cox-1

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Salicylamide (2-Hydroxybenzamide) is an over-the-counter drug with analgesic and antipyretic properties, which has similar medicinal properties to aspirin. In the over-the-counter pain remedies, Salicylamide is used in combination with both aspirin and caffeine.

Acetaminophen (APAP) is a COX inhibitor that inhibits COX-1 and COX-2 (IC50=113.7/25.8 μM). Acetaminophen has antipyretic and analgesic activity as well as weak anti-inflammatory activity.

Sodium salicylate (2-Hydroxybenzoic acid sodium salt), a metabolite of acetylsalicylic acid, can inhibit NF-kB and reduce oxidative stress.

Catechin (Cianidanol) is a flavan-3-ol, a type of natural phenol and antioxidant.

(-)-Catechin ((-)-Cianidanol), an isomer of catechin, inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.

(+)-Catechin Hydrate is an antioxidant flavonoid of plant origin; a free radical scavenger, preventing free radical-mediated damage in a variety of biological systems.

Roburic acid and phenethyl-trans-ferulate inhibit COX-1 and COX-2.

TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective cyclooxygenase-1 (COX-1) inhibitor

1. Columbin has anti-inflammatory activity. 2. Columbin has chemopreventive ability against human colon cancer. 3. Columbin inhibits PLA2 hydrolysis of ghost RBC in a dose-dependent fashion.

1. Benzoylpaeoniflorin is active against cyclooxygenase-1 and cyclooxygenase-2 enzymes.

α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.

Hamaudol, a chromone isolated from Saposhnikovia divaricata, exhibits analgesic and anti-inflammatory activities, demonstrating inhibitory effects on COX-1 and COX-2 with respective values of 0.30 and 0.57 mM.

Hyperforin, a natural product from Hypericum, is commonly used as an antidepressant and also has neurological, inflammatory, antimicrobial, antitumor and antiangiogenic effects. Hyperforin acts as a monoamine reuptake inhibitor (MRI) in vitro, including serotonin, norepinephrine, dopamine, GABA, and glutamate, with an IC 50 of ≈0.1 μg/mL. Hyperforin is also capable of inducing the cytochrome P450 enzymes, CYP3A4 and CYP2C9, through binding to and activation of the pregnane X receptor. Hyperforin is capable of activating TRPC6 channels by binding to a specific motif.

Tetrahydroamentoflavone is a potent XO inhibitor (IC50 = 92 nM, Ki = 982 nM) with anti-inflammatory effects. Tetrahydroamentoflavone can be used for studies about inflammation and gout.

Hexahydrocurcumin is a selective, orally active COX-2 inhibitor and inactive against COX-1.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

(-)-Epicatechin gallate ((-)-Epicatechin 3-O-gallate) is one of the catechin isomers and a potent antioxidant that can modulate a wide range of membrane proteins. Its bilayer-modifying potency was tested using gramicidin A (gA) channels as probes. All the catechins alter gA channel function and modify bilayer properties, with a 500-fold range in potency. The gallate group causes current block, as evident by brief downward current transitions.

Asaraldehyde (2,4,5-trimethoxy-Benzaldehyde), a natural COX-2 inhibitor, exhibits 17-fold selectivity than COX-1.

(-)-Epicatechin (Epicatechin) is an inhibitor of cyclooxygenase-1 (COX-1), inhibiting the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

Rutaecarpine (Rhetine) is an inhibitor of COX-2 with IC50 of 0.28 μM.

Xanthohumol, also known as 2', 4, 4'-trihydroxy-6'-methoxy-3'-prenylchalcone or desmethylxanthohumol, is a member of the class of compounds known as 3-prenylated chalcones. It inhibits COX-1 and COX-2 activity and shows chemopreventive effects.

1. trans-Cinnamaldehyde (Phenylacrolein) exhibits excellent anti-inflammatory activities and antidepressant-like effects in stressed mid-aged rats as a COX-2 inhibitor. 2. Cinnamic aldehyde induces apoptosis of CML cells in vitro, down-regulation of the expression and function of BCR-ABL may be one of its most important anti-leukemia mechanisms. 3. Cinnamic aldehyde and cinnamic acid are cardioprotective in a rat model of ischemic myocardial injury, the mechanism is related to anti-oxidative and anti-inflammatory properties.

2-Hydroxy Ibuprofen is a metabolite of ibuprofen, applicable in biochemical experiments and drug synthesis research. Ibuprofen inhibits both COX-1 and COX-2.