• YAKHAK HOEJI
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• v.42 no.1
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• pp.39-45
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• 1998

Kojic acid, antimelanogenic agent, has been widely used in cosmetics to lighten the skin color. However, it has skin irritancy and instability against pH, temperature and light. To overcome these problems and optimize the molecular structure of kojic acid (KA), a prodrug, kojic acid monostearate(KMS), has been synthesized to modify the topical drug delivery in the point of sustained release of the parent drug via enzymatic hydrolysis during skin absorption. The prodrug was tested for enzymatic hydrolysis with cytosolic fraction of hairless mouse, skin. From the in vitro skin permeation study through hairless mouse skin, we found that KMS was retained in the skin and generated KA continuously by the skin esterase cleavage. In addition, topical formulations of o/w type creams and polyolprepolymer-containing cream were further tested for whitening effects using in vivo yellow skin guinea pig model.

• 한국생물공학회:학술대회논문집
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• 2001.11a
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• pp.791-795
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• 2001

This study was conducted to develop a new biomaterial to be used for skin whitening. The melanin elimination effect of chondroitin sulfate and phelinus linteus mushroom in rabbit back skin were evaluated. Rabbit dorsum was exposed to chronic UV irradiation(320nm) once daily for 30 days after initial melanin injection (100mg/kg). And then, chondroitin sulfate and phelinus linteus mushroom at dose of 0.7g for 30days were applied on the zone. The dorsal skin was histologically examined. Furthermore, we investigated free-radical extinction effect, antioxidation and tyrosinase activity inhibition effects. The histological study indicated that chondroitin sulfate and phelinus linteus mushroom decreasd melanine pigment significantly. As a result, chondroitin sulfate and phelinus linteus mushroom have a remarkable effect on the skin whitening by melanin elimination.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.25 no.1
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• pp.1-11
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• 2012

Objective : Paeoniae radix alba(PRA) can enrich the blood and regulate menstruation, astringe yin and arrest sweating, calm the liver and arrest pain. This study was designed to investigate effects of PRA on skin whitening and elasticity using melanoma cells. Methods : In this experiment, effect of PRA on cell viability, inhibition of melanin synthesis and inhibitory effect on tyrosinase and elastase. Results : 1. More than $1,000\;{\mu}g/ml$ of PRA treated group showed lowered proliferation rates significantly compared to non-treated control group. 2. All of treated groups were lower levels of melanin synthesis respectively. 3. PRA did not show inhibitory effect on tyrosinase activities in vitro. But, PRA suppressed tyrosinase activities in B16F10 cells significantly. 4. PRA suppressed elastse type 1 activities in dose-dependent manner in vitro. But, PRA slightly suppressed elastase type 4 activities in vitro, and PRA also slightly suppressed elastase activities in vivo. Conclusion : These results suggest that PRA can inhibit melanin synthesis through ihhibitory action on tyrosinase activity and inhibt elastase activity, and also suggest that these results can be used for the study on maintaining skin whitening or elasticity.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2007.11a
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• pp.129-139
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• 2007

Many modalities of treatment for acquired skin hyperpigmentation are available including chemical agents or physical therapies, but none are completely satisfactory. The ideal depigmenting compound should have a potent. rapid and selective bleaching effect on hyperactivated melanocytes, carry no short- or long-term side-effects and lead to a permanent removal of undesired pigment. acting at one or more steps of the pigmentation process. Depigmentation can be achieved by regulating (i) the transcription and activity of tyrosinase, tyrosinase related protein-1 (TRP-1), tyrosinase related protein-2 (TRP-2), and/or peroxidase; (ii) the uptake and distribution of melanosomes in recipient keratinocytes and (iii) melanin and melanosome degradation and turnover of pigmented keratinocytes. One of the interesting point for development of skin whitening agent is Mitf(Microphthalmia-associated transcription factor). Mitf belongs to the basic helix-loop-helix-zip family of trabscription factors and it is crucial as it regulates both melanocyte proliferation as well as melanogenesis and is the major regulator of tyrosinase and the related enzymes (TRPs), as well as many melanosome structural proteins such as pMel17. Recently, we developed MITF-down-regulating agents from natural and synthetic sources, which have anti-melanogenic effect on in vitro and in vivo. We suggested that potent MITF-down regulating agents might be used for skin whitening cosmeceuticals.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.23 no.1
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• pp.23-43
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• 2010

