RESUMEN
In the course of this project, 133 plants were evaluated on their ability to inhibit tyrosinase, a key enzyme in melanogenesis. The screening was performed by means of a HPTLC autographic assay, resulting in the selection of three plants, Asplenium trichomanes, Pinus uncinata, and Scutellaria altissima, with promising tyrosinase inhibiting activities. With the aid of the HPTLC assay, it was not only possible to select the most interesting plant extracts, but also to monitor the activity-guided fractionation which, in a relatively short time period, led to the isolation of active principles. Benzoic acid, roseoside, and dihydrovomifoliol-O-ß-d-glucopyranoside could be identified as tyrosinase inhibitors present in P. uncinata. Globularin turned out to be the active principle of S. altissima, and 4-ethenylphenyl 6-O-(6-deoxy-α-l-mannopyranosyl)-ß-d-glucopyranoside was detected as tyrosinase inhibitor of A. trichomanes. The pure compounds were tested also in a 96 well-plate assay in order to determine their IC50 values. The lowest IC50 value (42â µm) could be obtained for globularin, whereas the other compounds, e. g., benzoic acid exhibited a rather high IC50 value (IC50 =552â µm). This stood in clear contrast to the autographic assay, but is has to be taken into account that the outcome of the autography assay is not only depending on the IC50 value of a compound, but also on the content of the respective constituent in the extract.
Asunto(s)
Inhibidores Enzimáticos/farmacología , Helechos/química , Monofenol Monooxigenasa/antagonistas & inhibidores , Pinus/química , Extractos Vegetales/farmacología , Scutellaria/química , Agaricales/enzimología , Ácido Benzoico/química , Ácido Benzoico/aislamiento & purificación , Ácido Benzoico/farmacología , Cromatografía en Capa Delgada , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Europa (Continente) , Glucósidos/química , Glucósidos/aislamiento & purificación , Glucósidos/farmacología , Conformación Molecular , Monofenol Monooxigenasa/metabolismo , Norisoprenoides/química , Norisoprenoides/aislamiento & purificación , Norisoprenoides/farmacología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Especificidad de la Especie , Relación Estructura-ActividadRESUMEN
NADPH oxidase 4 (Nox4) has recently been implicated as driving force in cellular senescence. Thus, there is growing interest to develop Nox4 inhibitors, which might be valuable agents for cosmeceutical applications. Alpine plants represent a valuable source for the identification of novel bioactive natural products with anti-ageing effects, especially substances that protect plants against UV radiation, which is also known to contribute to the ageing of human skin. Therefore, the aim of this study was to identify novel Nox4 inhibitors from alpine plants. Within an initial screening of extracts of alpine plants on their ability to inhibit Nox4 activity in HEK cells, the methanolic extract of the subaerial parts of Lycopus europaeus showed a strong inhibition of Nox4 (81% chemiluminescence quenching) and a simultaneously high cell viability (91% vitality). Rosmarinic acid was isolated and identified as the major compound in this bioactive extract. It showed a dose dependent inhibitory activity on Nox4 with an IC50 of 1 µM. Moreover, it also showed a significant inhibitory activity on Nox2 in the low micromolar range, whereas no inhibition of Nox5 was detected. Further investigations confirmed that the observed effects of rosmarinic acid on Nox2 and Nox4 are real inhibitory activities, and not due to ROS scavenging effects. Therefore, L. europaeus, which we demonstrated to be a good source of rosmarinic acid, has great potential for usage in cosmeceutical products with anti-ageing activity.
