Inhibitory Effects of 4′-Demethylnobiletin, a Metabolite of Nobiletin, on 12-<i>O</i>-Tetradecanoylphorbol-13-acetate (TPA)-Induced Inflammation in Mouse Ears

Wu, Xian; Song, Mingyue; Rakariyatham, Kanyasiri; Zheng, Jinkai; Wang, Minqi; Xu, Fei; Gao, Zili; Xiao, Hang

doi:10.1021/acs.jafc.5b05156

Cited by 39 publications

(32 citation statements)

References 42 publications

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“…In LPS-treated RAW 264.7 macrophages, 4′-demethylnobiletin downregulates the expression of proinflammatory cytokines IL-1 β , IL-6, PGE2, iNOS, and COX-2 and inhibits NF- κ B and AP-1 nuclear translocation, while upregulating the expression of transcription factor Nrf2 and its dependent genes HO-1 and NQO1 [ 83 ]. This is supported by the anti-inflammatory effects of 4′-demethylnobiletin on TPA-treated mice ear inflammation through inhibition of PI3K/Akt/ERK phosphorylation [ 84 ].…”

Section: The Metabolites Of Nobiletinmentioning

confidence: 99%

The Multifunctional Effects of Nobiletin and Its Metabolites In Vivo and In Vitro

Huang

Shi

et al. 2016

Evidence-Based Complementary and Alternative Medicine

124

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Nobiletin (NOB) chemically known as 5,6,7,8,3′,4′-hexamethoxyflavone is a dietary polymethoxylated flavonoid found in Citrus fruits. Recent evidences show that NOB is a multifunctional pharmaceutical agent. The various pharmacological activities of NOB include neuroprotection, cardiovascular protection, antimetabolic disorder, anticancer, anti-inflammation, and antioxidation. These events may be underpinned by modulation of signaling cascades, including PKA/ERK/MEK/CREB, NF-κB, MAPK, Ca2+/CaMKII, PI3K/Akt1/2, HIF-1α, and TGFβ signaling pathways. The metabolites may exhibit stronger beneficial effects than NOB on diseases pathogenesis. The biological activities of NOB have been clarified on many systems. This review aims to discuss the pharmacological effects of NOB with specific mechanisms of actions. NOB may become a promising candidate for potential drug development. However, further investigations of NOB on specific intracellular targets and clinical trials are still needed, especially for in vivo medical applications.

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Section: The Metabolites Of Nobiletinmentioning

confidence: 99%

The Multifunctional Effects of Nobiletin and Its Metabolites In Vivo and In Vitro

Huang

Shi

et al. 2016

Evidence-Based Complementary and Alternative Medicine

124

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“…In the mouse ear edema model, 20 µL of acetone vehicle was topically applied to the right ear and 20 µL of the treatment compounds at three different concentrations, which were dissolved in acetone, were used 5 minutes later after 20 µL of TPA (0.125 µg/mL in acetone) was previously applied to induce the inflammation model. 42 , 43 Dexamethasone at a concentration of 2,500 µg/mL (6.37 µmol/mL) in acetone was used as the positive control. Then, all of the mice were maintained at a standard condition and sacrificed 6 hours after TPA treatment.…”

Section: Methodsmentioning

confidence: 99%

The biological evaluation of fusidic acid and its hydrogenation derivative as antimicrobial and anti-inflammatory agents

Wu¹,

He²,

Hong³

et al. 2018

IDR

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BackgroundFusidic acid (FA) (WU-FA-00) is the only commercially available antimicrobial from the fusidane family that has a narrow spectrum of activity against Gram-positive bacteria.MethodsHerein, the hydrogenation derivative (WU-FA-01) of FA was prepared and both compounds were examined against a panel of six bacterial strains. In addition, their anti-inflammatory properties were evaluated using a 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema model.ResultsThe results of the antimicrobial assay revealed that both WU-FA-00 and WU-FA-01 displayed a high level of antimicrobial activity against Gram-positive strains. Moreover, killing kinetic studies were performed and the results were in accordance with the minimum inhibitory concentration and minimum bactericidal concentration results. We also demonstrated that the topical application of WU-FA-00 and WU-FA-01 effectively decreased TPA-induced ear edema in a dose-dependent manner. This inhibitory effect was associated with the inhibition of TPA-induced upregulation of proinflammatory cytokines IL-1β, TNF-α, and COX-2. WU-FA-01 significantly suppressed the expression levels of p65, IκB-α, and p-IκB-α in the TPA-induced mouse ear model.ConclusionOverall, our results showed that WU-FA-00 and WU-FA-01 not only had effective antimicrobial activities in vitro, especially to the Gram-positive bacteria, but also possessed strong anti-inflammatory effects in vivo. These results provide a scientific basis for developing FA derivatives as antimicrobial and anti-inflammatory agents.

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“…The mice were divided into nine groups: each group consisted of six mice, including a blank group, a TPA group, a dexamethasone group, and six groups for WU-FA-00 and WU-FA-01. In the mouse ear edema model, 20 μL of acetone vehicle was topically applied to the right ear, and 20 μL of the treatment compounds at three different concentrations, which were dissolved in acetone, were used 5 min later after 20 μL of TPA (0.125 μg/mL in acetone) was previously applied to induce the inflammation model (33, 34). Dexamethasone at a concentration of 2.5 μg/mL (6.37 μmol/mL) in acetone was used as the positive control.…”

Section: Methodsmentioning

confidence: 99%

The Biological Evaluation of Fusidic Acid and Its Hydrogenation Derivative as Antimicrobial and Anti-inflammatory Agents

Hong

et al. 2018

Preprint

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18Fusidic acid (WU-FA-00) is the only commercially available antimicrobial from 19 the fusidane family that has a narrow spectrum of activity against Gram-positive 20 bacteria. Herein, the hydrogenation derivative (WU-FA-01) of fusidic acid was 21 prepared, and both compounds were examined against a panel of six bacterial strains. 22In addition, their anti-inflammation properties were evaluated using a 23 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema model. The 24 results of the antimicrobial assay revealed that both WU-FA-00 and WU-FA-01 25 displayed a high level of antimicrobial activity against Gram-positive strains. 26 Moreover, killing kinetic studies were performed, and the results were in accordance 27 with the MIC and MBC results. We also demonstrated that the topical application of 28 WU-FA-00 and WU-FA-01 effectively decreased TPA-induced ear edema in a 29 dose-dependent manner. This inhibitory effect was associated with the inhibition of 30 TPA-induced up-regulation of pro-inflammation cytokines IL-1β, TNF-α and COX-2. 31 WU-FA-01 significantly suppressed the expression levels of p65, IκB-α, and p-IκB-α 32 in the TPA-induced mouse ear model. Overall, our results showed that WU-FA-00 and 33 WU-FA-01 not only had effective antimicrobial activities in vitro, especially to the 34 Gram-positive bacteria, but also possessed strong anti-inflammatory effects in vivo.35

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Inhibitory Effects of 4′-Demethylnobiletin, a Metabolite of Nobiletin, on 12-O-Tetradecanoylphorbol-13-acetate (TPA)-Induced Inflammation in Mouse Ears

Cited by 39 publications

References 42 publications

The Multifunctional Effects of Nobiletin and Its Metabolites In Vivo and In Vitro

The Multifunctional Effects of Nobiletin and Its Metabolites In Vivo and In Vitro

The biological evaluation of fusidic acid and its hydrogenation derivative as antimicrobial and anti-inflammatory agents

The Biological Evaluation of Fusidic Acid and Its Hydrogenation Derivative as Antimicrobial and Anti-inflammatory Agents

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