Glaucine

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Ivan Svinyarov - One of the best experts on this subject based on the ideXlab platform.

  • Ionic Liquid-Based Aqueous Biphasic Systems—A Facile Approach for Ionic Liquid Regeneration from Crude Plant Extracts
    Processes, 2015
    Co-Authors: Rozalina Keremedchieva, Ivan Svinyarov, Milen G. Bogdanov
    Abstract:

    The possibility for simultaneous controlled partition of the biologically active alkaloid S-(+)-Glaucine, presented in a crude ionic liquid-aqueous plant extract, and separation of the ionic liquid (IL) employed by means of ionic liquid-based aqueous biphasic systems (IL-ABS) was investigated in this study. The ABS were formed by the addition of inorganic salts with distinct water-structuring properties such as Na2CO3, MgSO4, (NH4)2SO4, and NaH2PO4 to an enriched of Glaucine extract of Glaucium flavum Cr. (Papaveraceae). The influence of the salt type and concentration on the phase-forming ability, as well as the pH value on the partition of Glaucine between the two phases formed, was comprehensively studied. It was found that the target alkaloid is predominantly transferred into the IL-rich phase, regardless the influential factors. The results obtained were further used as a platform for the development of an improved extractive procedure, ensuring simultaneous Glaucine recovery, IL recycling and water removal in a single technological step. Thus, based on the formation of a three-phase system consisting of butyl acetate, IL-rich phase, and salt-rich phase, nearly quantitative recovery of Glaucine (>99%), IL recycling (ca. 90%), and water removal (ca. 85%) were achieved by salt-induced separation of the crude plant extract.

  • ionic liquid supported solid liquid extraction of bioactive alkaloids iii ionic liquid regeneration and Glaucine recovery from ionic liquid aqueous crude extract of glaucium flavum cr papaveraceae
    Separation and Purification Technology, 2015
    Co-Authors: Milen G. Bogdanov, Rozalina Keremedchieva, Ivan Svinyarov
    Abstract:

    Abstract In continuation of a research project aiming at introducing ionic liquids (ILs) as an alternative to the widely applied for the recovery of natural products of industrial interest conventional molecular solvents, we developed a concise procedure for isolation of the biologically active alkaloid S -(+)-Glaucine from IL-based aqueous crude extract. To this end, a comparative study of the behavior of 1 M [C 4 C 1 im][Ace]-aqueous solution and methanol in a series of consecutive extractions with the same extractant was conducted. The results obtained proved the better performance of the IL-based system in the solid–liquid extraction step, since the latter showed constantly higher extraction efficiency (ca. 35% enhanced) compared to methanol. The above procedure allows Glaucine accumulation from at least ten successive extractions, while simultaneously reduces the total solid–liquid ratio from 1:40 to 1:7.2, without loss of efficiency. Furthermore, the loss of IL into the matrix pores after extraction was also considered, suggesting the need for IL recycling by posttreatment of the residual biomass. To recover Glaucine from the crude IL-based aqueous extract, a series of non-miscible with water molecular solvents were tested. As a result, optimal conditions for quantitative extraction into chloroform were found, from which, after solvent removal and subsequent crystallization from ethanol, the target compound was isolated as a hydrobromide salt, the latter being the marketed form of Glaucine.

  • Ionic liquid-supported solid–liquid extraction of bioactive alkaloids. III. Ionic liquid regeneration and Glaucine recovery from ionic liquid-aqueous crude extract of Glaucium flavum Cr. (Papaveraceae)
    Separation and Purification Technology, 2015
    Co-Authors: Milen G. Bogdanov, Rozalina Keremedchieva, Ivan Svinyarov
    Abstract:

    Abstract In continuation of a research project aiming at introducing ionic liquids (ILs) as an alternative to the widely applied for the recovery of natural products of industrial interest conventional molecular solvents, we developed a concise procedure for isolation of the biologically active alkaloid S -(+)-Glaucine from IL-based aqueous crude extract. To this end, a comparative study of the behavior of 1 M [C 4 C 1 im][Ace]-aqueous solution and methanol in a series of consecutive extractions with the same extractant was conducted. The results obtained proved the better performance of the IL-based system in the solid–liquid extraction step, since the latter showed constantly higher extraction efficiency (ca. 35% enhanced) compared to methanol. The above procedure allows Glaucine accumulation from at least ten successive extractions, while simultaneously reduces the total solid–liquid ratio from 1:40 to 1:7.2, without loss of efficiency. Furthermore, the loss of IL into the matrix pores after extraction was also considered, suggesting the need for IL recycling by posttreatment of the residual biomass. To recover Glaucine from the crude IL-based aqueous extract, a series of non-miscible with water molecular solvents were tested. As a result, optimal conditions for quantitative extraction into chloroform were found, from which, after solvent removal and subsequent crystallization from ethanol, the target compound was isolated as a hydrobromide salt, the latter being the marketed form of Glaucine.

