Recent development on COX-2 inhibitors as promising anti-inflammatory agents: The past 10 years

Zhang, Ju; Li, Menglan; Xu, Junde; Howell, Daniel C.; Li, Zhi-Yun; Chen, Fen‐Er

doi:10.1016/j.apsb.2022.01.002

Cited by 122 publications

(73 citation statements)

References 114 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…NF-κB is a key transcriptional regulator linking inflammation and tumorigenesis, which aberrantly activates in many cancer tissues and associates with cell proliferation, apoptosis, angiogenesis, inflammation, and metastasis . When under a non-stimulated status, NF-κB is present in a non-activated form and binds to IκB in the cytoplasm.…”

Section: Resultsmentioning

confidence: 99%

“…v) Considering that COX-2 inhibition was found to keep NF-κB in an inactive state of bondage to p-IκB in the downstream, thereby prohibiting the inflammatory cascade, 84 we evaluated the effects of 1H-30 on the NF-κB pathway. 1H-30 not only inhibited the NF-κB pathway of cancer cells under inflammatory and non-inflammatory stimulation conditions but also suppressed the nuclear translocation of NF-κB in LPS-stimulated RAW264.7 cells, which may explain the down-regulation of downstream inflammatory mediators such as nitric oxide, COX-2, and IL-1β by 1H-30.…”

Section: Discussionmentioning

confidence: 99%

“…NF-κB is a key transcriptional regulator linking inflammation and tumorigenesis, which aberrantly activates in many cancer tissues 55 and associates with cell proliferation, apoptosis, angiogenesis, inflammation, and metastasis. 84 When under a non-stimulated status, NF-κB is present in a nonactivated form and binds to IκB in the cytoplasm. Once stimulated, IκB is phosphorylation and eventual degradation, followed by phosphorylated NF-κB, translocating into the nucleus and triggering the expressions of the antiapoptotic proteins (such as Bcl-2), COX-2, and MMP-9.…”

Section: Inhibitory Effects On Cell Migration Ability and The Express...mentioning

confidence: 99%

See 2 more Smart Citations

N-2-(Phenylamino) Benzamide Derivatives as Dual Inhibitors of COX-2 and Topo I Deter Gastrointestinal Cancers via Targeting Inflammation and Tumor Progression

Zhang

et al. 2022

J. Med. Chem.

View full text Add to dashboard Cite

Given the close association between inflammation and cancer, combining anti-inflammation therapy is prominent to improve the anticancer effect. Based on I-1, a series of agents targeting COX-2 and Topo I were designed by combining fenamates and phenols. The optimal compound 1H-30 displayed an enhanced inhibitory effect on COX-2 compared to tolfenamic acid and I-1 and showed better inhibition of Topo I than I-1. Importantly, 1H-30 showed potential anticancer effects and suppressed the activation of the NF-κB pathway in cancer cells. 1H-30 inhibited the nuclear translocation of NF-κB and suppressed the production of NO, COX-2, and IL-1β in RAW264.7. In vivo, 1H-30 showed acceptable pharmacokinetic parameters, decreased the tumor growth without affecting the body weight, down-regulated COX-2 and MMP-9, and induced apoptosis in the CT26.WT tumor-bearing mice. Accordingly, 1H-30 as a potential Topo I/COX-2 inhibitor which possessed anti-inflammatory and anticancer effects, with inhibition of the NF-κB pathway, is promising for gastrointestinal cancer therapy.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Inhibitory Effects On Cell Migration Ability and The Express...mentioning

confidence: 99%

See 1 more Smart Citation

N-2-(Phenylamino) Benzamide Derivatives as Dual Inhibitors of COX-2 and Topo I Deter Gastrointestinal Cancers via Targeting Inflammation and Tumor Progression

Zhang

et al. 2022

J. Med. Chem.

View full text Add to dashboard Cite

show abstract

“…Allopathic anti-inflammatory drugs are known to reduce inflammation by inhibiting inflammatory enzymes such as cyclooxygenase-2 (COX-2). Unfortunately, these drugs also destroy the enzyme cyclooxygenase-1 (COX-1), which is necessary for the production of group 1 prostaglandins, which are an important part of cellular immunity and reduce blood viscosity (Attiq, et al, 2018;Ju, et al, 2022).…”

