10 research outputs found
Actividades biolĂłgicas de polifenoles de Polygonum lapathifolium
Polygonum lapathifolium es una planta invasora cuya presencia se extiende por todo el mundo y que ha sido utilizada en la medicina tradicional por sus actividades biolĂłgicas. Analizamos el perfil quĂmico de la parte superficial utilizando HPLC/DAD/ESI-MS. Ocho flavonoides, dos chalconas y ácido gálico fueron aislados, identificados y analizados en relaciĂłn a sus actividades en siete modelos experimentales (de actividad antioxidante, α/β-glucosidasa inhibitoria, antimicrobiana, anticholineserasa). Nuestros resultados demuestran que P. lapathifolium es una valiosa fuente de compuestos con actividades biolĂłgicas prometedoras
New diterpenoid glucoside and flavonoids from Plectranthus scutellarioides (L.) R. Br.
Abstract Three new compounds, diterpenoid glucoside (13S,15S)-6β,7α,12α-trihydroxy-13β,16-cyclo-8-abietene-11,14-dione 7-O-β-D-glucoside 1, flavonoids apigenin 7-O-(3′′-O-acetyl)-β-D-glucuronide 2 and apigenin 5-O-(3′′-O-acetyl)-β-D-glucuronide 3, together with known compounds caffeic acid 4, luteolin 5-O-β-D-glucoside 5 and rosmarinic acid 6 were isolated from the aerial parts of Plectranthus scutellarioides (L.) R. Br. The structures of the new compounds were elucidated by spectroscopic and mass-spectrometric analyses, including 1D- and 2D-NMR. Compound 1 inhibited hyaluronidase by 25% at the concentration of 200 μM, compounds 2 and 3 showed inhibitory activity on butyrylcholinesterase better than standard galanthamine at the concentration of 100 μM, and compound 6 is a potent antioxidant with an ORAC value of 2.15 ± 0.12
Arylaminopropanone Derivatives as Potential Cholinesterase Inhibitors: Synthesis, Docking Study and Biological Evaluation
Neurodegenerative diseases in which the decrease of the acetylcholine is observed are growing worldwide. In the present study, a series of new arylaminopropanone derivatives with N-phenylcarbamate moiety (1-16) were prepared as potential acetylcholinesterase and butyrylcholinesterase inhibitors. In vitro enzyme assays were performed; the results are expressed as a percentage of inhibition and the IC50 values. The inhibitory activities were compared with reference drugs galantamine and rivastigmine showing piperidine derivatives (1-3) as the most potent. A possible mechanism of action for these compounds was determined from a molecular modelling study by using combined techniques of docking, molecular dynamics simulations and quantum mechanics calculations.Fil: Hudcová, Anna. University Of Veterinary And Pharmaceutical Sciences; RepĂşblica ChecaFil: Kroutil, Ales. University Of Veterinary And Pharmaceutical Sciences; RepĂşblica ChecaFil: KubĂnová, Renata. University Of Veterinary And Pharmaceutical Sciences; RepĂşblica ChecaFil: Garro, Adriana. Consejo Nacional de Investigaciones CientĂficas y TĂ©cnicas. Centro CientĂfico TecnolĂłgico Conicet - San Luis. Instituto Multidisciplinario de Investigaciones BiolĂłgicas de San Luis. Universidad Nacional de San Luis. Facultad de Ciencias FĂsico Matemáticas y Naturales. Instituto Multidisciplinario de Investigaciones BiolĂłgicas de San Luis; ArgentinaFil: Gutierrez, Lucas Joel. Consejo Nacional de Investigaciones CientĂficas y TĂ©cnicas. Centro CientĂfico TecnolĂłgico Conicet - San Luis. Instituto Multidisciplinario de Investigaciones BiolĂłgicas de San Luis. Universidad Nacional de San Luis. Facultad de Ciencias FĂsico Matemáticas y Naturales. Instituto Multidisciplinario de Investigaciones BiolĂłgicas de San Luis; ArgentinaFil: Enriz, Ricardo Daniel. Consejo Nacional de Investigaciones CientĂficas y TĂ©cnicas. Centro CientĂfico TecnolĂłgico Conicet - San Luis. Instituto Multidisciplinario de Investigaciones BiolĂłgicas de San Luis. Universidad Nacional de San Luis. Facultad de Ciencias FĂsico Matemáticas y Naturales. Instituto Multidisciplinario de Investigaciones BiolĂłgicas de San Luis; ArgentinaFil: Oravec, Michal. Global Change Research Institute; RepĂşblica ChecaFil: Csöllei, Jozef. University Of Veterinary And Pharmaceutical Sciences; RepĂşblica Chec