  • ionic liquid supported solid liquid extraction of bioactive alkaloids ii kinetics modeling and mechanism of Glaucine extraction from glaucium flavum cr papaveraceae
    Separation and Purification Technology, 2013
    Co-Authors: Milen G. Bogdanov, Ivan Svinyarov
    Abstract:

    Abstract The temperature dependence on the global kinetics of both methanol and 1-butyl-3-methylimidazolium acesulfamate ([C4mim][Ace])-supported extraction of the bioactive alkaloid S-(+)-Glaucine from plant material of Glaucium flavum Crantz (Papaveraceae) was measured and a comparative analysis in respect to the extractant type was performed. The experimental data was fitted with high coefficients of determination by means of an empirical model showing that the extraction process in both cases follows second-order kinetics. The concentration at saturation, Cs, extraction rate constants, k2, initial rates of extraction, h, and activation energies of extraction, Ea, were then calculated and discussed. The obtained results give a considerable advantage to the Ionic liquid-supported (IL-supported) extraction procedure due to the faster and quantitative Glaucine transfer, regardless the temperature. A plausible extraction mechanism scenario, describing the whole system in terms of solute–solvent, solute–matrix and matrix–solvent interactions at every stage of the extraction process was proposed. As a result, the apparent kinetics and yield of the IL-supported extraction were attributed to the cell wall modification by H-bonding interactions between both ions of [C4mim][Ace] and cellulose, resulting in the plant tissues disruption. The latter was further unequivocally confirmed by means of scanning electron microscopy. The kinetics parameters obtained were then implemented into a model for the prediction of Glaucine amount extracted in 1 M [C4mim][Ace] water solution at any temperature and time with good predictive ability.

  • Ionic liquid-supported solid–liquid extraction of bioactive alkaloids. II. Kinetics, modeling and mechanism of Glaucine extraction from Glaucium flavum Cr. (Papaveraceae)
    Separation and Purification Technology, 2013
    Co-Authors: Milen G. Bogdanov, Ivan Svinyarov
    Abstract:

    Abstract The temperature dependence on the global kinetics of both methanol and 1-butyl-3-methylimidazolium acesulfamate ([C4mim][Ace])-supported extraction of the bioactive alkaloid S-(+)-Glaucine from plant material of Glaucium flavum Crantz (Papaveraceae) was measured and a comparative analysis in respect to the extractant type was performed. The experimental data was fitted with high coefficients of determination by means of an empirical model showing that the extraction process in both cases follows second-order kinetics. The concentration at saturation, Cs, extraction rate constants, k2, initial rates of extraction, h, and activation energies of extraction, Ea, were then calculated and discussed. The obtained results give a considerable advantage to the Ionic liquid-supported (IL-supported) extraction procedure due to the faster and quantitative Glaucine transfer, regardless the temperature. A plausible extraction mechanism scenario, describing the whole system in terms of solute–solvent, solute–matrix and matrix–solvent interactions at every stage of the extraction process was proposed. As a result, the apparent kinetics and yield of the IL-supported extraction were attributed to the cell wall modification by H-bonding interactions between both ions of [C4mim][Ace] and cellulose, resulting in the plant tissues disruption. The latter was further unequivocally confirmed by means of scanning electron microscopy. The kinetics parameters obtained were then implemented into a model for the prediction of Glaucine amount extracted in 1 M [C4mim][Ace] water solution at any temperature and time with good predictive ability.

Milen G. Bogdanov - One of the best experts on this subject based on the ideXlab platform.

