• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.32 no.3 s.58
• /
• pp.153-160
• /
• 2006

We synthesized 2',4'-dimethoxyflavone and investigated the effects on melanogenesis. To determine the effects as a whitening agent, various in uitro tests were performed such as free radical scavenging activity, melanin assay, tyrosinase activity and expression of tyrosinase, TRP-1 and TRP-2 (western blot and RT-PCR) in Bl6 melanoma cells. 2',4'-Dimethoxyflavone showed neither free radical scavenging activities against 1,1- diphenyl -2-picrylhydrazvl (DPPH) radical and inhibition of mushroom tyrosinase activity, 2',4'-dimethoxyflavone significantly inhibited melanin production in B16 melanoma cells. 2',4'-Dimethoxyflavone treatment (48h) suppressed the biosynthesis of melanin up to 27% at $5{\mu}g/mL$ and reduced tyrosinase activity up to 20% at $5{\mu}g/mL$ in B16 melanoma cells. 2',4'-Dimethoxyflavone was also able to significantly inhibit tyrosinase and TRP-1 expression in protein and mRNA level. These results suggest that 2',4'-dimethoxyflavone inhibits melanin biosynthesis at the level of enzyme activity and protein mRNA expression B16 melanoma cells. Therefore, 2',4'-dimethoxyflavone may be useful as a new whitening agent in cosmetics.

• Journal of Applied Biological Chemistry
• /
• v.58 no.3
• /
• pp.266-271
• /
• 2015

Recently many effort focused to understand the mechanical insights of melanogenesis to develop the agent for hyper-pigmentation. So this study was performed to investigate the depigmentation of Vitex rotundifolia. With B16F10 mouse melanoma cell, we have seen inhibition of the tyrosinase, MITF, TRP-1, TRP-2, and melanin synthesis, which eventually were dose dependently decreased by Vitex rotundifolia. Specially, Vitex rotundifolia decreased the protein levels of tyrosinase and TRP-1. In conclusion, Vitex rotundifolia showed the whitening activity in all the experiments mentioned above and we expect that it can be used for preventing melanin synthesis.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.37 no.3
• /
• pp.275-282
• /
• 2011

Novel whitening agents were prepared using peptide-Natural origin compound derivatives. The peptide could be an antagonist of MC1R and Natural origin compound were well-known material as a Tyrosinase inhibitor. We also suggest the new assay method which could evaluate the Antagonistic effectiveness to MC1R using cAMP signaling pathway. 24 candidates were synthesized and 11 peptide derivatives were selected by cAMP assay method. To evaluate cAMP assay, the selected peptide derivatives were assayed to evaluate their melanogensis inhibitory activity. At this work, we could know that the sequences which include -RW- have a melanogensis inhibitory activity, and cAMP assy could use as a evaluating method of MC1R antagonist. But, to evaluate the whitening activity of some material, cross-checking with melanin inhibitory assay method was recommended.

• Korean Journal of Plant Resources
• /
• v.29 no.2
• /
• pp.155-162
• /
• 2016

Melanin is produced by melanocytes of the melanoepidermic unit and other cell types. These cells secrete and distribute the melanin pigment, which provides protection from ultraviolet radiation. In this study, the inhibitory activity against tyrosinase and melanin biosynthesis in B16F10 melanoma cells and anti-wrinkling effects on human dermal fibroblasts of Dendrobium speciosum ethanol extract were investigated. The Dendrobium speciosum extract inhibited melanin biosynthesis and tyrosinase activity in a dose-dependent manner in comparison with an untreated control group. Treatment with the Dendrobium speciosum extract suppressed α-MSH-stimulated melanogenesis in B16F10 cells and the dendrite outgrowth of melanocyte/melanoma cells. The α-MSH-induced mRNA expression of tyrosinase-related protein-1 (TRP-1), tyrosinase-related protein-2 (TRP-2) and microphthalmia-associated transcription factor (MITF) was significantly attenuated in a concentration-dependent manner by Dendrobium speciosum treatment. In addition, Dendrobium speciosum treatment increased production of type I procollagen synthesis in human dermal fibroblasts. Dendrobium speciosum ethanol extract exhibited a potent inhibitory effect on melanin biosynthesis, tyrosinase activity and increased procollagen synthesis. These results indicate that Dendrobium speciosum shows promise as an ingredient in cosmeceutical products due to its whitening and anti-wrinkle effects.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.48 no.3
• /
• pp.287-293
• /
• 2022

Gray hair is a representative sign of aging. Intrinsic aging, stress, and the external environment cause hair graying. Stress is known to be a major factor in the early onset of hair graying. We previously found that Pueraia lobata root extract (PLRE) can prevent hair graying by promoting melanin formation. However, it remains unknown whether PLRE can prevent hair graying induced by conditions of stress. In this study, we confirmed the effect of PLRE on stress-induced hair graying. A reporter cell line was newly constructed to confirm the expression of microphthalamia-associated transcription factor (MITF), the main transcription factor for melanin production. MITF expression and melanin pigmentation were reduced in human hair follicle tissue treated with the stress hormone cortisol or H₂O₂ to induce oxidative stress. PLRE treatment restored MITF expression and increased the amount of melanin pigment in the hair follicle. The expression of Tyrosinase related proteins-2 (TRP-2), a melanin synthesis enzyme in the hair follicle, also increased. In conclusion, PLRE can effectively prevent the inhibition of melanin synthesis by stress hormones and oxidative stress.

