Human Neutrophil Elastase Inhibitory Alkaloids from Chelidonium majus L.

Kim, Jeong Yoon; Lee, Ji Hye; Song, Yeong Hun; Jeong, Won Min; Tan, Xuefei; Uddin, Zia; Park, Ki Hun

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자료유형: 학술저널

저자정보: Kim, Jeong Yoon (Division of Applied Life Science [BK21 plus], IALS, Graduate School of Gyeongsang National University) Lee, Ji Hye (Division of Applied Life Science [BK21 plus], IALS, Graduate School of Gyeongsang National University) Song, Yeong Hun (Division of Applied Life Science [BK21 plus], IALS, Graduate School of Gyeongsang National University) Jeong, Won Min (Division of Applied Life Science [BK21 plus], IALS, Graduate School of Gyeongsang National University) Tan, Xuefei (Division of Applied Life Science [BK21 plus], IALS, Graduate School of Gyeongsang National University) Uddin, Zia (Division of Applied Life Science [BK21 plus], IALS, Graduate School of Gyeongsang National University) Park, Ki Hun (Division of Applied Life Science [BK21 plus], IALS, Graduate School of Gyeongsang National University)

저널정보: 한국응용생명화학회 Journal of applied biological chemistry Journal of applied biological chemistry 제58권 제3호

발행연도: 2015.1

수록면: 281 - 285 (5page)

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Human neutrophil elastase (HNE) represents a good therapeutic target for the treatment of inflammatory diseases as well as invasion of microorganism. The methanol extract of a aerial part of Chelidonium majus L. showed high activity against the neutrophil elastase with an $IC_{50}$ value of $100{\mu}g/mL$. Due to its potency, subsequent bioactivity-guided fractionation of methanol extract led to six alkaloids (1-6), which were identified as dihydrosanguinarine (1), (s)-stylopine (2), arnottianamide (3), (+)-chelidonine (4), spallidamine (5), and N-trans-feruloyltyramine (6). Among of them, three alkaloids (2, 5, and 6) inhibited HNE in a dose-dependent manner with $IC_{50}$ ranging between 11.6 and $51.0{\mu}M$. Lineweaver-Burk and Dixon plots, and their secondary replots showed that alkaloids (2, 5, and 6) were mixed inhibitors of HNE. The analysis of $K_I$ and $K_{IS}$ value proved that all inhibitors (2, 5, and 6) had reversible mixed type I mechanism.

#Chelidonium majus L #human neutrophil elastase #inflammation #isoquinoline alkaloid

참고문헌 (16)

참고문헌 신청

Barens J / 2007 / Herbal Medicines: a guide for healthcare professional / Pharmaceutical Press

Barreto MC / 2003 / Inhibition of mouse liver respiration by Chelidonium majus isoquinoline alkaloids / Toxical Lett 146:37

Bode W / 1989 / Human leukocyte and porcine pancreatic elastase: x-ray crystal structures, mechanism, substrate specificity, and mechanism-based inhibitors / Biochemistry 28:1951~1963

Brice K / 2010 / Neutrophil elastase, Proteinase 3, and Cathepsin G as therapeutic Targets in Human diseases / Pharmacol Rev 62:726~759

Chiari ME / 2011 / Tyrosinase inhibitory activity of a 6-isoprenoid-substituted flavanone isolated from Dalea elegans / Bioorg Med Chem 19:3474~3482

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Kim, Jeong Yoon

소속기관 Division of Applied Life Science [BK21 plus], IALS, Gyeongsang National University

주요연구분야 농수해양학 > 농학

논문수 2 이용수 1

Lee, Ji Hye