  • Ionic Liquid-Based Aqueous Biphasic Systems—A Facile Approach for Ionic Liquid Regeneration from Crude Plant Extracts
    Processes, 2015
    Co-Authors: Rozalina Keremedchieva, Ivan Svinyarov, Milen G. Bogdanov
    Abstract:

    The possibility for simultaneous controlled partition of the biologically active alkaloid S-(+)-Glaucine, presented in a crude ionic liquid-aqueous plant extract, and separation of the ionic liquid (IL) employed by means of ionic liquid-based aqueous biphasic systems (IL-ABS) was investigated in this study. The ABS were formed by the addition of inorganic salts with distinct water-structuring properties such as Na2CO3, MgSO4, (NH4)2SO4, and NaH2PO4 to an enriched of Glaucine extract of Glaucium flavum Cr. (Papaveraceae). The influence of the salt type and concentration on the phase-forming ability, as well as the pH value on the partition of Glaucine between the two phases formed, was comprehensively studied. It was found that the target alkaloid is predominantly transferred into the IL-rich phase, regardless the influential factors. The results obtained were further used as a platform for the development of an improved extractive procedure, ensuring simultaneous Glaucine recovery, IL recycling and water removal in a single technological step. Thus, based on the formation of a three-phase system consisting of butyl acetate, IL-rich phase, and salt-rich phase, nearly quantitative recovery of Glaucine (>99%), IL recycling (ca. 90%), and water removal (ca. 85%) were achieved by salt-induced separation of the crude plant extract.

  • ionic liquid supported solid liquid extraction of bioactive alkaloids iii ionic liquid regeneration and Glaucine recovery from ionic liquid aqueous crude extract of glaucium flavum cr papaveraceae
    Separation and Purification Technology, 2015
    Co-Authors: Milen G. Bogdanov, Rozalina Keremedchieva, Ivan Svinyarov
    Abstract:

    Abstract In continuation of a research project aiming at introducing ionic liquids (ILs) as an alternative to the widely applied for the recovery of natural products of industrial interest conventional molecular solvents, we developed a concise procedure for isolation of the biologically active alkaloid S -(+)-Glaucine from IL-based aqueous crude extract. To this end, a comparative study of the behavior of 1 M [C 4 C 1 im][Ace]-aqueous solution and methanol in a series of consecutive extractions with the same extractant was conducted. The results obtained proved the better performance of the IL-based system in the solid–liquid extraction step, since the latter showed constantly higher extraction efficiency (ca. 35% enhanced) compared to methanol. The above procedure allows Glaucine accumulation from at least ten successive extractions, while simultaneously reduces the total solid–liquid ratio from 1:40 to 1:7.2, without loss of efficiency. Furthermore, the loss of IL into the matrix pores after extraction was also considered, suggesting the need for IL recycling by posttreatment of the residual biomass. To recover Glaucine from the crude IL-based aqueous extract, a series of non-miscible with water molecular solvents were tested. As a result, optimal conditions for quantitative extraction into chloroform were found, from which, after solvent removal and subsequent crystallization from ethanol, the target compound was isolated as a hydrobromide salt, the latter being the marketed form of Glaucine.

  • Ionic liquid-supported solid–liquid extraction of bioactive alkaloids. III. Ionic liquid regeneration and Glaucine recovery from ionic liquid-aqueous crude extract of Glaucium flavum Cr. (Papaveraceae)
    Separation and Purification Technology, 2015
    Co-Authors: Milen G. Bogdanov, Rozalina Keremedchieva, Ivan Svinyarov
    Abstract:

    Abstract In continuation of a research project aiming at introducing ionic liquids (ILs) as an alternative to the widely applied for the recovery of natural products of industrial interest conventional molecular solvents, we developed a concise procedure for isolation of the biologically active alkaloid S -(+)-Glaucine from IL-based aqueous crude extract. To this end, a comparative study of the behavior of 1 M [C 4 C 1 im][Ace]-aqueous solution and methanol in a series of consecutive extractions with the same extractant was conducted. The results obtained proved the better performance of the IL-based system in the solid–liquid extraction step, since the latter showed constantly higher extraction efficiency (ca. 35% enhanced) compared to methanol. The above procedure allows Glaucine accumulation from at least ten successive extractions, while simultaneously reduces the total solid–liquid ratio from 1:40 to 1:7.2, without loss of efficiency. Furthermore, the loss of IL into the matrix pores after extraction was also considered, suggesting the need for IL recycling by posttreatment of the residual biomass. To recover Glaucine from the crude IL-based aqueous extract, a series of non-miscible with water molecular solvents were tested. As a result, optimal conditions for quantitative extraction into chloroform were found, from which, after solvent removal and subsequent crystallization from ethanol, the target compound was isolated as a hydrobromide salt, the latter being the marketed form of Glaucine.