Abietane Diterpenes of the Genus Plectranthus sensu lato
Plectranthus (Lamiaceae), which—according to the latest systematic revision—includes three separate genera (Coleus, Plectranthus sensu stricto, and Equilabium), is a genus widely used in traditional medicine—mainly in the treatment of various ailments of the digestive tract, respiratory tract, and skin. Many species of Plectranthus s.l. have been shown to produce phenolic compounds and terpenes. Diterpenes, especially those of the abietane class, are the most studied group of secondary metabolites found in Plectranthus s.l., which is characterized by a significant structural diversity arising from the oxygenation and further rearrangement of the basic tricyclic abietane skeleton to a complete aromatization of the ring system. This review summarizes the known information on abietane diterpenes, showing their structures, sources, and biosynthesis. A classification of these compounds into nine groups, according to the arrangement of their ring C, is used. Royleanones, spirocoleons, and hydroquinones are the largest classes of abietane diterpenes, covering more than 70% of all the compounds reviewed
ANTIOXIDANT AND GLUCOSIDASE INHIBITION ACTIVITIES AND POLYPHENOL CONTENT OF FIVE SPECIES OF AGRIMONIA GENUS
Phytochemical analysis and a comparative study of antioxidant activity, inhibition of a-glucosidase and content of total polyphenols and flavonoids were established in five species of Agrimonia genus. Plants were collected in Medicinal Herbs Centre of Masaryk university Brno and these were Agrimonia eupatoria L., Agrimonia procera Wallr., Agrimonia leucantha Kunze, Agrimonia japonica (Miq.) Koidz and Agrimonia coreana Nakai. HPLC profile of Agrimonia herbs shows high content of quercetin and apigenin glycosides. The content of total polyphenols correlates with antioxidant activity and the content of flavonoids correlates with inhibition of a-glucosidase. Agrimonia procera works as an excellent antioxidant, the most used in traditional medicine Agrimonia eupatoria is richer on flavonoid glycosides
Anticholinesterase, antioxidant activity and phytochemical investigation into aqueous extracts from five species of Agrimonia
Anticholinesterase, antioxidant activity and phytochemical investigation into aqueous extracts from five species of <i>Agrimonia</i> genus
<p>Aqueous extracts of aerial flowering parts of five <i>Agrimonia</i> species (Rosaceae): <i>Agrimonia coreana</i> Nakai, <i>Agrimonia japonica</i> (Miq.) Koidz, <i>Agrimonia procera</i> Wallr., <i>Agrimonia eupatoria</i> L. and <i>Agrimonia leucantha</i> Kunze were investigated on their antioxidant activity, measured using five different methods; the best was the extract from <i>A. procera</i> with IC<sub>50</sub> values from 6 to 29Â ÎĽg/mL. All the extracts displayed inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) at the tested concentration of 100Â ÎĽg/mL. We found the highest inhibition of cholinesterase in the extract of <i>A. japonica</i> with inhibition 70.4% for AChE and 79.8% for BuChE. These findings are statistically significant in comparison with those of other extracts (<i>p</i>Â <Â 0.001). The phytochemical analyses showed that the antioxidant activity of <i>Agrimonia</i> extracts can be affected especially by hexahydroxydiphenoyl (HHDP)-glucose and quercetin glycosides, and inhibition of cholinesterases by apigenin, luteolin and quercetin glycosides.</p