RESUMEN
Antimicrobial and hemolytic activity of ethanol extract of brown seaweed Laminaria cichorioides Miyabe, its lipophilic fractions, various classes of substances of lipophilic fraction, such as chlorophylls, fucoxanthin, monogalactosyldiacylglycerols, digalactosyldiacylglycerols, sulfoquinovosyldiacylglycerols, and fatty acids were investigated. The antimicrobial activity was studied by means of yeast cells Safale S-04 and Candida albicans CMM 455, fungi Aspergillus niger CMM 4634 and Fusarium oxysporum CMM 4639, bacteria Staphylococcus aureus ATCC 21027 (gram-positive) and Escherichia coli ATCC 15034 (gram-negative) which demonstrated selective sensitivity to the studied substances. Hemolytic activity was investigated at concentrations of substances in the range of 0.2-2000 microg/ml at different pH of erythrocyte suspension. All investigated substances caused hemolysis. The dependence of hemolytic activity of substances on pH of media was determined.
Asunto(s)
Antiinfecciosos/farmacología , Hemolíticos/farmacología , Laminaria/química , Animales , Antiinfecciosos/aislamiento & purificación , Aspergillus niger/efectos de los fármacos , Candida albicans/efectos de los fármacos , Eritrocitos/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Fusarium/efectos de los fármacos , Hemólisis , Hemolíticos/aislamiento & purificación , Ratones , Staphylococcus aureus/efectos de los fármacosRESUMEN
Germination of buckwheat seeds in solutions of synthetic mono- and tricyclic cyclopentane-containing beta,beta'-triketones of various concentrations was accompanied by inhibition of seedling root growth and changes in the contents of glutamate, gamma-aminobutyric acid, proline, glutamine, and alanine. The monocyclic triketone also affected the amount of isoleucine. It is likely that the increase in proline content is a nonspecific response significant for enhancing stress tolerance in seedlings.
Asunto(s)
Aminoácidos/metabolismo , Ciclopentanos/farmacología , Fagopyrum/efectos de los fármacos , Cetonas/farmacología , Raíces de Plantas/efectos de los fármacos , Plantones/efectos de los fármacos , Fagopyrum/metabolismo , Germinación , Raíces de Plantas/metabolismo , Plantones/metabolismoRESUMEN
In this study we investigated the hemolytic, antimicrobial, and phytoregulatory activity of various classes of lipids (triacylglycerols, free fatty acids (FFA), the glyceroglycolipids monogalactosyl diacylglycerol (MGDG), sulfoquinovosyl diacylglycerol (SQDG)), sterols, all of them were obtained from the medical herb Kalanchoe diagremontiana, and also pigments, phenolic compounds (FC), polysaccharides, and ethanol extract (EE) of the herbal. It was established that EE, FC, FFA, and sterols display pH-dependent membranothropic activity. FFA showed antimicrobial activity and stimulated growth of buckwheat stalk sprouts. K. diagremontiana glyceroglycolopids did not display expressed biological activity. Caroteniods displayed pH-independent membranothopic action and antibacterial activity. Chlorophylls displayed antimicrobial action, but did not influence erythrocytes and buckwheat sprouts. Polysaccharides acted against the microorganisms Safale S-04, Candida albicans, Fusarium oxysperum and buckwheat sprouts.
Asunto(s)
Kalanchoe/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Plantas Medicinales/química , Animales , Antiinfecciosos/química , Antiinfecciosos/farmacología , Eritrocitos/metabolismo , Hongos/crecimiento & desarrollo , Hemolíticos/química , Hemolíticos/farmacología , Ratones , Reguladores del Crecimiento de las Plantas/química , Reguladores del Crecimiento de las Plantas/farmacologíaRESUMEN
The influence of cyclopentane beta,beta'-triketones on the ultrastructure of root cap meristematic cells of Cucumis sativus L. under inhibition of root growth by these compounds was studied. It was shown that treatment of the seedlings by these substances at the concentration of 100 microg/ml caused, on the one hand, stimulation of protein-synthesizing apparatus (increase in the nucleolus size and in the number of mitochondria and rough endoplasmic reticulum membranes) and, on the other hand, stimulation of lytic processes. The fact that the used compounds, causing inhibition of the seedling growth, do not suppress but stimulate protein-synthesizing activity of the cells, according to existing concept, testifies to the compound-mediated induction of the cell resistance to unfavourable factors. Consequently, these compounds, in contrast with growth inhibitors suppressing cell metabolism completely, possess properties peculiar to retardants, growth inhibitors valuable for crop production.
