원보령 Bo Ryoung Won , 강명규 Myung Kyu Kang , 안유진 You Jin Ahn , 박수남 Soo Nam Park

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Abstract

The objective of this study was to find out the stable formulation of nano-emulsion containing high concentration of quercetin and to investigate the effect of an ethanol on the nano-emulsion prepared by POE (30) hydrogenated castor oil (HCO-30)/oil/quercetin/ethanol/water system. Nano-emulsion was prepared using emulsion inversion point (EIP) method as low-energy method plus homogenizer as high-energy method. To evaluate effect of ethanol and other components on the nano-emulsion, physical properties such as droplet size, morphology, and size distribution were determined. The optimal quercetin concentration was 0.2 % on the nano-emulsion. The droplet diameter was below 300 nm at the HCO-30 concentration below 2.00 %. Nano-emmulsion containing 4.75 % HCO-30 was the most stable and its mean droplet size was 172.40 nm. Finally, the size of nano-emulsion containing 4.00 % ethanol was 128.15 nm and size distribution was also narrow. The results showed that the breakdown process of this nano-emulsion could be attributed to Ostwald ripening. This study about effect of ethanol on the nano-emulsion showed that loading capacity of drug could be increased by using a small amount of ethanol. As prepared stable nano-emulsion, this study showed that these results could be applied to pharmaceutics, cosmetic including skin-care products, perfume and etc.

Key Words

nano-emulsion, emulsion inversion point, quercetin, size distribution, Ostwald ripening

김재현 Jai Hyun Kim , 양희정 Hee Jung Yang , 원보령 Bo Ryoung Won , 안유진 You Jin Ahn , 강명규 Myung Kyu Kang , 박수남 Soo Nam Park

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Abstract

In this study, vitamin E acetate (VEA, tocopheryl acetate), a lipid-soluble vitamin which is widely used in the cosmetics and medical supply field as a antioxidant material. The stable nano particle emulsion of skin toner type containing VEA was prepared. To evaluate the skin permeation, experiments on VEA permeation to the skin of the ICR outbred albino mice (12 weeks, about 50 g, female) and on differences of solubility as a function of re-ceptor formulations was performed. The analysis of nano-emulsions containing VEA 0.07 % showed that the higher ethanol contents the larger emulsions were formed, while the higher surfactant contents the size became smaller. A certain contents of ethanol in receptor phase increased VEA solubility on the nano-emulsion. When the ethanol contents were 10.0 % and 20.0 %, the VEA solubility was higher than 5.0 % and 40.0 %, respectively. The type of surfactant in receptor solution influenced to VEA solubility. The comparison between three kind surfactants whose chemical structures and HLB values are different, showed that solubility of VEA was increased as order of sorbitan sesquioleate (Arlacel 83; HLB 3.7) > POE (10) hydrogenated castor oil (HCO-10; HLB 6.5) > sorbitan monostearate (Arlacel 60; HLB 4.7). VEA solubility was also shown to be different according to the type of antioxidant. In early time, the solubility of the sample including ascorbic acid was similar to those of other samples including other types of antioxidants. However, the solubility of the sample including ascorbic acid was 2 times high-er than others after 24 h. Franz diffusion cell experiment using mouse skin was performed with four nano-emulsion samples which have different VEA contents. The emulsion of 10 wt% ethanol was shown to be the most permeable at the amount of 128.8 μg/cm². When the result of 10 % ethanol content was compared with initial input of 220.057 μg/cm², the permeated amount was 58.53 % and the permeated amount at 10 % ethanol was higher 45.0 % and 15.0 % than the other results which ethanol contents were 1.0 and 20.0 wt%, respectively. Emulsion particle size used 0.5 % surfactant (HCO-60) was 26.0 nm that is one twentieth time smaller than the size of 0.007 % surfactant (HCO-60) at the same ethanol content. Transepidermal permeation of VEA was 54.848 μg/cm² which is smaller than that of particlesize 590.7 nm. Skin permeation of nano-emulsion containing VEA and difference of VEA sol-ubility as a function of receptor phase formulation were determined from the results. Using these results, optimal conditions of transepidermal permeation with VEA were considered to be set up.

