The major estrogen secreted by the premenopausal ovary.

Diethylstilbestrol (DES) is a synthetic estrogen receptor agonist that was prescribed to pregnant women in the late 1930s. It was banned in 1971 because of possible links to increased risk of breast cancer in mothers along with congenital abnormalities and increased risk of cancer in offspring. DES…

A methyl ester prodrug form of the NOS inhibitor L-NNA; exhibits Ki values of 15 nM, 39 nM, and 4.4 µM for nNOS (bovine), eNOS (human), and iNOS (mouse), respectively.

Estrone is one of the three naturally occurring estrogens, the others being estradiol and estriol. Estrone is synthesized from androstenedione by the aromatase enzyme system in the ovaries and placenta, and is also synthesized from estradiol by 17-hydroxy steroid dehydrogenase in the liver. Serum…

A non-selective NSAID exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2, respectively.

A long-chain saturated fatty acid that does not affect plasma total cholesterol or LDL-cholesterol but may reduce HDL-cholesterol.

Saturated fatty acids are synthesized by both plants and animals from acetyl coenzyme A as a form of long-term energy storage. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of the normal human dietary fat intake, and approximately 25% of the total plasma fatty acids in…

A major flavonolignan from the extracts of milk thistle seed, S. marianum; blocks the production of superoxide in PMA-activated rat Kupffer cells (EC50 = ~100 µM); inhibits the synthesis of LTB4 (IC50 = ~15 µM).

Palmitic acid ethyl ester is a neutral, lipid-soluble form of the free acid. It is one of the fatty acid ethyl esters that increase cytosolic Ca2+ concentration leading to pancreatic acinar cell injury due to excessive consumption of ethanol.

Bezafibrate is a well established pan-PPAR activator. This fibrate drug has over 25 years of therapeutic use with a good safety profile. The fibrate class of drugs are generally known as PPARα agonists, but bezafibrate appears to activate PPAR.delta. and PPARγ as well. Bezafibrate…

A PPARα agonist and hypolipidemic drug used clinically to treat dyslipidemia and cardiovascular disease; exhibits EC50 values of 18 and 30 µM for mouse and human PPARα, respectively.

Hydroxymethyl uracil is a product of oxidative damage to DNA, predominantly by hydroxyl radical via the Fenton reaction.

An alkaloid natural product that reduces total cholesterol, LDL cholesterol, and triglycerides in humans and hamsters; enhances LDL-receptor protein and mRNA levels in hepatocytes.

Nitroxyl (HNO) is the one electron reduced form of nitric oxide. Piloty’s acid is one of the best known and most widely used HNO donors. Under basic conditions Piloty’s acid decomposes to HNO and benzenesulfinate anion. The rate of HNO release at pH 7 is very slow (t½ = 5500…

Traumatic acid is a product of the hydroperoxide lyase pathway in plants. It is a wound healing agent that stimulates cell division near a wound site to form a protective callus.

Nitrotyrosine is formed by peroxynitrite-mediated nitration of protein tyrosine residues. Its presence on proteins can be used as a marker for peroxynitrite formation in vivo. Both free and protein-bound nitrotyrosine are commonly found in mammalian tissues and are increased in pathological…

TMPD is an easily oxidizable compound that serves as a reducing co-substrate for heme peroxidases. TMPD undergoes one-electron oxidation by the heme peroxidase higher oxidation states (compounds I and II) producing a highly colored product that absorbs at 611 nm. Thus, the stoichiometry of…

An NSAID thought to exert its actions by a prostanoid-independent mechanism; inhibits fMLP- and A23187-induced Ca2+ influx in human neutrophils with an IC₅₀ value of approximately 20 µM.

1,8-ANS is a fluorescent dye that binds with high affinity to hydrophobic surfaces of proteins. The emission maximum of 1,8-ANS undergoes a blue shift and fluorescence intensity increases significantly upon binding to low polarity regions of a protein surface. These properties make 1,8-ANS well…

A non-selective, reversible COX inhibitor. with IC₅₀ values for human recombinant COX-1 and -2 at 2.6 and 1.53 µM, respectively; Ki values for ovine COX-1 and -2 are both 9 µM.

Niflumic acid is a selective inhibitor of COX-2. The IC₅₀ values are 16 and 0.1 µM for human recombinant COX-1 and -2, respectively. The Ki values are 2 and 0.02 µM for ovine COX-1 and -2, respectively.

A non-selective COX inhibitor; inhibits human recombinant COX-1 and -2 with IC₅₀ values of 0.04 and 0.51 µM, respectively.

A non-selective inhibitor of both COX-1 and COX-2 with extensive epidemiology documenting its effective reduction of human colorectal cancer.