RESUMO
The appearance of hair plays an important role in people's overall physical appearance and self-perception. Silicon (Si) has been suggested to have a role in the formation of connective tissue and is present at 1-10 ppm in hair. Choline-stabilized orthosilicic acid ("ch-OSA") is a bioavailable form of silicon which was found to improve skin microrelief and skin mechanical properties in women with photoaged skin. The effect of ch-OSA on hair was investigated in a randomized, double blind, placebo-controlled study. Forty-eight women with fine hair were given 10 mg Si/day in the form of ch-OSA beadlets (n = 24) or a placebo (n = 24), orally for 9 months. Hair morphology and tensile properties were evaluated before and after treatment. Urinary silicon concentration increased significantly in the ch-OSA supplemented group but not in the placebo group. The elastic gradient decreased in both groups but the change was significantly smaller in the ch-OSA group (-4.52%) compared to placebo group (-11.9%). Break load changed significantly in the placebo group (-10.8%) but not in the ch-OSA supplemented group (-2.20%). Break stress and elastic modulus decreased in both groups but the change was smaller in the ch-OSA group. The cross sectional area increased significantly after 9 months compared to baseline in ch-OSA supplemented subjects but not in the placebo group. The change in urinary silicon excretion was significantly correlated with the change in cross sectional area. Oral intake of ch-OSA had a positive effect on tensile strength including elasticity and break load and resulted in thicker hair.
Assuntos
Suplementos Nutricionais , Cabelo/efeitos dos fármacos , Ácido Silícico/farmacologia , Adolescente , Adulto , Colina , Método Duplo-Cego , Feminino , Cabelo/anatomia & histologia , Cabelo/fisiologia , Humanos , Pessoa de Meia-Idade , Ácido Silícico/química , Ácido Silícico/farmacocinética , Resistência à Tração/efeitos dos fármacosRESUMO
Silicon (Si) deficiency in animals results in bone defects. Choline-stabilized orthosilicic acid (ch-OSA) was found to have a high bioavailability compared to other Si supplements. The effect of ch-OSA supplementation was investigated on bone loss in aged ovariectomized (OVX) rats. Female Wistar rats (n = 58, age 9 months) were randomized in three groups. One group was sham-operated (sham, n = 21), and bilateral OVX was performed in the other two groups. OVX rats were supplemented orally with ch-OSA over 30 weeks (OVX1, n = 20; 1 mg Si/kg body weight daily) or used as controls (OVX0, n = 17). The serum Si concentration and the 24-hour urinary Si excretion of supplemented OVX rats was significantly higher compared to sham and OVX controls. Supplementation with ch-OSA significantly but partially reversed the decrease in Ca excretion, which was observed after OVX. The increase in bone turnover in OVX rats tended to be reduced by ch-OSA supplementation. ch-OSA supplementation increased significantly the femoral bone mineral content (BMC) in the distal region and total femoral BMC in OVX rats, whereas lumbar BMC was marginally increased. Femoral BMD was significantly increased at two sites in the distal region in OVX rats supplemented with ch-OSA compared to OVX controls. Total lumbar bone mineral density was marginally increased by ch-OSA supplementation. In conclusion, ch-OSA supplementation partially prevents femoral bone loss in the aged OVX rat model.