Section: Gamma-mangostinmentioning

confidence: 99%

Molecular Docking of Zingerone and Gamma-Mangostin to Inhibit MAO-B and Catechol-O-Methyltransferase (COMT) in the Treatment of Parkinson’s Disease

Saraiva

Silva

Sousa

et al. 2022

RSD

View full text Add to dashboard Cite

Currently, there is no drug that has proven neuroprotective properties in Parkinson's disease. The best-known drug is levodopa, which acts as inhibitors of the MAO-B and COMT enzymes involved in dopamine degradation. Although levodopa is the "gold standard" of treatment, as the disease progresses, most patients develop complications from the therapy and side effects. In this sense, the combination of two abundant substances and phytotherapics as alternatives to the use of traditional medicines is approached, namely Zingerone and Gamma-Mangostin. In which they presented favorable results in molecular docking.

show abstract

“…Although COX has been identified for more than 20 years, it has been in recent years that it has become clear that there are two homologous isoforms, being referred to as COX-1 and COX-2 (Ju et al, 2022 ). In almost all normal tissues, the structural presence of COX-1 is detected, and in low to undetectable levels of COX-2, which can be expressed in greater amounts through the presence of cytokines, growth factors and tumor stimulants, suggesting its relevance.…”

Section: Introductionmentioning

confidence: 99%

Induced arthritis, hepatocytes cytotoxicity and non-steroidal anti-inflammatory drugs (NSAIDs) – experimental study

Morsoleto

Werneck

Moreira

et al. 2022

RSD

View full text Add to dashboard Cite

This study aimed to histologically evaluate the pharmacological activity of meloxicam, COX-2 inhibitor, on liver function in arthritic rats. Meloxicam is a non-steroidal anti-inflammatory drug (NSAID), COX-2 inhibitor, generally prescribed in the area of rheumatology. Thus, 18 Wistar rats were divided into 3 groups with 6 animals each: G1 (Negative Control), G2 (Arthritis induced with Zymosan [Zy]), G3 (Arthritis induced with Zymosan [Zy] and treated with meloxicam). The G3 treatment started on the 21st day after induction. The animals were sacrificed, by overdose of Ketamine/Xylazine, seven, 14 and 21 days after the beginning of the meloxicam treatment. Liver samples were collected from the animals, fixed in Millonig buffer containing 10% formaldehyde and processed for conventional histological analysis. G1 animals showed absence of inflammation and degeneration of hepatocytes. In the G2 group, a slight cytoplasmic alteration was observed at seven and 14 days. At 21 days, intense cytoplasmic and nuclear disorganization was detected, accompanied by cell necrosis. In G3, large spacing between sinusoid capillaries was detected. In some 14-day-old animals, amyloidosis was observed, with the presence of a large number of vacuolated hepatocytes involved in an amorphous mass of necrotic cells. Most of the hepatocyte nuclei had compacted chromatin, evidencing cellular degeneration. Meloxican, used as an anti-inflammatory in the synovial region, showed that, in addition to its beneficial effects for the treatment of rheumatological diseases, it is capable of, when administered orally, promoting a high level of liver damage.

show abstract

Recent development on COX-2 inhibitors as promising anti-inflammatory agents: The past 10 years

Cited by 122 publications

References 114 publications

N-2-(Phenylamino) Benzamide Derivatives as Dual Inhibitors of COX-2 and Topo I Deter Gastrointestinal Cancers via Targeting Inflammation and Tumor Progression

N-2-(Phenylamino) Benzamide Derivatives as Dual Inhibitors of COX-2 and Topo I Deter Gastrointestinal Cancers via Targeting Inflammation and Tumor Progression

Molecular Docking of Zingerone and Gamma-Mangostin to Inhibit MAO-B and Catechol-O-Methyltransferase (COMT) in the Treatment of Parkinson’s Disease

Induced arthritis, hepatocytes cytotoxicity and non-steroidal anti-inflammatory drugs (NSAIDs) – experimental study

Contact Info

Product

Resources

About