• Bulletin of the Korean Chemical Society
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• 제32권4호
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• pp.1411-1414
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• 2011

• Biomolecules & Therapeutics
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• 제13권1호
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• pp.32-34
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• 2005

Effect of isoliquiritigenin isolated from the heartwood of Dalbergia odorifera T. Chen (Leguminosae) on mushroom tyrosinase activity was investigated in vitro using L-tyrosine and L-3, 4-dihydroxyphenylalanine (L-DOPA) as the substrates. When L-tyrosine was used as a substrate, both isoliquiritigenin and kojic acid, a positive control, inhibited tyrosinase activity in a concentration-dependent manner. IC$_{50}$ values of isoliquiritigenin and kojic acid were 61.4 and 52.2 ${\muM}$, respectively. However, isoliquiritigenin showed week inhibitory effect on the oxidation of L-DOPA by tyrosinase with inhibition ratio of 9.1 ${\pm}$ 7.1% at 100 ${\muM}$. It is also suggested that 3-unsubstituted and 4-hydroxyl phenyl group in isoliquiritigenin plays an important role on the inhibition of tyrosinase activity when L-tyrosine was used as a substrate. Analysis of Lineweaver-Burk plot showed that isoliquiritigenin acts as a competitive inhibitor in case of L-tyrosine as a substrate.

• 약학회지
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• 제43권4호
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• pp.494-501
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• 1999

The skin whitening effects of pine needle extract, hop extract and chestnut inner shell extract were evaluated both in vitro and in B 16 mouse melanoma cell lines. Each extracts significantly inhibited tyrosinase activity, dopa auto-oxidation and melanin biosynthesis in vitro and in B 16 cell lines. In vitro, hop extract inhibited melanin biosynthesis 15 times stronger than kojic acid at $10{\;}\mu\textrm{g}/ml$ concentration. Each extracts were stronger inhibitors of melanin biosynthesis than kojic acid in B 16 mouse melanoma cell at less than $4{\;}\mu\textrm{g}/ml$ concentration. These results show that extracts fo pine needle, hop and chestnut inner shell could be developed as skin whitening component of cosmetics.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.321.1-321.1
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• 2002

To indentify inhibitors of melanogenesis. we compared the effect of some natural products on mushroom tyrosinase. human melanocytic tyrosinase activity and melanin content. The cytotoxicity of the component were also tested on cultured mouse melanoma cells, Each extract significantly inhibited tyrosinase activity and melanin synthesis in vitro and B 16 melanoma cell lines. In B 16 cell lines, watermelon's inner shell extract inhibited tyrosinase activity as strong as kojic acid at 150${\um}g$/${\mu}\ell$ concentration. And morning glory'seed extract inhibited melanin synthesis more than kojic acid at 150${\um}g$/${\mu}\ell$ concentration. Each extract were strong inhibitors of tyrosinase activity and total melanin synthesis in B 16 mouse melanoma cell lines at less than 100${\um}g$/${\mu}\ell$ concetration. These result show that extract of watermelon's inner shell. lettuce. morning glory's seed and licorice root could be developed as skin whitening component of cosmetics.

• 한국식품영양과학회지
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• 제42권4호
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• pp.505-511
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• 2013

막걸리 제조 시에 발생하는 부산물의 화장품 소재 가능성을 조사하기 위하여 항산화능, 페놀 함량, 코지산 함량, 미백, 주름 개선 효과 등을 분석하였다. 누룩박, 미박, 원주, 시판제품을 5가지 다른 용매(0, 25, 50, 75, 100% 에탄올)로 $20^{\circ}C$와 $50^{\circ}C$에서 각각 추출하였다. 총 페놀 함량은 $20^{\circ}C$에서 추출하였을 때 누룩박의 에탄올 75% 추출물에서 13.26 mg GAE/g으로 가장 높았으며, $50^{\circ}C$에서는 시판 제품의 에탄올 75% 추출물에서 16.66 mg GAE/g으로 가장 높았다. 가장 높은 코지산 함량은 $20^{\circ}C$에서 누룩박의 0% 에탄올 추출물에서 관찰되었고, $50^{\circ}C$에서 추출한 모든 시료에서 코지산은 검출되지 않았다. $20^{\circ}C$에서 제조한 누룩박, 미박 추출물에서 상당한 항산화능(DPPH와 ABTS 라디칼 소거능, 환원력)이 확인되었다. Tyrosinase 저해능으로 분석한 미백 효과는 $50^{\circ}C$에서 누룩박의 75% 에탄올 추출물이 가장 높았다. 누룩박과 미박은 elastase 저해능도 발견되어 주름 개선 효과가 있음을 확인하였으며, 특히 $20^{\circ}C$에서의 미박 추출물이 가장 높은 활성을 나타내었다. 이상의 결과는 막걸리 제조 부산물이 항산화, 미백, 주름 개선의 기능을 가진 화장품 소재로서의 가능성이 있음을 시사한다.

• 대한화장품학회:학술대회논문집
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• 대한화장품학회 2003년도 IFSCC Conference Proceeding Book II
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• pp.479-479
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• 2003

We investigated the tyrosinase inhibitory effect using whitening materials such as arbutin, ethyl ascorbyl ether, glabridin, kojic acid, magnesium ascorbyl phosphate and ascorbic acid. Tyrosinase inhibition rate were determined varying the enzyme concentration, reaction time, reaction temperature and pH. The optimal conditions to measure the inhibitory efficacy were as follows. : enzyme concentration 1,500 or 2,000IU/mL, reaction time 15min(for the enzyme concentration 1,500 IU/mL) and l0min(for the enzyme concentration 2,000IU/mL), reation temperature 42$^{\circ}C$, pH 6.5. Under these conditions $IC_{50}$/ of arbutin, ethyl ascorbyl ether, glabridin, kojic acid, magnesium ascorbyl phosphate and ascorbic acid were calculated. In the case of magnesium ascorbyl phosphate, the inhibitory effect of tyrosinase was very low and the $IC_{50}$/ of magnesium ascorbyl phosphate could not be calculated. Other five materials showed good inhibitory effect of tyrosinase and can be used for the whitening materials.

