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Restrict the search for
alpha-tocopherol acetate
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
PRT062607 (BIIB-057; P 50515 PRT-2607; PRT062607) is a highly specific and potent inhibitor of spleen tyrosine kinase (Syk). PRT062607 (BIIB-057) has a desirable pharmacokinetics profile and is capable of safely, potently, and selectively suppressing SYK kinase function in humans following once-daily oral dosing. The compound is being evaluated for the treatment of chronic inflammatory diseases; including rheumatoid arthritis, systemic lupus erythematosus, non-Hodgkin's lymphoma and chronic lymphocytic leukaemia. Phase I development is underway in the US and the UK for the treatment of patients with inflammation and cancer. Phase I development is also being conducted in rheumatoid arthritis and systemic lupus erythematosus, presumably in the US.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Dehydroabietic acid (DHA or DAA), a diterpene, is obtained from Commiphora oppbalsamum. DHA has potential as treatment for obesity and metabolic syndrome, obese diabetic KK-Ay mice treated with DHA showed decreased plasma glucose, insulin, and triglyceride levels. It has been reported that DHA inhibits the production of proinfammatory mediators such as TNF-α in macrophages and adipocytes and causes endothelium-dependent relaxation of pulmonary artery via PI3K/Akt-eNOS signaling pathway. Also was shown, that DHA could reverse several cell responses stimulated by TNF-α, including the activation of FOXO1 and the TGF-β1/Smad3 signaling pathway. Thus, DAA could be useful in improving the diabetic wound healing.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ellipticine (5,11-dimethyl-6H-pyrido[4,3-b]carbazole), an alkaloid isolated from Apocyanaceae plants (i.e. Ochrosia borbonica, Excavatia coccinea), and several its derivatives exhibit significant antitumor and anti-HIV activities. This compound is one of the simplest naturally occurring alkaloids, having a planar structure. It was first isolated in 1959 from the leaves of the evergreen tree Ochrosia elliptica, which grows wild in Oceania. Ellipticine and its more soluble derivatives (9-hydroxyellipticine, 9-hydroxy-N2-methylellipticinium, 9-chloro-N2 -methylellipticinium and 9-methoxy-N2 -methylellipticinium) exhibit promising results for the treatment of osteolytic breast cancer metastases, kidney cancer, brain tumors and acute myeloblastic leukemia. The main reason for the interest in ellipticine and its derivatives for clinical purposes is their high efficiencies against several types of cancer, their rather limited toxic side effects and their complete lack of hematological toxicity. Nevertheless, the mutagenicity of ellipticines should be evaluated as a potential risk factor for these anticancer agents. Most ellipticines are mutagenic to Salmonella typhimurium Ames tester strains, bacteriophage T4, Neurospora crassa, and mammalian cells and induce prophage lambda in Escherichia coli. The anti-tumor therapeutic ellipticine and its derivatives act as potent anticancer agents via a combined mechanism involving cell cycle arrest and induction of apoptosis. Cell death induced by ellipticine has been shown to engage a p53-dependent pathway, cell cycle arrest, interaction with several kinases and induction of the mitochondrial pathway of apoptotic cell death. Cell cycle arrest was shown to result from DNA damage caused by a variety of tumor chemotherapeutic agents; this is also the case for ellipticines. The prevalent DNA-mediated mechanisms of anti-tumor, mutagenic and cytotoxic activities of ellipticine are (i) intercalation into DNA, (ii) inhibition of DNA topoisomerase II activity, and (iii) covalent binding to DNA in vitro and in vivo after enzymatic activation by cytochrome P450 and/or peroxidase enzymes The mechanism leading to apoptosis by ellipticine is thought to also be associated with DNA damage, by inhibition of topoisomerase II and the covalent modification of DNA. In addition, the formation of ellipticine-DNA adducts ultimately can mutate cancer cells or initiate cell death.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Abietic acid (AA), a diterpene produced by conifer species, such as grand fir and lodgepole pine, has been reported to have anti-inflammatory and immunomodulatory effects and can be used as a wound-healing agent. Its treatment elevates cell migration and tube formation in human umbilical vein vascular endothelial cells by the activation of ERK and p38 MAPKs. In addition was shown, that abietic acid could be used as an antimetastatic agent or as an adjuvant for anticancer therapy. AA acts as a PPARα/γ dual activator to inhibit age-related inflammation by suppressing NF-κB and the MAPK/AP-1 pathway and can be a useful agent for improving skin photoaging.