Assuntos
Envelhecimento , Suplementos Nutricionais , Fêmur/efeitos dos fármacos , Osteoporose/dietoterapia , Osteoporose/prevenção & controle , Ácido Silícico/uso terapêutico , Absorciometria de Fóton , Animais , Densidade Óssea/efeitos dos fármacos , Cálcio/urina , Colina , Feminino , Fêmur/fisiologia , Vértebras Lombares/efeitos dos fármacos , Vértebras Lombares/fisiologia , Ovariectomia , Ratos , Ratos Wistar , Ácido Silícico/análise , Ácido Silícico/químicaRESUMO
Chronic exposure of the skin to sunlight causes damage to the underlying connective tissue with a loss of elasticity and firmness. Silicon (Si) was suggested to have an important function in the formation and maintenance of connective tissue. Choline-stabilized orthosilicic acid ("ch-OSA") is a bioavailable form of silicon which was found to increase the hydroxyproline concentration in the dermis of animals. The effect of ch-OSA on skin, nails and hair was investigated in a randomized, double blind, placebo-controlled study. Fifty women with photodamaged facial skin were administered orally during 20 weeks, 10 mg Si/day in the form of ch-OSA pellets (n=25) or a placebo (n=25). Noninvasive methods were used to evaluate skin microrelief (forearm), hydration (forearm) and mechanical anisotropy (forehead). Volunteers evaluated on a virtual analog scale (VAS, "none=0, severe=3") brittleness of hair and nails. The serum Si concentration was significantly higher after a 20-week supplementation in subjects with ch-OSA compared to the placebo group. Skin roughness parameters increased in the placebo group (Rt:+8%; Rm: +11%; Rz: +6%) but decreased in the ch-OSA group (Rt: -16%; Rm: -19%; Rz: -8%). The change in roughness from baseline was significantly different between ch-OSA and placebo groups for Rt and Rm. The difference in longitudinal and lateral shear propagation time increased after 20 weeks in the placebo group but decreased in the ch-OSA group suggesting improvement in isotropy of the skin. VAS scores for nail and hair brittleness were significantly lower after 20 weeks in the ch-OSA group compared to baseline scores. Oral intake of ch-OSA during the 20 weeks results in a significant positive effect on skin surface and skin mechanical properties, and on brittleness of hair and nails.
Assuntos
Colina , Cabelo/efeitos dos fármacos , Unhas/efeitos dos fármacos , Ácido Silícico/administração & dosagem , Pele/efeitos dos fármacos , Pele/efeitos da radiação , Raios Ultravioleta/efeitos adversos , Administração Oral , Adulto , Idoso , Fenômenos Biomecânicos , Método Duplo-Cego , Face , Feminino , Cabelo/patologia , Cabelo/fisiopatologia , Humanos , Hidroxiprolina/metabolismo , Pessoa de Meia-Idade , Unhas/patologia , Unhas/fisiopatologia , Ácido Silícico/farmacologia , Ácido Silícico/uso terapêutico , Silício/sangue , Pele/metabolismo , Pele/patologia , Fatores de TempoRESUMO
Eight antioxidants from five different polyphenolic classes (cinnamic acids, benzoic acids, flavonoids, proanthocyanidins and stilbenes), and the water-soluble vitamin E derivative trolox were examined for their antioxidant activity in-vitro. In addition, the compounds were tested for their cytotoxicity on growing fibroblasts and their inhibition of the classical pathway of the complement system. Procyanidin C1 was shown to be a good scavenger of both DPPH(*) and HO(*), and a strong inhibitor of lipid peroxidation and the classical pathway of the complement system. Consequently, procyanidin C1 was classified as the most promising antioxidant in-vitro of all compounds tested. In contrast, genistein exhibited a very low antioxidant activity in both the lipid peroxidation and the DPPH(*) scavenging assay, a high cytotoxicity and a low complement-inhibiting activity.