Key Words

vitamin E acetate, nano-emulsion, Franz diffusion cell, skin delivery, lipid-soluble antioxidant

조춘구 Choon Koo Zhoh , 이강연 Kang Yen Lee , 김동남 Dong Nam Kim

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Abstract

The objective of this study is to analyze the influences of fatty alcohols and fatty acids on rheological properties of oil in water (O/W) emulsions using viscosity and rheograms. As the chain length of fatty alcohols and fatty acids lengthened, the viscosity of emulsions was increased. The influence of fatty alcohols on viscosity enhancement was stronger than that of fatty acids. Both stearyl alcohol and cetearyl alcohol, which have carbon chain length similar to lipophilic portion of surfactant used in emulsion preparation, had showed the best increase in viscosity of O/W emulsions. O/W emulsions prepared with fatty alcohols and fatty acids were pseudo-plastic fluid and they showed shear thinning behaviour like as the common cosmetic emulsions. O/W emulsions prepared with cetyl alcohol, cetearyl alcohol and stearyl alcohol were thixotropic fluids and thixotropy increased with an increase in the concentration of fatty alcohols and fatty acids. Also O/W emulsions prepared with fatty alcohols were more thixotropic than those prepared with fatty acids. For the sake of viscosity increase related to O/W emulsions stability and spreadability enhancement related to payoff, it is thought that fatty alcohols are more useful than fatty acids in the O/W emulsions as the emulsion stabilizer.

Key Words

fatty acid, fatty alcohol, hysteresis loop, spreadability, pseudo-plastic

박창민 Chang Min Park , 정민석 Min Seok Joung , 최종완 Jong Wan Choi

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Abstract

Gymnema sylvestre, a traditional India medicine called a ‘Gagaimogouip' in Korea, has been used to regulate sugar metabolism in patients with diabetes mellitus. First, we induced callus from Gymnema sylvestre leaf and mode extract from cultured callus. In this study, we investigated the anti-obesity effect of tissue-cultured Gymnema sylvestre leaf extract in 3T3-L1 cells. The tissue-cultured Gymnema sylvestre extract inhibited the cytoplasmic lipid accumulation as well as adipogenic differentiation of preadipocytes. The tissue-cultured Gymnema sylvestre extract inhibited insulin-induced predipocyte differentiation through the inhibition of expression of the early adipogenic transcription factor C/EBP-α that regulate adipogenesis. These results indicate that tissue-cultured Gymnema sylvestre extract may be potential natural ingredient for slimming cosmetic products.

Key Words

Gymnema sylvestre, adipogenesis, C/EBP-α, anti-obesity, callus

김현주 Hyun Ju Kim , 이여명 Yeo Myeong Lee , 김연향 Yeon Hyang Kim , 원선임 Sun Im Won , 최성아 Sung A Choi , 최신욱 Shin Wook Choi

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Abstract

Magnolia extract, prepared from the Chinese herb Magnolia officinalis, is known for its potent anti-oxidative and anti-inflammatory effects. In this report, we showed that Magnolia extract inhibits adipocyte differentiation, as evidenced by reduced triglyceride (TG) accumulation. Also, Magnolia extract increased hormone sensitive lipase (HSL) protein level, and decreased the adipogenic transcription factor peroxisome proliferator activated receptor (PPAR)-γ protein and their corresponding mRNA. Our results suggest a potential apllication of Magnolia extract as anti-obesity agents inhibits adipocyte differentiation through the down-regulation of adipogenic transcription factors and other adipocyte-specific genes.