Asunto(s)
Cucumis sativus/efectos de los fármacos , Ciclopentanos/farmacología , Meristema/efectos de los fármacos , Reguladores del Crecimiento de las Plantas/farmacología , Cucumis sativus/ultraestructura , Ciclopentanos/química , Meristema/ultraestructura , Microscopía Electrónica , Plantones/efectos de los fármacos , Plantones/ultraestructuraRESUMEN
Triterpene glycosides are widespread in plants belonging to various families and in animals of the class of echinoderms (Echinodermata). They are situated in essential organs and tissues. Dependent upon the physiological condition of the organism, their concentration and the velocity of their biosynthesis are variable within sufficiently wide limits. They are used by the organism in the struggle for life and in maintaining the biological equilibrium in antagonistic interactions of biological systems. As to plants, they are factors of immunity against fungal diseases. Like exogenous substances, triterpene glycosides are physiologically active against warm-blooded animals. They affect the metabolism, the functional status of the organs, and the organism as a whole. In biological systems, they are integrated with the metabolism and, like low-molecular regulators, they exhibit polyfunctional properties.
Asunto(s)
Triterpenos/farmacología , Animales , Fenómenos Químicos , Química , Ecología , Glicósidos/metabolismo , Glicósidos/farmacología , Humanos , Triterpenos/metabolismoRESUMEN
A study was made of the ultrastructure of root cap meristematic cells in the seedlings of Cucumis sativus L., whose growth was inhibited by the action of 2-acetyl-4-metylcyclopent-4-en-1,3-dione (AMCD). It is shown that the treatment of seeds by this substance at a concentration of 100 microg/ml leads to the main root inhibition by 73% and, as compared to the control, causes the highest changes in mitochondria that do not reach normal dimensions and undergo degeneration. AMCD caused significant changes in the cell walls that in test samples unusually became electron-dense. Deposits of osmiophylic substance, presumably consisting of terpenoid-like compounds, were often found in the cytoplasm of treated cells as well as in the extracellular space. In many cells, plasmalemma and amiloplast membranes underwent destructive changes. We discuss a possible relation between inhibitory effect of AMCD on the root growth, and its influence on the ultrastructure in investigated cells.
Asunto(s)
Cucumis sativus/efectos de los fármacos , Ciclopentanos/farmacología , Inhibidores de Crecimiento/farmacología , Cucumis sativus/crecimiento & desarrollo , Cucumis sativus/ultraestructura , Ciclopentanos/síntesis química , Meristema/efectos de los fármacos , Meristema/ultraestructura , Raíces de Plantas/efectos de los fármacos , Raíces de Plantas/crecimiento & desarrollo , Raíces de Plantas/ultraestructura , Plantones/efectos de los fármacos , Plantones/ultraestructuraRESUMEN
Low concentrations of triterpene glycosides: holothurin A, stichoposide A and cauloside C sharply change the stability of bilayer lipid-sterine membranes. The glycosides activity decreases in the line: holothurin A, stichoposide A, cauloside C. The effective doses of glycosides are to a great extent determined by structural peculiarities of sterines which compose the films. A correlation was observed between the effect of triterpene glycosides on the stability of model bilayer membranes and their physiological activity. The model lipid-sterine membranes can be used in the primary screening of triterpene glycosides to estimate their physiological activity.
