Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents
AbstractIn 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 h...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2023-12-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/14756366.2022.2163241 |
| _version_ | 1797400979952369664 |
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| author | Yu-Shun Yang Bin Wang Junzhong Liu Qin Li Qin-Cai Jiao Pei Qin |
| author_facet | Yu-Shun Yang Bin Wang Junzhong Liu Qin Li Qin-Cai Jiao Pei Qin |
| author_sort | Yu-Shun Yang |
| collection | DOAJ |
| description | AbstractIn 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. |
| first_indexed | 2024-03-09T02:03:18Z |
| format | Article |
| id | doaj.art-f02744803eb04f5983842069dbcb86b4 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-03-09T02:03:18Z |
| publishDate | 2023-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-f02744803eb04f5983842069dbcb86b42023-12-08T03:24:21ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742023-12-0138110.1080/14756366.2022.2163241Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agentsYu-Shun Yang0Bin Wang1Junzhong Liu2Qin Li3Qin-Cai Jiao4Pei Qin5State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, ChinaState Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, ChinaState Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, ChinaState Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, ChinaState Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, ChinaState Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, ChinaAbstractIn 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.https://www.tandfonline.com/doi/10.1080/14756366.2022.2163241Coastal marine sourcesSpartina alternifloraxanthine oxidase inhibitionlowering uric acid |
| spellingShingle | Yu-Shun Yang Bin Wang Junzhong Liu Qin Li Qin-Cai Jiao Pei Qin Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents Journal of Enzyme Inhibition and Medicinal Chemistry Coastal marine sources Spartina alterniflora xanthine oxidase inhibition lowering uric acid |
| title | Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents |
| title_full | Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents |
| title_fullStr | Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents |
| title_full_unstemmed | Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents |
| title_short | Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents |
| title_sort | discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents |
| topic | Coastal marine sources Spartina alterniflora xanthine oxidase inhibition lowering uric acid |
| url | https://www.tandfonline.com/doi/10.1080/14756366.2022.2163241 |
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