Assuntos
Antioxidantes/farmacologia , Flavonoides/farmacologia , Fenóis/farmacologia , Antioxidantes/química , Benzoatos/farmacologia , Biflavonoides/química , Biflavonoides/farmacologia , Compostos de Bifenilo/química , Catequina/química , Catequina/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Cromanos/química , Cromanos/farmacologia , Cinamatos/farmacologia , Relação Dose-Resposta a Droga , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Flavonoides/química , Radicais Livres/metabolismo , Genisteína/química , Genisteína/farmacologia , Humanos , Hidrazinas/química , Radical Hidroxila/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Fenóis/química , Picratos , Polifenóis , Proantocianidinas/química , Proantocianidinas/farmacologia , Pele/citologia , Estilbenos/farmacologiaRESUMO
Thirty-five flavonoids of seven different types, namely isoflavonoids, chalcones, dihydroflavonols, flavanols, flavanones, flavones, and flavonols were investigated for their ability to inhibit ascorbate-induced microsomal lipid peroxidation and their cytotoxicity. For each activity a structure-activity relationship was established. Subsequently, an antioxidant selectivity index, i. e., the maximal non-toxic dose divided by the IC(50) value for lipid peroxidation, was introduced. Kaempferol showed the highest antioxidant selectivity index of all flavonoids tested.
Assuntos
Antioxidantes/farmacologia , Flavonoides/toxicidade , Peroxidação de Lipídeos/efeitos dos fármacos , Microssomos Hepáticos/efeitos dos fármacos , Animais , Células Cultivadas , Fibroblastos/efeitos dos fármacos , Flavonoides/antagonistas & inibidores , Flavonoides/química , Flavonoides/farmacologia , Humanos , Concentração Inibidora 50 , Masculino , Ratos , Ratos Wistar , Pele/efeitos dos fármacos , Relação Estrutura-AtividadeRESUMO
Aqueous EtOH (80%) extracts of seven plants used by Rwandan traditional healers to treat infections, were screened for antibacterial, antifungal, and antiviral activities. Only two of the selected plants showed a true antiviral activity against herpes simplex virus type 1, while all of them exhibited virucidal properties against several enveloped viruses including herpes simplex, measles, Semliki forest, and vesicular stomatitis viruses. Four plants were diversely active against gram-positive bacteria, two of these showing bactericidal effect against the acid-fast Mycobacterium fortuitum. None of the selected plants was active against gram-negative bacteria or the yeast Candida albicans. From a bioassay-guided fractionation procedure using herpes simplex virus type I as the target model, a virucidal mixture, the maesasaponin mixture A, was isolated from the MeOH extract of Maesa lanceolata. The maesasaponin mixture A exhibited a virucidal activity against herpes simplex types 1 and 2, and vesicular stomatitis viruses.
Assuntos
Anti-Infecciosos/uso terapêutico , Antivirais/uso terapêutico , Extratos Vegetais/uso terapêutico , Plantas Medicinais/química , Antibacterianos , Antifúngicos/uso terapêutico , Bactérias/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos/métodos , RuandaRESUMO
From a bioassay-guided fractionation procedure using Herpes simplex virus type 1 as the target model, a virucidal saponin mixture (maesasaponin mixture B) was isolated from the MeOH extract of leaves of Maesa lanceolata. The maesasaponin mixture B consisted of six homologous oleanane-type triterpenoid saponins 1-6, identified by 1H, 13C, and 2D NMR spectroscopy and mass spectrometry. The maesasaponin mixture B (1-6) showed several biological activities expected for saponins. It exhibited a moderate virucidal activity against enveloped viruses. The maesasaponin mixture B (1-6) was tested for further properties. The saponin mixture was found to be highly hemolytic and molluscicidal: it hemolyzed 50% of human erythrocytes (1% suspension) at a concentration estimated at 1.6 microg/mL and exerted against Biomphalaria glabrata snails a severe toxic effect with LD95 and LD50 values of 4.1 and 2.3 ppm, respectively. In addition, the maesasaponin mixture B (1-6) showed moderate fungistatic and antimutagenic properties. The evaluation of these diverse activities is described.
