Pseudoguaianolides isolated from Inula britannica var. chinenis as inhibitory constituents against inducible nitric oxide synthase

Hyun Tai Lee; Seung Won Yang; Ho Kim Kyeong; Eun Kyoung Seo; Woongchon Mar

doi:10.1007/BF02976555

Pseudoguaianolides isolated from Inula britannica var. chinenis as inhibitory constituents against inducible nitric oxide synthase

Hyun Tai Lee, Seung Won Yang, Ho Kim Kyeong, Eun Kyoung Seo, Woongchon Mar

Department of Pharmaceutical Sciences

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

26 Scopus citations

Abstract

Three pseudoguaianolide type sesquiterpenes, bigelovin (1), 2,3-dihydroaromaticin (2), and ergolide (3) were isolated as inhibitory constituents against inducible nitric oxide synthase (iNOS) from the flowers of Inula britannica var. chinensis. Bigelovin (1) exhibited a highly potent inhibitory activity on lipopolysaccharide (LPS)-induced iNOS in murine macrophage RAW 264.7 cells with an IC₅₀ value of 0.46 mM, which is about 8 times more potent than the known selective inhibitor of iNOS, L- N ⁶-(1-iminoethyl)lysine (IC₅₀ 3.49 μM). 2,3-Dihydroaromaticin (2) and ergolide (3) also exhibited potent inhibitory activities on LPS-induced iNOS with IC₅₀ values of 1.05 and 0.69 μM, respectively.

Original language	English
Pages (from-to)	151-153
Number of pages	3
Journal	Archives of Pharmacal Research
Volume	25
Issue number	2
DOIs	https://doi.org/10.1007/BF02976555
State	Published - 30 Apr 2002

Bibliographical note

Funding Information:
This study was supported by a grant from the Korea Health 21 R&D Project, Ministry of Health & Welfare, Republic of Korea (00-CD-01-0001).

Keywords

2,3-Dihydroaromaticin
Bigelovin
Ergolide
iNOS inhibitor
Inula britannica var. chinensis

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10.1007/BF02976555

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@article{f0fe222b72984fa9bd911aad3da64e47,

title = "Pseudoguaianolides isolated from Inula britannica var. chinenis as inhibitory constituents against inducible nitric oxide synthase",

abstract = "Three pseudoguaianolide type sesquiterpenes, bigelovin (1), 2,3-dihydroaromaticin (2), and ergolide (3) were isolated as inhibitory constituents against inducible nitric oxide synthase (iNOS) from the flowers of Inula britannica var. chinensis. Bigelovin (1) exhibited a highly potent inhibitory activity on lipopolysaccharide (LPS)-induced iNOS in murine macrophage RAW 264.7 cells with an IC50 value of 0.46 mM, which is about 8 times more potent than the known selective inhibitor of iNOS, L- N 6-(1-iminoethyl)lysine (IC50 3.49 μM). 2,3-Dihydroaromaticin (2) and ergolide (3) also exhibited potent inhibitory activities on LPS-induced iNOS with IC50 values of 1.05 and 0.69 μM, respectively.",

keywords = "2,3-Dihydroaromaticin, Bigelovin, Ergolide, iNOS inhibitor, Inula britannica var. chinensis",

author = "Lee, {Hyun Tai} and Yang, {Seung Won} and Kyeong, {Ho Kim} and Seo, {Eun Kyoung} and Woongchon Mar",

note = "Funding Information: This study was supported by a grant from the Korea Health 21 R&D Project, Ministry of Health & Welfare, Republic of Korea (00-CD-01-0001).",

year = "2002",

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doi = "10.1007/BF02976555",

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AU - Lee, Hyun Tai

AU - Yang, Seung Won

AU - Kyeong, Ho Kim

AU - Seo, Eun Kyoung

AU - Mar, Woongchon

N1 - Funding Information: This study was supported by a grant from the Korea Health 21 R&D Project, Ministry of Health & Welfare, Republic of Korea (00-CD-01-0001).

PY - 2002/4/30

Y1 - 2002/4/30

N2 - Three pseudoguaianolide type sesquiterpenes, bigelovin (1), 2,3-dihydroaromaticin (2), and ergolide (3) were isolated as inhibitory constituents against inducible nitric oxide synthase (iNOS) from the flowers of Inula britannica var. chinensis. Bigelovin (1) exhibited a highly potent inhibitory activity on lipopolysaccharide (LPS)-induced iNOS in murine macrophage RAW 264.7 cells with an IC50 value of 0.46 mM, which is about 8 times more potent than the known selective inhibitor of iNOS, L- N 6-(1-iminoethyl)lysine (IC50 3.49 μM). 2,3-Dihydroaromaticin (2) and ergolide (3) also exhibited potent inhibitory activities on LPS-induced iNOS with IC50 values of 1.05 and 0.69 μM, respectively.

AB - Three pseudoguaianolide type sesquiterpenes, bigelovin (1), 2,3-dihydroaromaticin (2), and ergolide (3) were isolated as inhibitory constituents against inducible nitric oxide synthase (iNOS) from the flowers of Inula britannica var. chinensis. Bigelovin (1) exhibited a highly potent inhibitory activity on lipopolysaccharide (LPS)-induced iNOS in murine macrophage RAW 264.7 cells with an IC50 value of 0.46 mM, which is about 8 times more potent than the known selective inhibitor of iNOS, L- N 6-(1-iminoethyl)lysine (IC50 3.49 μM). 2,3-Dihydroaromaticin (2) and ergolide (3) also exhibited potent inhibitory activities on LPS-induced iNOS with IC50 values of 1.05 and 0.69 μM, respectively.

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KW - Ergolide

KW - iNOS inhibitor

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JF - Archives of Pharmacal Research

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ER -

Pseudoguaianolides isolated from Inula britannica var. chinenis as inhibitory constituents against inducible nitric oxide synthase

Abstract

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Keywords

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