RESUMEN
This paper studies the effect of plant peptides of thionine Ns-W2 extracted from seeds of fennel flower (Nigella sativa) and ß-purothionine from wheat germs (Triticum kiharae), as well as a synthetic antimutagen (crown-compound), on the expression of several genes involved in the.control of cellular homeostasis, processes of carcinogenesis, and radiation response in human rhabdomyosarcoma cells (RD cells), T-lymphoblastoid cell line Jurkat, and blood cells. All of these agents acted as antimutagens-anticarcinogens, reducing the expression of genes involved in carcinogenesis (genes of families MMP, TIMP, and IAP and G-protein genes) in a tumor cell. A pronounced reduction in the mRNA level of these genes was caused by thionine Ns-W2, and the least effect was demonstrated by ß-purothionine. Antimutagens had very little effect on the mRNA levels of the several studied genes in normal blood cells.
Asunto(s)
Antimutagênicos/administración & dosificación , Péptidos/administración & dosificación , Fenotiazinas/administración & dosificación , Extractos Vegetales/administración & dosificación , Rabdomiosarcoma/genética , Antimutagênicos/química , Carcinogénesis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Humanos , Nigella sativa/química , Péptidos/química , Fenotiazinas/química , Extractos Vegetales/química , Radiación Ionizante , Rabdomiosarcoma/tratamiento farmacológico , Rabdomiosarcoma/patología , Triticum/química , Proteína p53 Supresora de Tumor/biosíntesisAsunto(s)
Antimutagênicos/farmacología , Benzodiazepinas/farmacología , Regulación Neoplásica de la Expresión Génica , Linfocitos/metabolismo , Rabdomiosarcoma/metabolismo , Línea Celular Tumoral , Humanos , Proteínas Inhibidoras de la Apoptosis/genética , Proteínas Inhibidoras de la Apoptosis/metabolismo , Linfocitos/efectos de los fármacos , Metaloproteinasas de la Matriz/genética , Metaloproteinasas de la Matriz/metabolismo , MicroARNs/genética , MicroARNs/metabolismo , FN-kappa B/genética , FN-kappa B/metabolismo , Inhibidor Tisular de Metaloproteinasa-1/genética , Inhibidor Tisular de Metaloproteinasa-1/metabolismo , Inhibidor Tisular de Metaloproteinasa-2/genética , Inhibidor Tisular de Metaloproteinasa-2/metabolismoAsunto(s)
Antimutagênicos/farmacología , Transcripción Genética/efectos de los fármacos , Péptidos Catiónicos Antimicrobianos/farmacología , Estudios de Casos y Controles , Síndrome de Down/genética , Síndrome de Down/metabolismo , Glutatión Peroxidasa/genética , Glutatión Peroxidasa/metabolismo , Proteínas de Choque Térmico/genética , Proteínas de Choque Térmico/metabolismo , Humanos , Linfocitos/efectos de los fármacos , Linfocitos/metabolismo , Tasa de Mutación , Proteínas Nucleares/genética , Proteínas Nucleares/metabolismo , Nucleofosmina , Proteínas Oncogénicas/genética , Proteínas Oncogénicas/metabolismo , Proteínas de Plantas/farmacología , ARN Mensajero/genética , ARN Mensajero/metabolismo , Superóxido Dismutasa/genética , Superóxido Dismutasa/metabolismoAsunto(s)
Péptidos Catiónicos Antimicrobianos/farmacología , Antimutagênicos/farmacología , Compuestos Corona/farmacología , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Linfocitos/metabolismo , Neoplasias Experimentales/metabolismo , Proteínas Oncogénicas/metabolismo , Proteínas de Plantas/farmacología , Células Cultivadas , Humanos , Linfocitos/efectos de los fármacosRESUMEN
Two amphiphilic butadienyl dyes 1 and 2 form stable monolayers at the air/water interface in the presence of various salts. Dye 1 consists of the basic amphiphilic butadienyl chromophore. In dye 2, the dimethoxybenzene part of dye 1 is substituted by benzodithia-15-crown-5. The monolayers have been characterized by surface pressure-area and surface potential-area isotherms as well as Brewster angle microscopy and reflection spectroscopy. In contrast to dye 1, dye 2 interacts specifically with Hg(2+) and Ag(+) cations forming complexes. No complex formation was observed with alkali and earth alkali metal ions. The nature of the anion (Cl(-) or ClO(4)(-)) influences the monolayer behaviour of both dyes. At the air/water interface, besides monomers of the dyes, two types of associates are coexisting in the pure dye monolayers on aqueous salt solutions, attributed to dimers and aggregates, respectively. Their equilibria depend on the nature of both cations and anions in the subphase, as in the case of dye 2, or only anions, as in the case of dye 1. The dimers may be organized as head-to-tail dimers with the intermolecular distances 0.38 and 0.45nm for dye 1 and dye 2, respectively. According to the extended dipole model, we propose formation of aggregates in which the chromophores are parallel to each other with the same intermolecular distances as in the dimers, and the centers of their transition moments shifted by 0.95nm (dye 1) and 1.2nm (dye 2).
