U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 111 - 120 of 226 results

Theaflavin is a black tea polyphenol, which possesses a wide variety of pharmacological properties including potent antioxidative, anti-apoptotic, anti-cancer and anti-inflammatory effects. Theaflavin (TF-1) can bind to, and inhibit the purified 20S proteasome, accompanied by suppression of tumour cell proliferation, suggesting that the tumour proteasome is an important target whose inhibition is at least partially responsible for the anticancer effects of black tea. Theaflavin is a potent inhibitor of interleukin-8 gene expression in vitro. The proximal mechanism of this effect involves, in part, inhibition of IkappaB kinase activation and activator protein-1 pathway. Theaflavin has been known to possess neuroprotective effects against ischemia, Alzheimer's disease and other neurodegenerative disorders.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)



Selenomethionine, DL- is the racemic mixture of the D and L enantiomers of Selenomethionine, that used us animal’s dietary supplement. Selenomethionine, DL- was tolerated by chickens for fattening at up to 1.5 mg selenium supplemented/kg feed; Selenomethionine, DL- is therefore safe for chickens for fattening provided total dietary selenium does not exceed 0.5 mg/kg complete feed; this conclusion is extended to all animal species. Based on available toxicity studies and previous assessments of closely related compounds, it is concluded that selenium from Selenomethionine, DL- does not elicit any adverse effects not expected in a selenium compound. The use of Selenomethionine, DL- in animal nutrition is expected to result in a similar increase in selenium deposition in animal tissues/products as that resulting from other sources of Selenomethionine, DL- . To ensure consumer safety from consumption of food originating from animals fed Selenomethionine, DL-, dietary selenium supplementation from the additive should not exceed a maximum of 0.2 mg Se/kg complete feed. Although a Selenomethionine, DL- containing additive did not release any measurable dust, the additive is considered as a hazard by inhalation, which requires protection measures for users since the additive is not the subject of authorisation, and selenium is highly toxic. The additive is not an irritant to skin and eyes and is not a dermal sensitiser. The use of Selenomethionine, DL- in feed does not pose an additional risk to the environment, compared with other sources of selenium for which it will substitute, as long as the maximum authorised content in complete feed is not exceeded.
Geraniol is a dietary monoterpene alcohol that is found in the essential oils of aromatic plants. To date, experimental evidence supports the therapeutic or preventive effects of geraniol on different types of cancer, such as breast, lung, colon, prostate, pancreatic, and hepatic cancer, and has revealed the mechanistic basis for its pharmacological actions. In addition, geraniol sensitizes tumor cells to commonly used chemotherapy agents. Geraniol controls a variety of signaling molecules and pathways that represent tumor hallmarks; these actions of geraniol constrain the ability of tumor cells to acquire adaptive resistance against anticancer drugs. It has been shown that geraniol inhibits HMG-CoA reductase in most types of tumor cells, which raises the possibility that the reduced prenylation of small G-proteins, such as Ras or RhoA, accounts for the antitumor effects of geraniol. In addition to its use in various commercial products, including cosmetics and fine fragrances, geraniol exerts a broad spectrum of pharmacological activities, such as anti-microbial, anti-inflammatory, anti-oxidant, anti-ulcer and neuroprotective activities. Geraniol is classified into the generally recognized-as-safe (GRAS) category by the Flavor and Extract Manufacturers Association (FEMA) and the Food and Drug Administration (FDA) of the United States.
Status:
US Previously Marketed
First approved in 1992

Class (Stereo):
CHEMICAL (ACHIRAL)