Asunto(s)
Cinamatos/aislamiento & purificación , Cinamatos/farmacología , Depsidos/aislamiento & purificación , Depsidos/farmacología , Inhibidores Enzimáticos/aislamiento & purificación , Inhibidores Enzimáticos/farmacología , Lycopus/química , NADPH Oxidasa 4/metabolismo , Línea Celular , Supervivencia Celular , Cinamatos/química , Depsidos/química , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Regulación de la Expresión Génica/efectos de los fármacos , Células HEK293 , Humanos , Metanol/química , Metanol/aislamiento & purificación , Metanol/farmacología , NADPH Oxidasa 2/metabolismo , Componentes Aéreos de las Plantas/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Especies Reactivas de Oxígeno/metabolismo , Ácido RosmarínicoRESUMEN
Solidago canadensis is an invasive species from North America that is spreading across Europe, Australia and temperate Asia. We hypothesized that the species' wide ecological amplitude is also based on its potential in hydraulic acclimation, and analyzed hydraulic and anatomical properties along a transect with decreasing soil humidity. Stem hydraulic conductivity, vulnerability to drought-induced embolism, stomatal closure during dehydration and xylem-anatomical parameters were quantified at three sites. At the humid site, specific hydraulic conductivity of stems (1.0 ± 0.2 kg m(-1) MPa(-1) s(-1)) was about twofold higher, and leaf-specific conductivity about 1.5 times higher (3.1 ± 0.5 kg m(-1) MPa(-1) s(-1)) than at the dry site. Water potential (Ψ) at 50% loss of conductivity was -3.7 ± 0.1 MPa at the dry site and -3.1 ± 0.2 MPa at the humid site (September). Vulnerability to drought-induced embolism decreased along the transect and over the vegetation period. At drier sites, stomata started closing at lower Ψ while complete stomatal closure was reached at less negative Ψ (12% of maximum stomatal conductance: -2.5 ± 0.0 and -3.0 ± 0.2 MPa at the dry and humid site). The safety margin between stomatal closure and 50% loss of conductivity was 1.2 and 0.2 MPa at the dry and humid sites. The observed variability indicated an efficient acclimation in hydraulic conductivity and safety: plants at dry sites exhibited lower specific hydraulic conductivity, higher embolism resistance and broader safety margins, signifying a trade-off between the hydraulic safety and efficiency. The observed intraspecific plasticity in hydraulic and anatomical traits may help to explain the invasive potential of this species.
Asunto(s)
Aclimatación/fisiología , Sequías , Solidago/fisiología , Estrés Fisiológico/fisiología , Hidrodinámica , Hojas de la Planta/fisiología , Raíces de Plantas/fisiología , Tallos de la Planta/fisiología , Estomas de Plantas/fisiología , Agua/metabolismo , Agua/fisiología , Xilema/fisiologíaRESUMEN
Many Polygonaceae taxa such as Bistorta officinalis, Persicaria amphibia, Persicaria hydropiper, Persicaria lapathifolia, Persicaria maculosa, Persicaria mitis, Polygonum aviculare occur naturally in the entire territory of Poland and are also common in other European countries. Many of these species are also utilised as medicinal plants. In this manuscript we establish the phytochemical profiles of selected taxa from the Polygonaceae focusing on phenolics. Additionally, we try to find chemophenetic markers for the species investigated. Compounds were detected and characterised based on HPLC-DAD-MS data, quantified, and furtherly analysed using multivariate analyses. Chemophenetic markers were identified also considering previous literature.
Asunto(s)
Plantas Medicinales , Polygonaceae , Polygonum , Polygonum/química , Cromatografía Líquida de Alta Presión , Quimiometría , Polygonaceae/química , Plantas Medicinales/química , Fenoles , Extractos Vegetales/químicaRESUMEN
The anti-melanogenic principle of peony (Paeonia officinalis subsp. officinalis) seeds was elucidated via activity-guided isolation. Resveratroloside (trans-resveratrol-4'-O-beta-d-glucopyranoside) was found to be the main metabolite of P. officinalis subsp. officinalis seeds and its tyrosinase inhibiting activity was confirmed via an enzymatic assay. Furthermore, the in vitro activity and the therapeutic window were studied employing the murine melanoma cell line B16F10. The results from the conducted stability assay and the high content of resveratroloside in the seeds (i.e. 10.4% dw) motivated us to push the extract forward to an in vivo tolerance assay. A clinical study with forty Caucasian participants proofed a good skin-tolerance with high moisture effect and reduction of pores.