• Journal of Haehwa Medicine
• /
• v.21 no.1
• /
• pp.125-133
• /
• 2012

본 논문은 피부미백에 관한 실험적 연구로서, 봉선화(Impatiens balsamina Linne)의 성분 중에서 하이드록시-나프타-퀴논(hydroxynaphthoquinone)이 멜라닌 생성억제 효능, 색소침착 저해 효과 등의 미백 활성이 있는 것으로 밝혀졌다. 피부흑화(melanogenesis)는 멜라닌 색소생성세포(melanocyte)에서 자외선 등의 자극에 대한 방어기작으로 멜라닌 생성 활동이 증가되고 이로 말미암아 만들어진 다량의 멜라닌이 각질형성세포(keratinocyte)로 전이되어 피부 표피층에 축척된 결과이다. 비록 멜라닌이 피부에 보호작용을 하나 피부의 과색소 침착은 기미, 주근깨, 피부염증 후의 피부흑화, 노인성 색소반점 등을 일으키며 이로 인해 피부미용 상의 불편뿐만 아니라 정신적으로 부정적인 영향을 미쳐 사회활동에 불편을 초래하기도 한다. 멜라닌 생성 과정은 아미노산의 일종인 티로신(tyrosine)에 티로시나제(tyrosinase)라는 효소가 작용하여 도파(DOPA), 도파퀴논(dopaquinone)으로 바뀐 후 비효소적인 산화 반응을 거쳐 만들어 지며, 이것이 피부 내에 이상 침착하여 기미, 검버섯 등이 생기는 것이라고 알려져 있다. 이와 같은 색소침착, 기미, 반점 등의 완화, 예방 및 치료에는 멜라닌 생성을 억제하는 물질, 예를 들면 하이드로퀴논(hydroquinone), 알부틴, 비타민 C 및 그 유도체 등이 개발되어 사용되고 있으나 이 중, 하이드로퀴논은 일단 효과가 인정되고 있지만 감작성이 있기 때문에 일반적으로 사용이 제한되고 있다. 아스콜빈산은 쉽게 산화되어, 이를 배합한 제품에는 변색, 변취가 되는 문제를 야기하고, 식물추출물 유래의 물질들은 식물의 산지에 따라 효능의 차이가 심하여 제품의 균질성이 유지되기 어렵다. 이러한 이유로 많은 멜라닌 생성을 억제하는 물질을 개발하기 위한 연구들이 계속 진행하고 있다. 2-히드록시-[1,4]나프토퀴논 유도체는 다음과 같은 구조를 나타낸다. 상기 구조에서 R은 포화 혹은 불포화된 직쇄 또는 분지쇄의 알킬로서, 바람직하게는 C1 내지 C10의 포화 혹은 불포화된 직쇄 또는 분지쇄의 알킬이고, 보다 바람직하게는 C1 내지 C5의 포화 혹은 불포화된 직쇄 또는 분지쇄의 알킬이다. 실험에 활용된 화합물은 다음과 같은 반응식으로 얻어졌다. 2-히드록시-[1,4]나프토퀴논과 포타슘카보네이트(K2CO3)를 아세토니트릴에 용해한 후, 저온수조로 냉각하고 알킬할라이드를 적당한 당량비로 천천히 적하하여 히드록시기와 에테르(ether) 반응을 통하여 얻어질 수 있다. 상기 반응식에서 R은 C1~10의 포화 또는 불포화된 알킬기로서 직쇄형 또는 분지쇄형 모두 가능하다. 상기 화합물인 2-히드록시-[1,4]나프토퀴논(2-hydroxynaphthoquinone)은 배양된 쥐의 멜라노마 세포에 대하여 하이드로퀴논과 대등한 멜라닌 생성 억제효과를 보였다. 하이드로퀴논은 저농도에서 강력한 멜라닌 생성 억제효과를 보이지만 상기 화합물들은 보다 낮은 농도에서도 세포독성을 나타내지 않으며 하이드로퀴논보다 높은 멜라닌 생성 억제 효과를 보였다.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.33 no.3
• /
• pp.203-208
• /
• 2007

