ABSTRACT
Objective: To compare the effects of softeners including ethanol, propylene glycol and mixed alcohol (ethanol-propylene glycol 2:8) on the preparation of glabridin ethosomes (GLA-ES), and provide the selection basis of the softeners for studying the ethosomes of insoluble drugs. Methods: GLA-ES were prepared by injection-ultrasonic binding method with ethanol, propylene glycol and mixed alcohol (ethanol-propylene glycol, 2:8) as softeners. The morphology, size, Zeta potential, entrapment efficiency, stability, and in vitro drug release of GLA-ES were investigated. Tyrosinase activity on melanoma B16-OVA cells were detected to evaluate the inhibition of GLA-ES on the synthesis of melanin, the experiment of potassium ferricyanide reducing power was performed to evaluate the antioxidant effect of GLA-ES, and human epidermal HaCaT cells and rat skin were used for preliminary safety evaluation. Results: GLA-ES were yellow translucent liquid, containing vesicular phospholipid bilayer structure, the average particle size of GLA-Et-ES, GLA-PG-ES and GLA-MA-ES were (34.24 ± 0.29), (62.31 ± 1.66) and (41.20 ± 1.13) nm, respectively; The Zeta potential were (-41.0 ± 1.8), (-32.9 ± 0.2) and (-35.8 ± 1.6) mV, the entrapment efficiency were (91.47 ± 2.39)%, (87.33 ± 1.31)% and (91.39 ± 3.59)%, respectively, which had good stability of storage at 4 ℃ for 20 d, in vitro drug release behaviors of GLA-ES fitted Higuchi equation, implying their sustained release properties. Compared with the glabridin suspension, the inhibitory effects of GLA-Et-ES, GLA-PG-ES and GLA-MA-ES on tyrosinase activity in melanoma B16-OVA cells were increased by 38.07%, 19.58% and 40.42%, respectively. The results of potassium ferricyanide reducing power also showed that GLA-ES had a stronger in vitro antioxidant effect than the glabridin suspension; GLA-ES were nearly nontoxic on normal cells and had no irritation to rat skin. Conclusion: GLA-ES can be obtained by hree kinds of softeners, which can inhibit the synthesis of melanin and enhance the antioxidant effect with good safety. The present research will provide the basis for further developing skin-whitening cosmetics or pharmaceutical external preparation. For the insoluble drugs such as glabridin, when mixed alcohol (ethanol-propylene glycol) was selected as the softener to prepare ethosome, it exhibited better encapsulation efficiency and stability than that of ethanol or propylene glycol as the softener alone.
ABSTRACT
Despite the development of modern medicine, alternative medicine, which has not lost its timeliness, remains attractive for the treatment of various diseases. Glabridin, a major flavonoid of Glycyrrhiza glabra, is known for its antioxidant and anti-inflammatory activity. The aim of this study was: 1) to determine the possible protective role of glabridin against ischemia/reperfusion (I/R) injury of the intestine; 2) to evaluate the in vitrocontractile responses of ileum smooth muscles to acetylcholine after an intestinal I/R; and 3) to explain the underlying molecular mechanism of its effect. Rats were assigned to groups of six rats each; 1) I/R, 2) gla10, 3) gla20, 4) gla40, 5) N5-[imino(nitroamino)methyl]-L-ornithine, methyl ester monohydrochloride (L-NAME)+gla40, and 6) Sham group. The healing effect of glabridin was abolished by L-NAME. Glabridin did not cause contractility of the smooth muscles to acetylcholine-induced contractile responses in intestinal I/R. Yet, it increased to spontaneous basal activity.