Assuntos
Moluscos/efeitos dos fármacos , Plantas Medicinais/química , Saponinas/farmacologia , Árvores/química , Triterpenos/farmacologia , Animais , Antifúngicos/química , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Antivirais/química , Antivirais/isolamento & purificação , Antivirais/farmacologia , Configuração de Carboidratos , Sequência de Carboidratos , Hemólise/efeitos dos fármacos , Humanos , Dados de Sequência Molecular , Folhas de Planta/química , Saponinas/química , Saponinas/isolamento & purificação , Triterpenos/química , Triterpenos/isolamento & purificaçãoRESUMO
The structure-activity relationship of flavonoids as inhibitors of xanthine oxidase and as scavengers of the superoxide radical, produced by the action of the enzyme xanthine oxidase, was investigated. The hydroxyl groups at C-5 and C-7 and the double bond between C-2 and C-3 were essential for a high inhibitory activity on xanthine oxidase. Flavones showed slightly higher inhibitory activity than flavonols. All flavonoid derivatives except isorhamnetin (30) were less active than the original compounds. For a high superoxide scavenging activity on the other hand, a hydroxyl group at C-3' in ring B and at C-3 were essential. According to their effect on xanthine oxidase and as superoxide scavengers, the flavonoids could be classified into six groups: superoxide scavengers without inhibitory activity on xanthine oxidase (category A), xanthine oxidase inhibitors without any additional superoxide scavenging activity (category B), xanthine oxidase inhibitors with an additional superoxide scavenging activity (category C), xanthine oxidase inhibitors with an additional pro-oxidant effect on the production of superoxide (category D), flavonoids with a marginal effect on xanthine oxidase but with a prooxidant effect on the production of superoxide (category E), and finally, flavonoids with no effect on xanthine oxidase or superoxide (category F).
Assuntos
Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Xantina Oxidase/antagonistas & inibidores , Inibidores Enzimáticos/classificação , Flavonoides/classificação , Relação Estrutura-AtividadeRESUMO
The bioavailability of silicon in stabilized orthosilicic acid was investigated in a double blind, placebo controlled supplementation study of calves maintained on a normal diet. The total dietary Si intake was increased by 4.9% in the form of stabilized orthosilicic acid. After 23 wk of Si supplementation, the serum Si concentration increased (p = 0.0001, n = 29) by 70% compared to control animals in spite of the low Si dose administered and the Si adequate diet. The individually administered Si dose was significantly associated with the serum Si concentration (r = 0.44, p = 0.016, n = 29). The collagen concentration in dermis was significantly higher (p = 0.019, n = 4) in the Si group and a positive correlation (r = 0.72, p = 0.018, n = 9) was found between the Si concentration in serum and the collagen concentration in cartilage. The calcium (Ca) and phosphorus (P) concentrations in serum were marginally higher for animals supplemented with Si compared to control animals. In serum, a significant linear relationship was found between the Si and the Ca concentration (r = 0.31, p = 0.019, n = 59), whereas the magnesium concentration correlated marginally with the Si concentration (r = 0.25, p = 0.068, n = 59). In summary, increasing the total dietary Si intake by 4.9% in the form of stabilized orthosilicic acid resulted in a 70% higher Si concentration in serum indicating a high bioavailability of Si in this supplement. The positive correlation between the serum Si concentration and the collagen concentration in cartilage and the serum Ca concentration, respectively, suggest the involvement of Si both in the formation of extracellular matrix components and in Ca metabolism.
