Preparation and anti-inflammatory activities of diarylheptanoid and diarylheptylamine analogs

Su Lin Lee; Wei Jan Huang; Wan Wan Lin; Shoei Sheng Lee; Chung Hsiung Chen

doi:10.1016/j.bmc.2005.06.058

Preparation and anti-inflammatory activities of diarylheptanoid and diarylheptylamine analogs

Su Lin Lee
, Wei Jan Huang
, Wan Wan Lin
, Shoei Sheng Lee
, Chung Hsiung Chen

研究成果: 雜誌貢獻 › 文章 › 同行評審

78 引文斯高帕斯（Scopus）

摘要

Seven diarylheptylamine (12a-g) and four diarylheptanoid analogs (3-5, 9), structurally related to the natural anti-inflammatory agent oregonin (1), have been prepared from curcumin (2) for evaluation of their activity against the expression of iNOS and COX-2. Diarylheptylamine 12b and diarylheptanoid analogs can inhibit iNOS and COX-2 responses of LPS, although less potently than 1. These compounds, however, possess stronger potency than 1 against COX-2-derived PGE₂ formation, of which hexahydrocurcumin (4) is the most potent one with an IC₅₀ value of 0.7 μM.

原文	英語
頁（從 - 到）	6175-6181
頁數	7
期刊	Bioorganic and Medicinal Chemistry
卷	13
發行號	22
DOIs	https://doi.org/10.1016/j.bmc.2005.06.058
出版狀態	已發佈 - 11月 15 2005

ASJC Scopus subject areas

生物化學
分子醫學
分子生物學
藥學科學
藥物發現
臨床生物化學
有機化學

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10.1016/j.bmc.2005.06.058

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引用此

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title = "Preparation and anti-inflammatory activities of diarylheptanoid and diarylheptylamine analogs",

abstract = "Seven diarylheptylamine (12a-g) and four diarylheptanoid analogs (3-5, 9), structurally related to the natural anti-inflammatory agent oregonin (1), have been prepared from curcumin (2) for evaluation of their activity against the expression of iNOS and COX-2. Diarylheptylamine 12b and diarylheptanoid analogs can inhibit iNOS and COX-2 responses of LPS, although less potently than 1. These compounds, however, possess stronger potency than 1 against COX-2-derived PGE2 formation, of which hexahydrocurcumin (4) is the most potent one with an IC50 value of 0.7 μM.",

keywords = "Anti-inflammatory activity, Curcumin, Diarylheptanoid, Diarylheptylamine, Preparation",

author = "Lee, \{Su Lin\} and Huang, \{Wei Jan\} and Lin, \{Wan Wan\} and Lee, \{Shoei Sheng\} and Chen, \{Chung Hsiung\}",

note = "Funding Information: This work was supported by the National Science Council, Taiwan, ROC, under Grant NSC 92-2320-B-002-082. ",

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AU - Lin, Wan Wan

AU - Lee, Shoei Sheng

AU - Chen, Chung Hsiung

N1 - Funding Information: This work was supported by the National Science Council, Taiwan, ROC, under Grant NSC 92-2320-B-002-082.

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KW - Curcumin

KW - Diarylheptanoid

KW - Diarylheptylamine

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Preparation and anti-inflammatory activities of diarylheptanoid and diarylheptylamine analogs

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ASJC Scopus subject areas

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