Asunto(s)
Derivados del Benceno/química , Butadienos/química , Colorantes/química , Éteres Corona/química , Sales (Química)/química , Aire , Microscopía/métodos , Soluciones , Propiedades de Superficie , AguaRESUMEN
Two new benzodiaza-15-crown-5 compounds containing two N-hydroxycarbonylmethyl or N-hydroxycarbonylpropyl substitutes were synthesized. The first of these compounds exhibited more pronounced protective effects towards human cells according to criteria of primary DNA injury and cell survival after exposure to gamma-radiation and CdCl2; by antimutagenic activity this compound was comparable to garlic extract. The antimutagenic effect of these compounds was realized not through the antioxidant mechanism.
Asunto(s)
Antimutagênicos/farmacología , Compuestos Aza/farmacología , Compuestos Corona/farmacología , Cloruro de Cadmio/farmacología , Daño del ADN , Rayos gamma , HumanosAsunto(s)
Antimutagênicos/farmacología , Éteres Corona/farmacología , Daño del ADN/efectos de los fármacos , Reparación del ADN/efectos de los fármacos , Leucocitos/efectos de los fármacos , Protectores contra Radiación/farmacología , Antimutagênicos/química , Éteres Corona/química , ADN/efectos de la radiación , Reparación del ADN/genética , Rayos gamma , Humanos , Leucocitos/efectos de la radiación , Mutación , Protectores contra Radiación/químicaRESUMEN
The novel amphiphilic benzodithia-18-crown-6 butadienyl dye (1) forms relatively stable insoluble monolayers on distilled water (collapse pressure of 41 mN/m) and on aqueous subphases containing alkali metal or heavy metal salts (collapse pressures in the range of 27-38 mN/m, respectively). The dye 1 monolayer organization depends on chromophore association and interactions (especially complex formation) with heavy and alkali metal ions as deduced from surface pressure-area and surface potential-area isotherms as well as reflection spectra and Brewster angle microscopy observations. Dye 1 undergoes specific interactions with Hg(2+) and Ag(+), respectively (formation of different complexes). Nonspecific interactions have been observed with other salts, such as KClO(4) or Pb(ClO(4))(2). Further, dye 1 monolayers on 1 mM Hg(ClO(4))(2) solution undergo reversible photoisomerization, in contrast to monolayers on water and other aqueous salt subphases.
RESUMEN
Antimutagenic activity of N-carboxyalkyl derivatives of aza- and benzoazacrown compounds was revealed and antimutagenic activity of garlic extract was confirmed. Specific genoprotective effect of crown compounds towards the effects of various mutagens was demonstrated. The antimutagenic effect of these compounds was not realized via antioxidant mechanisms, while the protective effect of garlic extract was associated with its antioxidant and reparative activities.
Asunto(s)
Antimutagênicos/metabolismo , Antioxidantes/metabolismo , Éteres Corona/metabolismo , Ajo/química , Extractos Vegetales/metabolismo , Antimutagênicos/farmacología , Antioxidantes/farmacología , Línea Celular , Éteres Corona/farmacología , ADN/efectos de los fármacos , Daño del ADN , Humanos , Leucocitos/citología , Leucocitos/efectos de los fármacos , Extractos Vegetales/farmacologíaAsunto(s)
Antimutagênicos/farmacología , Éteres Cíclicos/farmacología , 4-Nitroquinolina-1-Óxido/farmacología , Antimutagênicos/química , Antioxidantes/farmacología , Cloruro de Cadmio/farmacología , Células Cultivadas , ADN/efectos de los fármacos , ADN/metabolismo , ADN/efectos de la radiación , Daño del ADN , Reparación del ADN , Éteres Cíclicos/química , Rayos gamma , Ajo/química , Humanos , Estructura Molecular , Mutágenos/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacologíaRESUMEN
New amphiphilic photochromic benzo-15(18)-crown-5(6) ethers (APC) differing in the position of the octadecyl substituent and the size of the crown cavity were synthesized. The compounds form stable monolayers in the air/water and air/alkaline metal salt solution interfaces. The results of the pressure isotherm measurements, atomic force microscopy (AFM), and electronic spectroscopy show that the structure of the monolayers formed depends on the structure of the parent APC and the nature of the cation in salt solutions. The area per molecule of APC in the monolayer (specific area) is the smallest on the water surface and increases by 20-40% on the aqueous subphase surface with an increasing concentration of salts therein to indicate the formation of APC complexes with the metal cations. When the hydrophobic aliphatic substituent is displaced from position 3 to position 5 of the benzothiazole ring, the specific area on the surface of water and subphases decreases twofold, which indicates the compactization of the monolayer on this modification. A reversible E-Z-photoisomerization of APC was found in the monolayers formed in the salt solution/air interface. The features of the reaction are defined by the specific organization of the amphiphilic molecules in the monolayer and by the nature of the cation.