Assuntos
Cálcio/sangue , Cartilagem/metabolismo , Colágeno/metabolismo , Alimentos Fortificados , Magnésio/sangue , Fósforo/sangue , Ácido Silícico/farmacologia , Silício/sangue , Pele/metabolismo , Animais , Estatura , Peso Corporal , Bovinos , Colágeno/efeitos dos fármacos , Método Duplo-Cego , Estabilidade de Medicamentos , Crescimento/efeitos dos fármacos , Hidroxiprolina/química , Leite , Ácido Silícico/administração & dosagem , Ácido Silícico/metabolismo , Silício/deficiênciaRESUMO
The antimutagenicity of the Citrus flavonoids naringin, hesperidin, nobiletin, and tangeretin against the mutagens benzo[a]pyrene, 2-aminofluorene, quercetin, and nitroquinoline N-oxide was investigated in the Salmonella/microsome assay. Naringin and hesperidin showed a weak antimutagenic activity against benzo[a]pyrene. Tangeretin was antimutagenic against all indirectly-acting mutagens tested, but in general a large molar excess was necessary. Liquid preincubation increased the antimutagenicity of tangeretin against 2-aminofluorene. Nobiletin acted as an antimutagen against benzo[a]pyrene, but it enhanced the mutagenicity of 2-aminofluorene. However, in a liquid preincubation assay nobiletin also exhibited antimutagenicity against 2-aminofluorene. Both tangeretin and nobiletin inhibited the mutagenicity of quercetin. Quercetin itself acted as an antimutagen against 2-aminofluorene in a Salmonella strain (TA1538) where its mutagenicity was not expressed. Quercetin should not merely be regarded as a genotoxic risk factor in the human diet, since its mutagenicity may be inhibited by accompanying compounds including other flavonoids, and since quercetin itself also exhibits an antimutagenic action. Because of the antimutagenic properties the Citrus flavonoids tested, especially tangeretin and nobiletin, might play a role in the chemoprevention of cancer.
Assuntos
Antimutagênicos/farmacologia , Antioxidantes/farmacologia , Citrus , Flavanonas , Flavonas , Flavonoides/farmacologia , Mutagênicos/farmacologia , Salmonella typhimurium/efeitos dos fármacos , Anticarcinógenos , Antimutagênicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Benzo(a)pireno/farmacologia , Dieta , Flavonoides/isolamento & purificação , Hesperidina/farmacologia , Humanos , Testes de MutagenicidadeRESUMO
Phenylketonuric (PKU) subjects have a limited supply of selenium (Se) in their phenylalanine-restricted diet. A Se repletion (1 microgram Se/kg/day)/depletion study was conducted in PKU children to determine the effect of Se on thyroid function parameters. The initial plasma Se concentration (mean +/- SD: 0.26 +/- 0.12 mumol/L, p < 0.00003, n = 10) and glutathione peroxidase (GSH-Px) activity (140 +/- 58 U/L, p < 0.00003, n = 10) were significantly lower compared to age-matched controls. After 14 weeks of supplementation, the plasma Se concentration (mean +/- SD: 0.74 +/- 0.20 mumol/L) normalized (normal range: 0.57-1.15 mumol/L, mean +/- SD: 0.76 +/- 0.13 mumol/L, n = 32) and remained stable thereafter during repletion. Plasma GSH-Px activity reached normal values after 18 weeks of supplementation (312 +/- 57 U/L; normal range: 238-492 U/L, mean +/- SD: 345 +/- 54 U/L, n = 32) and increased significantly for up to eight weeks thereafter (332 +/- 52 U/L). Individual and mean thyroid parameters were initially normal in all cases. The mean concentrations of plasma thyroxine (T4: p < 0.025), free T4 (FT4: p < 0.01) and reverse triiodothyronine (rT3: p < 0.005) decreased to 75% of their initial value within three weeks of Se supplementation and remained stable thereafter, within a normal physiological range during selenium supplementation. They increased back to their initial values three weeks (T4: p < 0.05, FT4: p < 0.05) and six weeks (rT3: p < 0.025) respectively, after the end of the supplementation. In conclusion, Se supplementation modifies thyroid function parameters in Se-deficient PKU subjects most likely by an increase in activity of type I 5'-deiodinase (5'-DIase I).