To develop a new whitening agent for cosmetics from natural products, Pimpinella brachcarpa was selected for its inhibitory effect on melanogenesis in B16 melanoma cells. Crude ethanolic extract of P. brachycarpa and its four fractions-hexane, ethyl acetate(EtOAc), butanol and aqueous were evaluated for antioxidative effects and tyrosinase inhibitory activity. To elucidate the mechanism of active compounds of P. brachycarpa, we investigated the changes in protein level of tyrosinase, TRP-1 and TRP-2 using Western blotting and the changes in mRNA level of tyrosinase using RT-PCR technique. Following UV irradiation, expression of ET-1 in HaCaT keratinocytes was measured by quantitative enzyme immunoassay(EIA) using human ET-1 antibody. Crude ethanolic extract of P. brachycarpa and its four fractions-hexane, EtOAc, butanol and aqueous had free radical scavenging effect by 87.2, 2.5, 97.2, 80.5, 49.8% at 100 ${\mu}g/mL$ and tyrosinase inhibitory effect by 18.3, 15.1, 55.4, 13.1, 0 % at 100 ${\mu}g/mL$. P. brachycarpa EtOAc fraction significantly inhibited melanin production in B16 melanoma cells. Treatment with P. brachycarpa extract for 72 h suppressed the biosynthesis of melanin up to 58 % at 100 ${\mu}g/mL$. Especially, the EtOAc fraction of P. brachycarpa reduced the tyrosinase activity and tyrosinase expression in B16 melanoma cells in a dose-dependent manner. mRNA levels of tyrosinase and TRP-1 were markedly reduced by the EtOAc fraction of P. brachycarpa. Moreover, at the concentrations of $12.5{\sim}50{\mu}g/mL$ of the fraction, the production of UV-induced ET-1 in HaCaT keratinocytes(24 h after 8 $mJ/cm^2$ UVB irradiation) was reduced about 40%(p<0.05). P. brachycarpa could be used as a new natural skin-whitening agent due to the inhibitory effect of on melanin biosynthesis and endothelin-1 expression.

• Korean Journal of Food Science and Technology
• /
• v.32 no.2
• /
• pp.454-460
• /
• 2000

It is difficult to accurately evaluate the effect of lipophilic compounds in aqueous reaction system of enzymes because they are immiscible with water. To screen lipophilic inhibitors of tyrosinase which catalyzes the synthesis of melanin in vivo, an optically clear organic system composed of organic solvent, surfactant, and water, often called reverse micelles(RM), was introduced. Optimal RM to let tyrosinase act normally was composed of isooctane as an organic solvent and dioctyl sulfosuccinate(AOT) of 100 mM as a surfactant. When a molar ratio of water to surfactant was 15, tyrosinase(105.3 units) in RM showed a similar reactivity toward 3,4-dihydroxyphenylalanine(0.18 mM) as in the aqueous assay system. In the presence of cinnamic acid, the product formation of tyrosinase reaction was proportional to the reaction time. This indicates that the inhibitory effect of lipophilic compounds could be analyzed in RM.

• Korean Journal of Plant Resources
• /
• v.22 no.4
• /
• pp.317-322
• /
• 2009

In the present study, the effect of ethanol extracts of leaf and root of Rosa multiflora on the proliferation of B16 cells, tyrosinase activity and melanin synthesis were investigated. 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide(MTT) assay demonstrated that the cell viability upon treatment with Rosa multiflora extract(0-200 ${\mu}g$/ml) was similar to that of untreated control. Treatment with leaf or root extracts(200 ${\mu}g$/ml) decreased the in vitro tyrosinase activity to about 65% of that in untreated control. Similarly, the intracellular tyrosinase activity of B16 cells decreased in a concentration-dependent manner. Furthermore, the melanin synthesis of B16 cells decreased by the two extracts in a concentration dependent manner. However, the extracts did not change the level of tyrosinase mRNA, as determined by RT-PCR. These results demonstrated that the Rosa multiflora extracts inhibit the tyrosinase dependent melanin biosynthesis, and therefore, are candidates for skin-whitening agents.

• 한국생물공학회:학술대회논문집
• /
• 2005.04a
• /
• pp.541-543
• /
• 2005

Recently many efforts have been made to develop new therapeutic agents against skin pigmentation abnormalities. The aim of this study is to investigate the skin-whitening effect of Gleditsia Sinensis Lam and to develop new drug delivery carrier. Inhibitory effaces of Gleditsia Sinensis Lam extracts on melanin synthesis were studied. Namely, UV-absorbing ability, free radical scavenging activity and tyrosinase inhibitory of Gleditsia Sinensis Lam extracts were investigated As a result, the extracts of Gleditsia Sinensis Lam were found to inhibit the activity of tyrosinase. Moreover they absorbed wavelength in the UV-B and UV-C region, and extracts of Gleditsia Sinensis Lam had free radical scavenging activity. In this study, in order to administer these ingredient effectively, the shape of liposome observed by TEM was spherical and uniform.