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.

(-)-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.

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

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.

Loganin (Loganoside), an iridoid glucoside, has been reported to be an inhibitor of Cox-1 and also noted to suppress TNF-α formation. This compound also has displayed potent free-radical-scavenging activity and inhibitory effects on melanogenesis.

Bardoxolone (CDDO) is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM. By suppressing reactive oxygen and nitrogen species (ROS RNS) formation, it promotes the cellular control of ROS RNS levels that would lead to DNA damage associated with tumorigenesis. In various Y cell lines, Bardoxolone has been shown to specifically inhibit proliferation and induce apoptosis. Mechanism studies revealed that Bardoxolone is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2 iNOS expression.

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

1. Gamabufotalin (Gamabufagin) , a major bufadienolide of Chansu, has been used for treatment of COX-2-mediated diseases and cancer therapy due to its desirable metabolic stability and less adverse effect.

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

1. Cornuside (Comuside) has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3. Cornuside can treat myocardial I R and protect the liver from CCl4-induced acute hepatotoxicity, by reducing oxidative stress and suppressing inflammatory responses. 4. Cornuside has anti-inflammatory activity by downregulations of iNOS and COX-2 due to NF-κB inhibition as well as the negative regulation of ERK1 2, p38, and JNK1 2 phosphorylations in RAW 264.7 cells. 5. Cornuside has protective potential against cerebral ischemic injury, may be due to the suppression of intracellular Ca(2+) elevation and caspase-3 activity, and improvements in mitochondrial energy metabolism and antioxidant properties.

Morin monohydrate (oxylon pomiferum monohydrate) is a flavonoid extracted from Morus alba plant with anticancer, antioxidant, and anti-inflammatory activities, which reduces T-2 toxin-induced TNF-alpha, COX-2, IL-1β, IL-6, caspase-1, caspase-3, and caspase-11 mRNA. BML-286 is a WNP-containing WNP-containing BML-286, which reduces T-2 toxin-induced TNF-α, COX-2, IL-1β, IL-6, caspase-1, caspase-3, and caspase-11 mRNA expression, and ameliorates T-2 toxin-induced injury by decreasing malondialdehyde (MDA) and increasing superoxide dismutase (SOD), catalase (CAT), glutathione (GSH), and glutathione peroxidase (GSH-PX).

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

2-Hydroxy Ibuprofen, a metabolite of Ibuprofen, an anti-inflammatory inhibitor targeting COX-1 COX-2 (IC50s: 13 μM 370 μM).

Cinnamtannin B-1 (LDN 0022358) is an A-type proanthocyanidin contained in several plant species such as Vaccinium vitis-idaea, Laurus nobilis L., Cinnamomum zeylanicum, and Lindera umbellata. It is a potent antioxidant and protective agent against oxidative stress and apoptosis in human platelets. It is a Cox-2 inhibitor.