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

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Showing 331 - 340 of 1447 results

Androstanol is a steroid acting as the inverse agonist of constitutive androstane receptor. In addition, androstanol activates pregnane X receptor. In animal models, it protects from drug-induced liver injury. Androstanol appears to be a pheromone.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


(-)-Sesamin is a lignan present in sesam oil and a number of medicinal plants. It exerts various pharmacological effects, such as prevention of hyperlipidemia, hypertension, and carcinogenesis. Moreover, (-)-sesamin has chemopreventive and anticancer activity in vitro and in vivo. (-)-Sesamin is an inhibitor of human mitochondrial Lon protease and DNA damage agents to activate the DNA damage checkpoints as well induce apoptosis in NSCLC cells. (-)-Sesamin is an antioxidant, showing effective 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity.
ASARININ, (+)- ((+)-episesamin), an abundant lignan in sesame seed, has been identified as an active principle in an aqueous extract of Lindera obtusiloba (Japanese Spicebush) with a strong anti-inflammatory potential. (+)-episesamin (ES) is known to block the TNF-α-induced mitogenic VSMC response. Protective effect of (+)-episesamin against PDGF-BB-induced activation of vascular smooth muscle cells is mediated by induction of haem oxygenase-1 and inhibition of mitogenic signalling. ES interferes with inflammation-associated VSMC activation and subsequent decreased proliferation and migration due to anti-oxidative properties and impaired activation of NF-ĸB, known contributors to atherogenesis. These results suggest ES as a complemental treatment of VSMC specific vascular diseases such as atherosclerosis. (+)-Episesamin inhibits adipogenesis and exerts anti-inflammatory effects in 3T3-L1 (pre)adipocytes by sustained Wnt signaling, down-regulation of PPARγ and induction of iNOS. (+)-episesamin seems to be the active drug in the L. obtusiloba extract being responsible for the inhibition of adipogenesis and, thus, should be evaluated as a novel potential complementary treatment for obesity.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Domoic acid is one of the best-known marine toxins, causative of important neurotoxic alterations. In the year 1987, domoic acid was responsible for four deaths and the illness of more than 100 people after consuming blue mussels (Mytilus edulis) harvested in the Cardigan Bay of Prince Edward Island, Canada. The symptomatology comprised three kinds of signs: gastrointestinal (nausea, vomiting,), cardiovascular (unstable blood pressure and arrhythmias), and neurological signs (disorientation, confusion, hallucinations, coma, and memory impairment). After this event was discovered the domoic acid epileptic. Nearly a year after the amnesic shellfish poisoning event, an 84 years old male survivor re-experienced severe seizures and was diagnosed with temporal lobe epilepsy caused by domoic acid intoxication. This toxin has a high affinity for the glutamate receptors (GluRs) subtypes: alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and KA receptors. The binding of domoic acid to receptors provokes an increase of calcium (Ca2+) levels, causing the release of Glu to the extracellular space, and the activation of N-methyl-d-aspartate (NMDA) receptors. The histological consequences of these cellular alterations comprise astrocytosis, cytoskeletal disarrangement and, finally, cell death.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

5-eicosenoic acid (C20:1omega15), a cis-unsaturated free fatty acid, plays a significant role in PKC-epsilon activation and potentiation of nicotinic ACh receptor responses.
Solanesol is a naturally occurring isoprenoid and the most abundant lipid in tobacco leaves. It is also found in tomato, potato, eggplant, and pepper plants. Solanesol is widely used in the pharmaceutical industry as an intermediate for the synthesis of ubiquinone drugs, such as coenzyme Q10 and vitamin K2. Solanesol possesses antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, and anti-ulcer activities, and solanesol derivatives also have anti-oxidant and antitumor activities. Solanesol has been shown to increase the expression of HO-1 and Hsp70 which may contribute to the prevention of ethanol-induced cell damage. Solanesol is readily introduced into the body as a component of tobacco smoke.