Feprazone, a new anti-inflammatory agent. Studies of potency and gastrointestinal tolerance.

Fletcher, M R; Loebl, W Y; Scott, J. T.

doi:10.1136/ard.34.2.190

Cited by 22 publications

(3 citation statements)

References 6 publications

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“…It also reduces the production of prostaglandin E2 (PGE 2 ) in endothelial cells . Feprazone has been used for the treatment of multiple kinds of inflammatory diseases . In clinical trials, Feprazone has been utilized to treat osteoarthritis (OA) and rheumatoid arthritis with positive data.…”

Section: Introductionmentioning

confidence: 99%

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Feprazone Ameliorates TNF-α-Induced Loss of Aggrecan via Inhibition of the SOX-4/ADAMTS-5 Signaling Pathway

Xiong

Liu

et al. 2021

ACS Omega

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Background: Arthritis is a cartilage degenerative disease that is mainly induced by the degradation of the cartilage extracellular matrix (ECM), which is found to be regulated by the expression level of a disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMT-5), an enzyme degrading Aggrecans in the ECM. Feprazone is a classic nonsteroidal anti-inflammatory drug with promising efficacy in arthritis. The present study aims to investigate the protective effect of Feprazone on the degraded Aggrecan in the human chondrocytes induced with tumor necrosis factor-α (TNF-α) and to clarify the underlying mechanism. Methods: To investigate the effect of Feprazone, the CHON-001 chondrocytes were stimulated with TNF-α (10 ng/mL) in the presence or absence of Feprazone (3, 6 μM) for 24 h. Mitochondrial membrane potential was evaluated using the Rhodamine 123 assay. The gene expressions of interleukin-1β (IL-1β), interleukin-8 (IL-8), monocyte chemotactic protein 1 (MCP-1), and ADAMTS-5 in the treated chondrocytes were detected using real-time quantitative polymerase chain reaction (qRT-PCR), and the protein levels of these targets were determined using enzyme-linked immunosorbent assay (ELISA). SOX-4 was knocked down by transfecting the siRNA into the chondrocytes. Western blot analysis was utilized to evaluate the expression levels of SOX-4, Aggrecan, and protein kinase C (PKCα). Results: First, the reduced mitochondrial membrane potential (ΔΨm) and secretion of proinflammatory factors (IL-1β, IL-8, and MCP-1) induced by TNF-α were significantly reversed by treatment with Feprazone. Second, the expression of Aggrecan was significantly decreased by stimulation with TNF-α via upregulation of ADAMTS-5 but was dramatically reversed by the introduction of Feprazone. Third, we found that TNF-α elevated the expression of ADAMTS-5 by upregulating SOX-4, which was observed to be related to the activation of PKCα. Lastly, the elevated expression of SOX-4 induced by TNF-α was significantly reversed by Feprazone. Conclusions: Feprazone might ameliorate TNF-α-induced loss of Aggrecan via the inhibition of the SOX-4/ADAMTS-5 signaling pathway.

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Section: Introductionmentioning

confidence: 99%

“…15 Feprazone has been used for the treatment of multiple kinds of inflammatory diseases. 16 In clinical trials, Feprazone has been utilized to treat osteoarthritis (OA) 17 and rheumatoid arthritis 18 with positive data. However, the antiarthritis mechanism remains unknown.…”

Section: ■ Introductionmentioning

confidence: 99%

Feprazone Ameliorates TNF-α-Induced Loss of Aggrecan via Inhibition of the SOX-4/ADAMTS-5 Signaling Pathway

Xiong

Liu

et al. 2021

ACS Omega

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“…Dissolution of drug from a suppository may be the rate-limiting step for the overall absorption process and therefore particle size and suppositories formulations become significant factors affecting the absorption rate. The purpose of the study was to compare the bioavailability of the feprazone (4 -prenyl -1,2 -diphenyl -3,5 -pyrazolidinedione), effective drug in rheumatoid arthritis (Cherie Ligniere, Colombo, Carabba, Ferrari & Robotti, 1972;Billings, Burry, Grahame & Berry, 1975;Fletcher, Loebl & Scott, 1975;Sturrock, Isaacs & Hart, 1975), after rectal administration of three lots of suppositories with different formulations of the base and different particle size.…”

Section: Rectal Administration Of Feprazone In Healthy Volunteersmentioning

confidence: 99%

Rectal administration of feprazone in healthy volunteers [letter].

Ferrari¹,

Montanari²,

Sala³

et al. 1976

Brit J Clinical Pharma

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LETTERS TO THE EDITORS 339would indicate the presence of a second and longer elimination half life. Any accurate assessment of this longer half life could not be made due to the lack of information between the 8 and 24 h samples. It is clear from this study that the proposed method is capable of simply estimating plasma levels over an extended period after a single oral dose of this drug.The authors wish to thank Professor P. Turner for his encouragement and the use of facilities to carry out the work and to Ayerst Laboratories for samples of tandamine hydrochloride.

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Side-Effects of Anti-Inflammatory Drugs: are they Essential or can they be Circumvented?

Mw¹,

Kd²

1977

Inflammation: Mechanisms and Their Impact on Therapy

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Feprazone, a new anti-inflammatory agent. Studies of potency and gastrointestinal tolerance.

Cited by 22 publications

References 6 publications

Feprazone Ameliorates TNF-α-Induced Loss of Aggrecan via Inhibition of the SOX-4/ADAMTS-5 Signaling Pathway

Feprazone Ameliorates TNF-α-Induced Loss of Aggrecan via Inhibition of the SOX-4/ADAMTS-5 Signaling Pathway

Rectal administration of feprazone in healthy volunteers [letter].

Side-Effects of Anti-Inflammatory Drugs: are they Essential or can they be Circumvented?

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