Key Words

Magnolia officinalis, 3T3-L1 cell, adipocytes differentiation, peroxisome proliferator activated receptor-γ, hormone sensitive lipase

안유진 You Jin Ahn , 원보령 Bo Ryoung Won , 강명규 Myung Kyu Kang , 김재현 Jai Hyun Kim , 박수남 Soo Nam Park

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Abstract

In this study, the antioxidative effects, inhibitory effects on tyrosinase, and component of non-fermented and fermented Lavandula angustifolia extracts were investigated. The ethyl acetate fraction of fermented extract (5.95 μg/mL) showed the most prominent the free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity (FSC₅₀). Reactive oxygen species (ROS) scavenging activities (OSC₅₀) of L. angustifolia extracts on ROS generated in Fe³⁺-EDTA/H₂O₂ system were investigated using the luminol-dependent chemiluminescence assay. The ethyl acetate fraction of fermented extract (1.45 μg/mL) showed the most prominent ROS scavenging activity. The protective effects of extract/fractions of L. angustifolia on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The L. angustifolia extracts suppressed photohemolysis in a concentration dependent manner (1 ∼ 50 μg/mL). The inhibitory effect of L. angustifolia extracts on tyrosinase was investigated to assess their whitening efficacy. Inhibitory effects (IC₅₀) on tyrosinase were determined with ethyl acetate fraction of L. angustifolia extract (144.80 μg/mL) and ethyl acetate fraction of fermented extract (122.40 μg/mL). Fractions of ethyl acetate and fermented extracts showed both 3 band in TLC and 3 peaks, 2 peaks in HPLC (340 nm), respectively. In each chromatography, fractions of ethyl acetate both from non-fermented and fermented L. angusfifolia have rosmarinic acid in common. These results indicate that the component and content of non-fermented and fermented extracts of L. angustifolia are different. Both of the extract of L. angustifolia can be used as an antioxidant.

Key Words

Lavandula angustifolia, antioxidative activity, fermented, rosmarinic acid, cosmetics

김무곤 Moo Kon Kim , 오한진 Hanjin Oh , 이지영 Ji Young Lee , 이정용 Jeong Yong Lee , 이기훈 Ki Hoon Lee

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Abstract

In this study, we hydrolyzed hot-water extracted sericin with single or two enzymes and investigated anti-oxidative effect on DPPH free radical and inhibitory effect on tyrosinase activity of the sericin hydrolysates. Alcalase, flavourzyme, and protamex were effective in hydrolyzing sericin. Sericin was degraded into the range of 20 ~ 30 kDa. The sericin hydrolysate was shown to have stronger antioxidant properties than the original sericin. In the case of flavourzyme and protamex combination, the scavenging effect of sericin hydrolysate on DPPH radical was increased up to about 85 %. However, the inhibitory effect on tyrosinase activity of enzymatic hydrolysates was lower than that of the original sericin. After fractionation of sericin hydrolysates, we found that F2 and P3 fraction has higher inhibitory effect on tyrosinase activity compared to other fractions.

Key Words

silk sericin, antioxidative effect, tyrosinase activity, enzymatic hydrolysis, flavourzyme

김미진 Mi Jin Kim , 임경란 Kyung Ran Im , 정택규 Kyung Sup Yoon , 윤경섭 Sang Won Choi , 최상원

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Abstract

Several hydroxycinnamic acid derivatives, p-coumaric acid, ferulic acid, N,N'-dicoumaroylputrescine (DCP), N-p-coumaroyl-N'-feruloyl-putrescine (CFP), and N,N'-diferuloylputrescine (DFP) were isolated and purified from corn bran. To develop the skin whitening agent, we investigated the effects of hydroxycinnamic acid derivatives from corn bran, on melanogenesis. CFP and DFP inhibited melanin synthesis in a dose dependent manner up to 44.7 ± 6.0 %, and 58.5 ± 3.1 % at a concentration of 50 μg/mL, respectively. The intracellular tyrosinase activity decreased about 42.5 ± 14.6 %, and 9.0 ± 4.4 % at a concentration of 50 μg/mL of CFP and DFP, respectively. Our results suggest that inhibitory effects of hydroxycinnamic acid derivatives on melanogenesis are due to the inhibition of the intracellular tyrosinase activity. These results indicate that these hydroxycinnamic acid derivatives from corn bran may be potential natural skin whitening agents.

