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Competitive neutrophil elastase inhibitory isoflavones from the roots of Flemingia philippinensis.
Kim, Jeong Yoon; Wang, Yan; Uddin, Zia; Song, Yeong Hun; Li, Zuo Peng; Jenis, Janar; Park, Ki Hun.
Afiliación
  • Kim JY; Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, Republic of Korea.
  • Wang Y; College of Food and Biological Engineering, Qiqihar University, Qiqihar 161006, China.
  • Uddin Z; Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, Republic of Korea.
  • Song YH; Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, Republic of Korea.
  • Li ZP; Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, Republic of Korea.
  • Jenis J; Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, Republic of Korea.
  • Park KH; Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, Republic of Korea. Electronic address: khpark@gnu.ac.kr.
Bioorg Chem ; 78: 249-257, 2018 08.
Article en En | MEDLINE | ID: mdl-29614436
Flemingia philippinensis has been used throughout history to cure rheumatism associated with neutrophil elastase (NE). In this study, we isolated sixteen NE inhibitory flavonoids (1-16), including the most potent and abundant prenyl isoflavones (1-9), from the F. philippinensis plant. These prenyl isoflavones (2, 3, 5, 7, and 9) competitively inhibited NE, with IC50 values of 1.3-12.0 µM. In addition, they were reversible, simple, slow-binding inhibitors according to their respective parameters. Representative compound 3 had an IC50 = 1.3 µM, k3 = 0.04172 µM-1 min-1, k4 = 0.0064 min-1, and Kiapp = 0.1534 µM. The Kik/Kiv ratios (18.5 ∼ 24.6) for compound 3 were consistent with typical competitive inhibitors. The prenyl functionality of isoflavones significantly affected inhibitory potencies and mechanistic behavior by shifting the competitive mode to a noncompetitive one. The remaining flavonoids (10-16) were confirmed as mixed type I inhibitors that preferred to bind free enzyme rather than the enzyme-substrate complex. Fluorescence quenching analyses indicated that the inhibitory potency (IC50) closely followed the binding affinity (KSV).
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Raíces de Plantas / Elastasa de Leucocito / Isoflavonas / Fabaceae Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2018 Tipo del documento: Article Pais de publicación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Raíces de Plantas / Elastasa de Leucocito / Isoflavonas / Fabaceae Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2018 Tipo del documento: Article Pais de publicación: Estados Unidos