RESUMEN
Preliminary results have shown that merocyanines were cytotoxic for human adenocarcinoma cells in vitro. We report the synthesis of a series of new merocyanines and the structure-effect relationship as cytotoxic agents on human adenocarcinoma cells in vitro. Some of these new derivatives were found very cytotoxic for tumor cells in vitro, whereas their systemic toxicity in vivo was very low.
Asunto(s)
Adenocarcinoma/patología , Antineoplásicos/farmacología , Pirimidinonas/farmacología , Animales , Humanos , Ratones , Ratones Endogámicos C57BL , Pruebas de Mutagenicidad , Relación Estructura-Actividad , Células Tumorales Cultivadas/efectos de los fármacosRESUMEN
Lauryl sucrose has recently been shown to decrease the toxicity of amphotericin B (AmB), a widely used antifungal agent, probably through a modulation of its physical state. In this paper, we demonstrate using a lymphoproliferative assay, that lauryl sucrose and monosubstituted analogs in addition to their effects on AmB also possess significant immune enhancer properties. An anti-bell shape relationship was observed between stimulation of lymphoproliferation and chain length of ester's fatty acid, lauryl sucrose being the less active of the tested derivatives. These properties of sucrose esters are discussed in the specific context of antifungal therapy.
Asunto(s)
Ácidos Láuricos/farmacología , Activación de Linfocitos/efectos de los fármacos , Sacarosa/análogos & derivados , Adyuvantes Inmunológicos , Anfotericina B/antagonistas & inhibidores , Anfotericina B/toxicidad , Animales , Técnicas In Vitro , Ratones , Ratones Endogámicos BALB C , Sacarosa/farmacologíaRESUMEN
We report the synthesis of a series of merocyanines and the structure-effect relationship as cytotoxic agents for human adenocarcinoma cells in vitro. The cytotoxicity of these compounds in vitro makes them potential anticancer agents. One of these compounds was found active on human and mouse tumor models.
Asunto(s)
Antineoplásicos/síntesis química , Piridinas/farmacología , Adenocarcinoma/tratamiento farmacológico , Antineoplásicos/uso terapéutico , Humanos , Piridinas/síntesis química , Relación Estructura-Actividad , Células Tumorales CultivadasRESUMEN
A procedure was developed for gas chromatographic analysis of glycine-type amphoteric surfactants. The commercial samples contained N-alkylaminopropylglycines, N-alkylamines and N-alkylaminopropylamines. Some di- and triacids were also detected. The method proposed allows a good separation according to both the carbon number and the chemical function.
Asunto(s)
Aminoácidos Diaminos/análisis , Glicina/análogos & derivados , Tensoactivos/análisis , Cromatografía de Gases , Glicina/análisis , Indicadores y ReactivosRESUMEN
The amphotericin B (AmB) - ergosterol complex, formed by interaction of the antibiotic with ergosterol-containing phospholipid vesicles, is associated with the lipid bilayer. It has been shown by circular dichroism studies that the AmB-ergosterol complex formed in water-propanol binary mixtures has a similar structure to that observed in phospholipid vesicles. A positive cooperativity is found for the interaction of AmB with ergosterol. The similar AmB-cholesterol complex is much less stable and rearranges rapidly to a different conformation.