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1.
Molecules ; 25(15)2020 Jul 28.
Artículo en Inglés | MEDLINE | ID: mdl-32731392

RESUMEN

Plants from the Veronica genus are used across the world as traditional remedies. In the present study, extracts from the aerial part of the scarcely investigated Veronica austriaca L., collected from two habitats in Bulgaria-the Balkan Mountains (Vau-1) and the Rhodopi Mountains (Vau-2), were analyzed by nuclear magnetic resonance (NMR) spectroscopy. The secondary metabolite, arbutin, was identified as a major constituent in both extracts, and further quantified by high-performance liquid chromatography (HPLC), while catalpol, aucubin and verbascoside were detected at lower amounts. The effect of the extracts and of pure arbutin on the survival of neutrophils isolated from murine bone marrow (BM) were determined by colorimetric assay. The production of cytokines-tumor necrosis factor (TNF)-α and interferon (IFN)-γ was evaluated by flowcytometry. While Vau-1 inhibited neutrophil vitality in a dose-dependent manner, arbutin stimulated the survival of neutrophils at lower concentrations, and inhibited cell density at higher concentrations. The Vau-1 increased the level of intracellular TNF-α, while Vau-2 and arbutin failed to do so, and expanded the frequency of mature double TNF-α+/IFN-γhi neutrophils within the BM pool.


Asunto(s)
Médula Ósea/metabolismo , Interferón gamma/biosíntesis , Neutrófilos/metabolismo , Extractos Vegetales/farmacología , Factor de Necrosis Tumoral alfa/biosíntesis , Veronica/química , Animales , Ratones , Ratones Endogámicos BALB C , Neutrófilos/citología , Extractos Vegetales/química
2.
Nat Prod Res ; 34(19): 2779-2786, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-30938183

RESUMEN

Two new δ-tocotrienol derivatives with oxidized terminal chain: 5,6-dioxo-garcinoic acid (trans-13'-carboxy-5,6-dioxo-δ-tocotrienol) (2) and 5-hydroxy-8b-oxo garcinoic acid (trans-13'-carboxy-5-hydroxy-8b-oxo-δ-tocotrienol) (3), together with one known derivative garcinoic acid (trans-13'-carboxy-δ-tocotrienol) (1) were isolated from a Colombian propolis. Garcinoic acid was found as a propolis constituent for the first time. The isolated compounds and crude ethanolic extract demonstrated high antimicrobial activity against Staphylococcus aureus and Candida albicans (MICs range: 10-39 µg/ml) as well as promising antioxidant potential in DPPH assay. Compound 3 displayed highest radical scavenging activity, even higher than that of dl-α-tocopherol, used as a positive control.


Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Própolis/química , Vitamina E/análogos & derivados , Antibacterianos/química , Antibacterianos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Benzopiranos/análisis , Benzopiranos/farmacología , Candida albicans/efectos de los fármacos , Colombia , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Staphylococcus aureus/efectos de los fármacos , Vitamina E/química
3.
Food Chem Toxicol ; 111: 605-615, 2018 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-29208506

RESUMEN

The Verbascum species are widely used traditional herb remedies against respiratory, inflammatory conditions and disorders. In the present study methanol extract of the aerial parts of the endemic Verbascum nobile Velen, was investigated and two novel iridoid glycosides 1 and 2, together with nine known constituents: iridoids, phenylethanoids, and saponins characteristic of Verbascum genus were identified. Further, the biological activity of the extract and selected isolated compounds on concanavalin (Con A)-induced T cell proliferation and activation of human Jurkat T cell line and splenic murine CD3 T cells was evaluated. T cell growth was studied by colorimetric-based WST proliferation assay while DNA content, cell cycling, dynamic of cell proliferation, expression of activation markers, intracellular expression of cytokine IFN-γ, and phosphorylation of ERK were analyzed by flow cytometry. Caspase-mediated apoptosis resulting in a poly (ADP-ribose) polymerase (PARP) cleavage was assessed by colorimetric in-cell kit. It was found that the extract, and all tested compounds (1, 2, 3 and 9) inhibited lectin-induced cell growth of Jurkat T cell line. The novel compounds decreased the frequencies of cells in S phase without causing a significant cell cycle arrest at G1 phase, caspases-mediated apoptosis and/or a profound change in the dynamic of splenic murine CD3+ T cell proliferation. Both compounds showed stronger inhibitory effect on Con A-induced ERK phosphorylation than the known bioactive compounds 3 and 9, and suppressed the expression of early activation marker CD69, the intracellular level of IFN-γ, and the generation of CD3+IFN-γ+ effectors. Our data suggest that the novel iridoid glycosides might have a potential to modulate T cell-related pathologies.


