6-Acyl-4-aryl/alkyl-5,7-dihydroxycoumarins as anti-inflammatory agents

Chun Mao Lin; Sheng Tung Huang; Fu Wei Lee; Hsien Saw Kuo; Mei Hsiang Lin

doi:10.1016/j.bmc.2006.02.042

6-Acyl-4-aryl/alkyl-5,7-dihydroxycoumarins as anti-inflammatory agents

Chun Mao Lin, Sheng Tung Huang, Fu Wei Lee, Hsien Saw Kuo, Mei Hsiang Lin

Research output: Contribution to journal › Article › peer-review

81 Citations (Scopus)

Abstract

A series of coumarin derivatives were synthesized in two steps from phloroglucinol. The anti-inflammatory activities of these derivatives were evaluated by means of inhibiting NO production in LPS-induced RAW 264.7 cells. Derivatives 3, 8, 10, 11, and 13 exhibited low micromolar levels of anti-inflammatory activities, and these derivatives also protected DNA against hydroxyl radical attack. Coumarin derivative 8 was the most potent derivative among those tested herein against NO production in LPS-induced RAW 264.7 cells with an IC₅₀ value of 7.6 μM, and it effectively reduced the hydroxyl radical production by 50% at 100 μM in the electron spin resonance study.

Original language	English
Pages (from-to)	4402-4409
Number of pages	8
Journal	Bioorganic and Medicinal Chemistry
Volume	14
Issue number	13
DOIs	https://doi.org/10.1016/j.bmc.2006.02.042
Publication status	Published - Jul 1 2006

Keywords

Anti-inflammation
Coumarin
ROS
iNOS

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmc.2006.02.042

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title = "6-Acyl-4-aryl/alkyl-5,7-dihydroxycoumarins as anti-inflammatory agents",

abstract = "A series of coumarin derivatives were synthesized in two steps from phloroglucinol. The anti-inflammatory activities of these derivatives were evaluated by means of inhibiting NO production in LPS-induced RAW 264.7 cells. Derivatives 3, 8, 10, 11, and 13 exhibited low micromolar levels of anti-inflammatory activities, and these derivatives also protected DNA against hydroxyl radical attack. Coumarin derivative 8 was the most potent derivative among those tested herein against NO production in LPS-induced RAW 264.7 cells with an IC50 value of 7.6 μM, and it effectively reduced the hydroxyl radical production by 50% at 100 μM in the electron spin resonance study.",

keywords = "Anti-inflammation, Coumarin, ROS, iNOS",

author = "Lin, {Chun Mao} and Huang, {Sheng Tung} and Lee, {Fu Wei} and Kuo, {Hsien Saw} and Lin, {Mei Hsiang}",

note = "Funding Information: This study was supported by the National Science Council, Taiwan (NSC93-2113-M-038-004), and Taipei Medical University (TMU93-AE1-B-10).",

year = "2006",

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doi = "10.1016/j.bmc.2006.02.042",

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AU - Lin, Chun Mao

AU - Huang, Sheng Tung

AU - Lee, Fu Wei

AU - Kuo, Hsien Saw

AU - Lin, Mei Hsiang

N1 - Funding Information: This study was supported by the National Science Council, Taiwan (NSC93-2113-M-038-004), and Taipei Medical University (TMU93-AE1-B-10).

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Y1 - 2006/7/1

N2 - A series of coumarin derivatives were synthesized in two steps from phloroglucinol. The anti-inflammatory activities of these derivatives were evaluated by means of inhibiting NO production in LPS-induced RAW 264.7 cells. Derivatives 3, 8, 10, 11, and 13 exhibited low micromolar levels of anti-inflammatory activities, and these derivatives also protected DNA against hydroxyl radical attack. Coumarin derivative 8 was the most potent derivative among those tested herein against NO production in LPS-induced RAW 264.7 cells with an IC50 value of 7.6 μM, and it effectively reduced the hydroxyl radical production by 50% at 100 μM in the electron spin resonance study.

AB - A series of coumarin derivatives were synthesized in two steps from phloroglucinol. The anti-inflammatory activities of these derivatives were evaluated by means of inhibiting NO production in LPS-induced RAW 264.7 cells. Derivatives 3, 8, 10, 11, and 13 exhibited low micromolar levels of anti-inflammatory activities, and these derivatives also protected DNA against hydroxyl radical attack. Coumarin derivative 8 was the most potent derivative among those tested herein against NO production in LPS-induced RAW 264.7 cells with an IC50 value of 7.6 μM, and it effectively reduced the hydroxyl radical production by 50% at 100 μM in the electron spin resonance study.

KW - Anti-inflammation

KW - Coumarin

KW - ROS

KW - iNOS

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ER -

6-Acyl-4-aryl/alkyl-5,7-dihydroxycoumarins as anti-inflammatory agents

Abstract

Keywords

ASJC Scopus subject areas

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