• Korean Journal of Pharmacognosy
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• v.45 no.3
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• pp.209-213
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• 2014

The anti-melanogenic substance was isolated from the root of Angelica gigas Nakai by silica gel column chromatography, preparative HPLC and TLC. As a result of the structure analysis by mass, $^1H$-NMR, and $^{13}C$-NMR spectrometry, the compound was identified as demethylsuberosin. Demethylsuberosin reduced melanin contents of B16F1 melanoma cells in a dose-dependent manner and decreased to about 74% at a concentration $5{\mu}g/ml$. Demethylsuberosin inhibited the expression in microphthalmia associated transcription factor (MITF), tyrosinase, tyrosinase related protein-1 (TRP-1), and tyrosinase related protein-2 (TRP-2) in melanocytes. These results suggest that the whitening activity of demethylsuberosin may be due to the inhibition of the melanin synthesis by down-regulation of MITF, tyrosinase, TRP-1 and TRP-2 expression. Thus, our results provide evidence that demethylsuberosin might be useful as a potential skin-whitening agent.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.33 no.1 s.60
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• pp.23-28
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• 2007

Ascorbic acid (vitamin C, AsA) has been known as a strong reducing agent and is supposed to retard the synthesis of melanin pigment. A main problem that arose in using vitamin C in cosmetic formulation was its poor stability and low skin permeability, which result in low lightening efficacy in clinical trials. In this study, iontophoretic gel patch with flexible thin layer battery was employed in order to enhance skin permeation of vitamin c derivative (ascorbyl glucoside, AsAG) and to increase its lightening efficacy. in vitro iontophoretic skin permeation and stability of AsAG, safety and clinical lightening efficacy of iontophoretic patch containing 2% AsAG solution were examined. A optimun current of ionthophoretic patch for korean women was 0.1 mA, considering the skin permeability and skin irritation of consumers. We suggest that iontophoretic gel patch could be a safe system for enhancing the skin permeation of AsAG and lightning efficacy.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.72-79
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• 2017

Arbutin is a hydroquinone derivative with a glucose moiety. As a tyrosinase inhibitor, it is widely used as a skin-whitening cosmetic agent for the treatment of cutaneous hyperpigmentary disorders, such as melasma and freckles. In the medical field, many studies have addressed the use of arbutin in various tumors, but the mechanism for tumor uptake of arbutin is still unclear. In this paper, we radiolabeled arbutin using radioiodine and studied its pharmacokinetics and tumor uptake via biodistribution experiments and single-photon emission computed tomography (SPECT) imaging. Radiolabeled $^{131}I-arbutin$ was stable for up to 24 h in PBS and serum. Biodistribution studies and SPECT imaging indicated high uptake of the compound in the bladder and kidneys shortly after injection. Twenty-four hours post-injection, significant deiodination was observed. Apart from high thyroid uptake, selective tumor uptake was clearly observed. The tumor-to-muscle and tumor-to-blood ratios were 26 and 9, respectively.

• Natural Product Sciences
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• v.22 no.4
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• pp.252-258
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• 2016

Vitex trifolia L. has been used traditionally to treat various illnesses, such as inflammation, headache, migraine, and gastrointestinal infections. We analyzed and evaluated the composition of V. trifolia leaf oil. Based on the results, we isolated abietatriene from V. trifolia leaf oil and investigated the effect of V. trifolia leaf oil and its active compound abietatriene on melanogenesis in B16F10 melanoma cells. They significantly decreased melanin contents and melanogenic factors, such as tyrosinase, TRP-1, TRP-2, and MITF dose-dependently in both protein and mRNA levels. Protein and mRNA expressions were determined by Western blot analysis and quantitative real time RT-PCR. Findings indicate that V. trifolia leaf oil and abietatriene reduce melanogenesis by regulating the expression of melanogenic factors. These results suggest that V. trifolia leaf oil and abietatriene could comprise a useful therapeutic agent for treating hyperpigmentation and used as effective skin-whitening agents.

• Proceedings of the SCSK Conference
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• 2003.09a
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• pp.660-671
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• 2003

A chemical investigation of Peucedanum praeruptorum has resulted in the isolation of 3 khellactone derivatives, which have inhibitory effects on melanogenesis in B16 mouse melanoma cell lines. The khellactone derivatives were isolated from the crude extract of the roots of Pecedanum praeruptorum by a combination of adsorption chromatography and HPLC. The structures of isolated compounds were identified as 3', 4'-diangeloyl-cis-khellactone, 3'-angeloyl-4'-senecioyl-cis-khellactone and, 3', 4'-disenecioyl-cis-khellactone by $^1$H NMR, $^{13}$ C NMR and mass spectral studies and by comparisons of spectral data with reported literatures. These khellactone derivatives can be a good candidate for new skin whitening agent due to its strong inhibitory activity and safety.

