Lutein is a xanthophyll and one of 600 known naturally occurring carotenoids. Lutein is synthesized only by plants and like other xanthophylls is found in high quantities in green leafy vegetables such as spinach, kale and yellow carrots. In green plants, xanthophylls act to modulate light energy and serve as non-photochemical quenching agents to deal with triplet chlorophyll (an excited form of chlorophyll), which is overproduced at very high light levels, during photosynthesis. Xanthophylls are taken for nutritional supplementation, and also for treating dietary shortage or imbalance. Xanthophylls have antioxidant activity and react with active oxygen species, producing biologically active degradation products. They also can inhibit peroxidation of membrane phospholipids and reduce lipofuscin formation, both of which contribute to their antioxidant properties. Lutein is naturally present in the macula of the human retina. It filters out potentially phototoxic blue light and near-ultraviolet radiation from the macula. The protective effect is due in part, to the reactive oxygen species quenching ability of these carotenoids. Lutein is more stable to decomposition by pro-oxidants than are other carotenoids such as beta-carotene and lycopene. Lutein is abundant in the region surrounding the fovea, and lutein is the predominant pigment at the outermost periphery of the macula. Zeaxanthin, which is fully conjugated (lutein is not), may offer somewhat better protection than lutein against phototoxic damage caused by blue and near-ultraviolet light radiation. Lutein is one of only two carotenoids that have been identified in the human lens, may be protective against age-related increases in lens density and cataract formation. Again, the possible protection afforded by lutein may be accounted for, in part, by its reactive oxygen species scavenging abilities. Carotenoids also provide protection from cancer. One of the mechanisms of this is by increasing the expression of the protein connexin-43, thereby stimulating gap junctional communication and preventing unrestrained cell proliferation. Lutein was found to be present in a concentrated area of the macula, a small area of the retina responsible for central vision. The hypothesis for the natural concentration is that lutein helps protect from oxidative stress and high-energy light. Several studies show that an increase in macula pigmentation decreases the risk for eye diseases such as Age-related Macular Degeneration (AMD). There is also epidemiological evidence that increasing lutein and zeaxanthin intake lowers the risk of cataract development. Consumption of more than 2.4 mg of lutein/zeaxanthin daily from foods and supplements was significantly correlated with reduced incidence of nuclear lens opacities, as revealed from data collected during a 13- to 15-year period in the Nutrition and Vision Project (NVP).

L-isomer of selenomethionine (Se-met) is a major natural food-form of selenium, synthetic L-Se-met or enriched food sources thereof such as selenium yeast are appropriate supplemental forms of Se for humans; for animals, DL-Se-met is acceptable. Ingested Se-met is either metabolized directly to reactive forms of selenium or stored in place of methionine in body proteins. Se-met metabolism is closely linked to protein turnover. Selenium, which is nutritionally essential for humans, is a constituent of more than two dozen selenoproteins that play critical roles in reproduction, thyroid hormone metabolism, DNA synthesis, and protection from oxidative damage and infection.

LBA (4-O-beta-D-galactopyranosyl-D-gluconic acid) is an aldonic acid obtained from the oxidation of lactose, with high potential applications as an ingredient in foods and pharmaceutical products, because of its antioxidant, chelating and humectant properties.

CTI-01 (ethyl pyruvate) is an investigational anti-inflammatory agent for the treatment of critical inflammatory conditions. CTI-01 was developed by Critical Therapeutics as a stable prodrug of pyruvate, a potent antioxidant, and a free radical scavenger. The drug showed an anti-inflammatory and tissue protection activity in animal models of pancreatitis, ischemia-reperfusion injury, sepsis, renal injury, and endotoxemia. CTI-01 was investigated in phase 2 clinical trials on patients undergoing cardiac surgery with cardiopulmonary bypass, but despite positive results in animal models, administration of EP does not appear to confer any benefit to cardiac surgical patients undergoing cardiopulmonary bypass. Besides clinical applications, ethyl pyruvate is long used as an additive to pharmaceutical preparations and foods, including candy, beverages, and baked goods. It is generally recognized as safe by the FDA.