Objective : This study was performed to assess the effects of Aloe and Violae herba extracts on skin disease and skin beauty. Methods : Anti-oxidant effects were measured by the scavenging for DPPH radical, xanthine oxidase activity. Anti-inflammatory effects were examined by relations in NO synthesis, IL-$1{\beta}$, IL-6, TNF-$\alpha$, NF-kB, COX-2, MAP kinase. The skin wrinkle formation effects were measured by collagenase and elastase activities. The whitening effects were examined by tyrosinase activities, melanin synthesis in MNT-1 cell. Results : 1. In an anti-oxidant test, Aloe and Violae herba extracts showed high radical scavenging activity. 2. In an anti-inflammatory test, Aloe and Violae herba extracts strongly inhibited the lipopolysaccharide(LPS)-induced nitric oxide(NO) release from the RAW 246.7 macrophage cells. Aloe and Violae herba extracts also inhibited the LPS-induced IL-$1{\beta}$ and COX-2 expressions. The inhibitory effects of Aloe and Violae herba extracts on macrophage activation were via the inhibition of NF-kB, evidenced by transient transfection assay. Furthermore, Aloe and Violae herba extracts weakly inhibited the activation of Jun-N-terminal kinase(JNK) but they did not have any effects on p38 MAP kinase in RAW 264.7 cells. 3. In the skin wrinkle formation assay, Aloe extract strongly inhibited collagenase and elastase, whose activity are tightly related with the wrinkle formation. 4. In the skin whitening assay, Aloe and Viloae herba extracts weakly inhibited tyrosinase activity, however, it was not statistically significant. Besides they did not have any effects on melanin synthesis, indicating that they could not be applicable for skin whitening. Conclusion : This study show that Aloe and Violae herba extracts may play a significant role in skin disease and skin beauty.

• Korean Journal of Medicinal Crop Science
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• v.21 no.1
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• pp.54-60
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• 2013

According to previous reports, antioxidant activities of Codonopsis lanceolata could be increased by a steaming process. This study was performed to improve its antioxidant activity and skin whitening activities of C. lanceolata by high pressure and stepwise steaming complex process. The complex processed C. lanceolata showed highest free radical scavenging acitivity as 45.21%, and for phenol and flavonoid contents, complex processed C. lanceolata contained higher than those from conventional extraction process or steaming process alone. The Cytotoxicity of all C. lanceolata extracts also showed low cytotoxicity against human fibroblast cell (CCD-986sk) as 4.49 ~ 10.40%. In whitening activity, high inhibition of tyrosinase activity was estimated as 25.08% by adding the extracts from complex process. We found that whitening and antioxidant activity of complex processed C. lancolata extract was higher than those obtained from conventional extraction and a steaming process because various kinds of antioxidant compounds could be easily released by combined process, compared to one of each process.

• Herbal Formula Science
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• v.21 no.1
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• pp.91-98
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• 2013

Objective : The purpose of this study was to investigate the synergistic effect of Angelicae gigantis Radix (AG) and Lycii fructus (LF) ethanol extracts on skin-whitening effects. Method : LFAG extracts were prepared by extracting with 80% ethanol. The efficacy of LFAG was judged by measurement of cell viability, tyrosinase activity, melanin production, tyrosinase and microphthalmia-associated transcription factor (MITF) expression in B16F10 murine melanoma cells by lipopolysaccharides (LPS) treatment. Results : Each extract (LF or AG) inhibited the tyrosinase activity in a dose-dependent manner. The co-treatment of LFAG extracts ($25{\mu}g/mL$ LF plus $25{\mu}g/mL$ AG) markedly suppressed the LPS-induced cellular tyrosine activity, melanin production, tyrosinase and MMP-1 expression in B16F10 murine melanoma cells. These suppressive effects were synergistically increased by their combination. Conclusions : With these observations, we suggest that the extracts from Lycii fructus and Angelica gigantis Radix could be potent natural materials for whitening skin.

