• 대한화장품학회지
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• 제39권4호
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• pp.329-335
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• 2013

본 연구에서는 기질 화합물로써 일련의 4-hydroxybenzyl alchol (4-HBA) 유도체들의 치환기($R_1$ 및 $R_2$) 변화에 따른 tyrosinase 활성저해에 관한 3차원적인 구조-활성 상관관계(3D-QSARs) 모델을 유도하고 정량적으로 검토하였다. 그 결과, 입체장(S), 정전기장(E), 소수성장(Hy), 수소결합 받게장(HA) 및 수소결합 주게장(HD)의 조합조건에서 통계적으로 양호한 CoMSIA FF 모델(상관성; $r^2$ = 0.858 및 예측성; $q^2$ = 0.951)을 유도하였다. 등고도 분석결과에 의하면 기질분자의 $R_2$-치환기는 입체적으로 작고 음전하를 띄며, 소수성이면서 수소결합 주게장을 선호하지 않는 치환기가 올수록 tyrosinase 활성저해 작용이 용이하다. 그리고 $R_1$-치환기는 수소결합 주게장을 선호하는 치환기 이어서 $R_1$-치환체가 용이하게 탈 양성자화가 일어나야 tyrosinase 활성저해 작용을 용이하게 할 것이라고 예상되며, 이를 위해서는 $R_1$-치환기가 비 치환체(H)이어야 될 것으로 예상되었다.

• 대한화장품학회지
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• 제22권2호
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• pp.193-200
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• 1996

In eastern Asian region, cosmetic preparations containing the molecues possessing the whitening activity are promising. In this study, 100 plant extracts were screened in order to elucidate the whitening effects using in vitro tyrosinase assay and DOPA autooxidation. Several plant extracts such as Morus alba, Glycyrrhiza glabra showed the inhibitory activity (>50%) against mushroom tyrosinase at the concentration 333$mu extrm{m}$/ml. And plant extracts including Morus alba and Bupleurum falcatum showed the inhibitory activity (>50%) at the concentration of 500($\mu\textrm{g}$/ml against DOPA autooxidation. The IC50 values of the several extracts were also found.

• 동의생리병리학회지
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• 제22권3호
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• pp.672-677
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• 2008

In order to explore the anti-oxidization effect of oriental medicine and cereal medium(OCM) where Tricholoma matsutake mycelia were cultured, measurement of hot water extract and UMPM(extraction method using ultra sonic waves, micro waves, micro bubble) extract, the total polyphenol content of crude polysaccharide from each extract, SOD-like activity, electron donating ability(EDA), xanthine oxidase inhibitory activity, and tyrosinase inhibitory activity was conducted. The total polyphenol content of each extract was found to be 16.36% for hot water extract(HE) group and 15.73% for UMPM extract(UE) group and the amount of crude polysaccharide precipitated into ethanol of extracts was found to be 8.79% for UMPM ethanol extract(UEE) group and 6.48% for hot water ethanol extract(HEE) group. As a result of measurement of SOD-like activity by concentration of each extract, it was found to be 96.17% for UE group, 91.23% for HE group, 91.33% for UEE group, and 87.11% for HEE group at 20 mg/mL. In the case of EDA, it was found to be 47.55% for UE group, 44.93% for HE group, 25.38% for UEE group, and 18.36% for HEE group. And in the cases of the rates of xanthine oxidase inhibitory activity and tyrosinase inhibitory activity, as the concentration of each extract increased, the inhibition rate increased accordingly. As a result of comparison between hot water extract method and UMPM extract method using extracts obtained from oriental medicine compound medium where Tricholoma matsutake mycelia were cultured, all of the extracts were judged to have a high anti-oxidization effect. In particular, UMPM extracts were found to have higher polyphenol content, SOD-like activity, EDA, xanthine oxidase inhibitory activity and tyrosinase inhibitory activity compared to hot water extract method. In this regard, extracts obtained from OCM where Tricholoma matsutake mycelia were cultured are considered to have high availability as functional material when and if they are prepared using UMPM extract method.

