6b,11b-Dihydroxy-6b,11b-dihydro-7H-indeno[1,2-b]naphtho[2,1-d]furan-7-one (DHFO), a small molecule targeting NF-κB, demonstrates therapeutic potential in immunopathogenic chronic inflammatory conditions

Mathew, Geetha; Jacob, Anija; Durgashivaprasad, Ega; Reddy, Neetinkumar D.; Unnikrishnan, M.K.

doi:10.1016/j.intimp.2012.10.028

Cited by 21 publications

(16 citation statements)

References 29 publications

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“…Other prostaglandin‐independent mechanisms may be involved in the diclofenac‐induced anti‐inflammation (Gan, ; Ortiz, ; Ortiz et al, , ; Veale et al, ; Voilley, ). Diclofenac can reduce leucocyte and neutrophil counts (Mathew, Jacob, Durgashivaprasad, Reddy, & Unnikrishnan, ) and affect the rolling, sticking, and migrating capacity of leukocytes after a carrageenan stimulus (Martinez, Aparecida De Oliveira, & Fortes, ).…”

Section: Discusionmentioning

confidence: 99%

Synergistic interaction between docosahexaenoic acid and diclofenac on inflammation, nociception, and gastric security models in rats

Miranda-Lara

Ortiz

Rodríguez-Ramos

et al. 2018

Drug Development Research

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Preclinical Research & Development The addition of polyunsaturated fatty acids to nonsteroidal anti-inflammatory drugs can increase their antinociceptive activity and produce a gastroprotective effect. The aim of the present study was to examine the effects of the interaction between docosahexaenoic acid (DHA) and diclofenac on inflammation (fixed ratios 1:1, 1:3, and 3:1), nociception (fixed ratio 1:3), and gastric injury in rats. DHA, diclofenac, or combinations of DHA and diclofenac produced anti-inflammatory and antinociceptive effects in rat. The administration of diclofenac produced significant gastric damage, but this effect was not observed with either DHA or the DHA-diclofenac combinations. Effective dose (ED ) values were estimated for each individual drug and analyzed isobolographically. The anti-inflammatory experimental ED values were 6.97 mg/kg (1:1 fixed ratio), 1.1 mg/kg (1:3 fixed ratio), and 11.34 mg/kg (3:1 fixed ratio). These values were significantly lower (p < .05) than the theoretical ED values: 67.94 mg/kg (1:1), 35.37 mg/kg (1:3), and 100.51 mg/kg (3:1). The antinociceptive experimental value was 1.25 mg/kg (1:3 fixed ratio). This value was lower (p < .05) than the theoretical ED , which was predicted to be 15.92 mg/kg. These data indicate that the DHA-diclofenac combinations interact at the systemic level, produce minor gastric damage, and potentially have therapeutic advantages for the clinical treatment of inflammatory pain.

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Section: Discusionmentioning

confidence: 99%

Synergistic interaction between docosahexaenoic acid and diclofenac on inflammation, nociception, and gastric security models in rats

Miranda-Lara

Ortiz

Rodríguez-Ramos

et al. 2018

Drug Development Research

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“…The murine macrophage RAW264.7 cell line was purchased from the National Centre for Cell Science (NCCS; Pune, India). Cells were maintained and viability was determined as described previously . In vitro anti‐inflammatory activity of PAT1 and NAT1 was evaluated in the RAW264.7 cell line as described previously .…”

Section: Methodsmentioning

confidence: 99%

“…Cells were maintained and viability was determined as described previously . In vitro anti‐inflammatory activity of PAT1 and NAT1 was evaluated in the RAW264.7 cell line as described previously . Briefly, 5 × 10 4 cells/well were incubated in a 96‐well black plate with different concentrations of NAT1 or PAT1 (3.125–200 µmol/L), standard inhibitors (see below), or vehicle for 2 h before the addition of 10 µg/mL LPS.…”

Section: Methodsmentioning

confidence: 99%

Dose‐related antihyperglycemic and hypolipidemic effects of two novel thiazolidin‐4‐ones in a rodent model of metabolic syndrome

Karot

Surenahalli

Kishore

et al. 2015

Journal of Diabetes

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“…[14] Briefly, 5 × 10 4 cells/well were treated with various concentrations of test compounds and LPS (10 μg/ml) for 20 h. Nω-nitro-L-arginine methyl ester hydrochloride (L-NAME hydrochloride) and diphenylene iodonium (DPI) (both from Sigma-Aldrich Co. LLC., St.Louis, MO, USA) were used as standards.…”

Section: Methodsmentioning

confidence: 99%

Novel 2,5-disubstituted-1,3,4-oxadiazoles as anti-inflammatory drugs

et al. 2014

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Objective:1,3,4-oxadiazole ring is a versatile moiety with a wide range of pharmacological properties. The present work deals with the synthesis and evaluation of the anti-inflammatory activity of two novel 2,5-disubstituted-1,3,4-oxadiazoles (OSD and OPD).Materials and Methods:Carrageenan-induced rat hind paw edema was employed as an acute model of inflammation. For evaluating sub-acute anti-inflammatory activity, carrageenan-induced inflammation in rat air pouch was employed. Complete Freund's adjuvant-induced arthritis in rats was used as a model of chronic inflammation. To evaluate in vitro anti-inflammatory activity, lipopolysaccharide (LPS)-stimulated RAW264.7 cells were used.Results:OSD (100 mg/kg) reduced carrageen-induced paw edema by 60%, and OPD (100 mg/kg) produced a modest 32.5% reduction. OSD also reduced leukocyte influx and myeloperoxidase in carrageenan-induced rat air pouch model. In complete Freund's adjuvant-induced arthritis model, both OSD and OPD (200 mg/kg for 14 days) reduced paw edema and NO levels. In LPS-stimulated RAW264.7 cells, OSD and OPD inhibited formation of nitric oxide and reactive oxygen species, with OPD showing a better activity in comparison to OSD.Conclusions:OSD was the better of the two compounds in in vivo models of inflammation. The o-phenol substitution at position 2 of oxadiazole ring in OSD may be responsible for its better in vivo anti-inflammatory activity. The ability of the compounds to inhibit LPS-induced pro-inflammatory mediator release suggests an anti-inflammatory mechanism targeting LPS-TLR4-NF-κB signalling pathway, which needs to be explored in detail. The disparate efficacy in vitro and in vivo also requires in-depth evaluation of the pharmacokinetics of these novel oxadiazoles.

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6b,11b-Dihydroxy-6b,11b-dihydro-7H-indeno[1,2-b]naphtho[2,1-d]furan-7-one (DHFO), a small molecule targeting NF-κB, demonstrates therapeutic potential in immunopathogenic chronic inflammatory conditions

Cited by 21 publications

References 29 publications

Synergistic interaction between docosahexaenoic acid and diclofenac on inflammation, nociception, and gastric security models in rats

Synergistic interaction between docosahexaenoic acid and diclofenac on inflammation, nociception, and gastric security models in rats

Dose‐related antihyperglycemic and hypolipidemic effects of two novel thiazolidin‐4‐ones in a rodent model of metabolic syndrome

Novel 2,5-disubstituted-1,3,4-oxadiazoles as anti-inflammatory drugs

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