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논문 기본 정보

자료유형
학술저널
저자정보
Choo, Soo-Jin (Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology) Ryoo, In-Ja (Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology) Kim, Kwan Chul (Innoskin Co., Ltd., Korea Research Institute of Bioscience and Biotechnology) Na, Minkyun (College of Pharmacy, Chungnam National University) Jang, Jae-Hyuk (Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology) Ahn, Jong Seog (Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology) Yoo, Ick-Dong (Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology)
저널정보
대한약학회 Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 제37권 제5호
발행연도
2014.1
수록면
567 - 574 (8page)

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During the course of screens to identify anti-melanogenic agents from natural resources, we found that the methanol extract of the dried flower of Inula britannica L. inhibited melanin synthesis in cultured melanoma cells stimulated with 3-isobutyl-1-methylxanthine (IBMX). A bioassay-guided isolation of the chloroform fraction of the I. britannica using an in vitro melanogenesis inhibition assay led to the isolation of sesquiterpenes, 1-O-acetylbritannilactone (1), britannilactone (2) and neobritannilactone B (3). Compounds 1 and 2 significantly reduced melanin production in a dose-dependent manner with $IC_{50}$ values of 13.3 and $15.5{\mu}M$, respectively, whereas compound 3 was found to be cytotoxic. Compound 1 also inhibited the tyrosinase activity only in cell based-systems. Western blot analysis indicated that compound 1 inhibited melanogenesis by activating extracellular signal-regulated kinase (ERK) and Akt signaling and also inhibiting cAMP related binding protein, which regulates its downstream pathway, including tyrosinase, tyrosinase related protein-1 and TRP-2. These results demonstrated that compound 1, a major sesquiterpene from the flowers of I. britannica, exhibited anti-melanogenic activity by suppression of tyrosinase expression via ERK and Akt signaling. Taken together, our results suggest that these compounds may act as potent natural skin-lightening agents.

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