A novel selective prostaglandin E2 synthesis inhibitor relieves pyrexia and arthritis in Guinea pigs inflammatory models

Sugita, Ryusuke; Kubota, Kazufumi; Sugimoto, Kotaro; Tachida, Yuki; Shibayama, Takahiro; Kiho, Toshihiro; Kawakami, Katsuhiro; Shimada, Kohei

doi:10.1016/j.jphs.2016.01.009

Cited by 3 publications

(2 citation statements)

References 29 publications

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“…Other papers reported that mPGES-1 deficiency or a pharmacological inhibition of mPGES-1 also shows the prostanoids' redirection [ 24 – 27 ]. However, the inhibitory profile against each prostanoid differs among them [ 28 ], suggesting that reactivity may differ depending on the expression profile of terminal synthases in target cells or tissues.…”

Section: Discussionmentioning

confidence: 99%

Simultaneous Inhibition of PGE₂and PGI₂Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models

Sugita

Kuwabara

Kubota

et al. 2016

Mediators of Inflammation

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Prostaglandin E2 (PGE2) is well known as a mediator of inflammatory symptoms such as fever, arthritis, and inflammatory pain. In the present study, we evaluated the analgesic effect of our selective PGE2 synthesis inhibitor, compound I, 2-methyl-2-[cis-4-([1-(6-methyl-3-phenylquinolin-2-yl)piperidin-4-yl]carbonyl amino)cyclohexyl] propanoic acid, in rat yeast-induced acute and adjuvant-induced chronic inflammatory pain models. Although this compound suppressed the synthesis of PGE2 selectively, no analgesic effect was shown in both inflammatory pain models. Prostacyclin (PGI2) also plays crucial roles in inflammatory pain, so we evaluated the involvement of PGI2 signaling in rat inflammatory pain models using prostacyclin receptor (IP) antagonist, RO3244019. RO3244019 showed no analgesic effect in inflammatory pain models, but concomitant administration of compound I and RO3244019 showed analgesic effects comparable to celecoxib, a specific cyclooxygenase- (COX-) 2 inhibitor. Furthermore, coadministration of PGE2 receptor 4 (EP4) antagonist, CJ-023423, and RO3244019 also showed an analgesic effect. These findings suggest that both PGE2 signaling, especially through the EP4 receptor, and PGI2 signaling play critical roles in inflammatory pain and concurrent inhibition of both signals is important for suppression of inflammatory hyperalgesia.

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Section: Discussionmentioning

confidence: 99%

Simultaneous Inhibition of PGE₂and PGI₂Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models

Sugita

Kuwabara

Kubota

et al. 2016

Mediators of Inflammation

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“…Nevertheless the extract showed antpyretic activity in dose dependant manner. Prostaglandins have been known since long for their role in the pyrexia (Milton, 1982;Sugita et al, 2016;Engström et al, 2012). So it is obvious that inhibition in prostaglandin pathway could lead to antipyretic potential.…”

Section: Controlmentioning

confidence: 99%

Raphanus sativus L. Var. caudatus as an Analgesic and Antipyretic Agent in Animal Models

Younus¹

2022

PJZ

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Raphanus sativus L. Var. caudatus belongs to Radish plant has been reported for analgesic potential thus it might have antipyretic potential. The present investigation was undertaken to evaluate analgesic and antipyretic activities of ethanol extract of Raphanus sativus var. caudatus in albino mice. The analgesic and antipyretic activities were determined at three different doses (50, 100 and 200 mg/kg) using different pain models (writhing induced, tail flick) and yeast induced pyrexia tests, respectively. The extract exhibited significant (p < 0.05) in vivo analgesic and antipyretic potential in term of % writhes inhibition, increased latency time and reduced rectal temperature when compared with control. The extract displayed noteworthy analgesic and antipyretic capabilities especially at the dose of 200 mg/kg that are almost comparable with standard drug (aspirin). Although the finding of present investigation highlighted the medicinal importance of the plant but there is dire need to carry out the fractional extraction of crude extract with different solvents based on polarity to identify the active constituents with exact analgesic and antipyretic mechanistic action of Raphanus caudatus as well as clinical trials are required in future for medicinal use of the plant in humans.

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The Analgesic Effect of Aspirin on Inflammatory Pain in Rats Is Affected by Pain Intensity and Administration Timing

et al. 2020

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Non-steroidal anti-in‰ammatory drugs (NSAIDs) are widely known as painkillers. The analgesic action of NSAIDs is attributable to the inhibition of prostaglandin synthesis that occurs in response to blocking cyclooxygenase activity. The eŠective dose of NSAIDs can vary depending on pain intensity and administration timing; however, there are few studies on this. This study aimed to elucidate whether the analgesic eŠect of NSAIDs changes depending on the situation in which they are taken and we focused on the NSAID, aspirin (ASP). In a rat model of brewer's yeast-induced in‰ammation, pain caused by 20％ (w/v) brewer's yeast-treatment was deˆned as``strong pain'' and that caused by 2.5％ (w/v) was deˆned as``weak pain''. The analgesic eŠect of ASP (low-dose; 44 mg/kg or high-dose; 66 mg/kg) against strong pain was dose-dependent, but that against weak pain was the same. Furthermore, we deˆned drug administration after 3 h of brewer's yeast-treatment as``late administration'' and that after 20 min as``early administration''. In the case of strong pain, the analgesic eŠect of``late ASP administration'' was dose-dependent, but that of``early ASP administration'' was the same. These results suggest that low-dose NSAIDs have an analgesic eŠect against weak pain or when taken early.

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A novel selective prostaglandin E2 synthesis inhibitor relieves pyrexia and arthritis in Guinea pigs inflammatory models

Cited by 3 publications

References 29 publications

Simultaneous Inhibition of PGE₂and PGI₂Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models

Simultaneous Inhibition of PGE₂and PGI₂Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models

Raphanus sativus L. Var. caudatus as an Analgesic and Antipyretic Agent in Animal Models

The Analgesic Effect of Aspirin on Inflammatory Pain in Rats Is Affected by Pain Intensity and Administration Timing

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A novel selective prostaglandin E2 synthesis inhibitor relieves pyrexia and arthritis in Guinea pigs inflammatory models

Cited by 3 publications

References 29 publications

Simultaneous Inhibition of PGE2and PGI2Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models

Simultaneous Inhibition of PGE2and PGI2Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models

Raphanus sativus L. Var. caudatus as an Analgesic and Antipyretic Agent in Animal Models

The Analgesic Effect of Aspirin on Inflammatory Pain in Rats Is Affected by Pain Intensity and Administration Timing

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Simultaneous Inhibition of PGE₂and PGI₂Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models

Simultaneous Inhibition of PGE₂and PGI₂Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models