A pesar del desarrollo de la medicina moderna, la medicina alternativa, sin perder su vigencia, sigue siendo atractiva para el tratamiento de varias enfermedades. Glabradina, el flavonoide mayoritario de Glycyrrhiza glabra, es conocido por su actividad antioxidante y antiinflamatoria. Los propósitos de este estudio fueron: 1) Determinar el posible rol protector de glabradina ante daños intestinales por isquemia/reperfusion (I/R) 2) Evaluar in vitrolas respuestas de contracción de los músculos lisos del ileum ante acetilcolina después de I/R intestinal; y 3) Explicar el mecanismo molecular subyacente de este efecto. Se asignaron grupos de seis ratas: 1) I/R, 2) gla10, 3) gla20, 4) gla40, 5) N5-[imino(nitroamino)metil]-L-ornithina, metil ester monohidrochloruro (L-NAME)+gla40, y 6) Grupo testigo. El efecto curativo de glabridina fue abolido por L-NAME. Glabridina no causó contracción en el músculo liso como respuesta acetilcolina-inducida I/R. Además, incrementa la actividad basal expontánea.
Subject(s)
Animals , Rats , Phenols/administration & dosage , Reperfusion Injury/drug therapy , Cyclic AMP/metabolism , Glycyrrhiza , Isoflavones/administration & dosage , Phenols/pharmacology , Rats, Wistar , Cyclic AMP/analysis , Cyclic GMP/metabolism , Oxidative Stress/drug effects , NG-Nitroarginine Methyl Ester , Ileum/drug effects , Ileum/chemistry , Isoflavones/pharmacology , Malondialdehyde/analysis , Muscle, Smooth/drug effectsABSTRACT
Glycyrrhiza glabra, commonly known as licorice, has traditionally been used in various medicinal preparations as expectorant, antimicrobial, antiviral, anticancer, anti allergic agent. It has also prominent role in skin whitening and has anti-inflammatory and esterogenic properties. This study aims to the characterization of the bioactive constituent glabridin in plant extract of Glycyrrhiza glabra in ethanol, methanol and ethyl acetate using UV-VIS and FTIR and HPLC. A wavelength scan (200-600 nm) by UV-Vis spectrophotometer was performed and the characteristic peaks were recorded. The scan confirmed presence of glabridin with λmax at 281 nm with a small number of additional phytochemicals indicated by the extra peaks. FTIR spectrum of 62% pure glabridin was compared to the spectra shown by the three extracts. Presence of glabridin in all the three extracts was corroborated by HPLC analysis with the retention time of 4.05 minute. Glabridin was also evaluated for its antibacterial activity against Propionibacterium acne, causative agent of Acne vulgaris and found to have the detrimental effect at concentration 500, 1000 and 1500 ppm.
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Introduction: Life style of humans, with changes in diet, exercise and life style practices which play an important role in enhancing the progression of age related degenerative problems like dementia. The most common cause of dementia in the world is Alzheimer’s disease which ultimately decrease the cognitive function mainly learning and memory. The objective of the study was to find the multi target potential efficacy of the ligands, Glabridin and Diosmetin in altering the two main molecular targets of Alzheimer’s disease (AD). The target enzymes were amyloid binding alcohol dehydrogenase (ABAD) and β-site amyloid precursor protein cleaving enzyme 1(BACE1). Material and methods: In this study, we analyzed that multitarget potential of the two natural compounds on the two prior target enzymes of Alzheimer’s disease which are mainly involved in producing neurodegeneration. Drug likeness properties, absorption, digestion metabolic and toxicity profile and molecular docking were analyzed to determine therapeutic aspect by virtual methods. Results: Binding energy and Vander Waals force of Diosmetin were higher than Glabridin with the target ABAD and less than with BACE1 which showed that both drugs can be used in modulating the enzyme phosphorylation in Alzheimer’s disease. Conclusion: Glabridin and Diosmetin could be used as promising drug candidates as ABAD inhibitor and BACE1 inhibitor in Alzheimer’s disease
ABSTRACT
It is reported that energy metabolism is the core feature of tumor cells. This study is aimed to investigate the regulatory effect of two flavonoids( glabridin and quercetin) on energy supply and glycolysis of breast cancer cells,and provide reference for developing some anticancer herbal drugs with the function of regulating tumor energy metabolism. Based on the characteristics of each pathway during energy metabolism,in the present study,the triple negative breast cancer tumor cells( MDA-MB-231) were selected to investigate the effects of glabridin and quercetin on the energy metabolism of breast cancer cells and discuss the possible mechanisms from the following five potential targets: glucose uptake,protein expression of glucose transporter 1( GLUT1),adenosine triphosphate( ATP) level,lactate dehydrogenase( LDH) activity,and lactic acid( LD) concentration. The results showed that both quercetin and glabridin could decrease the glucose uptake capacity of breast cancer cells by down-regulating the protein expression of GLUT1. Quercetin had no significant effect on LDH activity and LD concentration; it did not affect the glycolysis process,but increased the intracellular ATP level. Glabridin decreased the activity of LDH and reduced LD concentration,thereby inhibiting the glycolysis metabolism of breast cancer cells. Therefore,both quercetin and glabridin can regulate the energy metabolism of breast cancer cells and can be used as potential anticancer agents or anti-cancer adjuvants.