Assuntos
Fenilcetonúrias/fisiopatologia , Selênio/administração & dosagem , Glândula Tireoide/fisiopatologia , Adolescente , Criança , Feminino , Glutationa Peroxidase/sangue , Humanos , Iodeto Peroxidase/sangue , Masculino , Selênio/sangue , Hormônios Tireóideos/sangueRESUMO
The superoxide scavenging activities of 12 flavonoids were measured. The superoxide anions were generated by a hypoxanthine-xanthine oxidase system and measured by the nitrite method. The results showed that the scavenging ability enhanced with an increasing number of hydroxyl groups in ring B. Substitution at C3 position with a hydroxyl group increased the activity. Compared to a methoxyl group or a glycoside in this position, a free hydroxyl group showed the highest activity. A saturated C2-C3 bond showed a higher activity than a unsaturated bond. The absence of a carbonyl group at C4 position increased the activity.
Assuntos
Flavonoides , Sequestradores de Radicais Livres , Superóxidos , Flavonoides/química , Hipoxantina , Hipoxantinas/metabolismo , Cinética , Estrutura Molecular , Nitritos , Relação Estrutura-Atividade , Xantina Oxidase/metabolismoRESUMO
Type I 5'-deiodinase was recently characterized as a selenocysteine-containing enzyme in humans and other mammals. Up to now, the effect of selenium (Se) supplementation on thyroid hormone metabolism in humans has only been reported in the very peculiar nutritional environment of Central Africa, where combined severe iodine and Se deficiency occurs. In this study, a group of phenylketonuria subjects with a low selenium status, but a normal iodine intake were supplemented with selenium to investigate changes in their thyroid hormone metabolism. After 3 wk of selenium supplementation (1 microgram/kg/d), both the concentrations of the prohormone thyroxine (T4) and the metabolic inactive reverse triiodothyronine (rT3) decreased significantly. Clinically, the phenylketonuria subjects remained euthyroid before and after selenium supplementation. The individual changes of plasma Se and glutathione peroxidase activity were closely associated with individual changes of plasma T4 and rT3.
Assuntos
Glutationa Peroxidase/sangue , Fenilcetonúrias/sangue , Selênio/farmacologia , Tiroxina/sangue , Tri-Iodotironina Reversa/sangue , Tri-Iodotironina/sangue , Adolescente , Animais , Criança , Humanos , Mamíferos , Fenilalanina , Fenilcetonúrias/dietoterapia , Fenilcetonúrias/fisiopatologia , Selênio/administração & dosagem , Tireotropina/sangue , Proteínas de Ligação a Tiroxina/análise , Fatores de TempoRESUMO
Lactic acid bacteria are nonpathogenic bacteria commonly used in food processing. An evaluation was made of the capacity to concentrate selenium in species of Lactobacillus. A selenium concentration of 1 microgram/mL in the culture medium yielded in a bacterial content of 400 micrograms/g dry biomass. Dialysis and TCA precipitation experiments of a native intracellular extract proved that at least 80% of the total selenium is associated with organic molecules. Seleno-cysteine was identified as the only seleno-amino acid present in the intracellular selenoproteins. This study shows that species of the lactic acid bacteria are able to concentrate selenium intracellular as seleno-cysteine, which could be applied in supplementation studies.
Assuntos
Lactobacillus/metabolismo , Selênio/metabolismo , Autorradiografia , Proteínas de Bactérias/isolamento & purificação , Proteínas de Bactérias/metabolismo , Técnicas Bacteriológicas , Biomassa , Meios de Cultura , Eletroforese em Gel de Poliacrilamida , Liofilização , Lactobacillus/química , Lactobacillus/crescimento & desenvolvimento , Lacticaseibacillus casei/química , Lacticaseibacillus casei/crescimento & desenvolvimento , Lacticaseibacillus casei/metabolismo , Selênio/análise , Radioisótopos de Selênio , Especificidade da EspécieRESUMO
Two children with severe neurodevelopmental retardation and elevated liver function tests developed intractable seizures during the first year of life. Detectable neurometabolic conditions have been ruled out. At the time of seizures evidence for systemic selenium deficiency could be documented. The youngest patient, who manifested intractable fits from the fourth day of life, died at the age of ten months. Neuropathologic examination was consistent with Progressive Neuronal Degeneration of Childhood (PNDC) with liver disease or formerly known as Alpers disease. In the oldest child, whose diet was normally balanced, fits started from the age of 11 months and features of long-standing selenium deficiency became apparent from the age of 1 1/2 years and consisted of liver function disturbances, depigmented hair and osteoarthropathy. Oral substitution with selenium supplements in both children (3-5 micrograms/kg body weight) resulted in reduction of seizures and improvement of the EEG recordings after two weeks while liver function became normal. Two of the seleno-dependent enzymes Glutathione Peroxidase (GPX) and Phospholipid Hydroperoxide Glutathione Peroxidase (PHGPX) are speculated to play a key-role in the defence of neuronal cells against oxygen radical formation and peroxidative processes. Our findings support the hypothesis that the presence of selenium depletion in the brain amongst patients with epilepsy constitutes an important triggering factor for the origin of intractable seizures and subsequent neuronal damage.