• Biomolecules & Therapeutics
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• v.29 no.1
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• pp.98-103
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• 2021

The demand for natural substances with anti-melanogenic activity is increasing due to the recent interest in skin whitening. Intensive investigation on the culture broth of Streptomyces sp. SCO-736, a marine bacterium from the Antarctica coast, has led to the isolation of a new natural product named antaroide (1). The chemical structure was established through the interpretation of MS, UV, and NMR spectroscopic data. Antaroide is a nine-membered macrolide with lactone and lactam moieties. To investigate its applicability in skin whitening cosmetics, its anti-melanogenic activity in B16F10 murine melanoma cells was examined. As a result, antaroide displayed strong inhibitory activities against melanin synthesis and also attenuated the dendrite formation induced by the α-melanocyte stimulating hormone (α-MSH). Antaroide suppressed the mRNA expression of the melanogenic enzymes such as tyrosinase, TRP-1 and TRP-2. This suggests that it may serve as a transcriptional regulator of melanogenesis. Collectively, the discovery of this novel natural nine-membered macrolide and its anti-melanogenic activity could give new insights for the development of skin whitening agents.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.37 no.1
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• pp.91-96
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• 2011

Deficiency of collagen regeneration, denaturalization of fibers, increased melanin synthesis and reactive oxygen species are important factors inducing deterioration of healthy skin function. They induce freckles and decrease in skin elasticity. Vitamin C, vitamin A and their derivatives have been used as cosmetic ingredients for improvement of these problems but they have various problems. We have been developing the various derivatives of these ingredients. In this study, we investigated whitening effect of 3-o-cetyl-L-ascorbic acid (VCCE), a new vitamin C derivative. The VCCE inhibited melanogenesis in a dose dependent manner(44 % at $20\;{\mu}g/mL $) and tyrosinase expression. For 8 weeks, we also investigated skin brightening effect of VCCE on pigmented spots in UV-irradiated human skin. In results, VCCE showed a statistically significant skin whitening effect by mechanical and visual evaluation. Taken together, our findings suggest that the VCCE has potential benefits as an active ingredient for whitening cosmetics.

• Journal of Acupuncture Research
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• v.32 no.3
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• pp.117-126
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• 2015

Objectives : This study was an analysis of the anti-inflammatory, anti-oxidative and skin whitening properties of Gamioncheong-decoctione(GMOCD) extract. Methods : GMOCD(96 g) and 2 L of distilled water were heated at $100^{\circ}C$ for four hours and then concentrated, frozen, freeze-dried, dissolved in distilled water and filtered. The following analysis was completed: cell cytotoxic effect using MTT assay, oxidative products of NO by griess assay, concentration of prostaglandin $E_2(PGE_2)$ by commercially competitive enzyme immunoassay, and cytokines($IL-1{\beta}$, IL-6 and TNF-${\alpha}$) by Bio-Plex$^{(R)}$ Suspension Array System's Bio-Plex Pro$^{TM}$ mouse cytokine, chemokine, and growth factor assay. Anti-oxidative effect was measured using the DPPH method and skin whitening effect using tyrosinase inhibition assay. Results : GMOCD water-extract did not show any toxicity at all doses and cell viability was more than 90 % at all doses. GMOCD water-extract significantly inhibited NO production at doses of 100, 200, $400{\mu}g/ml$, significantly inhibited $PGE_2$ production at doses of 200 and $400{\mu}g/ml$ and reduced the LPS-induced IL-$1{\beta}$, IL-6 and TNF-${\alpha}$ production in a dose-dependent manner. $IL-1{\beta}$ production was significantly reduced at a dose of $400{\mu}g/ml$ and IL-6 production was significantly reduced at doses of 200 and $400{\mu}g/ml$. DPPH free radical scavenging capability had a skin whitening effect rate of more than 50%. Tyrosinase inhibition activity was apparent in a dose-dependent manner. Conclusions : This study suggests that GMOCD water-extract suppressed NO and $PGE_2$ production and inhibited cytokines($IL-1{\beta}$, IL-6 and TNF-${\alpha}$). GMOCD also improved DPPH free radical scavenging capability. GMOCD water-extract increased tyrosinase inhibitory activity in a dose-dependent manner but this was not a statistically significant result.