These results may suggest new insights into corosolic acid from food sources as a potential α‐glucosidase inhibitor that could better control diabetes. © 2019 Society of Chemical Industry

show abstract

“…In the adjuvant-induced arthritis mice models, baicalin can control inflammation by blocking the IL-17 pathway and reducing the expression of IL-6, TNF- α , ICAM-1, and VCAM-1 [ 35 ]. It also showed significant inhibition of XOD [ 95 ]. Therefore, baicalin may treat gout and hyperuricemia by regulating IL-17, TNF, and HIF-1 pathways.…”

Section: Discussionmentioning

confidence: 99%

Potential Molecular Mechanisms of Plantain in the Treatment of Gout and Hyperuricemia Based on Network Pharmacology

Liu

Shi

et al. 2020

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

Background. The incidence of gout and hyperuricemia is increasing year by year in the world. Plantain is a traditional natural medicine commonly used in the treatment of gout and hyperuricemia, but the molecular mechanism of its active compounds is still unclear. Based on network pharmacology, this article predicts the targets and pathways of effective components of plantain for gout and hyperuricemia and provides effective reference for clinical medication. Method. Traditional Chinese medicine systems pharmacology database and analysis platform (TCMSP) and SymMap databases were used to screen out the active compounds and their targets in plantain. GeneCards, Therapeutic Target Database (TTD), and Online Mendelian Inheritance in Man (OMIM) databases were used to find the targets corresponding to gout and hyperuricemia. Venn diagram was used to obtain the intersection targets of plantain and diseases. The interaction network of the plantain active compounds-targets-pathways-diseases was constructed by using Cytoscape 3.7.2 software. Finally, Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were carried out. Result. Seven active compounds were identified by network pharmacological analysis, including dinatin, baicalein, baicalin, sitosterol, 6-OH-luteolin, stigmasterol, and luteolin. Plantain plays a role in gout and hyperuricemia diseases by regulating various biological processes, cellular components, and molecular functions. The core targets of plantain for treating gout are MAPK1, RELA, TNF, NFKBIA, and IFNG, and the key pathways are pathways in cancer, hypoxia-inducible factor-1 (HIF-1) signaling pathway, interleukin (IL)-17 signaling pathway, Chagas disease (American trypanosomiasis), and relaxin signaling pathway. The core targets of plantain for hyperuricemia are RELA, MAPK1, NFKBIA, CASP3, CASP8, and TNF, and the main pathways are pathways in cancer, apoptosis, hepatitis B, IL-17 signaling pathway, and toxoplasmosis. Conclusion. This study explored the related targets and mechanisms of plantain for the treatment of gout and hyperuricemia from the perspective of network pharmacological analysis, reflecting the characteristics of multiple components, multiple targets, and multiple pathways, and it provides a good theoretical basis for the clinical application of plantain.

show abstract

Inhibition mechanism of baicalein and baicalin on xanthine oxidase and their synergistic effect with allopurinol

Cited by 63 publications

References 41 publications

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

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

Inhibitory effect of corosolic acid on α‐glucosidase: kinetics, interaction mechanism, and molecular simulation

Potential Molecular Mechanisms of Plantain in the Treatment of Gout and Hyperuricemia Based on Network Pharmacology

Contact Info

Product

Resources

About