Asunto(s)
Glicósidos , Holoturina , Membrana Dobles de Lípidos , Ácido Oleanólico/análogos & derivados , Sapogeninas , Saponinas , Triterpenos , Estabilidad de Medicamentos , Holoturina/análogos & derivados , Cinética , Relación Estructura-ActividadRESUMEN
Behavior of hydrophobic probes of 5-doxylstearol acid and pyrene in phosphatidylcholine liposomes modified by sterols isolated from Far East holothurian tissues was studied. The introduction of delta 7-sterol xylosides and delta 5-sterol sulfates into liposomes was shown to result in an increase of the membranes microviscosity. When the liposome suspension was added with holotoxin A1 a supplementary increase of microviscosity was observed, which was obviously a consequence of glycosides +non built into the membranes.
Asunto(s)
Glicósidos/farmacología , Holoturina , Saponinas , Triterpenos/farmacología , Óxidos N-Cíclicos , Liposomas , Membranas , Fosfatidilcolinas , Pirenos , Marcadores de Spin , ViscosidadRESUMEN
The effect of cauloside C from Caulophyllum robustum M., theasaponine from Thea sinensis L. and stichoposide A from Stichopus japonicus S. on the biosynthesis of sterols and fatty acids by the yeast Saccharomyces carlsbergensis was studied. In in vivo and in vitro experiments cauloside C and theasaponine inhibited ergosterol biosynthesis at the stage of squalene-to-lanosterol transformation. In in vivo experiments stichoposide A inhibited squalene biosynthesis. The triterpene glycosides tested showed a typical feature: in in vivo and in vitro experiments they blocked the biosynthesis of fatty acids.
Asunto(s)
Ácidos Grasos/biosíntesis , Fitosteroles/biosíntesis , Saccharomyces/metabolismo , Triterpenos/farmacología , Ergosterol/biosíntesis , Glucósidos/farmacología , Glicósidos/farmacología , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/farmacología , Saccharomyces/efectos de los fármacos , Escualeno/biosíntesisRESUMEN
The effect of triterpene glycosides (cauloside C from Caulophyllum robustum, theasaponine from Thea sinensis, cucumarioside G from Cucumaria fraudatrix stichoposide A from Stichopus japonicus S., holothurines A and B from Holothuria mexicana, holothurine C from Bohadschia sp.) on the membrane permeability for K+ ions and UV-absorbing substances was compared with that of polyene antibiotics, viz., amphotericine B and nystatine. As a biological model fertilized eggs of sea urchin Strongylocentrotus nudus and yeast Saccharomyces carlsbergensis were used. In the sea urchin study most triterpene glycosides in low concentrations induced the outflux of K+ and in hgih concentrations that of both K+ and UV-absorbing agents. In the yeast study triterpene glycosides at identical doses induced the outflux of both K+ and UV-absorbing agents. The membranotropic effect of triterpene glycosides depended on the medium temperature and the biological system used.
Asunto(s)
Antibacterianos/farmacología , Permeabilidad de la Membrana Celular/efectos de los fármacos , Glicósidos/farmacología , Polienos/farmacología , Potasio/metabolismo , Triterpenos/farmacología , Rayos Ultravioleta , Relación Dosis-Respuesta a Droga , Femenino , Óvulo/efectos de los fármacos , Saccharomyces/efectos de los fármacos , Erizos de Mar/efectos de los fármacosRESUMEN
Seasonal variations and distribution of holotoxins in tissues of the sea cucumber Stichopus japonicus have been studied. It was shown that holotoxin content in the ovaries is higher than that in other organs during the breeding season. In the course of a year, the amount of glycosides in other holothurian organs changed a little. It has been found out that high concentrations of glycosides inhibit oocyte maturation in the holothurian Stichopus japonicus.