Butylated hydroxytoluene, commonly known as BHT, is an organic compound that is used in the food, cosmetic, and pharmaceutical industry as an antioxidant. BHT is a substituted derivative of phenol. BHT helps to prevent the formation of free radicals and oxidation. When used in food products, it delays oxidative rancidity of fats and oils, and prevents loss of activity of oil-soluble vitamins. It may be found in pharmaceutical gels, creams and liquid or gelatin capsules, tablets and other pharmaceutical dosage forms. The ability of oral BHT to lead to cancer is a controversial topic, but most food industries have replaced it with butylated hydroxyanisole (BHA). BHT was first used as an antioxidant food additive in 1954. BHT does have other commercial uses, as in animal feeds and in the manufacture of synthetic rubber and plastics, where it also acts as an antioxidant. The U.S. Food and Drug Administration has deemed that BHT is safe enough when used in limited concentrations. It currently permits its use in concentrations of about 0.01% to 0.02% in most foods. As an emulsion stabilizer in shortening, it may be used in a somewhat higher concentration, 200 parts per million.

Tocophersolan (Vedrop, tocofersolan) or d-alpha-Tocopheryl Polyethylene Glycol 1000 Succinate (TPGS) is a watersoluble derivative of the natural active (d-alpha) isomer of vitamin E. The active constituent of the medicinal product is essentially vitamin E (alpha tocopherol). Chronic congenital or hereditary cholestasis is a clinical condition where vitamin E deficiency results from an impaired bile secretion. Decreased intestinal absorption observed in chronic congenital or hereditary cholestatic patients is due to decreased bile secretion and the resulting decrease in intestinal cellular absorption. As a result, fatsoluble vitamins (i.e. vit. E) are not absorbed properly and deficiency can occur. Tocophersolan (Vedrop) is used to treat or prevent vitamin E deficiency (low vitamin E levels). It is used in children up to the age of 18 years who have congenital or hereditary chronic cholestasis and who cannot absorb vitamin E from the gut. Tocophersolan (Tocofersolan) can be absorbed from the gut in children who have difficulty absorbing fats and vitamin E from the diet. This can increase vitamin E levels in the blood and help to prevent neurological deterioration (problems in the nervous system) due to vitamin E deficiency. No treatment-related findings were reported, as all clinical observations and findings at autopsy were similar in treatment and control groups. In many of the studies, the LD50 was not determined as tocofersolan was well tolerated.

Propyl Gallate is the n-propyl ester of gallic acid (3,4,5-trihydroxybenzoic acid). It is soluble in ethanol, ethyl ether, oil, lard, and aqueous solutions of polyethylene glycol (PEG) ethers of cetyl alcohol, but only slightly soluble in water. Propyl Gallate currently is used as an antioxidant in a reported 167 cosmetic products at maximum concentrations of 0.1%. Propyl Gallate is a generally recognized as safe (GRAS) antioxidant to protect fats, oils, and fat-containing food from rancidity that results from the formation of peroxides. The biological activity of Propyl Gallate is consistent with its free-radical scavenging ability, with effects that include antimicrobial activity, enzyme inhibition, inhibition of biosynthetic processes, inhibition of the formation of nitrosamines, anesthesia, inhibition of neuromuscular response to chemicals, ionizing/ultraviolet (UV) radiation protection, chemoprotection, antimutagenesis, anticarcinogenesis and antitumorigenesis, antiteratogenesis, and anticariogenesis. Propyl gallate has being shown to be a hepatoprotector in vitro and in vivo.

