Search results for "AGENTS"
showing 10 items of 7330 documents
Oxidation of carbidopa by tyrosinase and its effect on murine melanoma
2009
Oxidation of the anti-Parkinsonian agent carbidopa by tyrosinase was investigated. The products of this reaction were identified as 3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid and 6,7-dihydroxy-3-methylcinnoline. These results demonstrate that after oxidation of the catechol moiety to an o-quinone either a redox exchange with the hydrazine group or a cyclization reaction occur. The cyclization product underwent additional oxidation reactions leading to aromatization. The cyclization reaction is undesired in the case of hydrazine-containing anti-melanoma prodrugs and will have to be taken into account in designing such compounds. Carbidopa was tested against B16(F10) melanoma cells in cul…
Indirect oxidation of the antitumor agent procarbazine by tyrosinase—Possible application in designing anti-melanoma prodrugs
2008
The interaction of tyrosinase with the anticancer drug procarbazine has been investigated. In the presence of the enzyme alone no oxidation of this dialkylhydrazine above the background level was observed. However, when phenolic substrates (4-tert-butylcatechol or N-acetyl-l-tyrosine) were included in the reaction mixture, procarbazine was rapidly degraded. Oxygen consumption measurements showed that in a mixture both the phenolic substrate and the drug were oxidized. The major product of procarbazine degradation was isolated and identified as azoprocarbazine, the first active metabolite of this drug detected in previous in vivo and in vitro studies. This indirect oxidation of the hydrazine…
Spectrophotometric investigation of the binding of vitamin E to water-containing reversed micelles.
2002
The distribution constants of vitamin E partitioned between apolar organic phase and water-containing reversed micelles of sodium bis (2-ethylhexyl) sulfosuccinate (AOT), didodecyldimethylammonium bromide (DDAB), soybean phosphatidylcholine (lecithin) and tetraethylene glycol monododecyl ether (C12E4) have been evaluated by a spectrophotometric method. The results suggest that in the presence of domains from apolar organic solvent to surfactant and to water, vitamin E is partitioned between the micellar palisade layer and the organic solvent and also that its binding strength to reversed micelles depends mainly by specific interactions between the head group of vitamin E and that of the sur…
Analytical methodologies for atomic spectrometric determination of metallic oxides in UV sunscreen creams.
2000
In this study, methodologies for determining titanium oxide, zinc oxide and iron oxide are proposed and assayed in commercial sunscreen products. The proposed methodology for TiO2, determination in sunscreens is based on a microwave-assisted treatment for digesting the organic components in a closed teflon reactor in presence of HNO3 and HCl. Titanium is determined by inductive coupled plasma emission spectrometry (ICP-AES). The proposed methodologies for measuring ZnO and Fe2O3 are based on a sample emulsification in water with a non ionic tensioactive and IBMK, followed by Zn and Fe determination by flame atomic absorption spectrometry (FAAS). The methodologies allow a precise and accurat…
UV-induced cross-linking of proteins to plasmid pBR322 containing 8-azidoadenine 2′-deoxyribonucleotides
1988
Abstract An efficient method of cross-linking DNA to protein is described. The method is based on the incorporation of photoactive 8-azidoadenine 2′-deoxyribonucleotides into DNA. We have found that 8-N 3 dATP is a substrate for E. coli DNA polymerase I and that 8-N 3 dATP can be incorporated into plasmid pBR322 by nick-translation. Subsequently we were able to cross-link a set of different proteins to 8-azido-2′-deoxyadenosine-containing pBR322 by UV irradiation (366 nm). No DNA-protein photocross-linking was observed under the same conditions when the non-photoactive plasmid pBR322 was used.
Pyrrolo[2,3-h]quinolinones: A new ring system with potent photoantiproliferative activity
2006
A new class of compounds, the pyrrolo[2,3-h]quinolin-2-ones, nitrogen isosters of the angular furocoumarin Angelicin, was synthesized with the aim of obtaining new photochemotherapeutic agents with increased antiproliferative activity and lower undesired toxic effects than the lead compound. Two synthetic pathways were approached to allow the isolation both of the dihydroderivatives 10-17 and of the aromatic ring system 23. Compounds 10-17 showed a remarkable phototoxicity and a great UVA dose dependence reaching IC(50) values at submicromolar level. Intracellular localization of these compounds has been evaluated by means of fluorescence microscopy using tetramethylrhodamine methyl ester a…
More about the developing of invisible lipstick-contaminated lipmarks on human skin: The usefulness of fluorescent dyes
2006
At the present time fingerprints are one of the simplest, and most reliable means of identification. Increasingly, crime scene investigators look for palm, foot, ear or lip prints. With regard to lip prints, the use, very common today, of protective or permanent lipsticks allow the production an invisible lipmark (or invisible lipstick-contaminated lipmark) which is possible to develop. Some results have already been published about developers useful for different kinds of surfaces (both porous and non-porous) as well as those which are more efficient in case of old or recent prints. The latest studies are about the developing on human skin, and they prove the usefulness of lysochromes (spe…
Antioxidant betalains from cactus pear (Opuntia ficus-indica) inhibit endothelial ICAM-1 expression.
2004
It has been suggested that some pigments would have antioxidant properties and that their presence in dietary constituents would contribute to reduce the risk of oxidative stress–correlated diseases. Among others, inflammatory response depends on redox status and may implicate oxidative stress. Vascular endothelial cells are a direct target of oxidative stress in inflammation. We have tested the impact of the free radical scavenger and antioxidant properties of betalains from the prickle pear in an in vitro model of endothelial cells. Here we show the capacity of betalains to protect endothelium from cytokine- induced redox state alteration, through ICAM-1 inhibition. KEYWORDS: endothelial …
Wet-chemical approach for the cell-adhesive modification of polytetrafluoroethylene
2011
Polytetrafluoroethylene (PTFE), a frequently utilized polymer for the fabrication of synthetic vascular grafts, was surface-modified by means of a wet-chemical process. The inherently non-cell-adhesive polymer does not support cellular attachment, a prerequisite for the endothelialization of luminal surface grafts in small diameter applications. To impart the material with cell-adhesive properties a treatment with sodium-naphthalene provided a basis for the subsequent immobilization of the adhesion promoting RGD-peptide using a hydroxy- and amine-reactive crosslinker. Successful conjugation was shown with cell culture experiments which demonstrated excellent endothelial cell growth on the m…
Tranexamic acid in cardiac surgery: Are low doses enough?
2020
OBJECTIVES Tranexamic acid is used to prevent hyperfibrinolysis and reduce postoperative bleeding and blood transfusions in on-pump cardiac surgery. We evaluate the efficacy of low or high dose tranexamic acid in a prospective cohort study conducted in Valencia. MATERIALS AND METHODS A total of 427 patients were recruited between January 2019 and January 2020, 207 in the Hospital General Universitario (low dose [LD]) and 220 in the Hospital Universitario y Politecnico La Fe (high dose [HD] and intermediate dose [ID]). We recorded the presence of hyperfibrinolysis on rotational thromboelastometry, intra- and postoperative administration of blood products, chest tube output within the first 1…