The purpose of this study was to develop liposomal formulations of Asparagus racemosus root extract(AR1-6)as well as evaluate the physicochemical properties and in vitro tyrosinase inhibitory activity.Liposomes compos...The purpose of this study was to develop liposomal formulations of Asparagus racemosus root extract(AR1-6)as well as evaluate the physicochemical properties and in vitro tyrosinase inhibitory activity.Liposomes composed of AR1-6 to lipid weight ratio of 1:10 and lecithin(LEC)or Phospholipon90G(PC90G)as structural phospholipid at 7:3 molar ratio to CHOL were prepared by various methods,i.e.chloroform-film(CF),reverse-phase evaporation(REV),polyol dilution(PD),and freeze-drying of monophase solution(MFD)methods.The results revealed that vesicles prepared by CF and MFD were multilamellar whereas those prepared by REV and PD were oligolamellar in nature with particle sizes ranging from 0.26 to 13.83 mm.The zeta potentials were in the range of1.5 to39.3 mV.AR1-6 liposomes with LEC possessed significantly higher entrapment than those with PC90G.The highest entrapment efficiency and in vitro tyrosinase inhibitory activity of 69.08%and 25%,respectively,were obtained from liposomes having LEC and prepared by PD method.The tyrosinase inhibitory activity were in the rank order of LEC>PC90G,and PD>CF>REV>MFD.It could be concluded that the mechanism of vesicle forming in each method of preparation was the key factor influencing physicochemical properties,particularly vesicle type,size,surface charge,and entrapment,which were well correlated with the biological activity.展开更多
Objective:To evaluate the effects of phenolic acids(caffeic,ferulic,and coumaric acids)and flavones(luteolin and apigenin)on the proliferation and melanogenesis in murine melanoma B16-F10 cells.Methods:Cell proliferat...Objective:To evaluate the effects of phenolic acids(caffeic,ferulic,and coumaric acids)and flavones(luteolin and apigenin)on the proliferation and melanogenesis in murine melanoma B16-F10 cells.Methods:Cell proliferation was determined after 24 and 48 hours of incubation using MTT assay.The effects of these tested compounds on cell cycle progression were analyzed by flow cytometry.Moreover,the melanin content and tyrosinase activity were measured spectrophotometrically at 475 nm.Results:Luteolin and apigenin exhibited significant anti-proliferative activity against B16-F10 cells,while caffeic,ferulic,and coumaric acids induced slight inhibition after 24 and 48 hours of incubation.The tested compounds disturbed cell cycle progression of B16-F10,by a subsequent decrease in G1 and arrested cycle progression in either G1/S or G2/M phase.Furthermore,apigenin provoked an increase in melanin content of B16-F10 cells.In contrast,luteolin,caffeic,ferulic and coumaric acids induced a decrease in melanin content of B16-F10 cells by inhibiting tyrosinase activity.Conclusions:These active polyphenols may be used as skin whitening agents or natural tanning agents to treat skin pigmentation disorders.展开更多
基金The financial support from the Thai Herbal NanoCosmeceuticals Coordinated Research Program,National Nanotechnology Center,National Science and Technology Development Agency,Thailand is gratefully acknowledged.
文摘The purpose of this study was to develop liposomal formulations of Asparagus racemosus root extract(AR1-6)as well as evaluate the physicochemical properties and in vitro tyrosinase inhibitory activity.Liposomes composed of AR1-6 to lipid weight ratio of 1:10 and lecithin(LEC)or Phospholipon90G(PC90G)as structural phospholipid at 7:3 molar ratio to CHOL were prepared by various methods,i.e.chloroform-film(CF),reverse-phase evaporation(REV),polyol dilution(PD),and freeze-drying of monophase solution(MFD)methods.The results revealed that vesicles prepared by CF and MFD were multilamellar whereas those prepared by REV and PD were oligolamellar in nature with particle sizes ranging from 0.26 to 13.83 mm.The zeta potentials were in the range of1.5 to39.3 mV.AR1-6 liposomes with LEC possessed significantly higher entrapment than those with PC90G.The highest entrapment efficiency and in vitro tyrosinase inhibitory activity of 69.08%and 25%,respectively,were obtained from liposomes having LEC and prepared by PD method.The tyrosinase inhibitory activity were in the rank order of LEC>PC90G,and PD>CF>REV>MFD.It could be concluded that the mechanism of vesicle forming in each method of preparation was the key factor influencing physicochemical properties,particularly vesicle type,size,surface charge,and entrapment,which were well correlated with the biological activity.
基金supported by the Tunisian Ministry of Higher Education and Scientific Research.
文摘Objective:To evaluate the effects of phenolic acids(caffeic,ferulic,and coumaric acids)and flavones(luteolin and apigenin)on the proliferation and melanogenesis in murine melanoma B16-F10 cells.Methods:Cell proliferation was determined after 24 and 48 hours of incubation using MTT assay.The effects of these tested compounds on cell cycle progression were analyzed by flow cytometry.Moreover,the melanin content and tyrosinase activity were measured spectrophotometrically at 475 nm.Results:Luteolin and apigenin exhibited significant anti-proliferative activity against B16-F10 cells,while caffeic,ferulic,and coumaric acids induced slight inhibition after 24 and 48 hours of incubation.The tested compounds disturbed cell cycle progression of B16-F10,by a subsequent decrease in G1 and arrested cycle progression in either G1/S or G2/M phase.Furthermore,apigenin provoked an increase in melanin content of B16-F10 cells.In contrast,luteolin,caffeic,ferulic and coumaric acids induced a decrease in melanin content of B16-F10 cells by inhibiting tyrosinase activity.Conclusions:These active polyphenols may be used as skin whitening agents or natural tanning agents to treat skin pigmentation disorders.
