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Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents

In this work, a series of novel compounds Spartinin C1-C24 were screened, synthesised and evaluated for inhibiting xanthine oxidase thus lowering serum uric acid level. The backbones were derived from the components of coastal marine source Spartina alterniflora and marketed drugs. The top hits Spar...

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Published in:Journal of enzyme inhibition and medicinal chemistry 2023-12, Vol.38 (1), p.2163241-2163241
Main Authors: Yang, Yu-Shun, Wang, Bin, Liu, Junzhong, Li, Qin, Jiao, Qin-Cai, Qin, Pei
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creator Yang, Yu-Shun
Wang, Bin
Liu, Junzhong
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Jiao, Qin-Cai
Qin, Pei
description In this work, a series of novel compounds Spartinin C1-C24 were screened, synthesised and evaluated for inhibiting xanthine oxidase thus lowering serum uric acid level. The backbones were derived from the components of coastal marine source Spartina alterniflora and marketed drugs. The top hits Spartinin C10 & C22 suggested high inhibition percentages (78.54 and 93.74) at 10 μM dosage, which were higher than the positive control Allopurinol. They were low cytotoxic onto human normal hepatocyte cells. Treatment with Spartinin C10 could lower the serum uric acid level to 440.0 μM in the hyperuricemic model mice (723.0 μM), comparable with Allopurinol (325.8 μM). Spartinin C10 was more appreciated than Allopurinol on other serum indexes. The preliminary pharmacokinetics evaluation indicated that the rapid absorption, metabolism and elimination of Spartinin C10 should be further improved. The discovery of pharmaceutical molecules from coastal marine source here might inspire the inter-disciplinary investigations on public health.
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source Taylor & Francis Open Access; Publicly Available Content Database; PubMed Central
subjects Allopurinol
Allopurinol - pharmacology
Allopurinol - therapeutic use
Animal models
Animals
Antioxidants
Biotechnology
Chromatography
Coastal marine sources
Coumaric acid
Coumaric Acids
Cytotoxicity
Humans
Hyperuricemia - drug therapy
Libraries
Life sciences
lowering uric acid
Mice
Nonnative species
Pharmaceuticals
Pharmacokinetics
Public health
Research Paper
Software
Spartina alterniflora
Uric acid
Uric Acid - therapeutic use
Xanthine oxidase
Xanthine Oxidase - metabolism
xanthine oxidase inhibition
title Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents
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