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Drug
Enzyme
Compound
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Target Concepts:
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Query: UMLS:C0279530 (
bone cancer
)
1,036
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Phytochemical investigation of Eupatorium hualienense (C. H. Ou, S. W. Chung, C. I. Peng) has resulted in the isolation of the new sesquiterpene lactones 1-5, named eupahualins A-E, along with the known heliangolide eupasimplicin B (6). The structures of the isolated compounds were established through detailed spectral analyses, especially by means of 2D-
NMR
techniques. Compounds 1-4 and 6 showed significant activities against cell lines of human chronic myelogenous leukemia (K562) and human
bone cancer
(U2OS).
...
PMID:New gemacranolides from Eupatorium hualienense. 1719 77
Anti-cancer activities of vanadium compounds have generated recent interest because of a combination of desirable properties for chemotherapy, i.e., strong cytotoxicities, anti-metastatic activities and relatively low systemic toxicities. Certain hydrophobic vanadium(v) Schiff base/catecholate compounds, which as shown herein, have increased stability in aqueous media and affinity for membrane interfaces. Depending on their hydrophobicity, they may be able to enter cells intact. In this manuscript, two hydrophobic V(v) catecholate substituted analogues, [VO(Hshed)(cat)] and [VO(Hshed)(dtb)], (Hshed = N-(salicylideneaminato)-N'-(2-hydroxyethyl)-1,2-ethanediamine, cat = pyrocatechol, and dtb = 3,5-di(tert-butyl)catechol and the vanadium(v) precursor [V(O)2(Hshed)]) were synthesized for their ability to interact with membranes and their anti-cancer effects. Using 51V and 1H
NMR
spectroscopy, the presence and location of the free ligand, H2shed, and the three V(v) complexes were examined in a model membrane microemulsion system. The stability of the three complexes was measured in aqueous solution, cell media and an inhomogeneous microemulsion system. Our results demonstrated that free ligand H2shed and the intact V(v) complexes associated with the interface but that the V-complexes hydrolyzed to some extent because oxovanadates were observed by 51V
NMR
spectroscopy and decreasing complex by absorption spectroscopy in cell media. When determining the effects of V(v) catecholate complexes on
bone cancer
cells, the strongest effects were observed with the more stable hydrophobic complex [VO(Hshed)(dtb)] that was able to best associate and penetrate the model membrane system intact. These studies are consistent with the membrane permeability studies being a good predictor for in vitro cytotoxicity assays because [VO(Hshed)(dtb)] can pass through the cellular membrane intact, which may enhance its anti-cancer activities.
...
PMID:Hydrophobicity may enhance membrane affinity and anti-cancer effects of Schiff base vanadium(v) catecholate complexes. 3094 80