Asunto(s)
Proliferación Celular/efectos de los fármacos , Iridoides/farmacología , Extractos Vegetales/farmacología , Linfocitos T/efectos de los fármacos , Linfocitos T/inmunología , Verbascum/química , Animales , Apoptosis/efectos de los fármacos , Línea Celular , Humanos , Lectinas/inmunología , Activación de Linfocitos/efectos de los fármacos , Ratones , Linfocitos T/citología
4.
Curr Pharm Biotechnol ; 16(5): 414-23, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25543689

RESUMEN

Treatment of osteoporosis remains a therapeutic challenge. The effect of Apium Nodiflorum extract on development of experimental osteoporosis, pain thresholds and carrageenan-induced inflammation has been studied in ovariectomized osteoporotic Wistar rats. After osteoporosis verification rats were randomized and received vehicle only, HPLC-standardized Apium extract (equal to 2.4 mg/kg Quercetin) or Genistein (2.5 mg/kg) for 8 weeks. To verify the effect of Apium on the development of osteoporosis, bone mineral density (BMD) and bone mineral content (BMC), bone histology and plasma levels of IL-6 and RANKL were measured 6 months after ovariectomy and 8 weeks after treatment with Apium extract or Genistein as comparator. Inflammatory hyperalgesia was induced by intraplantar injection of 1% Carrageenan. Apium extract and Genistein impeded the development of osteoporosis (significant differences were shown for BMC and BMD levels in drug vs. vehicle treated rats) and improved bone histology and histological score. Apium and Genistein decreased IL-6 level. Both treatments alleviated mechanical hyperalgesia, decreased exudative reaction and lowered inflammatory pain threshold. The results suggested that Apium extract could be an alternative therapy for post-menopausal osteoporosis.


Asunto(s)
Antiinflamatorios/uso terapéutico , Apiaceae , Osteoporosis/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Animales , Antiinflamatorios/farmacología , Densidad Ósea/efectos de los fármacos , Carragenina , Femenino , Fémur/efectos de los fármacos , Fémur/metabolismo , Fémur/patología , Flavonoides/análisis , Genisteína/farmacología , Hiperalgesia/tratamiento farmacológico , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Interleucina-6/sangre , Osteoporosis/sangre , Osteoporosis/metabolismo , Osteoporosis/patología , Ovariectomía , Fenoles/análisis , Extractos Vegetales/química , Extractos Vegetales/farmacología , Ligando RANK/sangre , Ratas Wistar , Tibia/efectos de los fármacos , Tibia/metabolismo , Tibia/patología
5.
Phytochemistry ; 70(10): 1262-71, 2009 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-19698962

RESUMEN

Five terpenes, the diterpenes: 14,15-dinor-13-oxo-8(17)-labden-19-oic acid and a mixture of labda-8(17),13E-dien-19-carboxy-15-yl oleate and palmitate as well as the triterpenes, 3,4-seco-cycloart-12-hydroxy-4(28),24-dien-3-oic acid and cycloart-3,7-dihydroxy-24-en-28-oic acid were isolated from Cretan propolis. Moreover, 18 known compounds were also isolated, seven of them for the first time as propolis components. All structures were established on the basis of spectroscopic analysis and chemical evidence. All isolated compounds were tested for antimicrobial activity against some Gram-positive and Gram-negative bacteria as well as against some human pathogenic fungi showing a broad spectrum of antimicrobial activity.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Antifúngicos/química , Antifúngicos/farmacología , Própolis/química , Terpenos/química , Terpenos/farmacología , Candida/efectos de los fármacos , Diterpenos/química , Diterpenos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Triterpenos/química , Triterpenos/farmacología
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