Inhibitory effect of Cyrtomium falcatum on melanogenesis in α-MSH-stimulated B16F10 murine melanoma cells

Objective:To explore the anti-melanogenic potential of Cyrtomium falcatum.Methods:The effects of Cyrtomium falcatum crude extract and its solvent fractions on tyrosinase activity,melanin content,and the expressions of melanogenesis-related genes and proteins were analyzed inα-melanocyte-stimulating hormone(α-MSH)-stimulated B16F10 cells.Results:α-MSH treatment significantly increased tyrosinase activity,and extracellular and intracellular melanin content,as well as the expression levels of tyrosinase,microphthalmia-associated transcription factor(MITF),tyrosinase-related protein(TRP)-1,and TRP-2 in B16F10 cells.Treatment with Cyrtomium falcatum crude extract and its solvent fractions reduced tyrosinase activity and extracellular and intracellular melanin content and downregulated the expression levels of tyrosinase,MITF,TRP-1,and TRP-2 in a dose-dependent manner.Conclusions:Cyrtomium falcatum has potential anti-melanogenesis effects and can be used as a potential source material in cosmeceutical industry for the research and development of novel lead molecules with whitening properties.

Anti-Melanogenesis Activity of Supercritical Carbon Dioxide Extract from Perilla frutescens Seeds

Perilla frutescens seed (PFS) oil is reported to inhibit skin photoaging;however, its effect on melanogenesis has not yet been investigated. Herein, we tested the anti-melanogenesis activity of an oil-based extract from PFS with supercritical carbon dioxide (scCO2). In a cell culture system, B16 mouse melanoma cells were treated with the PFS scCO2 extract and other samples. The PFS scCO2 extract decreased melanin production by approximately 90% in B16 mouse melanoma cells without cytotoxicity at 100 μg/mL. This effect was greater than that of the well-known melanogenesis inhibitor, kojic acid. Although a hexane-extracted PFS oil and a squeezed PFS oil also decreased melanin production in the B16 cells, the inhibitory effect of the PFS scCO2 extract was higher than both of these. Chemical analysis of the PFS scCO2 extract and squeezed PFS oil showed that almost 90% of the components of both oils were α-linolenic acid, linoleic acid, and oleic acid. Furthermore, the ratio of those three fatty acids across both samples was almost the same. When the three fatty acids were mixed in the same ratio as in the PFS scCO2 extract, the IC50 of the mixture for melanin production in B16 melanoma cells was identical to that of the PFS scCO2 extract. However, the IC50 of the squeezed PFS oil was approximately 6.6 times higher than that of the mixture. Although those fatty acids are the main inhibitory ingredients against melanin production in all of the extracts, some factor(s) in the squeezed PFS reduce their affinity with the cells. These results indicated that the PFS scCO2 extract could be a superior melanogenesis inhibitor. Although its main ingredients are probably the same as those of the squeezed PFS oil, it is necessary to extract with scCO2 for stronger anti-melanogenesis activity.

Detraining after tumor-bearing accelerates tumor growth while continuous training decreases tumor growth in mice

Objective:Previous studies have shown that exercise suppresses tumor growth.However,the effects of exercise with different intensities and exercise detraining after tumor-bearing on tumor progression remain unclear.The purpose of this study was to investigate the effects of continuous and disrupted free and exhausted swimming training after tumor-bearing on tumor progression in melanoma B16-F10-bearing C57BL/6 mice.Methods:C57BL/6 mice were subjected to free or exhausted swimming exercise training for 4 weeks prior to the injection of melanoma B16-F10 cells.Subsequently,the B16-F10-bearing mice were maintained with training consisting of free or exhausted swimming or without exercise for 2 weeks during the tumor challenge.Results:The tumor weight was increased by 42%and 109%in mice with 4-week exhausted swimming prior to B16-F10 tumor cells inoculation followed by 2-week training cessation compared with the tumor-bearing control(P<.05)and continuous training groups(P<.01).Tumor weights in groups with exercise detraining after tumor cell inoculation tended to be increased,while the proliferation of splenic T lymphocytes tended to be decreased compared with the group that maintained exercise intensity.After 6-weeks continuous free or exhausted swimming training,the tumor weight of mice was decreased and the proliferation of splenic T lymphocytes was increased compared with the tumor-bearing control group.The frequency of natural killer cells in tumors was increased in all exercise training groups of mice.Conclusions:These results suggest that maintaining exercise intensity after tumor-bearing slows tumor growth in mice,possibly because of the enhanced proliferative activity of splenic lymphocytes rather than natural killer cell infiltration.However,detraining after tumor-bearing might accelerate tumor progression because of the reduced proliferation of splenic T lymphocytes.