  • ionic liquid supported solid liquid extraction of bioactive alkaloids ii kinetics modeling and mechanism of Glaucine extraction from glaucium flavum cr papaveraceae
    Separation and Purification Technology, 2013
    Co-Authors: Milen G. Bogdanov, Ivan Svinyarov
    Abstract:

    Abstract The temperature dependence on the global kinetics of both methanol and 1-butyl-3-methylimidazolium acesulfamate ([C4mim][Ace])-supported extraction of the bioactive alkaloid S-(+)-Glaucine from plant material of Glaucium flavum Crantz (Papaveraceae) was measured and a comparative analysis in respect to the extractant type was performed. The experimental data was fitted with high coefficients of determination by means of an empirical model showing that the extraction process in both cases follows second-order kinetics. The concentration at saturation, Cs, extraction rate constants, k2, initial rates of extraction, h, and activation energies of extraction, Ea, were then calculated and discussed. The obtained results give a considerable advantage to the Ionic liquid-supported (IL-supported) extraction procedure due to the faster and quantitative Glaucine transfer, regardless the temperature. A plausible extraction mechanism scenario, describing the whole system in terms of solute–solvent, solute–matrix and matrix–solvent interactions at every stage of the extraction process was proposed. As a result, the apparent kinetics and yield of the IL-supported extraction were attributed to the cell wall modification by H-bonding interactions between both ions of [C4mim][Ace] and cellulose, resulting in the plant tissues disruption. The latter was further unequivocally confirmed by means of scanning electron microscopy. The kinetics parameters obtained were then implemented into a model for the prediction of Glaucine amount extracted in 1 M [C4mim][Ace] water solution at any temperature and time with good predictive ability.

  • Ionic liquid-supported solid–liquid extraction of bioactive alkaloids. II. Kinetics, modeling and mechanism of Glaucine extraction from Glaucium flavum Cr. (Papaveraceae)
    Separation and Purification Technology, 2013
    Co-Authors: Milen G. Bogdanov, Ivan Svinyarov
    Abstract:

    Abstract The temperature dependence on the global kinetics of both methanol and 1-butyl-3-methylimidazolium acesulfamate ([C4mim][Ace])-supported extraction of the bioactive alkaloid S-(+)-Glaucine from plant material of Glaucium flavum Crantz (Papaveraceae) was measured and a comparative analysis in respect to the extractant type was performed. The experimental data was fitted with high coefficients of determination by means of an empirical model showing that the extraction process in both cases follows second-order kinetics. The concentration at saturation, Cs, extraction rate constants, k2, initial rates of extraction, h, and activation energies of extraction, Ea, were then calculated and discussed. The obtained results give a considerable advantage to the Ionic liquid-supported (IL-supported) extraction procedure due to the faster and quantitative Glaucine transfer, regardless the temperature. A plausible extraction mechanism scenario, describing the whole system in terms of solute–solvent, solute–matrix and matrix–solvent interactions at every stage of the extraction process was proposed. As a result, the apparent kinetics and yield of the IL-supported extraction were attributed to the cell wall modification by H-bonding interactions between both ions of [C4mim][Ace] and cellulose, resulting in the plant tissues disruption. The latter was further unequivocally confirmed by means of scanning electron microscopy. The kinetics parameters obtained were then implemented into a model for the prediction of Glaucine amount extracted in 1 M [C4mim][Ace] water solution at any temperature and time with good predictive ability.

Rozalina Keremedchieva - One of the best experts on this subject based on the ideXlab platform.

  • Ionic Liquid-Based Aqueous Biphasic Systems—A Facile Approach for Ionic Liquid Regeneration from Crude Plant Extracts
    Processes, 2015
    Co-Authors: Rozalina Keremedchieva, Ivan Svinyarov, Milen G. Bogdanov
    Abstract:

    The possibility for simultaneous controlled partition of the biologically active alkaloid S-(+)-Glaucine, presented in a crude ionic liquid-aqueous plant extract, and separation of the ionic liquid (IL) employed by means of ionic liquid-based aqueous biphasic systems (IL-ABS) was investigated in this study. The ABS were formed by the addition of inorganic salts with distinct water-structuring properties such as Na2CO3, MgSO4, (NH4)2SO4, and NaH2PO4 to an enriched of Glaucine extract of Glaucium flavum Cr. (Papaveraceae). The influence of the salt type and concentration on the phase-forming ability, as well as the pH value on the partition of Glaucine between the two phases formed, was comprehensively studied. It was found that the target alkaloid is predominantly transferred into the IL-rich phase, regardless the influential factors. The results obtained were further used as a platform for the development of an improved extractive procedure, ensuring simultaneous Glaucine recovery, IL recycling and water removal in a single technological step. Thus, based on the formation of a three-phase system consisting of butyl acetate, IL-rich phase, and salt-rich phase, nearly quantitative recovery of Glaucine (>99%), IL recycling (ca. 90%), and water removal (ca. 85%) were achieved by salt-induced separation of the crude plant extract.

