• 제목/요약/키워드: B16F1 melanoma cell

검색결과 197건 처리시간 0.027초

슈퍼자미(SuperC3GHi) 미강 발효물의 생리활성 (Evaluation of Biological Activities of Fermented Rice Bran from Novel Black Colored Rice Cultivar SuperC3GHi)

  • 김동주;최수민;김화영;김중학;류수노;한상준;홍성길
    • 한국작물학회지
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    • 제56권4호
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    • pp.420-426
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    • 2011
  • 슈퍼자미(SuperC3GHi) 쌀 품종은 색소 성분인 cyanidine-3-glucoside(C3G)의 함량을 크게 증대시킨 품종이다. 슈퍼자미 벼품종을 활용한 새로운 기능성 소재 및 제품으로의 개발 가능성을 타진하기 위하여 본 연구에서는 슈퍼자미 벼품종의 버섯 균사체 발효물을 이용하여 항염증, 항알러지, 항암 기능의 검증을 수행하였다. 1. 슈퍼자미 미강 발효물의 항염 활성을 분석하기 위하여 ear-edema test를 수행한결과 약 35.6%의 염증 억제율을 나타내었다. 2. 슈퍼자미 미강 발효물의 항알러지 활성을 확인하기 위하여 비만세포인 RBL-2H3 세포의 hexoamidase 및 histamine 유리 활성을 조사한 결과 슈퍼자미 미강 발효물을 처리하였을 때 각각 약 40% 및 57%의 억제 활성을 나타내어 항알러지 활성을 확인하였다. 3. 슈퍼자미 미강 발효물의 항암 활성을 조사한 결과 복수암 모델 및 고형암 모델에서 모두 암세포의 증식을 억제하는 활성을 나타내었고, 혈액중 백혈구의 수치를 유의적으로 증가하는 것으로 나타나 슈퍼자미 미강 발효물이 항암 활성을 있음을 확인 할 수 있었다. 4. 이상의 결과에서 슈퍼자미 품종의 미강을 버섯 균사체 발효를 통해 얻어진 기능성 소재는 항염, 항알러지, 항암 활성을 통해서 우수한 기능성 소재로서의 개발 가능성이 매우 높다고 판단된다.

양이온성 지질이 포함된 PEG 리포솜의 세포내 이입 및 항암효력 평가 (Intracellular delivery and anti-tumor activity of polyethyleneglycol liposomes containing cationic lipid)

  • 정순화;김성규;정석현;성하수;조선행;신병철
    • Journal of Pharmaceutical Investigation
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    • 제38권3호
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    • pp.163-169
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    • 2008
  • Liposomes are spherical vesicles composed of lipid bilayer membranes. However, the conventional liposomes have been found to be plagued by rapid opsonization and taken up by the reticuloendothelial system (RES), resulting in shortened circulation time and limited intracellular uptake to target cell. In this study, polyethyleneglycol-cationic liposomes (PCL) containing cationic lipid and DSPE-mPEG were prepared by thin film cast-hydration method. The PEG liposomes had approximately $97.0{\pm}1.3\;nm$ of mean particle diameter and $-21.7{\pm}1.2\;mV$ of zeta potential value. PCL had $96.4{\pm}1.8\;nm$ of mean particle diameter and $-8.7{\pm}1.1\;mV$ of zeta potential value with a decrease of about 10 mV compared to the PEG liposomes. Loading of model drug, doxorubicin (DOX), in liposomes were carried out by using remote loading method and the loading efficiency of DOX in liposomes was about $95.0{\pm}1.9%$. Intracellular uptake and cytotoxicity of PCL were higher than that of PEG liposomes to murine B16F10 melanoma cells. In addition, anti-tumor activity of PCL was similar to that of PEG liposomes on growth of A549 human lung carcinoma in BALB/c mice. Consequently, PCL modified with cationic lipid may be applicable as anticancer drug carriers that can increase intracellular uptake and therapeutic efficacy.

