Inhibitory Effects of N-Amido-3,3-difluoropyrrolidin-2-ones on LPS-induced Nitric Oxide Production in RAW 264.7 Macrophages

Aim: Over the years, indole has proved to be a versatile scaffold for the design of molecules acting as anti-inflammatory agents. Materials & Methods: A small library of 3-amino-alkylated indoles has been obtained by an optimized Mannich green approach. The anti-inflammatory activity of the new 3-amino-alkylated indoles, GLYC 0–10, was evaluated in RAW 264.7 macrophages. Results: The anti-inflammatory activity of the new 3-amino-alkylated indoles, GLYC 0–10, was evaluatedn and, among them, GLYC 4, 5 and 9 displayed the greatest inhibitory effects on nitric oxide production, with IC50 values of 5.41, 4.22 and 6.3 μM, respectively. Conclusion: Our outcomes, overall, highlight the importance of the indole substitution in the anti-inflammatory activity of these compounds, exerted by acting on the interlinked NF-κB/ERK1/2 pathways.

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Phenolic components fromRhus parviflorafruits and their inhibitory effects on lipopolysaccharide-induced nitric oxide production in RAW 264.7 macrophages

Natural Product Research ◽

10.1080/14786419.2013.814050 ◽

2013 ◽

Vol 27 (23) ◽

pp. 2244-2247 ◽

Cited By ~ 6

Author(s):

Sabina Shrestha ◽

Dae-Young Lee ◽

Ji-Hae Park ◽

Jin-Gyeong Cho ◽

Dong-Sung Lee ◽

...

Keyword(s):

Nitric Oxide ◽

Raw 264.7 ◽

Nitric Oxide Production ◽

Inhibitory Effects ◽

Raw 264.7 Macrophages ◽

Oxide Production ◽

Phenolic Components

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Inhibitory Effect of Trimidox on Lipopolysaccharide-Induced Nitric Oxide Production in RAW 264.7 Macrophages

Journal of Pharmacological Sciences ◽

10.1254/jphs.sc0070073 ◽

2007 ◽

Vol 104 (3) ◽

pp. 278-281 ◽

Cited By ~ 3

Author(s):

Syu-ichi Kanno ◽

Mai Kakuta ◽

Yasue Kitajima ◽

Yuu Osanai ◽

Kaori Kurauchi ◽

...

Keyword(s):

Nitric Oxide ◽

Inhibitory Effect ◽

Raw 264.7 ◽

Nitric Oxide Production ◽

Raw 264.7 Macrophages ◽

Oxide Production

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Pomegranate juice down‐regulates nitric oxide production in RAW 264.7 macrophages challenged with lipopolysaccharides

The FASEB Journal ◽

10.1096/fasebj.20.4.a606 ◽

2006 ◽

Vol 20 (4) ◽

Author(s):

Jennifer A Powell ◽

Sachin Mahajan ◽

Shirin Hooshmand ◽

Brenda J Smith ◽

Bahram H Arjmandi ◽

...

Keyword(s):

Nitric Oxide ◽

Pomegranate Juice ◽

Raw 264.7 ◽

Nitric Oxide Production ◽

Raw 264.7 Macrophages ◽

Oxide Production

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Diarylheptanoids of Curcuma comosa with Inhibitory Effects on Nitric Oxide Production in Macrophage RAW 264.7 Cells

Natural Product Communications ◽

10.1177/1934578x1501000123 ◽

2015 ◽

Vol 10 (1) ◽

pp. 1934578X1501000 ◽

Cited By ~ 1

Author(s):

Nilubon Sornkaew ◽

Yuan Lin ◽

Fei Wang ◽

Guolin Zhang ◽

Ratchanaporn Chokchaisiri ◽

...

Keyword(s):

Nitric Oxide ◽

Inhibitory Activity ◽

Raw 264.7 Cells ◽

Racemic Mixture ◽

Raw 264.7 ◽

Nitric Oxide Production ◽

Inhibitory Effects ◽

Curcuma Comosa ◽

Oxide Production ◽

Potent Inhibitory Activity

Eight new diarylheptanoids, a 1.2:1 mixture of (3S)- and (3 R)-1-(4-hydroxyphenyl)-7-phenyl-(4 E,6 E)-4,6-heptadien-3-ol (1a and 1b), a racemic mixture of (3S)- and (3 R)-1-(4-hydroxyphenyl)-3-methoxy-7-phenyl-(4 E,6 E)-4,6-heptadiene (2a and 2b), a ca. 1:1 mixture of (3S)- and (3 R)-1-(4-hydroxy-3-methoxyphenyl)-3-methoxy-7-phenyl)-(4 E,6 E)-4,6-heptadiene (3a and 3b), 3-acetoxy-1-(3,4-dihydroxyphenyl)-7-phenylheptan-5-ol (4), (3 R)-1-(4,5-dihydroxyphenyl)-7-phenyl-(6 E)-6-hepten-3,2′-epoxide (5), and thirteen known diarylheptanoids, 6-12, a 3:1 mixture of 13a and 13b, and 14-17, were isolated from the rhizomes of Curcuma comosa from Sakon Nakhon, northeastern part of Thailand. The isolated compounds were evaluated for their antiinflammatory activities on the inhibition of lipopolysaccharide-induced nitric oxide production in macrophage RAW 264.7 cells and the diarylheptanoids 1a and 1b mixture and 14 exhibited potent inhibitory activity.

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