Inhibition of tyrosinase activity and melanine pigmentation by 2-hydroxytyrosol

2-Hydroxytyrosol(2-HT),originally reported as a synthetic compound,was isolated for the first time as a fungal metabolite.2-HT was found to inhibit mushroom tyrosinase with an IC_(50) value of 13.0 mmol/L.Furthermore,2-HT dose-dependently inhibited tyrosinase activity(IC_(50),32.5 mmol/L)in the cell-free extract of B16 melanoma cells andα-melanocyte stimulating hormone(α-MSH)-stimulated melanin formation in intact B16 melanoma cells.

Synthesis of poly(amidoamine)-poly(ethyleneglycol)-poly(amidoamine) and preparation of its hydrogel solution containing doxorubicin

Many pH-and temperature-responsive polymers have been designed for preparing hydrogel.In the present study,in order to decrease the pH sensitivity of reported poly(amidoamine)-poly(ethyleneglycol)-poly(amidoamine)(PAA1580-PEG4600-PAA1580),we designed and synthesized poly(amidoamine)-poly(ethyleneglycol)-poly(amidoamine)(PAA-PEG-PAA)with shorter length of PAA chain by decreasing reaction temperature for preparing PAA-PEG-PAA hydrogel solution containing doxorubicin(DOX).The PAA-PEG-PAA was synthesized via the Michael-addition polymerization.The characteristic of PAA-PEG-PAA was evaluated.The PAA-PEG-PAA hydrogel solution was prepared and investigated.DOX-loaded PAA-PEG-PAA hydrogel solution was prepared,and its in vitro DOX release and in vitro anti-tumor activity were evaluated.Our results indicated that the viscosity of PAA-PEG-PAA hydrogel solution was concentration-and temperature-dependent.The sol-gel transition temperature of PAA-PEG-PAA hydrogel solution(12%,w/w)ranged from 35 to 29℃,and its pH ranged from 6.0 to 7.4.The released DOX from DOX-loaded PAA-PEG-PAA hydrogel showed sustained release characteristics.The in vitro anti-tumor activity of DOX-loaded PAA-PEG-PAA hydrogel was confirmed in B16 F10 cell line.Considering the acidic tumor microenvironment,this DOX-loaded PAA-PEG-PAA hydrogel solution would be easy in situ administration for intra-tumor injection or para-tumor injection forming hydrogel at body temperature.We suggested that this DOX-loaded PAA-PEG-PAAhydrogel solution,if containing photothermal conversion agents,would have a potential further use for photothermal therapy.

Design,synthesis and bioactivity of chalcones and its analogues

The Vernohia anthelmintica L.＇s extract is one of the most popular Uygur medicines used for vitiligo. It is believed that the chalcone compounds of the plant play an important role in the treatment since they may activate tyrosinase and improve melanin production. In this study, twenty-one chalcones and nine analogues were synthesized in view of three different components of chalcone（A, B ring and a,b-unsaturated carbonyl）. After biological evaluation of their activity on tyrosinase in cell-free systems,the result showed that most compounds（except polyhydroxy chalcones） possess activator effect on the tyrosinase, especially for 13a–15a, 20 a and 1b, which bearing a comparable activity to the positive control8-MOP. SAR of these tyrosinase activator was summed up for the first time as well. Finally, compound 13 a was found to increase melanin contents and tyrosinase activity 1.75 and 1.3 fold, respectively, compared with that of untreated murine B16 cells at the concentration of 40 mg/m L.