Hexane Extract of Kaempferia galanga L. Suppresses Melanogenesis via p38, JNK and Akt

  • In, Myung-Hee;Jeon, Byoung Kook;Mun, Yeun-Ja;Woo, Won-Hong
    • 동의생리병리학회지
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    • 제30권1호
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    • pp.47-53
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    • 2016
  • Kaempferia galanga L. is one of the plants in Zingiberaceae family. It is used by people in many regions of Asia and Africa for relieving toothache, abdominal pain, muscular swelling and rheumatism. Tyrosinase is a key enzyme for melanogenesis, and hyperpigmentation is associated with abnomal accumulation of melanin pigment. This study aimed to investigate the inhibition of melanogenesis by hexane extract of Kaempferia galanga L. (HKG) in B16F10 melanoma cells. Cell-free tyrosinase, melanin contents, intracellular tyrosinase activity and western blot analysis were performed to elucidate the effects on anti-melanogenesis. Cytotoxicity of the extracts was measured using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and determined the concentration of 12.5, 25 μg/ml. HKG significantly inhibited to activities of intracellular tyrosinase and melanin synthesis in the absence or presence of α-melanocyte stimulating hormone (α-MSH) with dose-dependent manner. And HKG inhibited the expression of tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2), regardless of the presence or absence of α-MSH. HKG also down-regulated phosphorylation of p38 and JNK, and up-regulated phosphorylation of Akt. These effects were not related to its cytotoxicity action. These results indicate that HKG has the potential to be a useful therapeutic agent for treating hyperpigmentation disorders and as a beneficial additive in whitening agents in cosmetics industry.

Synthesis and Evaluation of Coumaroyl Dipeptide Amide as Potential Whitening Agents

  • Lee, Hye-Suk;Shin, Kyong-Hoon;Ryu, Geun-Seog;Cho, In-Shik;Kim, Jae-Il;Lee, Jae-Ho;Kim, Han-Young
    • Bulletin of the Korean Chemical Society
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    • 제34권10호
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    • pp.3017-3021
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    • 2013
  • Coumaroyl dipeptide amide, Coumaric acid-LG-$NH_2$, was prepared successfully using the solid-phase method, and its efficacy as a skin whitening agent was studied. Coumaric acid-LG-$NH_2$ was prepared with Rink-amide resin, and 96.354% of purity was obtained. Using MTT assay and LDH release assay, we found that it exhibited very low cytotoxicity. And, we found that Coumaric acid-LG-$NH_2$ inhibited tyrosinase activity dose-dependently and showed superior tyrosinase inhibitory activity to well-known whitening agent, arbutin. $IC_{50}$ value of Coumaric acid-LG-$NH_2$ was 182.4 ${\mu}M$, and $IC_{50}$ value of arbutin was 384.6 ${\mu}M$. Also, in measurement of melanin contents using B16F1 melanoma cell lines, Coumaric acid-LG-$NH_2$ reduced melanin production induced by ${\alpha}$-MSH statistically significant, and showed superior melanin inhibitory activity to p-coumaric acid or arbutin. In addition, Coumaric acid-LG-$NH_2$ reduced MC1R mRNA expression level. Thus, we concluded that MC1R pathway is the significant pathway of Coumaric acid-LG-$NH_2$, and Coumaric acid-LG-$NH_2$ has great potential to be used as novel whitening agents.

Analysis of Immunomodulating Gene Expression by cDNA Microarray in $\beta$-Glucan-treated Murine Macrophage

  • Sung, Su-Kyong;Kim, Ha-Won
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2003년도 Annual Meeting of KSAP : International Symposium on Pharmaceutical and Biomedical Sciences on Obesity
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    • pp.98-98
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    • 2003
  • ${\beta}$-(1,3)-D-Glucans have been known to exhibit antitumor and antimicrobial activities. The presence of dectin-1,${\alpha}$, ${\beta}$-glucan receptor of dendritic cell, on macrophage has been controvertial. RT-PCR analysis led to the detection of dectin-1${\alpha}$ and ${\beta}$ in murine macrophage Raw264.7 cell line. Among the various organs of mouse, dectin-1${\alpha}$ and ${\beta}$ were detected in the thymus, lung, spleen, stomach and intestine. To analyze gene expression modulated by ${\beta}$-glucan treated murine Raw264.7 macrophage, total mRNA was applied to cDNA microarray to interrogate the expression of 7,000 known genes. cDNA chip analysis showed that ${\beta}$-glucan of P. osteatus increased gene expressions of immunomodulating genes, membrane antigenic proteins, chemokine ligands, complements, cytokines, various kinases, lectin associated genes and oncogenes in Raw 264.7 cell line. When treated with ${\beta}$-glucan of P. osteatus and LPS, induction of gene expression of TNF-${\alpha}$ and IFN-R1 was confirmed by RT-PCR analysis. Induction of TNF-R type II expression was confirmed by FACS analysis. IL-6 expression was abolished by EDTA in ${\beta}$-glucan and LPS treated Raw264.7 cell line, indicating that ${\beta}$-glucan binds to dectin-l in a Ca$\^$++/ -dependent manner. To increase antitumor efficacy of ${\beta}$-glucan, ginsenoside Rh2 (GRh2) was co-treated with ${\beta}$-glucan in vivo and in vitro tests. IC$\sub$50/ values of GRh2 were 20 and 25 $\mu\textrm{g}$/$m\ell$ in SNU-1 and B16 melanoma F10 cell line, respectively. Co-treatment with ${\beta}$-glucan and GRh2 showed synergistic antitumor activity with cisplatin and mitomycin C both in vitro and in vivo. Single or co-treatment with ${\beta}$-glucan and GRh2 increased tumor bearing mouse life span. Co-treatment with ${\beta}$-glucan and GRh2 showed more increased life span with mitomycin C than that with cisplatin. Antitumor activities were 67% and 72 % by co-injection with ${\beta}$-glucan and GRh2 in the absence or presence of mitomycin C, respectively.