Ethyl vanillin is an important food additive and flavouring agent approved by FAO/WHO, has a vanilla odor four times that of vanillin and shows anti-mutagenic activity. It is used as flavoring agent and/or as an additive by the food, cosmetic, or pharmaceutic industries. Ethyl vanillin possesses antioxidant and anti-inflammatory properties. The antioxidant activity of ethyl vanillin was much stronger than that of vanillin in the oxidative hemolysis inhibition assay, but was the same as that of vanillin in the ORAC assay. Oral administration of ethyl vanillin to mice increased the concentration of ethyl vanillic acid, and effectively raised antioxidant activity in the plasma as compared to the effect of vanillin. The antioxidant activity of ethyl vanillin might be more beneficial than has been thought in daily health practice. The anti-angiogenic, anti-inflammatory and anti-nociceptive properties of EVA are based on its suppressive effect on the production of nitric oxide possibly via decreasing the reactive oxygen species level.

Hydroxyresveratrol (Oxyresveratrol) is a major active compound in the heartwood of Artocarpus lacucha. It was first isolated from the heartwood of Artocarpus lakoocha, and has also been found in various plants, including Smilax China, Morus alba, Varatrum nigrum, Scirpus maritinus, and Maclura pomifera. Oxyresveratrol, an aglycone of mulberroside A, has been produced by microbial biotransformation or enzymatic hydrolysis of a glycosylated stilbene mulberroside A, which is one of the major compounds of the roots of M. alba. Oxyresveratrol plays an important role in anti-tyrosinase, antioxidant, anti-inflammatory, antiviral and neuroprotective properties. There are many A. lacucha commercial products available on the market for skin whitening and anti-aging effects. OxyResvenox™ is the registered trademark of Oxyresveratrol from Sabinsa. Oxyresveratrol is an analog of Resveratrol and is of synthetic origin. The hydroxystilbene compounds including oxyresveratrol and resveratrol showed the potent inhibitory effect on tyrosinase activity. Oxyresveratrol is also naturally present in Morus alba L., Morus bombycis. Oxyresveratrol exhibits a potent inhibitory effect on dopa oxidase activity of tyrosinase which catalyzes rate-limiting steps of melanin biosynthesis. Oxyresveratrol showed superoxide scavenging effects with the IC50 values 3.81 ± 0.5 uM, Oxyresveratrol exhibited a DPPH free radical scavenging effect (IC50 = 23.4 ± 1.5 uM). Oxyresveratrol also showed hepatoprotective effects with EC50 values 32.3 ± 2.62 uM, on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells. Oxyresveratrol significantly inhibited LPS-evoked nuclear translocation of NF-kappaB and cyclooxygenase-2 (COX-2) activity in RAW 264.7 cells. The results suggest that the anti-inflammatory properties of oxyresveratrol might be correlated with inhibition of the iNOS expression through down-regulation of NF-kappaB binding activity and significant inhibition of COX-2 activity. Oxyresveratrol revealed a dose-dependent neuroprotective effect in an in vivo stroke model. This may prove to be beneficial for a therapeutic strategy to limit brain injury in acute brain ischemia.

Bufexamac is a nonsteroidal antiinflammatory drug (NSAID) used in topical formulations to treat dermatological diseases (eczema and dermatitis) and proctological conditions (haemorrhoids and anal fissure). Bufexamac-containing medicines have been available in EU Member States since the 1970s. In 2010 European Medicines Agency recommends revocation of marketing authorisations for bufexamac due to high risk of contact allergies. The phenolic bufexamac decomposition products could be the reason for its eczema-provoking properties frequently described in the literature. Bufexamac is a class IIb histone deacetylase (HDAC6, HDAC10) inhibitor. Bufexamac also triggered an HDAC6-independent, hypoxia-like response by stabilizing Hypoxia-inducible factor 1-alpha, providing a possible mechanistic explanation of its adverse, pro-inflammatory effects. Bufexamac was capable of specifically inhibiting leukotriene A4 hydrolase and attenuating lung inflammation in acute lung injury mouse model.