Asunto(s)
Equinodermos/análisis , Glicósidos/análisis , Oocitos/crecimiento & desarrollo , Pepinos de Mar/análisis , Toxinas Biológicas/análisis , Triterpenos/análisis , Animales , Femenino , Glicósidos/fisiología , Pepinos de Mar/fisiología , Estaciones del Año , Distribución Tisular , Triterpenos/fisiologíaRESUMEN
Cytotoxic activity of dammarane triterpenoids isolated from beach leaves was studied. These substances differ from the native ginseng genin (20(S)-protopanaxadiol) by the number, location, or configuration of OH-groups. Using fertilized egg cells of sea urchin Stronglyocentrotus intermedius we demonstrate that the orientation of C-3 OH-group has no effect on cytotoxic activity of triterpenoids as well as a higher activity of a triterpenoid with 3 alpha,12 beta-OH as compared to a C-3 ketone but lower activity as compared to a triterpenoid with 3 alpha,17 alpha-OH. Depending on the number of OH-groups the cytotoxic activity of triterpenoids decreases in the row: tetraol > pentaol > triol. Dammar-24-ene-3 alpha 2 beta,17 alpha,20(S)-tetraol (compound IV) is cytotoxic for the Ehrlich ascite carcinoma cells and this effect is additive to cytotoxic activity of anthracycline antibiotic carminomycin in vitro. Compound IV changes the permeability and microviscosity of the tumor cell membranes.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Betula/química , Triterpenos/farmacología , Animales , Antibióticos Antineoplásicos/farmacología , Antineoplásicos Fitogénicos/química , Carcinoma de Ehrlich , Carubicina/farmacología , Membrana Celular/efectos de los fármacos , Permeabilidad de la Membrana Celular/efectos de los fármacos , Evaluación Preclínica de Medicamentos/métodos , Sinergismo Farmacológico , Embrión no Mamífero/efectos de los fármacos , Femenino , Masculino , Hojas de la Planta/química , Erizos de Mar/efectos de los fármacos , Erizos de Mar/embriología , Relación Estructura-Actividad , Timidina/metabolismo , Triterpenos/química , Células Tumorales Cultivadas , ViscosidadRESUMEN
We studied the effect of extractive substances (ES) and total glycoside fraction (TGF) from Panax ginseng on plant cell growth. The seeds of cucumber Cucumis sativus L., KIT variety, were used for the biological assay. The tested substances inhibited the primary root growth in Cucumis sativus seedlings. Actively growing seedlings were most sensitive to this effect.
Asunto(s)
Cucumis sativus/efectos de los fármacos , Glicósidos/farmacología , Panax/química , Reguladores del Crecimiento de las Plantas/farmacología , Fenómenos Fisiológicos de las Plantas , Cucumis sativus/crecimiento & desarrollo , Glicósidos/aislamiento & purificación , Extractos Vegetales/farmacología , Reguladores del Crecimiento de las Plantas/aislamiento & purificación , Raíces de Plantas/efectos de los fármacos , Raíces de Plantas/crecimiento & desarrollo , Plantones/efectos de los fármacos , Plantones/crecimiento & desarrolloRESUMEN
The effect of triterpene glycosides synthesized on the basis of betulafolientriol, ginsenoside Rb1 from gingseng, betulafolientriol and its 3-epimer on the growth of the Ehrlich tumor cell cultures was studied. It was shown that, in relation to the quantitative composition and sites of carbohydrate residue linkage to aglycone as well as configuration of the alpha- or beta-hydroxyl group at C-3, the activity of the triterpenoids of the dammaranic series changed within wide ranges. 3- and 12-0-beta-D-glycosides of 3-epibetulafolientriol proved to be the most active.
Asunto(s)
Carcinoma de Ehrlich/patología , Glicósidos/farmacología , Extractos Vegetales/farmacología , Árboles , Triterpenos/farmacología , Animales , Antineoplásicos , División Celular/efectos de los fármacos , Células Cultivadas , Fenómenos Químicos , Química , Medios de Cultivo , Técnicas In VitroRESUMEN
We studied membranotropic effect of dammarane-type triterpenes (isolated from birch leaves) with a variable side chain structure, as well as the number and configuration of OH groups as a function of temperature and pH. Polyols with an acyclic side chain and four OH groups proved to have a higher hemolytic activity as compared to polyols with three or five hydroxyl groups. The triterpenes, with tetrahydrofurane cycle as the side chain, exert a hemolytic effect at a more acidic pH (5.0) and higher temperature (45 degrees C), as compared to the polyols with acyclic side chain. Irrespective of the side chain structure, the compounds with a 24(S) configuration lysed the erythrocytes at lower rate, as compared to the compounds with a 24(R) configuration.