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

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Showing 381 - 390 of 1447 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Ricinine is an alkaloid originally isolated from the Ricinus communis, or castor-oil plant. Ricinine can be found in all parts of the plant and it is a quite strong insecticide. The castor seeds contain approximately 0.2% of the alkaloid. Ricinine or 3-cyano-4-methoxy-N-methyl-2-pyridone (CAS 524-40-3) belongs to the group of piperidine alkaloids. Ricinine is a useful scaffold for the synthesis of new antimicrobial and antiquorum-sensing derivatives in spite of its poor contribution to the antimicrobial activity of the plant extracts. Ricinine activated the Wnt signaling pathway by inhibiting casein kinase 1α. Ricinine-elicited seizures as a novel chemical model of convulsive seizure.
Enniatin B is a cyclic hexadepsipeptide it contains three N-methyl-Lvaline and three a-hydroxy-D-isovaleric molecules. It is generated by multiple Fusarium strains. It has ionophoric, antibiotic and insecticidal activity. A mixture of Enniatins A, A1, B and B1 (called fusafungine) was originally patented as local antibiotic for the topically treatment of nose and throat infections. Enniatin B is a mycotoxin contaminant found in vegetables, cereals and coffee. Enniatin B did not show genotoxic activity but demonstrated cytotoxicity at low micromolar concentrations. The observed activities included the specific inhibition of acyl-CoA cholesterol acyltransferase, depolarization of mitochondria, inhibition of osteoclastic bone resorption, and induction of apoptosis in cancer cells as well as the interaction with ATP-binding cassette transporters such as P-glycoprotein. Enniatin B demonstrated synergistic activity against cervical cancer in vitro and in vivo.
Coptisine (COP), a protoberberine alkaloid, is widely found in Chinese medicinal plants (family Berberidaceae, Ranunculaceae and Papaveraceae). It is reported that COP has a wide range of pharmacological and biological activities, including antibacterial, hypoglycemic, anti-tumorigenic, and gastric-mucous membrane protection. Considerable attention has been focused on its activity against central nervous system disorders, such as improving the symptoms of Alzheimer’s disease and even preventing its onset, by exerting antidepressant effects as a potent type A monoamine oxidase inhibitor. Coptisine was found to be an efficient uncompetitive Indoleamine 2,3-dioxygenase inhibitor. Coptisine is a potent inhibitor of human organic cation transporters.
Potassium tetrachloroplatinate is used in the preparation of platinum (Pt) nanoparticles. Ligands like ammonia or triphenyl phosphine can able to replace the chloride ligands to afford various derivatives. The replacement by ammonia results in the preparation of cisplatin, which is used in the cancer treatment. Further, it is used as catalyst in the hydroarylation reaction. Cisplatin and potassium tetrachloroplatinate are shown to bind to DNA that encapsulates SWNTs in aqueous solution. The bound platinum salt can then be reduced to decorate the DNA-encapsulated SWNTs with platinum nanoparticles. The unique combination of catalytic activity of nanoscale platinum, biological functionality of DNA, and optoelectronic properties of SWNTs suggests a myriad of applications including fuel cells, catalysts, biosensors, and electrochemical devices.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Ergocornine is an ergot alkaloid. Ergocornine can inhibit prolactin release by a direct action on the anterior pituitary. It can modulate activity at both dopamine and serotonin receptors.
Xanthoxyletin is a coumarin isolated from Erythrina variegata. It has been reported that Xanthoxyletin possesses antibacterial, fungicidal, and algicidal properties. Xanthoxyletin induces S phase arrest and apoptosis in human gastric adenocarcinoma SGC-7901 cells. Xanthoxyletin may be promising anticancer agent and has worth for further mechanistic and therapeutic studies against gastric cancer.
Dihydromethysticin is one of the six major kavalactones found in the roots of kava plant. Dihydromethysticin was found to be very effective in producing analgesia in the tail immersion test. Dihydromethysticin kavalactone induces apoptosis in osteosarcoma cells through modulation of PI3K/Akt pathway, disruption of mitochondrial membrane potential and inducing cell cycle arrest. Dihydromethysticin was identified as a promising lung cancer chemopreventive agent. Low concentrations of the kavalactone (+)-dihydromethysticin enhanced the binding of ligands to the GABAA receptors on freeze-dried rat cortex preparations.
AG-126 is the putative protein tyrosine kinase (PTK) inhibitor. It was found to rescue mice from lethal consequences of bacterial lipopolysaccharide (LPS) administration in a model of septic shock. AG126 treatment has beneficial effects in experimental autoimmune encephalomyelitis (EAE), a model for multiple sclerosis. AG126 alleviates the clinical symptoms, diminishes encephalitogenic Th17 differentiation, reduces inflammatory CNS infiltration as well as microglia activation and attenuates myelin damage. AG-126 have recently been shown to protect from acute kidney injury in experimental animal models of ischemia-reperfusion and sepsis-induced injury. AG-126 modulates secondary damage in experimental spinal cord trauma.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Pheophorbide A is a product of chlorophyll breakdown in plants. It is an active component of the Chinese medicinal herb Scutellaria barbata. Others report on extraction of the drug from sources as varied as spinach leaves and silkworm excreta, and on its confounding appearance in the digestive tracts of animals fed chlorophyll-containing food. Pheophorbide A acts as a photosensitizer in photodynamic therapy. Photoactivated pheophorbide A induces lipid peroxidation, arrests cell growth by activating apoptosis and/or necrosis. In vitro and animal studies have suggested some efficacy for pheophorbide A-mediated photodynamic therapy of cancers.