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1.
Molecules ; 25(20)2020 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-33081083

RESUMO

Olfactory receptors (ORs) are expressed and active in various human tissues, including the skin. Although the sense of smell plays an important physiological role in the regulation of mood and stress, a link between olfactive compounds, ORs, and skin stress has yet to be established. This study aims to investigate the role of newly identified skin ORs and agonists in the modulation of skin stress. Screening for odorant molecules was done with cAMP functional assay to identify OR agonists. RT-qPCR and immunofluorescence microscopy were conducted to identify and quantify ORs in epidermal keratinocytes (NHEKs) and human skin explants, as well as to evaluate specific markers (G6PDH, loricrin, and γH2AX) of stress-induced skin alterations. A randomized double-blinded, split-face clinical study was performed on a panel of stressed women to measure the benefits of OR agonist treatment for skin. Three new ORs (OR10A6, OR2AG2, and OR11H4) were identified in skin. A specific Rose extract and its major constituent (phenylethyl alcohol) were found to activate these ORs. The extract composition was revealed by both GC/FID and GC/MS analyses simultaneously and showed the presence of 34 volatiles molecules. Moreover, epinephrine induces a skin stress response characterized by increased expression of G6PD, loricrin, and γH2AX biomarkers, and a decrease of OR expression. These effects were prevented in the presence of rose extract and its benefits were confirmed clinically by a decrease in the appearance of under-eye dark circles. Altogether, our findings suggest that ORs may represent a new, promising way to treat stress-associated skin disorders.


Assuntos
Extratos Vegetais/farmacologia , Receptores Odorantes/genética , Rosa/química , Pele/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Queratinócitos/efeitos dos fármacos , Extratos Vegetais/química , Substâncias Protetoras/química , Substâncias Protetoras/farmacologia , Transdução de Sinais/efeitos dos fármacos , Pele/efeitos dos fármacos , Compostos Orgânicos Voláteis/química , Compostos Orgânicos Voláteis/farmacologia
2.
Planta Med ; 77(9): 900-6, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21240840

RESUMO

Owing to their high content of flavonoids and saponins, plantlets of Avena sativa L. (Poaceae) are likely to possess anti-inflammatory and immunoregulatory properties of value in the treatment of atopic dermatitis (AD). With a view to its potential use in atopic subjects at risk of developing sensitisation to dietary proteins, we prepared a plantlet extract without proteins and isolated 2 flavonoids, isoorientin-2''- O-arabinoside (1) and isovitexin-2''- O-arabinoside (2), and two saponins, avenacosides A (3) and B (4). The absence of protein in this extract was evidenced by electrophoresis and Western immunoblotting. Furthermore, Western immunoblotting demonstrated the absence of cross-reaction between grain and plantlet proteins. We evaluated the anti-inflammatory activity of the plantlet extract and its compounds IN VITRO in a model of keratinocyte inflammation: 6-keto prostaglandin F1 α production was inhibited by the plantlet extract (- 35 % and - 57 % at 10 and 30 µg/mL, respectively; p < 0.001) and isoorientin-2''- O-arabinoside (- 31 %, - 51 %, and - 56 % at 3, 10, and 30 µg/mL, respectively; p < 0.001). Intracellular interleukin-2 production in activated T lymphocytes was also inhibited by 16 %, 27 %, and 31 % with 3, 10, and 30 µg/mL plantlet extract, respectively, and by 23 % and 32 % with 3 and 10 µg/mL avenacoside A, respectively, (p < 0.001), demonstrating their immunoregulatory activity IN VITRO. The plantlet extract was also effective on the phenotype and function of dendritic cells (DC) differentiated from monocytes. It decreased the expression of major histocompatibility complex class II molecules on DC and significantly impaired their stimulatory activity on autologous T-cell proliferation (-25 %, p < 0.05). In conclusion, this protein-free oat plantlet extract exhibits anti-inflammatory and immunoregulatory activities in vitro.


Assuntos
Anti-Inflamatórios/farmacologia , Avena/química , Flavonoides/farmacologia , Fatores Imunológicos/farmacologia , Extratos Vegetais/química , Saponinas/farmacologia , 6-Cetoprostaglandina F1 alfa/antagonistas & inibidores , 6-Cetoprostaglandina F1 alfa/metabolismo , Anti-Inflamatórios/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Células Dendríticas/efeitos dos fármacos , Células Dendríticas/metabolismo , Epoprostenol/metabolismo , Humanos , Interleucina-2/antagonistas & inibidores , Interleucina-2/metabolismo , Queratinócitos/efeitos dos fármacos , Queratinócitos/metabolismo , Fenótipo , Componentes Aéreos da Planta/química , Linfócitos T/efeitos dos fármacos , Linfócitos T/imunologia
3.
Steroids ; 70(13): 873-8, 2005 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-16081116

RESUMO

The apolar fraction of the crude alcoholic extract of the sponge Euryspongia n. sp. was shown to display anti-inflammatory activity. Bioassay guided chromatographic purification led to the isolation of a known compound petrosterol (1) of 3beta-hydroxy-24-norchol-5-en-23-oic acid (2), which has never yet been found as a natural substance, and of a new steroid, 3beta-hydroxy-26-norcampest-5-en-25-oic acid (3). The absolute configurations of 2 and 3 were deduced from comparative 1H NMR data of the (S)- and (R)-phenylglycine methyl ester derivatives. These compounds were evaluated for their anti-inflammatory activity against 6-keto-prostaglandinF1alpha release in a human keratinocyte cell line HaCaT.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Poríferos/química , Esteroides/isolamento & purificação , 6-Cetoprostaglandina F1 alfa/metabolismo , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Linhagem Celular , Humanos , Queratinócitos/citologia , Espectroscopia de Ressonância Magnética , Estereoisomerismo , Esteroides/química , Esteroides/farmacologia , Esteróis/isolamento & purificação
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