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

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Showing 341 - 350 of 609 results

Paeonol (2-hydroxy-4-methoxyacetophenone) is a major phenolic component of the dried root bark of Paeonia suffruticosa Andrews (Paeoniaceae). Paeonol exhibits a wide variety of bioactivities including anti-inflammatory, antioxidative, immunoregulatory, antihypertensive, anti-hyperglycemic, antibacterial, anti-thrombotic, and antitumor effects. Paeonol inhibits anaphylactic reaction by regulating histamine and TNF-α. Paeonol tablets have been used for the treatment of rheumatic arthritis, fever, headache and neuralgia in Chinese clinics.
Cucurbitacin B (CuB), an oxygenated tetracyclic triterpenoid compound extracted from Cucurbitaceae plant species, is a long-term anticancer agent by disruption of microtubule polymerization. Cucurbitacin B is a naturally occurring compound that is found abundantly in cucumbers and other vegetables, and it is known to exert anti-cancer activities (primarily via apoptosis-induction) in several human cancers. Cucurbitacin B also protects against cardiac hypertrophy through increasing the autophagy level in cardiomyocytes, which is associated with the inhibition of Akt/mTOR/FoxO3a signal axis. ACLY over-expression abrogated CuB's apoptotic effects in prostate cancer cells, confirming ACLY as a direct target of CuB. Thus, CuB harbors potent chemopreventive activity for prostate cancer, and we revealed a novel anti-tumor mechanism of CuB via inhibition of ACLY signaling in human cancer. It has being suggested that cucurbitacin B exerts an anticancer effect by inhibiting telomerase via down regulating both the hTERT and c-Myc expression in breast cancer cells.
Dihydroquercetin (also known as taxifolin) is a flavonoid found in grapes, citrus fruits, onions, green tea, olive oil, and several herbs (such as milk thistle). Besides its antitumor, hepatoprotective, and anti-inflammatory activities, it is a potent antioxidant, which may contribute to its cardiovascular and neuroprotective properties. The drug was tested in vitro against cancer cells and in vivo, in preclinical models of liver diseases and cardiovascular diseases. The possible mechanism of actions involves the induction of phase II detoxifying enzymes and the suppression of cytochrome P450-dependent monooxygenases, apoptosis and disruption of cancer cell cycle progression.
Angelicin (isopsoralen), is a furocoumarin, occuring in a number of plants belonging to the Umbelliferae family. It acts as a photosensitizer by forming DNA monoadducts. Angelicin is able to inhibit monoamine oxidase (MAO) activities in rat brain mitochondria. Angelicin exerts antineoplastic and antidiabetic properties in animal models.
Sesamin is the most prominent lignan compound found in sesame seeds, one of the two highest sources of lignans in the human diet (the other being flax). Sesamin is catered to be a nutritional supplement that confers antioxidant and antiinflammatory effects (if touting its health properties) or possibly being an estrogen receptor modulator and fat burner (if targeting atheltes or persons wishing to lose weight). Sesamin has a few mechanisms, and when looking at it holistically it can be summed up as a fatty acid metabolism modifier. It appears to inhibit an enzyme known as delta-5-desaturase (Δ5-desaturase) which is a rate-limiting enzyme in fatty acid metabolism; inhibiting this enzyme results in lower levels of both eicosapentaenoic acid (EPA, one of the two fish oil fatty acids) as well as arachidonic acid, and this mechanism appears to be relevant following oral ingestion. The other main mechanism is inhibiting a process known as Tocopherol-ω-hydroxylation, which is the rate limiting step in the metabolism of Vitamin E; by inhibiting this enzyme, sesamin causes a relative increase of vitamin E in the body but particularly those of the gamma subset (γ-tocopherol and γ-tocotrienol) and this mechanism has also been confirmed to be active following oral ingestion. Sesamin is a potent and specific inhibitor of delta 5 desaturase in polyunsaturated fatty acid biosynthesis. Sesamin inhibits a particular CYP3A enzymes that is involved in vitamin E metabolism, where the enzyme initially ω-hydroxylates vitamin E (required step) and then the rest of vitamin E is subject to fat oxidation. By inhibiting this step, sesamin causes an increase in circulating and organ concentrations of vitamin E. Sesamin is thought to have PPARα activating potential in the liver, but it is uncertain how much practical relevance this has in humans due to this being a mechanism that differs between species.
Safrole is a natural product obtained from essential oil of the root bark of Sassafras tree. Safrole has been used as a flavoring agent in drugs and in the manufacture of heliotropin, perfumes, soaps, and piperonyl butoxide. Oil of sassafras, which contains safrole, was formerly used to flavor some soft drinks, such as root beer. However, this use or any other addition of safrole or oil of sassafras to food was banned in the United States in 1960 due to evidence of carcinogenicity. Numerous studies have shown that safrole from betel quid-containing safrole might be involved in the pathogenesis of hepatocellular carcinoma in human due to the formation of DNA adducts. Safrole has also been used in the illicit production of the drug 3,4-methylenedioxymethamphetamine (MDMA, or ecstasy), and the U.S. Drug Enforcement Administration has designated safrole a List I Chemical. Anticancer and anti-diabetic properties of safrole were investigated in vitro and in vivo.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)



