Structure-activity Relationship of Indomethacin Derivatives as IDO1 Inhibitors

Obata, Tohru; Shiratani, Sara; Nada, Tomomi; Kasaya, Yayoi; Arisawa, Mitsuhiro; Shuto, Satoshi; Tanaka, Motohiro

doi:10.21873/anticanres.15004

Cited by 5 publications

(4 citation statements)

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“…It had insignificant impact on CNS Indoleamine 2,3 dioxygenase activity but CNS Tryptophan & kynurenine levels become raised after the indomethacin therapy. Similar results are observed by [19,20] who said that it inhibits IDO activity. Previously it was reported that Diclofenac Sodium prevents hepatic tryptophan-2,3-dioxygenase enzyme activity in chronic therapy, whereas augments CNS Indoleamine 2,3 dioxygenase activity following both acute and chronic Diclofenac Sodium therapy, resulting in raised cerebral kynurenic acid and/or quinolinic acid concentrations [22].…”

Section: Discussionsupporting

confidence: 87%

“…IDO act as main immunoregulator & transforms tryptophan into kynurenine, which causes cytotoxicity and apoptosis in tumor histology [15,16]. Indomethacin cox-2 inhibitor exhibited raised IDO1 inhibitory activity, which is beneficial for the malignant cells immunotherapy by suppressing interleukin-10 & prostaglandin E2 [19,20].…”

Section: Discussionmentioning

confidence: 99%

“…IDO1 activity is low in normal tissues while raised in cancers due to induction by interferons [17,18]. Indomethacin cox-2 inhibitor exhibited raised IDO1 inhibitory activity, which is beneficial for the malignant cells immunotherapy by suppressing interleukin-10 & prostaglandin E2 [19,20]. In this investigational study we want to evaluate the effects of indomethacin on IDO activities.…”

Section: Nsaidsmentioning

confidence: 99%

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Effects of Anti-inflammatory Medication on Indoleamine 2,3 Dioxygenase Activity

Dawood

Bano²,

Sundus

et al. 2022

JPRI

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Objective: To study the effects of anti-inflammatory medication on Indoleamine 2,3 dioxygenase activity. Research Design: This was an investigational study. Methodology: Eighteen fully grown albino rats separated into control and two treated sets, both treated sets were given indomethacin (50mg/1000g) orally. For acute treatment first treated set was sacrificed after 3.5 hrs & for chronic treatment second set was sacrificed after 3 days. However, control set animals were given an equivalent amount of vehicle. Results: Outcomes shows that serum Indoleamine 2,3 dioxygenase (IDO) enzyme activity was suppressed after acute treatment while serum IDO activity were increased after chronic treatment however no significant effect was seen on brain IDO. Conclusion: It is concluded that indomethacin has not shown any significant effect on brain IDO. But inhibits serum IDO activity.

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Section: Discussionsupporting

confidence: 87%

Section: Discussionmentioning

confidence: 99%

Section: Nsaidsmentioning

confidence: 99%

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Effects of Anti-inflammatory Medication on Indoleamine 2,3 Dioxygenase Activity

Dawood

Bano²,

Sundus

et al. 2022

JPRI

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“…Apart from changing the way drugs are delivered, the chemical modification of drugs can be employed to improve potency and reduce by-effects [ 50 ]. Quy et al (2020) discussed the therapeutic effect of PTL derivatives with different structures containing aniline on chronic leukemia cells.…”

Section: Discussionmentioning

confidence: 99%

Trends in parthenolide research over the past two decades: A bibliometric analysis

Liu

Cui

Wang

et al. 2023

Heliyon

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Indomethacin Derivatives as Potential Anticancer Agents ‐ Daybreak of New Epoch

Gogic,

Vesovic,

Nedeljkovic

et al. 2024

ChemistrySelect

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Non‐steroidal anti‐inflammatory drugs (NSAIDs) are extensively prescribed pharmaceutical agents worldwide. Due to their analgesic, antipyretic, and anti‐inflammatory properties, they are used in clinical practice for the treatment of numerous inflammatory diseases. The mechanism of action primarily involves the inhibition of prostaglandin synthesis mediated by cyclooxygenases (COX), key enzymes of the inflammatory cascade. Indomethacin, a non‐selective derivative of indole‐3‐acetic acid exhibits diverse mechanisms to exert its anti‐tumor effects, including angiogenesis suppression, induction of apoptosis, and reduction of tumorigenesis through immune modulation. Numerous studies suggest that derivatives of indomethacin may inhibit cell proliferation and reduce levels of anti‐apoptotic proteins through COX‐independent mechanisms. Given the diverse potential mechanisms through which indomethacin impacts cancer progression, this review provides an overview of structural analogs that possess antitumor activity and outlines future directions in developing new candidates that may have substantial efficacy in cancer therapy.

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Structure-activity Relationship of Indomethacin Derivatives as IDO1 Inhibitors

Cited by 5 publications

References 0 publications

Effects of Anti-inflammatory Medication on Indoleamine 2,3 Dioxygenase Activity

Effects of Anti-inflammatory Medication on Indoleamine 2,3 Dioxygenase Activity

Trends in parthenolide research over the past two decades: A bibliometric analysis

Indomethacin Derivatives as Potential Anticancer Agents ‐ Daybreak of New Epoch

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