• 생약학회지
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• 제34권2호통권133호
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• pp.138-141
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• 2003

In order to screen new tyrosinase inhibiting principle which is expected to be a new biofunctional skin whitening cosmetics, we have isolated 600 strains of the marine- derived fungi and investigated tyrosinase inhibiting activity for their acetone extracts. The significant activities (>70% Inhibition) were observed in the extract of 10 strains of fungi (MFA7, MFA27, MFA58, MFA317, MFA318, MFA345, MFA412, MFA552, MFA562, MFA581). These active strains were cultured in SWS medium with 1 L scale and the resulting broth and mycelium were extracted to afford mycelium extract (000M) and broth extract (000B), respectively. Tyrosinase inhibiting activity for all extracts has been tested. As the results, the broth extracts of 4 strains (27B, 58B, 552B and 581B) exhibited relatively high levels of activity of $IC_{50}$ values of $3.0-19.0\;{\mu}g/mL$. The active component of 581B was purified by assay-guided isolation to yield the known kojic acid (1), and its structure was determined by physicochemical evidence. Kojic acid showed the significant tyrosinase inhibitory activity with $IC_{50}$ values of $12.0\;{\mu}M$.

• Asian Pacific Journal of Cancer Prevention
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• 제15권1호
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• pp.291-297
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• 2014

The radioprotective effects of a single administration of kojic acid (KA) against ionizing radiation were evaluated via assessment of 30-day survival and alterations of peripheral blood parameters of adult C57BL/6 male mice. The 30-day survival rate of mice pretreated with KA (75 or 300 mg/kg body weight, KA75 or KA300) subcutaneously 27 h prior to a lethal dose (8 Gy, 153.52 cGy/min) of gamma irradiation was higher than that of mice irradiated alone (40% or 60% vs 0%). It was observed that the white blood cell (WBC) count/the red blood cell (RBC) count, haemoglobin content, haematocrit and platelet count of mice with or without KA pretreatment as exposed to a sub-lethal dose (4 Gy, 148.14 cGy/min) of gamma irradiation decreased maximally at day 4/day 8 post-irradiation. Although the initial WBC values were low in KA300 or WR-2721 (amifostine) groups, they significantly recovered to normal at day 19, whereas in the control group they did not. The results from the cytotoxicity and cell viability assays demonstrated that KA could highly protect Chinese hamster ovary (CHO) cells against ionizing radiation with low toxicity. In summary, KA provides marked radioprotective effects both in vivo and in vitro.

• Journal of Pharmaceutical Investigation
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• 제28권3호
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• pp.177-183
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• 1998

Low toxicity, reverse thermal gelation and high drug loading capabilities suggest that poloxamer 407 gels have great potential as a topical drug delivery system. Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of skin irritancy due to its acidic pH. Poloxamer gels of different polymer contents were formulated to overcome the problem and compared to the cream type formulations of either w/o/w multiple emulsion cream or o/w type emulsion cream. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solutions. Drug release from w/o/w multiple emulsion cream was controlled by oil membrane, showing the apparent zero order release kinetics. The KA release from the poloxamer gels was also controlled by the gel matrix, showing that drug release increased linearly as KA contents increase, but decreased exponentially as the polymer contents increase. In the skin irritancy test, the primary irritancy index(PII) of poloxamer gel base was lower than those of multiple emulsion cream base and o/w cream. Depending on KA contents or polymer contents in the gel. PH values in poloxamer gels were ranged from 1.3 to 2.0, which are interpreted as low or negligible irritation on skin. There was a good correlation between the log value of flux in drug release and PII value in skin irritation. It was possible to conclude that the poloxamer gels containing KA might be a good candidate for an antimelanogenic topical delivery system by virtue of the controlled release of the drug and the reduced skin irritancy.

• Journal of Pharmaceutical Investigation
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• 제28권2호
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• pp.87-92
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• 1998

Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of the skin irritancy and the instability against the pH, temperature, and light. In order to overcome these problems, various topical gels and multiple emulsion creams which can control the release of active ingredient, KA, were formulated employing cream bases of mineral oil with caprylic capric triglyceride and hydrophilic polymers such as chitosan, carbopol. and pluronics. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solution. Drug release from chitosan-based gels (ChitoGel) obeyed to the first order kinetics with a rapid release especially in the initial period. However, pluronic-based gels (PluGel) and carbopol-based gels (CarboGel) revealed controlled release of drug to some extent, followed by the square root-time kinetics. Moreover, the release of KA was further controlled with the W/O/W multiple emulsion creams (MultiCream), showing the apparent zero order release kinetics by virtue of dynamic ratecontrolling membrane of the oil layer. The flux $(J,\;{\mu}g/cm^2/hr)$ of ChitoGel. CarboGel. PluGel. and MultiCream in the initial period of 6hr were 73.30, 28.67. 24.04 and 7.72, respectively. On the other hand, the skin irritancy score of ChitoGel and MultiCream were observed as 2.5 and 2.3 respectively, in the rabbit skin irritation test. Although there were insignificant differences at p<0.05 between those formulations, it was possible to conclude that the W/O/W multiple emulsion creams containing KA might be a good candidate for an antimelanogenic drug delivery system due to the controlled release of acidic drug molecules.