Misoprostol is an antineoplastic drug used to treat skin growths caused by sun exposure. Masoprocol is a novel antineoplastic agent was used for the treatment of actinic keratoses (precancerous skin growths that can become malignant if left untreated). Masoprocol was withdrawn from the U.S. market in June 1996. It is not known exactly how Masoprocol works. Studies have shown that masoprocol is a potent 5-lipoxygenase inhibitor and has antiproliferative activity against keratinocytes in tissue culture, but the relationship between this activity and its effectiveness in actinic keratoses is unknown. Masoprocol also inhibits prostaglandins but the significance of this action is not yet known. Symptoms of overdose or allergic reaction include bluish coloration of skin, dizziness, severe, or feeling faint, wheezing or trouble in breathing.
Status:
US Previously Marketed
Source:
Selacryn by Smith Kline & French
(1979)
Source URL:
First approved in 1979
Source:
Selacryn by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Ticrynafen, or tienilic acid, is a diuretic drug with uric acid-lowering action, formerly marketed for the treatment of hypertension. It was withdrawn from the market only months after its introduction because of reports of serious incidents of drug-induced liver injury including some fatalities. Its hepatotoxicity is considered to be primarily immunoallergic in nature. Tienilic acid is a thiophene-containing mechanism-based inactivator of P450 2C9, resulting from covalent modification of the P450 2C9 protein. The bioactivation mechanism involves oxidation of the thiophene ring system.
Status:
US Previously Marketed
Source:
Reneal by Squibb
(1962)
Source URL:
First approved in 1962
Source:
Reneal by Squibb
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Phytate Sodium is a complex sodium salt of the corn-derived plant component Phytic Acid , that used as a chelating agent in all types of cosmetic products, including soaps, shampoos, balms and leave-on products for the face or body. Phytate Sodium is a biodegradable product and appears in the form of a dark-coloured liquid, is soluble in water and has a characteristic odour. It can be used in all types of cosmetic products, including soaps, shampoos, balms and leave-on products for the face or body. In vivo and in vitro experiments have demonstrated striking anticancer (preventive as well as therapeutic) effects of phytic acid. Research shows anti-carcinogenic effects, albeit to a lesser extent and it acts in inhibiting cancer. In addition to reduction in cell proliferation, phytic acid increases differentiation of malignant cells often resulting in reversion to the normal phenotype. Phytates participation in important intracellular biochemical pathways, normal physiological presence in human cells, tissues, plasma, urine, etc., the levels of which fluctuate with intake, epidemiological correlates of phytate deficiency with disease and reversal of those conditions by adequate intake, and safety – all strongly suggest for phytates inclusion as an essential nutrient, perhaps a vitamin. Phytic acid, mostly as Phytate Sodium or other phytates, is found within the hulls of nuts, seeds, and grains. No detectable phytate (less than 0.02 % of wet weight) was observed in vegetables such as scallion and cabbage leaves or in fruits such as apples, oranges, bananas, or pears. In-home food preparation techniques can break down the phytic acid in all of these foods. Simply cooking the food will reduce the phytic acid to some degree. More effective methods are soaking in an acid medium, sprouting and lactic acid fermentation such as in sourdough and pickling.
Sulfinpyrazone was approved by the U.S. Food and Drug Administration (FDA) on May 13, 1959. It was developed and marketed as Anturane® by Novartis. Sulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4). Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs). Branded and generic forms of sulfinpyrazone have been discontinued in the US.
Status:
US Previously Marketed
Source:
Methischol by USV Pharmaceutical
(1961)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

DL-Methionine is a racemic form of the respective sulfur aminoacid. DL-Methionine participates in synthesis of tissue proteins, vitamins, enzymes and hormones taking part in nitrogen, carbohydrate and fat metabolisms, and it is the important source of methyl groups for synthesis of all nucleic acids, as well as the sulfur source for sulfonic compounds. Methionine is used to prevent liver damage in acetaminophen (Tylenol) poisoning. It is also used for increasing the acidity of urine, treating liver disorders, and improving wound healing. Other uses include treating depression, alcoholism, allergies, asthma, copper poisoning, radiation side effects, schizophrenia, drug withdrawal, and Parkinson's disease. It is also used as a food additive in livestock to boost performance. DL-Methionin is the first limiting amino acid in poultry, and probably also in high-yielding cows, and is the second or third limiting amino acid in pigs fed conventional diets.
Zoxazolamine is a centrally acting muscle relaxant. It decreased striatal dopamine metabolism without affecting striatal dopamine concentrations. More specifically, Zoxazolamine was shown to decrease striatal dopamine turnover without directly affecting dopamine synthesis, catabolism, reuptake, or release. It is the IK(Ca) channel opener. It was approved for the relief of muscle spasm in conditions such as musculoskeletal disorders and neurological diseases. Later, it was submitted for the drug's use as a uricosuric agent to treat gout. It was withdrawn from the market due to hepatotoxicity.

Showing 111 - 120 of 226 results