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

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Showing 1 - 10 of 15 results

Luteolin, 3',4',5,7-tetrahydroxyflavone, is a common flavonoid that exists in many types of plants including fruits, vegetables, and medicinal herbs. Plants rich in luteolin have been used in Chinese traditional medicine for treating various diseases such as hypertension, inflammatory disorders, and cancer. Luteolin possesses a variety of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial and anticancer activities. Numerous studies have shown that luteolin possesses beneficial neuroprotective effects both in vitro and in vivo.
Status:
Investigational
Source:
NCT00000650: Not Applicable Interventional Completed HIV Infections
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Ditiocarb, the sodium salt of diethyldithiocarbamate, is a drug with strong antioxidant capacity and chelating activities. It improves the depressed immune responses of newborn and aged mice and mice that are treated with chemotherapy or irradiation. Ditiocarb prevents cisplatin nephrotoxicity in animals without reducing the drug's antitumor activity. Ditiocarb has therapeutic activity in the LP-BM5 murine retrovirus-induced immunodeficiency disease. In that AIDS model, it reduces lymphadenopathy and hypergammaglobulinemia, restores immunocompetence, and prolongs survival. Ditiocarb was safe and reduced the incidence of opportunistic infections in patients with symptomatic HIV infection but ditiocarb had no positive effect on HIV patients. The administration of ditiocarb did not induce any major adverse clinical or biological reactions. Sixty-four patients with nonmetastatic high-risk breast cancer were randomized in a double-blind trial of adjuvant immunotherapy with sodium ditiocarb (DDC) versus placebo. At 6 years, overall survival was 81% in DDC group versus 55%.
Isorhamnetin, a flavonol aglycone, isolated from the traditional Chinese medicine H. rhamnoides L., was frequently used in traditional medicine to prevent and treat diverse diseases. Isorhamnetin has been shown to play a variety of roles in anti-oxidation, anti-inflammation, anti-tumor, anti-viral, and neurodegenerative injury protection. Isorhamnetin could inhibit the H2O2-induced activation of the intrinsic apoptotic pathway by scavenging free ROS and extracellular signal-regulated kinase 1/2 (ERK1/2) inactivation. In the type 2 diabetic rat model, isorhamnetin was found to be able to inhibit the NF-κB signaling activity, attenuate oxidative stress, and decrease the production of inflammatory mediators. Isorhamnetin can suppress skin cancer, breast cancer, colon cancer and atherosclerosis by inhibiting PI3K/AKT activation. Isorhamnetin shows inhibitory activity toward CYP1B1 expression and function.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Formononetin, an isoflavone, derived from Astragalus membranaceus, possesses the potential to reduce obesity and associated metabolic disorders. Formononetin displays estrogenic properties and induces angiogenesis activities. It regulates adipocyte thermogenesis as a partial PPARγ agonist and produces proangiogenesis effects through estrogen receptor alpha (ERα)-enhanced ROCK-II signaling pathways, by direct binding to the ligand-binding domain (LBD) of ERα. Besides, was shown, that formononetin inhibits HMGB1 release by decreasing HMGB1 acetylation via upregulating SIRT1 in a PPARδ-dependent manner and the identification of this process may help to treat inflammation-related disorders.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Biochanin A, a natural organic compound derived from herbal plants such as peanuts, soy, and red clover, possesses various pharmacological properties including antioxidant and anti-inflammatory. In addition, the compound has anticancer activity, which was shown in the following cells: head and neck squamous cell carcinoma and in osteosarcoma. In both cases, biochanin A induced apoptotic signaling pathway. It has also been found biochanin-A was an inhibitor of fatty acid amide hydrolase.
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:

Genistin is an 7-O-beta-D-glucosideform of genistein and is the predominant form of the isoflavone naturally occurring in a number of dietary plants like soy and kudzu. In vitro study have shown that both genistin and genistein are capable of enhancing bone metabolism in the femoral-metaphyseal tissues of elderly rats. The presence of genistein or genistin in the tissue culture caused a significant increase in alkaline phosphatase activity, deoxyribonucleic acid (DNA) and calcium contents. The effect of genistein was greater than that of genistin. It is also revealed that genistin has a strong bone loss preventive activity on experimental rats, and is especially enhanced by combination with fructooligosaccharides. The amount of new bone produced by grafting genistin in collagenmatrix was compared to the bone produced by collagen matrix alone in New Zealand White rabbits, and was observed that genistin caused significant increase in bone formation.
Naringenin is one of the most abundant flavonoids in natural citrus fruits and has been studied as an antioxidant and anti-inflammatory agent. Besides, it has been investigated for its ability to inhibit the growth of breast, colon, gastric and prostate cancer cells. Experiments on rodents have revealed, that naringenin is a component of Drynaria Rhizome and can enhance memory function and ameliorate Alzheimer's disease pathologies. Using the experimental autoimmune encephalomyelitis, a rodent model of human multiple sclerosis was determined that naringenin may have a potential to ameliorate autoimmune disease by favorably modulating autoimmune response. The precise mechanism of action of naringenin compound is not clear, but it is known, that it is a partial agonist of estrogen receptor that can act as a competitive antagonist in the presence of a potent (or full) agonist. In addition, it binds to collapsin response mediator protein 2 protein (CRMP2) and reduces the Aβ-induced phosphorylation of CRMP2, resulting in axonal growth facilitation.
Chrysin (aka 5,7-dihydroxyflavone) is a naturally occurring flavone found in honey, propolis, honeycomb, passion flowers, and Oroxylum indicum. Chrysin is used as an ingredient in dietary supplements and topical medications which are marketed to improve physical performance o treat various conditions. It has also been investigated for its immunoregulatory, anti-inflammatory an neuroprotective properties. Chrysin appears to be poorly absorbed and readily metabolize.
Status:
Possibly Marketed Outside US
Source:
NCT02796794: Phase 4 Interventional Unknown status Sepsis
(2015)
Source URL:
First approved in 2007
Source:
Fosteum by Primus Pharmaceuticals, Inc.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GENISTEIN is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA topoisomerases, type II) activity and is used as an antineoplastic and antitumor agent. Experimentally, it has been shown to induce G2 phase arrest in human and murine cell lines. Additionally, genistein has antihelmintic activity. It has been determined to be the active ingredient in Felmingia vestita, which is a plant traditionally used against worms. It has also been demonstrated to be effective against intestinal parasites such as the common liver fluke, pork trematode and poultry cestode. Further, genistein is a phytoestrogen which has selective estrogen receptor modulator properties. It has been investigated in clinical trials as an alternative to classical hormone therapy to help prevent cardiovascular disease in postmenopausal women. Genistein can be found in food sources such as tofu, fava beans, soybeans, kudzu, and lupin. It is also present in certain cell cultures and medicinal plants.

Showing 1 - 10 of 15 results