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Efficient Anti-Tumor Immunotherapy Using Tumor Epitope-Coated Biodegradable Nanoparticles Combined With Polyinosinic-Polycytidylic Acid and an Anti-PD1 Monoclonal Antibody

  • Sang-Hyun Kim;Ji-Hyun Park;Sun-Jae Lee;Hee-Sung Lee;Jae-Kyung Jung;Young-Ran Lee;Hyun-Il Cho;Jeong-Ki Kim;Kyungjae Kim;Chan-Su Park;Chong-Kil Lee
    • IMMUNE NETWORK
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    • 제22권5호
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    • pp.42.1-42.20
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    • 2022
  • Vaccination with tumor peptide epitopes associated with MHC class I molecules is an attractive approach directed at inducing tumor-specific CTLs. However, challenges remain in improving the therapeutic efficacy of peptide epitope vaccines, including the low immunogenicity of peptide epitopes and insufficient stimulation of innate immune components in vivo. To overcome this, we aimed to develop and test an innovative strategy that elicits potent CTL responses against tumor epitopes. The essential feature of this strategy is vaccination using tumor epitope-loaded nanoparticles (NPs) in combination with polyinosinic-polycytidylic acid (poly-IC) and anti-PD1 mAb. Carboxylated NPs were prepared using poly(lactic-co-glycolic acid) and poly(ethylene/maleic anhydride), covalently conjugated with anti-H-2Kb mAbs, and then attached to H-2Kb molecules isolated from the tumor mass (H-2b). Native peptides associated with the H-2Kb molecules of H-2Kb-attached NPs were exchanged with tumor peptide epitopes. Tumor peptide epitope-loaded NPs efficiently induced tumor-specific CTLs when used to immunize tumor-bearing mice as well as normal mice. This activity of the NPs significantly was increased when co-administered with poly-IC. Accordingly, the NPs exerted significant anti-tumor effects in mice implanted with EG7-OVA thymoma or B16-F10 melanoma, and the anti-tumor activity of the NPs was significantly increased when applied in combination with poly-IC. The most potent anti-tumor activity was observed when the NPs were co-administered with both poly-IC and anti-PD1 mAb. Immunization with tumor epitope-loaded NPs in combination with poly-IC and anti-PD1 mAb in tumor-bearing mice can be a powerful means to induce tumor-specific CTLs with therapeutic anti-tumor activity.

Passiflora caerulea 추출물의 화장품 소재 활용 가능성 (The Possibility of Passiflora Caerulea Extract as Cosmetic Material)

  • 이재남
    • 한국응용과학기술학회지
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    • 제39권5호
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    • pp.710-719
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    • 2022
  • 본 연구는 Passiflora caerulea 추출물의 항산화 활성 및 멜라닌 생합성 억제 효과 측정을 통해 화장품 소재로서의 활용 가능성을 확인하고자 하였다. Passiflora caerulea 추출물은 70% 에탄올로 추출하였고, TEAC assay를 이용한 ABTS radical 소거능을 측정하였다. 또한 Neutral red assay를 이용한 세포 생존율, DCF-DA를 통한 세포 내 ROS 생성 억제, 멜라닌 생합성 억제 효과를 측정하였다. 연구결과, Passiflora caerulea 추출물의 ABTS radical 소거능은 농도 의존적 소거활성이 확인되었으며, positive control(양성대조군)로 이용한 trolox와 0.1 mg/mL 농도에서는 유사한 radical 소거 활성을 확인하였다. CFDA를 통한 세포 내 활성산소종(ROS) 생성은 농도 의존적으로 억제되었고, B16F10 melanoma 세포에 대한 세포 독성은 나타나지 않았다. 또한 𝛼-MSH로 유도된 멜라닌 생합성 억제 효과를 확인하였다. 따라서 본 연구를 통해 Passiflora caerulea 추출물은 화장품 소재로서의 활용 가능성이 있는 것으로 판단된다.

