RESUMEN
Sebum production and excretion is a primary function of the sebaceous glands, but abnormally increased sebum production is a major cause of acne vulgaris. To identify a new candidate that regulates sebum production, we investigated the possible inhibitory effects of apple polyphenols (APP) purified from unripe apples on primary cultured human sebocytes and in patients with acne vulgaris. Dexamethasone (Dex) increased lipid synthesis and expression of the sterol response element-binding protein 1 (SREBP 1) and its target enzymes, acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS), in the sebocytes. However, APP inhibited Dex-induced lipid production and expression of SREBP-1, ACC and FAS. APP also inhibited the increase in the expression and activation of glucocorticoid receptor in the sebocytes. Taken together, these results suggest that APP may be useful to regulate sebum production and may alleviate sebum-involved skin disease, such as acne vulgaris.
Asunto(s)
Ácido Clorogénico/farmacología , Flavonoides/farmacología , Expresión Génica/efectos de los fármacos , Lipogénesis/efectos de los fármacos , Extractos Vegetales/farmacología , Proteína 1 de Unión a los Elementos Reguladores de Esteroles/genética , Proteína 1 de Unión a los Elementos Reguladores de Esteroles/metabolismo , Taninos/farmacología , Acetil-CoA Carboxilasa/genética , Acetil-CoA Carboxilasa/metabolismo , Células Cultivadas , Dexametasona/farmacología , Acido Graso Sintasa Tipo I/genética , Acido Graso Sintasa Tipo I/metabolismo , Glucocorticoides/farmacología , Humanos , Lípidos/biosíntesis , Cultivo Primario de Células , Glándulas Sebáceas/citología , Glándulas Sebáceas/efectos de los fármacos , Glándulas Sebáceas/metabolismoRESUMEN
BACKGROUND: Ultraviolet (UV) irradiation triggers skin photoaging processes, which disrupt the normal three-dimensional integrity of skin. UV-induced oxidative stress, both directly and indirectly, stimulates complex signaling pathways. UV radiation activates skin cell surface receptors on a molecular level and triggers severe changes in extracellular matrix (ECM) proteins, resulting in skin photoaging. AIMS: Sclareol isolated from Salvia officinalis is widely used as a fragrance material. Sclareol is known to exert various biological activities, but its antiphotoaging effect has not been elucidated to date. Therefore, we evaluated wrinkle improvement efficacy of sclareol. METHODS: Human dermal fibroblast cell line (Hs68) and a reconstructed human epidermis (RHE) model were used to evaluate the antiphotoaging effect of sclareol in vitro. A clinical study treated with 0.02% sclareol-containing cream was conducted to identify the ability of sclareol to improve wrinkles. RESULTS: First, sclareol enhanced cellular proliferation and blocked UVB-induced cell death. Sclareol inhibited the UVB-induced mRNA expression of matrix metalloproteinases (MMPs) by regulating the protein expression of AP-1 constituents. In RHE model, sclareol recovered the UVB-induced decrease in epidermal thickness and the expression of proliferating cell nuclear antigen (PCNA). In clinical trial, visually assessed changes and several wrinkle parameters were considered to be statistically different between the test and control groups at 12 weeks. CONCLUSIONS: In this study, sclareol inhibited various photoaging phenomena in human fibroblasts and RHE model. In addition, sclareol-containing cream improved wrinkles in a clinical trial. Taken together, sclareol alleviates facial wrinkle formation via an antiphotoaging mechanism and may be an effective candidate ingredient.
Asunto(s)
Diterpenos/farmacología , Extractos Vegetales/farmacología , Salvia officinalis , Envejecimiento de la Piel/efectos de los fármacos , Adulto , Muerte Celular/efectos de los fármacos , Muerte Celular/efectos de la radiación , Línea Celular , Proliferación Celular/efectos de los fármacos , Diterpenos/uso terapéutico , Epidermis/efectos de los fármacos , Cara , Femenino , Fibroblastos , Expresión Génica/efectos de los fármacos , Expresión Génica/efectos de la radiación , Humanos , Metaloproteinasas de la Matriz/genética , Persona de Mediana Edad , Fitoterapia , Extractos Vegetales/uso terapéutico , Antígeno Nuclear de Célula en Proliferación/metabolismo , Crema para la Piel/uso terapéutico , Factor de Transcripción AP-1/efectos de los fármacos , Factor de Transcripción AP-1/metabolismo , Rayos UltravioletaRESUMEN
Polymer-hybridized liposomes (PHLs) of saturated lecithin were formed by association of poly(asparagines) grafted with alkyl chains (PAsn-g-Cn). The thermal, physical, and surface properties of the polymer-hybridized liposomes were examined with varying polymer concentration, alkyl chain length (C(8), C(12), C(18), C(22)), and degree of substitution (DS) in the polymer. The inclusion of the polymer raised the membrane fluidity of liposomes. By the incorporation of small amount of polymer, the membrane rigidity of liposomes dropped sharply and then increased close to the original level as the polymer concentrations increased in the cases of PAsn-g-C(18) and PAsn-g-C(22). Also, the membrane rigidity and stability of PHLs increased with alkyl chain length at the same polymer concentration. The surface charge of PHL associated with PAsn-g-C(22) was changed by DS of alkyl chains. The polymer bearing long alkyl chains (C(12), C(18), C(22)) formed PHLs well at low polymer concentration and the number of disk-shaped polymer-lipid mixed micelles increased with polymer concentration. The anchored polymers induced shifts in gel-to-liquid crystal transition temperature (Tc) of the vesicles and Tc varied with polymer concentration, alkyl chain length, and DS of the polymer.