Assuntos
Peroxidação de Lipídeos/fisiologia , Selênio/deficiência , Espasmos Infantis/fisiopatologia , Atrofia , Encéfalo/patologia , Esclerose Cerebral Difusa de Schilder/patologia , Esclerose Cerebral Difusa de Schilder/fisiopatologia , Eletroencefalografia/efeitos dos fármacos , Feminino , Radicais Livres , Glutationa Peroxidase/fisiologia , Humanos , Lactente , Recém-Nascido , Masculino , Degeneração Neural/fisiologia , Exame Neurológico , Fosfolipídeo Hidroperóxido Glutationa Peroxidase , Espécies Reativas de Oxigênio/metabolismo , Selênio/administração & dosagem , Selênio/líquido cefalorraquidiano , Espasmos Infantis/patologiaRESUMO
Dragon's blood is a red viscous latex extracted from the cortex of various Croton spp. (Euphorbiaceae), most commonly Croton lechleri, Croton draconoides (or Croton palanostigma), and Croton erythrochilus. It is used in South American popular medicine for several purposes, including wound healing. Bioassay-guided fractionation of dragon's blood, using an in vitro test system for the stimulation of human umbilical vein endothelial cells, has resulted in the isolation of a dihydrobenzofuran lignan, 3',4-O-dimethylcedrusin or 4-O-methyldihydrodehydrodiconiferyl alcohol [2-(3',4'-dimethoxyphenyl)-3-hydroxymethyl-2,3-dihydro-7-methoxybenzo furan-5- propan-1-ol] [1] as the biologically active principle. A related compound, 4-O-methylcedrusin [2-(3',4'-dimethoxyphenyl)-3-hydroxymethyl-2,3-dihydro-7-hydroxybenzo furan-5- propan-1-ol] [2], and the alkaloid taspine [3], also isolated from dragon's blood, were not active in the same assay. A cell proliferation assay, measuring the incorporation of tritiated thymidine in endothelial cells, showed that compound 1 did not stimulate cell proliferation, but rather inhibited thymidine incorporation, while protecting cells against degradation in a starvation medium.
Assuntos
Antineoplásicos Fitogênicos/química , Plantas Medicinais/química , Alcaloides/química , Alcaloides/farmacologia , Anisóis/química , Anisóis/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Benzofuranos/química , Benzofuranos/farmacologia , Divisão Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Feminino , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Conformação Molecular , Gravidez , América do Sul , Timidina/metabolismo , Veias Umbilicais/citologia , Veias Umbilicais/efeitos dos fármacosRESUMO
The mutagenicity of a series of pyrrolizidine alkaloids, and of extracts from several Italian Senecio species containing pyrrolizidine alkaloids, including S. inaequidens, S. fuchsii and S. cacaliaster, were tested using the Salmonella typhimurium/mammalian microsome system. Retrorsine, senecivernine, seneciphylline and the Senecio extracts showed a weakly mutagenic activity.