  • ionic liquid supported solid liquid extraction of bioactive alkaloids iii ionic liquid regeneration and Glaucine recovery from ionic liquid aqueous crude extract of glaucium flavum cr papaveraceae
    Separation and Purification Technology, 2015
    Co-Authors: Milen G. Bogdanov, Rozalina Keremedchieva, Ivan Svinyarov
    Abstract:

    Abstract In continuation of a research project aiming at introducing ionic liquids (ILs) as an alternative to the widely applied for the recovery of natural products of industrial interest conventional molecular solvents, we developed a concise procedure for isolation of the biologically active alkaloid S -(+)-Glaucine from IL-based aqueous crude extract. To this end, a comparative study of the behavior of 1 M [C 4 C 1 im][Ace]-aqueous solution and methanol in a series of consecutive extractions with the same extractant was conducted. The results obtained proved the better performance of the IL-based system in the solid–liquid extraction step, since the latter showed constantly higher extraction efficiency (ca. 35% enhanced) compared to methanol. The above procedure allows Glaucine accumulation from at least ten successive extractions, while simultaneously reduces the total solid–liquid ratio from 1:40 to 1:7.2, without loss of efficiency. Furthermore, the loss of IL into the matrix pores after extraction was also considered, suggesting the need for IL recycling by posttreatment of the residual biomass. To recover Glaucine from the crude IL-based aqueous extract, a series of non-miscible with water molecular solvents were tested. As a result, optimal conditions for quantitative extraction into chloroform were found, from which, after solvent removal and subsequent crystallization from ethanol, the target compound was isolated as a hydrobromide salt, the latter being the marketed form of Glaucine.

  • Ionic liquid-supported solid–liquid extraction of bioactive alkaloids. III. Ionic liquid regeneration and Glaucine recovery from ionic liquid-aqueous crude extract of Glaucium flavum Cr. (Papaveraceae)
    Separation and Purification Technology, 2015
    Co-Authors: Milen G. Bogdanov, Rozalina Keremedchieva, Ivan Svinyarov
    Abstract:

    Abstract In continuation of a research project aiming at introducing ionic liquids (ILs) as an alternative to the widely applied for the recovery of natural products of industrial interest conventional molecular solvents, we developed a concise procedure for isolation of the biologically active alkaloid S -(+)-Glaucine from IL-based aqueous crude extract. To this end, a comparative study of the behavior of 1 M [C 4 C 1 im][Ace]-aqueous solution and methanol in a series of consecutive extractions with the same extractant was conducted. The results obtained proved the better performance of the IL-based system in the solid–liquid extraction step, since the latter showed constantly higher extraction efficiency (ca. 35% enhanced) compared to methanol. The above procedure allows Glaucine accumulation from at least ten successive extractions, while simultaneously reduces the total solid–liquid ratio from 1:40 to 1:7.2, without loss of efficiency. Furthermore, the loss of IL into the matrix pores after extraction was also considered, suggesting the need for IL recycling by posttreatment of the residual biomass. To recover Glaucine from the crude IL-based aqueous extract, a series of non-miscible with water molecular solvents were tested. As a result, optimal conditions for quantitative extraction into chloroform were found, from which, after solvent removal and subsequent crystallization from ethanol, the target compound was isolated as a hydrobromide salt, the latter being the marketed form of Glaucine.

  • ionic liquid supported solid liquid extraction of bioactive alkaloids i new hplc method for quantitative determination of Glaucine in glaucium flavum cr papaveraceae
    Separation and Purification Technology, 2012
    Co-Authors: Milen G. Bogdanov, Rozalina Keremedchieva, Ivan Svinyarov, Atanas Sidjimov
    Abstract:

    Abstract A series of hydrophilic 1-alkyl-3-methylimidazolium-based ionic liquids were used as extractants for the effective extraction of S -(+)-Glaucine from plant material of Glaucium flavum Crantz (Papaveraceae). The extractions were carried out both under ultrasonic and conventional heating conditions and the extraction efficiency was monitored by HPLC. The influence of the anion (chloride, bromide, acesulfamate and saccharinate), alkyl chain length in the imidazolium ion, concentration, extraction time, and plant material/extractant ratio was investigated. A comparative study between conventional Soxhlet extraction with methanol as a solvent (total extraction) and water solutions of ILs shows the same extraction ability of ILs, but with significantly reduced extraction time. Moreover, the extraction efficiency was shown to be strongly anion dependent. The results obtained provide a fast and safe method for determination of Glaucine in G. flavum Cr.