• Bulletin of the Korean Chemical Society
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• 제32권4호
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• pp.1241-1248
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• 2011

Three dimensional quantitative structure-activity relationships (3D-QSARs) between new thiosemicarbazone analogues (1-31) as a substrate molecule and their inhibitory activity against tyrosinase as a receptor were performed and discussed quantitatively using CoMFA (comparative molecular field analysis) and CoMSIA (comparative molecular similarity indices analysis) methods. According to the optimized CoMSIA 2 model obtained from the above procedure, inhibitory activities were mainly dependent upon H-bond acceptor favored field (36.5%) of substrate molecules. The optimized CoMSIA 2 model, with the sensitivity of the perturbation and the prediction, produced by a progressive scrambling analysis was not dependent on chance correlation. From molecular docking studies, it is supposed that the inhibitory activation of the substrate molecules against tyrosinase (PDB code: 1WX2) would not take place via uncompetitive inhibition forming a chelate between copper atoms in the active site of tyrosinase and thiosemicarbazone moieties of the substrate molecules, but via competitive inhibition based on H-bonding.

• 한방안이비인후피부과학회지
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• 제23권1호
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• pp.135-148
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• 2010

Recently, the demands for the effective and safe depigmentating and anti-aging agents of the skin have increased due to the medical, pharmaceutical and cosmetic reasons. The aim of this study is to search Galla Rhois (GR) inhibitory activity against aging process of skin in vitro. GR was screened for their inhibitory activity against elastase. GR (final concentration 1 mg/ml) appeared over 40% of inhibition of elastase activity. So we investigated anti wrinkle effects of GR look through MMP-1 inhibition activity. Also Extracts of GR showed higher anti-tyrosinase activity than arbutin (final concentration 1 mg/ml). These results suggest that GR could be potential sources of anti-aging and whitening effects for the skin. Objective : Galla Rhois extracts, Elastase (pancreatic from porcine pancreas), N-Succinyl-(Ala)3-p-nitroanilide, Ursolic acid, mushroom tyrosinase, L-tyrosine, arbutin, Amicon Ultra, Hand Hold UV lamp, MMP-1 primary antibody, MMP-1 secondary antibody Result : 1. GR appeared over 40% of elastase inhibitory activity. 2. GR had MMP-1 inhibition activity. 3. GR showed higher anti-tyrosinase activity than arbutin. Conclusion : According to above results, it is supposed that Galla Rhois could be strong potential sources of anti-aging and whitening effects for the skin.

• 한국약용작물학회지
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• 제25권1호
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• pp.10-15
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• 2017

Background: We investigated the antioxidative and tyrosinase inhibitory activities of 70% ethanol extract, and its fractions, of the root of Rumex japonicus HOUTT. Methods and Results: The total phenolic compound contents of the 70% ethanol extract and ethyl acetate fraction were 168.99 mg/g and 651.78 mg/g, respectively. The antioxidant activity was compared through the DPPH radical and nitric oxide (NO) scavenging assays. The ethyl acetate fraction showed the highest DPPH radical and NO scavenging abilities, which confirmed the antioxidant activity. Specifically, the ethyl acetate fraction showed a higher DPPH radical scavenging ability than ascorbic acid. These results were related to the total phenolic compound content of the ethyl acetate fraction. Moreover, in the tyrosinase inhibition assay, the ethyl acetate fraction exhibited stronger inhibitory activity than arbutin, which was used as the positive control. The cell viability of L929 cells was analyzed by MTT assay after treatment with 70% ethanol extract and all fractions; no changes in viability were observed, which demonstrated the nontoxic nature of the extract and fractions. Conclusions: These results suggested that the extract from the root of R. japonicus and its ethyl acetate fraction could be a novel resource for the development of a cosmetic with antioxidant and tyrosinase inhibitory activity.

• KSBB Journal
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• 제23권2호
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• pp.125-130
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• 2008

해수클로렐라 (Chlorella elliposidea C020) 에탄올 추출물로부터 항균 및 항곰팡이 활성, 항산화활성, tyrosinase inhibitory 활성 (미백효과)과 용혈활성을 실험하였다. 효율적인 추출을 위해서 동결건조 후 95% 에탄올로 2시간 추출하는 것이 가장 좋다는 것을 알 수 있었다. 해수클로렐라 에탄올 추출물의 항균 및 항곰팡이에 대한 활성을 측정한 결과, B. subtilis PM125와 B. licheniformis, V. parahemolyticus와 E. tarda NUF251에서 활성을 나타내었다. 그러나, 곰팡이인 C. albicanse에 대하여서는 활성을 나타내지 않았으며, 인간의 적혈구로 용혈활성 실험한 결과, 아주 낮은 활성을 나타내었다. DPPH방법을 이용하여 항산화 능력을 측정한 결과, 2 mg/mL에서 75% 라디칼 소거능력을 나타내었다. 해수클로렐라 에탄올 추출물의 tyrosinase 저해활성 $IC_{50}$는 10.87 mg/mL로 나타났다. 이러한 결과를 바탕으로 해수클로렐라 에탄올 추출물로부터 다양한 생리활성물질을 개발하여 고부가가치 제품을 창출할 수 있을 것으로 판단된다.