In vitro studies of anti-inflammatory and anticancer activities of organic solvent extracts from cultured marine microalgae

  • Samarakoon, Kalpa W.;Ko, Ju-Young;Shah, Md. Mahfuzur Rahman;Lee, Ji-Hyeok;Kang, Min-Cheol;Kwon, O-Nam;Lee, Joon-Baek;Jeon, You-Jin
    • ALGAE
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    • 제28권1호
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    • pp.111-119
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    • 2013
  • Marine microalgae are a promising source of organisms that can be cultured and targeted to isolate the broad spectrum of functional metabolites. In this study, two species of cyanobacteria, Chlorella ovalis Butcher and Nannchloropsis oculata Droop, one species of bacillariophyta, Phaeoductylum tricornutum Bohlin, and one species of Dinophyceae, Amphidinium carterae (Hulburt) were cultured and biomasses used to evaluate the proximate comical compositions. Among the determined proximate chemical compositions of the cultured marine microalgae, the highest content of crude proteins and lipids were exhibited in P. tricornutum and A. carterae, respectively. Solvent-solvent partition chromatography was subjected to fractionate each of the cultured species and separated n-hexane, chloroform, ethyl acetate, and aqueous fractions. Nitric oxide production inhibitory level (%) and cytotoxicity effect on lipo-polysaccharide-induced RAW 264.7 macrophages were performed to determine the anti-inflammatory activity. N. oculata hexane and chloroform fractions showed significantly the strongest anti-inflammatory activity at $6.25{\mu}g\;mL^{-1}$ concentration. The cancer cell growth inhibition (%) was determined on three different cell lines including HL-60 (a human promyelocytic leukemia cell line), A549 (a human lung carcinoma cell line), and B16F10 (a mouse melanoma cell line), respectively. Among the extracts, C. ovalis ethyl acetate and A. carterae chloroform fractions suppressed the growth of HL-60 cells significantly at 25 and $50{\mu}g\;mL^{-1}$ concentrations. Thus, the cultured marine microalgae solvent extracts may have potentiality to isolate pharmacologically active metabolites further using advance chromatographic steps. Hence, the cultured marine microalgae can be described as a good candidate for the future therapeutic uses.

Melanogenesis regulatory constituents from Premna serratifolia wood collected in Myanmar

