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

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Showing 171 - 180 of 432 results

Galangin is a flavanol that is found in high concentrations in Alpinia officinarum and Helichrysum aureonitens. It can also be found in the rhizome of Alpinia galanga and in propolis. Galangin has been shown to have antibacterial, antiviral, anticancer and neuroprotective properties in vitro and in animal models.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

1,2-Dipalmitoyl-sn-glycero-3-phosphate monosodium salt (Phosphatidic Acid, DPPA) is a bioactive phospholipid. Dipalmitoylphosphatidic acid (DPPA) is a minor phospholipid metabolite that is involved in lipid biosynthesis. DPPA has two palmitic acid moieties instead of AA and can convert to lyso-PA to increase Bcl-2 expression in Hela cells but not in B lymphoma cells. DPPA significantly inhibited tumor growth, cell proliferation and tumor angiogenesis. Furthermore, DPPA strongly arrested the G2/M transition and further inhibited cell cycle progression in MDA-MB-231 cells. cyclin B1 (CCNB1) was the DPPA target that regulated cellular proliferation in human TNBC. DPPA, as an anti-cancer drug, inhibited the expression of CCNB1 to arrest the G2/M transition in human TNBC.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dihydroandrostenedione (Androstanedione) is a steroid metabolite and a precursor of both testosterone and estrone normally produced by the adrenal gland and gonads and is converted to testosterone through the action of 17β-hydroxysteroid dehydrogenase, which is found in most body tissues. Androstenedione is also produced by some plants and has recently been marketed as a product for increasing blood testosterone concentrations to be used as a natural alternative to anabolic steroid use. However, androstenedione administration during resistance training did not significantly alter the serum testosterone concentration in normotestosterogenic young men. The increased muscle size and strength observed with resistance training were also not augmented with androstenedione administration. The use of androstenedione increased the serum concentrations of estradiol and estrone, suggesting an increased aromatization of the ingested androstenedione and/or testosterone derived from the exogenous androstenedione. The use of androstenedione was associated with decreased levels of HDL-C. These data provide evidence that androstenedione does not enhance adaptations to resistance training and may result in potentially serious adverse health consequences in young men.
2-Methoxynaphthoquinone is a naturally occurring naphthalene derivative, first synthesized by L. Fieser in 1926, and afterward found in Impatiens balsamina (garden balsam). 2-Methoxynaphthoquinone possess antifungal activity. In vitro studies showed that compound inhibits Wnt signaling and suppresses the invasion of breast cancer cell lines, and is able to induce gastric adenocarcinoma necrosis.
Chelidonine is the major alkaloid component of Chelidonium majus. Chelidonine is an isolate of Papaveraceae with acetylcholinesterase and butyrylcholinesterase (a nonspecific cholinesterase) inhibitory activity. It showed strong cytotoxicity in cancer cells. While several modes of death have been identified, most of anti-cancer attempts have focused on stimulation of cells to undergo apoptosis. Chelidonine seems to trigger multiple mechanisms in MCF-7 breast cancer cells. It induces both apoptosis and autophagy modes of cell death in a dose dependent manner. Alteration of expression levels of bax/bcl2, and dapk1a by increasing concentration of chelidonine approves switching the death mode from apoptosis induced by very low to autophagy by high concentrations of this compound. On the other hand, submicromolar concentrations of chelidonine strongly suppressed telomerase at both enzyme activity and hTERT transcriptional level. Long exposure of the cells to 50 nanomolar concentration of chelidonine considerably accelerated senescence. Altogether, chelidonine may provide a promising chemistry from nature to treat cancer. Chelidonine exhibits a broad spectrum of pharmacological properties, such as anti-inflammatory and antiviral activities Its biological activities and clinical applications have been extensively investigated. Especially the usage of chelidonine as an anticancer drug is very important lately. It also has profound inhibitory effects on airway inflammation, which means chelidonine can improve allergic asthma in mice and may also work for human medicine.
Status:
US Previously Marketed
First approved in 1977

Class (Stereo):
CHEMICAL (ABSOLUTE)



Quinestrol is a synthetic estrogen that is effective in hormone replacement therapy. It is a 3-cyclopentyl ether of ethynyl estradiol. After gastrointestinal absorption, it is stored in adipose tissue, where it is slowly released and metabolized in the liver to its active form, ethinyl estradiol. Quinestrol has found limited use in suppressing lactation in postpartum women and, in combination with synthetic progestogens, as contraceptive therapy, although additional studies are needed for both applications. Estrogens diffuse into their target cells and interact with a protein receptor (the estrogen receptor). Estrogen interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).
Status:
US Previously Marketed
First approved in 1969

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Testolactone (Teslac brand name) is an anti-cancer agent, which was used as adjunctive therapy in the palliative treatment of advanced or disseminated breast cancer. The mechanism of testolactone action is reported to be related to the inhibition of aromatase enzymatic activity. Testolactone is no longer available in the USA.
Phenformin is a biguanide hypoglycemic agent with actions and uses similar to those of metformin. It activates AMP-activated protein kinase (AMPK) and inhibits mTORC1 signaling. Phenformin used for the treatment of diabetes. Phenformin was removed from the U.S. market 20 years ago because of a high incidence of lactic acidosis. Risk factors for the development of lactic acidosis include renal deficiency, hepatic disease, cardiac disease, and drug interaction such as cimetidine. Phenformin exerts potential anti-neoplastic action.
Novobiocin (also known as streptonivicin) is an aminocoumarin antibiotic, active against Staphylococcus epidermidis. Novobiocin and other aminocoumarin antibiotics act as a potent competitive inhibitor of DNA gyrase B. The oral form of the drug was withdrawn from the market in 1999 due to safety or effectiveness reasons. Later it was discovered that novobiocin inhibited Hsp90 and topoisomerase II, and novobiocin was investigated in clinical trials against metastatic breast cancer and non-small cell lung cancer. Topical form of novobiocin was investigated in combination with nalidixic acid for treatment of psoriasis.
Status:
US Previously Marketed
Source:
CYTELLIN by LILLY
(1961)
Source URL:
First approved in 1956
Source:
Cytellin by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Beta-sitosterol is one of the main dietary phytosterols found in plants which have a similar skeleton as cholesterol. In human clinical trials, beta-sitosterol has been shown to have cholesterol-lowering effects and to relieve symptoms of benign prostatic hyperplasia. There has been a large amount of basic research conducted for potential applications of beta-sitosterol in a diverse range of conditions including cervical cancer, breast cancer, cystic fibrosis, and others. Beta-sitosterol is available over the counter as a natural health supplement and is marketed for a wide range of applications including headaches, tuberculosis, allergies, cancers, fibromyalgia, lupus, asthma, hair loss and many others.

Showing 171 - 180 of 432 results