NCX 2057, a novel NO‐releasing derivative of ferulic acid, suppresses inflammatory and nociceptive responses in <i>in vitro</i> and <i>in vivo</i> models

Ronchetti, Daniela; Borghi, Valentina; Gaitán, Gema; Herrero, Juan F.; Impagnatiello, Francesco

doi:10.1111/j.1476-5381.2009.00324.x

Cited by 34 publications

(26 citation statements)

References 48 publications

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“…Three distinctive motifs (3-methoxy and 4-hydroxy groups on the benzene ring, and the carboxylic acid group) of ferulic acid are responsible for its free radical scavenging capability. It has been also reported that ferulic acid or related ester derivatives inhibited the release of ROS and RNS via suppression of iNOS (Jiang et al, 2009) and COX-2 (Hirata et al, 2005, Ronchetti et al, 2009) in LPS-stimulated macrophages. Its reduced form, ferulaldehyde possesses the same structural characteristic and main molecular motifs as ferulic acid up to the aldehyde group.…”

Section: Reactive Oxygen and Nitrogen Speciesmentioning

confidence: 96%

Anti-Inflammatory Role of Natural Polyphenols and Their Degradation Products

Veres¹

2012

Severe Sepsis and Septic Shock - Understanding a Serious Killer

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Section: Reactive Oxygen and Nitrogen Speciesmentioning

confidence: 96%

Anti-Inflammatory Role of Natural Polyphenols and Their Degradation Products

Veres¹

2012

Severe Sepsis and Septic Shock - Understanding a Serious Killer

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“…Additional evidence of NO-mediated effects in neuropathic pain models was later obtained with compounds possessing both antioxidant and NO-releasing properties (Ronchetti et al, 2009). Other investigators reported the beneficial effect of NO when combined with gabapentin despite the different experimental conditions employed (Curros-Criado and Herrero, 2009).…”

Section: Introductionmentioning

confidence: 98%

Repeated Dosing with NCX1404, a Nitric Oxide-Donating Pregabalin, Re-establishes Normal Nociceptive Responses in Mice with Streptozotocin-Induced Painful Diabetic Neuropathy

Varani

Vincenzi

Targa

et al. 2016

Journal of Pharmacology and Experimental Therapeutics

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NCX1404 [(3S)-5-methyl-3-(((1-(4-(nitrooxy)butanoyloxy)ethoxy) carbonylamino) methyl)hexanoic acid] is a novel nitric oxide (NO)-donating pregabalin that is readily absorbed and processed in vivo to pregabalin and NO. We determined the antiallodynic response of NCX1404 after acute or after 7, 14, and 21 days of repeated daily oral dosing in mice with streptozotocin (STZ)-induced painful diabetic neuropathy (PDN). Pregabalin and its combination with the NO donor isosorbide mononitrate (ISMN) were used for comparison. The blood levels of pregabalin and nitrites, used as surrogate marker of NO release, after NCX1404 or pregabalin dosing were monitored in parallel experiments using liquid chromatography with tandem mass spectrometry (LC-MS/MS). NCX1404 and pregabalin resulted in similar pregabalin levels as it was their antiallodynic activity after acute dosing in STZ mice. However, NCX1404 resulted in disease-modifying properties when administered daily for 21 days, as indicated by the time-and dose-dependent reversal of STZ-induced mechanical allodynia (paw withdrawal threshold [PWT] Veh_21d 5 1.3 6 0.15 g for vehicle; PWT NCX1404_21d 5 1.4 6 0.5 g, 2.9 6 0.2 g* and 4.1 6 0.2 g*, respectively for 19, 63, and 190 mmol/kg, oral gavage [PO] of NCX1404; *P , 0.05 versus vehicle). This effect was not shared by pregabalin at equimolar doses (190 mmol/kg, PO, PWT Pregab_21d 5 1.4 6 0.1 g*, *P , 0.05 versus equimolar NCX1404). In addition, the NO donor ISMN (52.3 mmol/kg, PO) alone or combined with pregabalin (63 mmol/kg) was active at 7 days (PWT Veh_7d 5 1.7 6 0.16 g; PWT ISMN_7d 5 3.9 6 0.34 g*; PWT Pregab_7d 5 1.3 6 0.07 g; PWT ISMN1pregab_7d 5 3.8 6 0.29 g*; *P , 0.05) but not at later time points. The long-term effect of NCX1404 was independent of residual drug exposure and lasted for several days after the treatment was stopped. In summary, like pregabalin, NCX1404 is an effective antiallodynic agent. Differently from pregabalin, repeated dosing of NCX1404 re-established normal nociceptive responses in STZ-induced PDN in mice.

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“…Many studies have indicated that ferulic acid has antioxidant effects, photoprotective effects and antitumor activity, and protects against amyloid peptide toxicity [23][24][25][26][27][28][29][30][31][32][33]. In addition, it has been shown to have antihypertensive activity in spontaneously hypertensive rats.…”

Section: Introductionmentioning

confidence: 99%

Laser-induced carotid artery injury model in the rat for therapeutic agent screening

Chang

Chen

et al. 2011

Lasers Med Sci

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The aims of this study were to establish a rat model of carotid artery injury and to evaluate its suitability for evaluating therapeutic agents active against endothelial proliferation. Wistar-Kyoto rats were injected intravenously with the photochemically reactive dyes rose bengal or Evans blue, and the carotid artery was then focally irradiated with laser light of the appropriate wavelength. Histological sections of the carotid artery were analyzed to determine the appropriate parameters for this model. Ferulic acid was used to assess the suitability of this model for drug screening. No animal died as a result of the photochemical treatment. Endothelial proliferation in the carotid artery was observed in rats injected with rose Bengal and exposed to green laser light. Ferulic acid (400 mg/kg per day) significantly (p<0.05) reduced endothelial proliferation in the carotid artery 28 days after injury in dye-treated animals compared with vehicle-treated animals. This simple experimental rat model is suitable for studying factors inhibiting endothelial thickening after vessel damage and for developing therapeutic strategies active against endothelial proliferation.

show abstract

NCX 2057, a novel NO‐releasing derivative of ferulic acid, suppresses inflammatory and nociceptive responses in in vitro and in vivo models

Cited by 34 publications

References 48 publications

Anti-Inflammatory Role of Natural Polyphenols and Their Degradation Products

Anti-Inflammatory Role of Natural Polyphenols and Their Degradation Products

Repeated Dosing with NCX1404, a Nitric Oxide-Donating Pregabalin, Re-establishes Normal Nociceptive Responses in Mice with Streptozotocin-Induced Painful Diabetic Neuropathy

Laser-induced carotid artery injury model in the rat for therapeutic agent screening

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