Key Words

corn bran extract, hydroxycinnamic acid derivatives, N,N'-diferuloylputrescine (DFP), N-p-coumaroyl-N'-feruloylputrescine (CFP), melanin

추수진 Soo Jin Choo , 류인자 In Ja Ryoo , 김영희 Young Hee Kim , 허광화 Guang Hua Xu , 김기호 Ki Ho Kim , 한창성 Chang Sung Han , 김수진 Su Jin Kim , 김진웅 Jin Woong Kim , 손의동 Eui Dong Son , 유익동 Ick Dong Yoo

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Abstract

We found that silymarin exhibited the inhibitory effect on melanogenesis in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab. Silymarin is a standardized extract obtained from the dried seeds of milk thistle (Silybum marianum Gaertn.). Silymarin significantly prevented melanin production in a dose-dependent manner with an IC₅₀ value of 28.2 μg/mL without effects on cell viability. Also, silymarin inhibited tyrosinase activity in melanocyte, while it did not affect the catalytic activity of cell-free tyrosinase. Furthermore, Western blot analysis indicated that silymarin decreased the expression of tyrosinase protein. Silybin A/B and isosilybin A/B were also able to inhibit melanin production and tyrosinase expression in protein level. Double blind study on the clinical efficacy of a cream containing 2 % silymarin showed that silymarin have a significant skin whitening effect. Therefore, this study suggests that silymarin may be useful as a natural skin whitening agent.

Key Words

melanogenesis, silymarin, tyrosinase activity, silybin, skin whitening

김소이 So I Kim , 안유진 You Jin Ahn , 김은희 Eun Hee Kim , 박수남 Soo Nam Park

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Abstract

In this study, the antibacterial activity, antioxidative effects, inhibitory effects on tyrosinase, inhibitory effects on elastase, and components of Quercus acutissima Carruth leaf extracts were investigated. MIC values of ethyl acetate fraction from Q. acutissima Carruth leaf on P. acnes, S. aureus, P. ovale, and E. coli were 0.13 %, 0.25 %, 0.13 % and 0.25 %, respectively. The results showed that the antibacterial activity of the ethyl acetate fraction was the highest in the S. aureus, P. acnes, and P. ovale. The free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity (FSC₅₀) of extract/fractions of Q. acutissima Carruth. leaf was in the order: 50 % ethanol extract (12.13 μg/mL) < ethyl acetate fraction (7.07 μg/mL) < deglycosylated flavonoid aglycone fraction (6.20 μg/mL). Reactive oxygen species (ROS) scavenging activities (OSC₅₀) of some Q. acutissima Carruth leaf extracts on ROS generated in Fe³⁺-EDTA/H₂O₂ system were investigated using the luminol-dependent chemiluminescence assay. The order of ROS scavenging activity was 50 % ethanol extract (OSC50, 1.81 μg/mL) < ethyl acetate fraction (1.70 μg/mL) < deglycosylated flavonoid aglycone fraction (0.70 μg/mL). Deglycosylated flavonoid aglycone fraction showed the most prominent scavenging activity. The protective effects of extract/fractions of Q. acutissima Carruth leaf on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The Q. acutissima Carruth leaf extracts suppressed photohemolysis in a concentration dependent manner, particularly deglycosylated flavonoid aglycone fraction exhibited the most prominent celluar protective effect (τ50, 220.00 min at 25 μg/mL). Aglycone fractions obtained from the deglycosylation reaction of ethyl acetate fraction among the Q. acutissima Carruth leaf extracts, showed 3 bands (QA 1, QA2 and QA3) on TLC. TLC chromatogram of ethyl acetate fraction of Q. Carruth. leaf extract revealed 4 bands (QA 1 ~ QA 4), Among them, kaempferol (QA 1), quercetin (QA 2), and gallic acid (QA 3) were identified. The inhibitory effect (IC50) of aglycone fraction on tyrosinase was 65.7 μg/mL. The inhibitory effect (IC50) of aglycone fraction on elastase was 24.50 μg/mL. These results indicate that extract/fractions of Q. acutissima Carruth. can functionized as antioxidants in biological systems, particularly skin exposed to UV radiation by scavenging 1O2 and other ROS, and protect cellular membranes against ROS. Extract/fractions of Q. acutissima Corruth can be applicable to new functional cosmetics for antioxidant, antiaging, antibacterial activity.

Key Words

Quercus acutissima carruth, antibacterial activity, antioxidative activity, tyrosinase, cosmetics