Fulvic acid is primarily studied for its effects on plants and soil. Fulvic acid is an organic and natural electrolyte. Depending on the situation, Fulvic acid can act as an electron donor or acceptor and an oxidizer or reducer. Fulvic acid has exhibited the ability to enhance the availability and adsorption of nutrients as well as prolong their time of residence. In the chick animal model Fulvic acid disturbed the processing of procollagen II in articular cartilage. Fulvic acid has being shown to attenuate homocysteine-induced cyclooxygenase-2 expression in human monocytes. Fulvic acid, the main active principle of Shilajit (a natural substance found mainly in the Himalayas), blocks tau self-aggregation, opening an avenue toward the study of Alzheimer's therapy. People take fulvic acid by mouth for brain disorders such as Alzheimer’s disease, as well as respiratory tract infections, cancer, fatigue, heavy metal toxicity, and preventing a condition in which the body tissues do not receive enough oxygen (hypoxia).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Imidazole is a planer five-member heterocyclic ring with 3C and 2N atom and in ring N is present in 1st and 3rd positions. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. The imidazole derivatives possess extensive spectrum of biological activities such as antibacterial, anticancer, antitubercular, antifungal, analgesic, and anti-HIV activities. The organic compound is used in the chemical industry as an intermediate in the production of pharmaceuticals, pesticides, dye intermediates, auxiliaries for textile dyeing and finishing, photographic chemicals and corrosion inhibitors. The chemical possesses properties (corrosivity to skin, irreversible damage to eyes, teratogenic effects) indicating a hazard for human health. Humans are exposed by consumer products (chemical concentrations up to 10%) and at the workplace. Therefore, the chemical is a candidate for further work. An exposure assessment and if indicated a risk assessment is recommended.
Nerolidol (aka peruviol) is a naturally occurring sesquiterpene found in the essential oils of many types of plants and flowers. The aroma of nerolidol is woody and reminiscent of fresh bark. It is used as a flavoring agent and in perfumery. It is also used in non-cosmetic products such as detergents and cleansers. Additionally, it is known for several biological activities including antioxidant, anti-fungal, anticancer, and antimicrobial activities.
Wogonin is an O-methylated flavone compound isolated from Scutellaria baicalensis. Wogonin is an a positive allosteric modulator of benzodiazepine site of the GABAA ion channel, and displays anxiolytic properties in animal models. It possesses anti-tumor effect in models of osteosarcoma and lung cancer. Hepatoprotective action of wogonin was demonstrated in the mouse model of alcoholic liver disease and in a model of nonalcoholic fatty liver disease, where it was shown that wogonin upregulates PPAR-gamma and PPARalpha respectively. Wogonin possess chondroprotective action which was demonstrated in models of osteoarthritis.

Showing 341 - 350 of 609 results