Subject(s)
Humans , Breast Neoplasms , Metabolism , Cell Line, Tumor , Energy Metabolism , Glucose , Metabolism , Glucose Transporter Type 1 , Metabolism , Isoflavones , Pharmacology , Phenols , Pharmacology , Quercetin , PharmacologyABSTRACT
Objective: To evaluate the anti-inflammatory property of both glycyrrhizic acid (GA) and glabridin in reducing inflammation to accelerate wound regeneration on 3T3-L1 and NIH-3T3 fibroblast cell lines. Methods: Cell proliferation and viability assay (MTT assay), scratch wound healing assays, and quantitative real-time PCR were conducted to investigate the effects on cell proliferation, cell migration, and expression of CXC chemokine ligand 5 inflammation gene respectively. Results: Results showed that at a low concentration of 1 × 10
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OBJECTIVE:To establish a method for the content determination of glabridin in Clycyrrhizae Radix et Rhizoma from different regions. METHODS:HPLC was performed on the column of Inertsil ODS-SP with mobile phase of acetoni-trile-0.05%phosphoric acid(gradient elution)at a flow rate of 0.8 ml/min,detection wavelength was 280 nm,the column tempera-ture was 35 ℃,and the injection volume was 20 μl. RESULTS:The linear range of glabridin was 0.906-18.12 μg/ml(r=0.999 7), RSDs of precision,stability and reproducibility tests were lower than 3%;recovery was 98.73%-101.90%(RSD=1.25%,n=6). There were obvious differences among the glabridin contents in G. uralensis from different regions. CONCLUSIONS:The method is simple and accurate with high precision,and can be used for the content determination of glabridin in Clycyrrhizae Radix et Rhi-zoma.
ABSTRACT
Glabridin (Glab) is an isoflavonoid originally isolated from the roots of Glycyrrhiza glabra L. (Fabaceae). Glab is widely considered to be a phytoestrogen and has been associated with numerous biological properties ranging from antioxidant, anti-inflammatory, neuroprotective, anti-atherogenic effects, to the regulation of energy metabolism. In this paper, a review on its biological activity was reviewed.
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Objective To study the effects of glabridin on human melanocytes and B16 murine melanoma cells. Methods After glabridin was added into the two kinds of cultured melanocytes, the cell viability, tyrosinase activity and melanin contents were measured, respectively. The effects of glabridin were compared with those of hydroquinone. Results It was shown that the effects of glabridin and hydroquinone on two kinds of cells were different. Compared with hydroquinone, glabridin had a concentration-dependent inhibition on melanogenesis and little influence on melanocyte viability. Conclusion There is a biological diversity between human melanocytes and murine melanoma cells. It is indicated that glabridin is a safe and active ingredient for depigmentation.