  • Ionic liquid-supported solid–liquid extraction of bioactive alkaloids. I. New HPLC method for quantitative determination of Glaucine in Glaucium flavum Cr. (Papaveraceae)
    Separation and Purification Technology, 2012
    Co-Authors: Milen G. Bogdanov, Rozalina Keremedchieva, Ivan Svinyarov, Atanas Sidjimov
    Abstract:

    Abstract A series of hydrophilic 1-alkyl-3-methylimidazolium-based ionic liquids were used as extractants for the effective extraction of S -(+)-Glaucine from plant material of Glaucium flavum Crantz (Papaveraceae). The extractions were carried out both under ultrasonic and conventional heating conditions and the extraction efficiency was monitored by HPLC. The influence of the anion (chloride, bromide, acesulfamate and saccharinate), alkyl chain length in the imidazolium ion, concentration, extraction time, and plant material/extractant ratio was investigated. A comparative study between conventional Soxhlet extraction with methanol as a solvent (total extraction) and water solutions of ILs shows the same extraction ability of ILs, but with significantly reduced extraction time. Moreover, the extraction efficiency was shown to be strongly anion dependent. The results obtained provide a fast and safe method for determination of Glaucine in G. flavum Cr.

Mohamed M Badawi - One of the best experts on this subject based on the ideXlab platform.

Francisco Orallo - One of the best experts on this subject based on the ideXlab platform.

  • study of the in vivo and in vitro cardiovascular effects of Glaucine and n carbethoxysecoGlaucine in rats
    British Journal of Pharmacology, 1995
    Co-Authors: Francisco Orallo, Alejandro Fdez Alzueta, Manuel Campostoimil, J M Calleja
    Abstract:

    1 The cardiovascular and vasorelaxant effects of (+)-Glaucine and of a semisynthetic derivative (N-carbethoxysecoGlaucine) were studied in rats. 2 N-carbethoxysecoGlaucine did not modify either systolic arterial pressure or heart rate values in conscious (25 mg kg−1, p.o.) and anaesthetized normotensive rats (5 mg kg−1, i.v.). Furthermore, this compound showed no activity in the experiments carried out on rat isolated aorta [contractility and 45Ca2+ influx assays (5 μm)] and did not modify the rate and force of contraction in rat isolated atria (5 μm). 3 In conscious normotensive rats, oral administration of (+)-Glaucine (25 mg kg−1) did not modify either systolic arterial pressure or heart rate. 4 In anaesthetized normotensive rats, (+)-Glaucine (5 mg kg−1, i.v.) produced a remarkable fall in mean arterial pressure (MAP) accompanied by a significant decrease in heart rate. In the same preparation, (+)-Glaucine (5 mg kg−1, i.v.) did not modify the cardiovascular effects induced by noradrenaline (NA) (5 μg kg−1) and 5-hydroxytryptamine (5-HT) (300 μg kg−1) but markedly inhibited those induced by nicotine (200 μg kg−1). 5 In isolated intact aorta of rat, (+)-Glaucine (0.15-5 μm) competitively inhibited the contractions induced by NA (with a pA2 value of 7.14) and non-competitively those induced by 5-HT (in normal Krebs solution) and Ca2+ (in depolarizing Ca2+-free high-K+ 50 mM solution), with depression of the maximal response and with pD2′ values of 5.56 and 5.26, respectively. 6 In experiments in Ca2+-free medium, (+)-Glaucine (3 μm) inhibited the contractions induced by NA and had no effect on either 5-HT- or caffeine-induced contractions. 7 Furthermore, in the experiments with radioactive Ca2+, (+)-Glaucine (3 μm) did not modify the basal uptake of 45Ca2+ but strongly inhibited the influx of 45Ca2+ induced by NA, 5-HT and K+. 8 (+)-Glaucine (5 μm) had no effect on rate and force of contraction in rat isolated atria. 9 These results indicate that: (a) the cardiovascular effects (hypotension and bradycardia) of (+)-Glaucine in anaesthetized normotensive rats (5 mg kg−1) may be due, at least in part, to a ganglioplexic effect; (b) the vasorelaxant action of (+)-Glaucine (0.15-5 μm) in rat isolated aorta can be attributed to an α1adrenoceptor blocking property (which may explain its inhibition of noradrenaline-induced 45Ca2+ influx and contractions in normal Krebs solution and noradrenaline-induced contractions in Ca2+-free medium) and to a Ca2+-antagonist activity (which may be responsible, at least in part, for the inhibition of 45Ca2+ uptake induced by NA, 5-HT and K+ and the contractions induced by both NA and 5-HT in normal Krebs solution and by Ca2+ in Ca2+-free high-K+ medium) and (c) there is no correlation between the mechanisms of action observed for (+)-Glaucine in vivo and in vitro, which suggests that the vasorelaxant activity of this alkaloid does not contribute to its hypotensive activity.