  • WOO, SO-YEUN
    • 한국자원식물학회:학술대회논문집
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    • 한국자원식물학회 2019년도 춘계학술대회
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    • pp.21-22
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    • 2019
  • Melanin is a mixture of pigmented biopolymers synthesized by epidermal melanocytes that determine the skin, eye, and hair colors. Melanocytes produce two different kinds of melanin, eumelanin (dark brown/black insoluble pigments found in dark skin and dark hair and pheomelanin (lighter red/yellow). The biological role of melanin is to prevent skin damage by ultraviolet (UV) radiation. However, the overproduction or deficiency of melanin synthesis could lead to serious dermatological problems, which include melasma, melanoderma, lentigo, and vitiligo. Therefore, regulating melanin production is important to prevent the pigmentation disorders. Myanmar has a rich in natural resources. However, the chemical constituents of these natural resources in Myanmar have not been fully investigated. In the effort to search for compounds with anti-melanin deposition activity from Myanmar natural resources, five plants were collected in Myanmar. Extracts of these collected five plants were tested for anti-melanin deposition activity against a mouse melanoma cell line (B16-F10) induced with ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH) and 3-isobutyl-1-methylxanthine (IBMX), and their anti-melanin deposition activities were compared with the positive control, arbutin. Among the tested extracts, the CHCl3 extracts of the Premna serratifolia (syn: P. integrifolia) wood showed anti-melanin deposition activities with IC50 values of $81.3{\mu}g/mL$. Hence, this study aims to identify secondary metabolites with anti-melanin deposition activity from P. serratifolia wood of Myanmar. P. serratifolia belongs to the Verbenaceae family and is widely distributed in near western sea coast from South Asia to South East Asia, which include India, Malaysia, Vietnam, Cambodia, and Sri Lanka. People in Tanintharyi region located in the southern part of Myanmar utilize the P. serratifolia, Sperethusa crenulata, Naringi crenulata, and Limonia acidissima as Thanaka, traditional cosmetics in Myanmar. Thanaka is applied in the form of paste onto skins to make it smooth and clear, as well as to prevent wrinkles, skin aging, excessive facial oil, pimples, blackheads, and whiteheads. However, the chemical constituents responsible for their cosmetic properties are yet to be identified. Moreover, the chemical constituents of P. serratifolia was almost uncharacterized. Investigation of the P. serratifolia chemical constituents is thus an attractive endeavor to discover new anti-melanin deposition active compounds. The investigation of the chemical constituents of the active CHCl3 extract of P. serratifolia led to isolation of four new lignoids, premnan A (1), premnan B (2), taungtangyiol C (3), and 7,9-dihydroxydolichanthin B (4), together with premnan C (5) (assumed to be an artifact), one natural newlignoid,(3R,4S)-4-(1,3-benzodioxol-5-ylcarbonyl)-3-[(R)-1-(1,3-benzo dioxol-5-yl)-1-hydroxy methyl]tetrahydro-2-furanone (6), and five known compounds (7-11)1,2). The structures of all isolated compounds were determined on the basis of their spectroscopic data and by comparison with the reported literatures. The absolute configurations of 1-3 and 5 were also determined by optical rotation and circular dichroism (CD) data analyses1). The anti-melanin deposition activities of all the isolated compounds were evaluated against B16-F10 cell line. 7,9-Dihydroxydolichanthin B (4) and ($2{\alpha},3{\alpha}$)-olean-12-en-28-oic acid (11) showed strong anti-melanin deposition activities with IC50 values of 18.4 and $11.2{\mu}M$, respectively, without cytotoxicity2). On the other hand, compounds 1-3, 5, and 7 showed melanogenesis enhancing activities1). To better understand their anti-melanin deposition mechanism, the effects of 4 and 11 on tyrosinase activities were investigated. The assay indicated that compounds 4 and 11 did not inhibit tyrosinase. Furthermore, we also examined the mRNA expression of microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), tyrosinase-related protein-1 (TRP-1), and tyrosinase-related protein-2 (TRP-2). Compounds 4 and 11 down-regulated the expression of Tyr and Mitf mRNAs, respectively. Although the P. serratifolia wood has been used as traditional cosmetics in Myanmar for centuries, there are no scientific evidences to support its effectiveness as cosmetics. Investigation of the anti-melanin deposition activity of the chemical constituents of P. serratifolia thus provided insight into the effectiveness of the P. serratifolia wood as a cosmetic agent.

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말오줌나무 추출물의 미백활성 검증 (Whitening Activity of Sambucus Sieboldiana Var. Pendula (Nakai) Extract)

  • 유단희;김진태;오민정;염현지;이진영
    • 생명과학회지
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    • 제29권3호
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    • pp.279-286
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    • 2019
  • 본 연구는 말오줌나무 70% 에탄올 추출물의 항산화 효과와 미백 효과를 검증하였다. 말오줌나무 추출물의 전자공여능 측정실험은 $1,000{\mu}g/ml$에서 86.21%의 효과를 나타내었고, ABTS 소거능을 측정한 결과 $1,000{\mu}g/ml$ 농도에서 97.9%의 소거능을 보였다. Tyrosinase 저해활성 측정은 $1,000{\mu}g/ml$ 농도에서 37%의 효과를 보였다. 말오줌나무 추출물의 세포 생존율을 melanoma cell (B16F10)에서 확인하기 위해 MTT assay를 진행하였는데 세포 생존율을 측정한 결과, $100{\mu}g/ml$ 농도에서 90% 이상의 생존율을 보였다. 말오줌나무 추출물의 MITF, TRP-1, TRP-2 및 tyrosinase의 단백질 발현 효과를 25, 50, $100{\mu}g/ml$ 농도에서 측정하였으며 양성 대조군으로 ${\beta}-actin$을 사용하였다. 그 결과, MITF, TRP-1, TRP-2 및 tyrosinase의 각각 $100{\mu}g/ml$ 농도에서 34.5%, 45.6%, 58.4%, 79.6%의 단백질 발현 억제 효과를 보였다. MITF, TRP-1, TRP-2 및 tyrosinase의 mRNA발현을 RT-PCR로 25, 50, $100{\mu}g/ml$ 농도에서 측정하였고, 양성 대조군으로 GAPDH를 사용하였다. 그 결과, 말오줌나무 추출물의 $100{\mu}g/ml$ 농도에서 각각 85.4%, 67.5%, 85.2%, 67.1%의 mRNA 발현이 감소함을 확인 할 수 있었다. 따라서, 말오줌나무 추출물이 미백 소재로서의 가능성을 확인할 수 있었다.