• 한국식품영양과학회지
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• 제42권9호
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• pp.1357-1362
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• 2013

형개(Schizonepeta tenuifolia) 2 g을 70, 90, $110^{\circ}C$에서 30분간 원적외선 처리 후 물 100 mL와 함께 $60^{\circ}C$에서 1, 3, 5시간 추출하였다. 원적외선을 고온에서 처리함에 따라 추출물의 항산화 활성 및 tyrosinase 저해능이 증가하였다. 시료에 원적외선을 처리하였을 때 무처리구에 비해서 항산화능 및 tyrosinase 저해능이 증가하였으며, 특히 고온에서 원적외선을 처리할수록 좋은 활성을 보였다. 총 페놀 함량, DPPH 라디칼 소거능, ABTS 라디칼 소거능, tyrosinase 저해능이 $110^{\circ}C$에서 원적외선을 처리하였을 때 각각 약 2.5, 2.6, 2.3, 4.4배 증가하였고, 추출시간이 항산화 활성과 tyrosinase 저해능에 미치는 영향은 크지 않았다. 이러한 형개 추출물의 생리적 활성은 페놀성 화합물에 근거한 것으로 생각되며 형개를 건강기능식품이나 미백화장품의 소재로서 적용하고자 할 때 원적외선 처리는 매우 긍정적인 영향을 미칠 것으로 여겨진다.

• Preventive Nutrition and Food Science
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• 제7권4호
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• pp.447-450
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• 2002

Previously, a methanol extract from seeds of Paeonia lactiflora was shown to have a potent inhibitory activities against tyrosinase and soybean lipoxygenase (SLO). Seven stilbenes, trans-resveratrol-4-Ο-$\beta$-D-glucoside, trans resveratrol, trans-$\varepsilon$-viniferin, cis-$\varepsilon$-viniferin, gnetin H, suffruticosol A and B were isolated from the seeds as active principles for inhibition of the enzymatic activity. Among them, the resveratrol trimer, gnetin H exhibited the most potent inhibitory activities against tyrosinase and SLO, respectively. Additionally, the resveratrol dimers, trans-$\varepsilon$-viniferin and cis-$\varepsilon$-viniferin exhibited significant inhibitory activity against the two oxidative enzymes. Meanwhile, three other stilbene derivatives, such as trans-resveratrol, suffruticosol A and suffruticosol B had also weak inhibition activity. The least inhibitory activity was observed in transresveratrol-4-Ο-$\beta$-D-glucoside. These results suggest that resveratrol dimers and trimer in the seeds of Paeonia lactiflora are potentially useful therapeutic agents against pathological disorders such as hyperpigmentation and inflammation.

• 생약학회지
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• 제44권3호
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• pp.220-223
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• 2013

In the course of screening tyrosinase inhibitory activity, total methanolic extract and EtOAc-soluble fraction of Smilax china leaves showed significant inhibitory activity. Further fractionation and isolation of the EtOAc-soluble fraction resulted in 12 phenolic compounds, which were identified as 4-hydroxybenzoic acid (1), 3,4-dihydroxybenzaldehyde (2), 3,4-dihydroxybenzoic acid (3), 3,4-dihydroxyacetophenone (4), 3-hydroxy-4-methoxy benzoic acid (5), trans-p-hydroxycinnamic acid (6), cis-p-hydroxycinnamic acid (7), trans-resveratrol (8), cis-resveratrol (9), dihydroresveratrol (10), moracin M (11) and kaempferol (12). Compounds 1-11 were first reported from this plant. Among the isolated compounds, compounds 2, 8, 9 and 12 showed strong inhibition on tyrosinase activity.