  • Study of the in vivo and in vitro cardiovascular effects of (+)-Glaucine and N-carbethoxysecoGlaucine in rats.
    British Journal of Pharmacology, 1995
    Co-Authors: Francisco Orallo, Alejandro Fdez Alzueta, Manuel Campos-toimil, J M Calleja
    Abstract:

    1 The cardiovascular and vasorelaxant effects of (+)-Glaucine and of a semisynthetic derivative (N-carbethoxysecoGlaucine) were studied in rats. 2 N-carbethoxysecoGlaucine did not modify either systolic arterial pressure or heart rate values in conscious (25 mg kg−1, p.o.) and anaesthetized normotensive rats (5 mg kg−1, i.v.). Furthermore, this compound showed no activity in the experiments carried out on rat isolated aorta [contractility and 45Ca2+ influx assays (5 μm)] and did not modify the rate and force of contraction in rat isolated atria (5 μm). 3 In conscious normotensive rats, oral administration of (+)-Glaucine (25 mg kg−1) did not modify either systolic arterial pressure or heart rate. 4 In anaesthetized normotensive rats, (+)-Glaucine (5 mg kg−1, i.v.) produced a remarkable fall in mean arterial pressure (MAP) accompanied by a significant decrease in heart rate. In the same preparation, (+)-Glaucine (5 mg kg−1, i.v.) did not modify the cardiovascular effects induced by noradrenaline (NA) (5 μg kg−1) and 5-hydroxytryptamine (5-HT) (300 μg kg−1) but markedly inhibited those induced by nicotine (200 μg kg−1). 5 In isolated intact aorta of rat, (+)-Glaucine (0.15-5 μm) competitively inhibited the contractions induced by NA (with a pA2 value of 7.14) and non-competitively those induced by 5-HT (in normal Krebs solution) and Ca2+ (in depolarizing Ca2+-free high-K+ 50 mM solution), with depression of the maximal response and with pD2′ values of 5.56 and 5.26, respectively. 6 In experiments in Ca2+-free medium, (+)-Glaucine (3 μm) inhibited the contractions induced by NA and had no effect on either 5-HT- or caffeine-induced contractions. 7 Furthermore, in the experiments with radioactive Ca2+, (+)-Glaucine (3 μm) did not modify the basal uptake of 45Ca2+ but strongly inhibited the influx of 45Ca2+ induced by NA, 5-HT and K+. 8 (+)-Glaucine (5 μm) had no effect on rate and force of contraction in rat isolated atria. 9 These results indicate that: (a) the cardiovascular effects (hypotension and bradycardia) of (+)-Glaucine in anaesthetized normotensive rats (5 mg kg−1) may be due, at least in part, to a ganglioplexic effect; (b) the vasorelaxant action of (+)-Glaucine (0.15-5 μm) in rat isolated aorta can be attributed to an α1adrenoceptor blocking property (which may explain its inhibition of noradrenaline-induced 45Ca2+ influx and contractions in normal Krebs solution and noradrenaline-induced contractions in Ca2+-free medium) and to a Ca2+-antagonist activity (which may be responsible, at least in part, for the inhibition of 45Ca2+ uptake induced by NA, 5-HT and K+ and the contractions induced by both NA and 5-HT in normal Krebs solution and by Ca2+ in Ca2+-free high-K+ medium) and (c) there is no correlation between the mechanisms of action observed for (+)-Glaucine in vivo and in vitro, which suggests that the vasorelaxant activity of this alkaloid does not contribute to its hypotensive activity.