• Herbal Formula Science
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• v.10 no.2
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• pp.199-211
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• 2002

Acquired pigmentary skin diseases such as abnormal melanogenesis, vitiligo, chloasma and inflammatory pigmentation are related to regulate the melanin production. The aim of this study was to investigate the effect of Codonopsis lanceolata on the melanogenesis of HM3KO human melanoma cells biologically. The cells were treated for 5 days with Codonopsis lanceolata at several concentrations. Treatment with Codonopsis lanceolata suppressed melanin contents as a dose dependent manner without cytotoxicity and morphological change. And the extract of Codonopsis lanceolata also inhibited tyrosinase, a key enzyme forming melanin, in a dose-dependent manner. And it did not affect the DOPAchrome tautomerase(TRP-2) activity. These results suggest that Codonopsis lanceolata is a candidate for an efficient whitening agent which supresses melanogenesis by a Raper-Mason pathway.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.353-358
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• 1998

The MeOH extract of the bark of Paeonia moutan showed potent inhibitory effect on the mushroom tyrosinase activity in vitro. The activity-guided fractionation of t he MeOH extract resulted in the isolation of three active compounds. The chemical structures of these compounds were elucidated by chemical and spectroscopic evidence as catechin, 1,2,3,6-tetra-O-galloyl-${\beta}$-D-glucose and 1,2,3,4,6-penta-0-galloyl-${\beta}$-D-glucose, respectively. Among them, the inhibitory activity by 1,2,3,6-tetra-galloyl-${\beta}$-D-glucose on mushroom tyrosinase was more potent $(IC_{50}=3.5\;{\mu}M)$ than that of kojic acid $(IC_{50}=8.7\;{\mu}M)$ ,but catechin enhanced the mushroom tyrosinase activity 50% in the concentration of 34.5M.

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

• Journal of the Society of Cosmetic Scientists of Korea
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• v.31 no.1 s.49
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• pp.17-23
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• 2005

We had previously reported that Selina (selina-4(14), 7(11)-dien-8-one) was isolated from methanol extract of Afractylodes rhizome and has strong whitening activity in B16 melanoma cells. In this report, we demonstrated its action mechanism in melan-a cells, non-tumorigenic melanocytes. We also investigated the clinical efficacy of cosmetic preparation containing Selina. Selina reduced the melanin synthesis of Melan-a cells by $50\%$ at a concentration of $10 {\mu}g/mL$ without any apparent cytotoxicity. We also found that the treatment of cells with Selina decreased tyrosinase activity by $60\%$ at a concentration of $10 {\mu}g/mL$ but Selina was not a direct inhibitor of tyrosinase activities. To elucidate the action mechanism of Selina, we investigated the changes in mRNA and protein level of tyrosinase, TRP-1 and TRP-2 using RT-PCR and western blotting, respectively. As a result, the mRNA and protein level of tyrosinase were markedly reduced at $10 {\mu}g/mL$ of Selina without any effect on TRP-1 and TRP-2. These results suggest that Selina exerts its whitening effect mainly through regulating expression of tyrosinase. A 7 week-clinical trial using formulation containing $0.2\%$ selina-4(14), 7(11)-dien-8-one with 20 volunteers resulted in statistically significant whitening effect (p < 0.05), without any adverse effect. Based on these results, Selina (selina-4(14), 7(11)-dien-8-one) can be s useful and safe ingredient for the cleanness and brightness of skin.

• Journal of Ginseng Research
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• v.42 no.3
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• pp.389-399
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• 2018

Background: The antioxidant effects of Panax ginseng have been reported in several articles; however, little is known about the antimelanogenesis effect, skin-protective effect, and cellular mechanism of Panax ginseng, especially of P. ginseng calyx. To understand how an ethanol extract of P. ginseng berry calyx (Pg-C-EE) exerts skin-protective effects, we studied its activities in activated melanocytes and reactive oxygen species (ROS)-induced keratinocytes. Methods: To confirm the antimelanogenesis effect of Pg-C-EE, we analyzed melanin synthesis and secretion and messenger RNA and protein expression levels of related genes. Ultraviolet B (UVB) and hydrogen peroxide ($H_2O_2$) were used to induce cell damage by ROS generation. To examine whether this damage is inhibited by Pg-C-EE, we performed cell viability assays and gene expression and transcriptional activation analyses. Results: Pg-C-EE inhibited melanin synthesis and secretion by blocking activator protein 1 regulatory enzymes such as p38, extracellular signal-regulated kinases (ERKs), and cyclic adenosine mono-phosphate response element-binding protein. Pg-C-EE also suppressed ROS generation induced by $H_2O_2$ and UVB. Treatment with Pg-C-EE decreased the expression of matrix metalloproteinases, mitogen-activated protein kinases, and hyaluronidases and increased the cell survival rate. Conclusion: These results suggest that Pg-C-EE may have antimelanogenesis properties and skin-protective properties through regulation of activator protein 1 and cyclic adenosine monophosphate response element-binding protein signaling. Pg-C-EE may be used as a skin-improving agent, with moisture retention and whitening effects.