Evaluation of Anti‐inflammatory and Analgesic Activity of a Novel Rigid 3, 4‐Dihydroxy Chalcone in Mice

Heidari, Mahnaz; Foroumadi, Alireza; Amirabadi, A.; Samzadeh‐Kermani, Alireza; Azimzadeh, Behzad Sarvar; Eskandarizadeh, Ali

doi:10.1111/j.1749-6632.2009.04904.x

Cited by 31 publications

(16 citation statements)

References 19 publications

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“…27, 28 They have been reported to possess many biological properties including anti-cancer 29, 30 , anti-malarial 31, 32 , anti-inflammatory 33–35 , antileishmanial 33–35 , anti-tuberclulosis 36 , nitric oxide inhibition 37, 38 , anti-mitotic 39 , analgesic, antipyretic, antioxidant 40–43 , antibacterial, anti-HIV 44 , antifungal 45 and antiprotozoal activities. 46–48 They are also reported to be gastric protectant 49 , anti-mutagenic, and anti-tumorogenic.…”

Section: Introductionmentioning

confidence: 99%

Novel Chalcone Derivatives as Potent Nrf2 Activators in Mice and Human Lung Epithelial Cells

et al. 2011

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Nrf2-mediated activation of antioxidant response element is a central part of molecular mechanisms governing the protective function of phase II detoxification and antioxidant enzymes against carcinogenesis, oxidative stress and inflammation. Nrf2 is sequestered in the cytoplasm by its repressor, Keap1. We have designed and synthesized novel chalcone derivatives as Nrf2 activators. The potency of these compounds was measured by the expression of Nrf2 dependent antioxidant genes, GCLM, NQO1 and HO1, in human lung epithelial cells; while the cytotoxicity was analyzed using MTT assay. In vivo potency of identified lead compounds to activate Nrf2 was evaluated using mouse model. Our studies showed 2-trifluoromethyl-2’-methoxychalone (2b) to be a potent activator of Nrf2, both, in vitro and in mice. Additional experiments showed that the activation of Nrf2 by this compound is independent of reactive oxygen species or redox changes. We have discussed a quantitative structure-activity relationship and proposed a possible mechanism of Nrf2 activation.

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Section: Introductionmentioning

confidence: 99%

Novel Chalcone Derivatives as Potent Nrf2 Activators in Mice and Human Lung Epithelial Cells

et al. 2011

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“…9,10) Many benzofuran derivatives were reported to show potent anti-inflammatory activity and were among COX-2 inhibitors. 11,12) On the other hand, salicylic acid and salicylates exhibit a pronounced anti-inflammatory activity, for example the salicylanilides A and B are selective inhibitors of interlukin-12 (IL-12) p40 production which is a subunit component of IL-12 and IL-6-23. IL-12 is involved in type 1 helper T cell (TH1) mediated inflammation in both normal immune defence as well as inflammatory diseases such as rheumatoid activities, asthma, psoriases and Crohn's disease.…”

mentioning

confidence: 99%

Synthesis and Anti-inflammatory Activity of Some Benzofuran and Benzopyran-4-one Derivatives

Ragab¹,

Eid²,

Hassan³

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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New series of furosalicylic acids 3a-c, furosalicylanilides 6a-n, furobenzoxazines 8a-f, 1-benzofuran-3-arylprop-2-en-1-ones 12a,b, 6-(aryl-3-oxoprop-1-enyl)-4H-chromen-4-ones 16a-c and 6-[6-aryl-2-thioxo-2,5-dihydropyrimidin-4-yl]-4H-chromen-4-ones 17a-c were synthesized. Anti-inflammatory activity evaluation was performed using carrageenan-induced paw edema model in rats and prostaglandin E 2 (PGE 2 ) synthesis inhibition activity. Some of the tested compounds revealed comparable activity with less ulcerogenic effect than Diclofenac at a dose 100 mg/kg. All the synthesized compounds were docked on the active site of cyclooxygenase-2 (COX-2) enzyme and most of them showed good interactions with the amino acids of the active site comparable to the interactions exhibited by Diclofenac.

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“…The intensity of the apparatus was set to 50 and a cut off value of 10 s was considered to lessen the animals suffer. In one group of mice, Naloxone (4 mg/kg, sc) was used as morphine antagonist 15 min before administration of the test compound, 6f (50 mg/kg, ip) (Heidari et al, 2009;Sharifzadeh et al, 2006). The whole procedure was in accord with the ethics rules of Tehran University of Medical Sciences.…”

Section: Tail Flick Testmentioning

confidence: 99%

Antinociceptive activity of some 1,4-substituted piperidine derivatives using tail flick method in mice

Sakhteman¹,

Sharifzadeh²,

Moradi³

et al. 2011

Afr. J. Pharm. Pharmacol.

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We have examined the potential antinociceptive effects of some piperidine derivatives (6a-f), using tail flick method in mice. Morphine was used as positive control drug. The results showed that compound 6b, having a bromine atom at 4 position, was the most active agent tested. The activity of this compound at 50 mg/kg was comparable to morphine (3 mg/kg). Based on the similarities between our compounds and meperidine like structures such as fentanyl, a group of mice was treated with naloxone before administration of 6f. It was concluded that opioid receptors could be the dominant mechanism for the antinociceptive activity of these types of structures. Electrostatic map, distance analysis and superimposition between fentanyl and compound 6b were also studied.

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Evaluation of Anti‐inflammatory and Analgesic Activity of a Novel Rigid 3, 4‐Dihydroxy Chalcone in Mice

Cited by 31 publications

References 19 publications

Novel Chalcone Derivatives as Potent Nrf2 Activators in Mice and Human Lung Epithelial Cells

Novel Chalcone Derivatives as Potent Nrf2 Activators in Mice and Human Lung Epithelial Cells

Synthesis and Anti-inflammatory Activity of Some Benzofuran and Benzopyran-4-one Derivatives

Antinociceptive activity of some 1,4-substituted piperidine derivatives using tail flick method in mice

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