  • study of the mechanism of the relaxant action of Glaucine in rat vas deferens
    British Journal of Pharmacology, 1993
    Co-Authors: Francisco Orallo, Alejandro Fdez Alzueta, Isabel M Loza, Nuria M Vivas, Albert Badia, Manuel Gromaz Campos, Angeles M Honrubia, Isabel M Cadavid
    Abstract:

    Abstract 1. Effects of the aporphinoid alkaloid, (+)-Glaucine, on rat vas deferens were investigated. 2. (+)-Glaucine (2-18 microM) competitively inhibited contractions induced by noradrenaline and methoxamine with a pA2 value of about 6. 3. (+)-Glaucine (2 and 18 microM) did not change the accumulation of tritium during incubation of the vas deferens with [3H]-noradrenaline. 4. (+)-Glaucine (0.3 nM-0.1 mM) inhibited specific [3H]-prazosin binding to membranes from rat vas deferens with a pKi value of 6.63, which is close to the pA2 value obtained against noradrenaline and methoxamine in functional studies. 5. In electrically-stimulated rat vas deferens, (+)-Glaucine (0.3-10 microM) enhanced twitch contractions and competitively antagonized the inhibitory effect of clonidine with a pA2 value of 5.91. 6. In tissues incubated in depolarizing calcium-free high-potassium medium, (+)-Glaucine (30-80 microM) inhibited Ca(2+)-induced contractions with depression of the maximal response at higher doses and with a pD'2 value of 3.65. Furthermore, (+)-Glaucine (50 microM) did not modify basal 45Ca uptake but strongly inhibited the influx of 45Ca induced by K+. 7. These results suggest that (+)-Glaucine has non-selective alpha 1- and alpha 2-adrenoceptor blocking properties. At higher doses, (+)-Glaucine shows calcium antagonist activity which may be responsible, at least in part, for the inhibition of the contractions induced by Ca2+ in calcium-free high-potassium medium.

  • Study of the mechanism of the relaxant action of (+)‐Glaucine in rat vas deferens
    British Journal of Pharmacology, 1993
    Co-Authors: Francisco Orallo, Alejandro Fdez Alzueta, Nuria M Vivas, Albert Badia, Manuel Gromaz Campos, M. Isabel Loza, M. Angeles Honrubia, M. Isabel Cadavid
    Abstract:

    Abstract 1. Effects of the aporphinoid alkaloid, (+)-Glaucine, on rat vas deferens were investigated. 2. (+)-Glaucine (2-18 microM) competitively inhibited contractions induced by noradrenaline and methoxamine with a pA2 value of about 6. 3. (+)-Glaucine (2 and 18 microM) did not change the accumulation of tritium during incubation of the vas deferens with [3H]-noradrenaline. 4. (+)-Glaucine (0.3 nM-0.1 mM) inhibited specific [3H]-prazosin binding to membranes from rat vas deferens with a pKi value of 6.63, which is close to the pA2 value obtained against noradrenaline and methoxamine in functional studies. 5. In electrically-stimulated rat vas deferens, (+)-Glaucine (0.3-10 microM) enhanced twitch contractions and competitively antagonized the inhibitory effect of clonidine with a pA2 value of 5.91. 6. In tissues incubated in depolarizing calcium-free high-potassium medium, (+)-Glaucine (30-80 microM) inhibited Ca(2+)-induced contractions with depression of the maximal response at higher doses and with a pD'2 value of 3.65. Furthermore, (+)-Glaucine (50 microM) did not modify basal 45Ca uptake but strongly inhibited the influx of 45Ca induced by K+. 7. These results suggest that (+)-Glaucine has non-selective alpha 1- and alpha 2-adrenoceptor blocking properties. At higher doses, (+)-Glaucine shows calcium antagonist activity which may be responsible, at least in part, for the inhibition of the contractions induced by Ca2+ in calcium-free high-potassium medium.

  • a study of Glaucine induced relaxation of rat aorta
    Planta Medica, 1993
    Co-Authors: I Loza, Francisco Orallo, I Verde, I Cadavid, Jose Gillongo, J M Calleja
    Abstract:

    The vasorelaxant effect of Glaucine, the major alkaloid of Platycapnos spicata (L.) Bernh., was studied. At concentrations of 10 μM-0.3 mM in normal Krebs solution it was almost equieffective in relaxing K + -induced and noradrenaline-induced tension in rat aortic rings without endothelium, with IC 50 values of 160±16 μM and 90±14 μM respectively. In experiments in a calcium-free medium, 10 μM Glaucine strongly inhibited noradrenaline-induced contractions. Glaucine (0.3 mM) did not affect basal uptake of 45 Ca, but induced uptake was reduced to 100% (K + ) and 97.7% (noradrenaline) of the basal value

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