COX-2 Inhibitor

Phenyl β-D-glucopyranoside is a component isolated from Phellodendron amurense, which has anti-inflammatory and anti-tumor activities. Phenyl β-D-glucopyranoside inhibits nitric oxide (NO) production, and the expression of iNOS and COX-2. Phenyl β-D-glucopyranoside also inhibits the nuclear translocation of NF-κB. Phenyl β-D-glucopyranoside inhibits the expression of pro-inflammatory cytokines and related genes.

Timosaponin A1, a natural steroidal saponin, is a 5-lipoxygenase (5-LO), COX-2, and dipeptidyl peptidase 4 (DPP-4) inhibitor with IC₅₀s of 3.29 µM, 36.43 µM, and 33.25 µM, respectively.

Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level.

(E)-Ethyl p-methoxycinnamate is a natural product found in Kaempferia galangal with anti-inflammatory, anti-neoplastic and anti-microbial effects. (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 in vitro with IC₅₀s of 1.12 and 0.83 μM, respectively.

Sericin is an orally active globular protein produced by silkworm cocoons. Sericin inhibits the expression of COX2, iNOS, TLR4, MAPK and NF-κB; reduces the levels of IL-18, IL-1 and CCL2; antagonizes the activity of AChE; and downregulates the expression of Bcl-2. Sericin enhances the PI3K/AKT-mediated insulin signaling pathway. Sericin inhibits the activity of tyrosinase (Tyrosinase), scavenges ROS, chelates metal ions, and increases the levels of antioxidant enzymes. Sericin induces apoptosis and arrests the cell cycle. Sericin exhibits antibacterial, moisturizing, cardioprotective and anticoagulant properties. Sericin can be used in research related to type 2 diabetes, hyperlipidemia, obesity, Alzheimer's disease, colon cancer, peripheral nerve injury and ischemic myocardial infarction.

α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.

CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 1 nM and a selectivity index (SI; COX-1 IC₅₀/COX-2 IC₅₀) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.

Felbinac is a metabolite of fenbufen, an orally active nonsteroidal anti-inflammatory agent and a cyclooxygenase (COX) inhibitor with an IC₅₀ of 865.68 nM for COX1 and 976 nM for COX2. Felbinac reduces the production of prostaglandins by inhibiting COX to relieve pain, reduce inflammation and reduce fever. Felbinac can inhibit CHIKV viral activity.

Rehmannioside A is a compound that can be isolated from Rehmanniae radix. Rehmannioside A is an inhibitor of CYP3A4, 2C9 and 2D6, with IC₅₀ values of 10.08, 12.62 and 16.43 μM, respectively. Rehmannioside A has anti-inflammatory, antioxidant, anti-apoptosis, anti-ferroptosis, cognitive improvement and neuroprotective activities. Rehmannioside A can be used for the research of nervous system and inflammation-related diseases.

SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC₅₀ of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo. SC-58125 also can inhibit edema at the inflammatory site and has analgesic effect.

Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.

Columbin is an orally active diterpenoid furanolactone from Calumbae radix, has anti-inflammatory and anti-trypanosomal effects. Columbin selectively inhibits COX-2 (EC₅₀=53.1 μM) over COX-1 (EC₅₀=327 μM).

2'-Hydroxy-5'-methoxyacetophenone is an acetophenone derivative with acaricidal activities. 2'-Hydroxy-5'-methoxyacetophenone attenuates the inflammatory response via NF-κB signaling pathway. 2'-Hydroxy-5'-methoxyacetophenone exhibits significant inhibitory activity against α-amylase, collagenase and aldose reductase (AR) with IC₅₀s of 0.928, 3.264 and 20.046 μM, highlighting its potential in combating diabetes. 2'-Hydroxy-5'-methoxyacetophenone exhibits anti-ovarian cancer activity.

Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC₅₀ of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC₅₀ of 7.5 μM). Firocoxib has anti-inflammatory effects.

Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC₅₀s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

Ramifenazone (Isopropylaminoantipyrine) is a pyrazolone non-steroidal anti-inflammatory agent (NSAID) and a potent COX-2 inhibitor. Ramifenazone exhibits analgesic, antipyretic, anti-inflammatory, and antibacterial activities. Ramifenazone can be used for research on inflammation.

7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid with multiple biological activities. 7,3',4'-Tri-O-methylluteolin inhibits soybean lipoxygenase (LOX), with an IC₅₀ value of 23.97 µg/mL. 7,3',4'-Tri-O-methylluteolin possesses anti-inflammatory effects in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 macrophages. 7,3',4'-Tri-O-methylluteolin inhibits the binding of MDM2 with p53 and induces apoptosis in MCF-7 breast cancer cells. 7,3',4'-Tri-O-methylluteolin also has antioxidant, antifungal and antitrypanosomal activities.

Cholesteryl eicosapentaenoate (CE(20:5(5Z,8Z,11Z,14Z,17Z)), a cholesteryl ester, is a COX-1 and COX-2 inhibitor with IC₅₀ values of 14.6 μg/mL and 17.3 μg/mL, respectively. Cholesteryl eicosapentaenoate shows strong anti-inflammatory and antioxidant activities.

Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory agent (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A₂ (sPLA₂) and COX-2.

Darutoside is an orally effective diterpene compound with significant anti-inflammatory, analgesic, wound healing promotion, and immunomodulatory activities. Darutoside reduces edema and pain responses by inhibiting the expression of COX-2 and the migration of inflammatory cells. It regulates macrophage polarization towards the M2 type by inhibiting the NF-κB pathway, alleviating inflammation and promoting wound healing. Through multi-target regulation of metabolic networks, Darutoside significantly alleviates acute gouty arthritis.