SavedAdd your journal

Journals / Records of Natural Products / 2017 / Cilt: 11 - Sayı: 6

Prenylated Flavonoids from Epimedium koreanum Nakai and their Human Neutrophil Elastase Inhibitory Effects

Ki Hun PARK
Soo Min LEE
Yeong Hun SONG
Zia UDDİN
Yeong Jun BAN
Pages
514–536
DOI
—
🏛️Bibliographic metadata and full text access for this article are provided via DergiPark.
DergiPark Record ↗
✨

AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

In a detailed kinetic study, compound 1 was assigned to mixed type I and exhibited the greatest binding to the free enzyme (KI = 11.7 μM, KIS = 40.9 μM)

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Human neutrophil elastase (HNE) has been linked to immune system functions, including inflammation, as well as the development of skin wrinkles, suggesting that HNE inhibitors have many practical applications.
📊
Key Findings & Data:In this study, the methanol extract of Epimedium koreanum Nakai contained potent HNE inhibitory flavonoids (1–4) with IC50 values of 6.06–125.80 μM.
💡
Conclusion & Impact:In a detailed kinetic study, compound 1 was assigned to mixed type I and exhibited the greatest binding to the free enzyme (KI = 11.7 μM, KIS = 40.9 μM)
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Abstract

Human neutrophil elastase (HNE) has been linked to immune system functions, including inflammation, as well as the development of skin wrinkles, suggesting that HNE inhibitors have many practical applications. In this study, the methanol extract of Epimedium koreanum Nakai contained potent HNE inhibitory flavonoids (1–4) with IC50 values of 6.06–125.80 μM. Prenyl groups within these flavonoids were critical for the inhibitory effects. For example, epimedokoreanin B (1) (IC50 = 6.06 μM) showed 6-fold higher efficacy than that of its parent luteolin (IC50 = 36.01 μM). A similar trend was observed for compound 2 (IC50 = 6.28 μM) and its parent, apigenin (IC50 = 37.94 μM). Lineweaver–Burk plots showed that the compounds exhibit mixed-type inhibition. In a detailed kinetic study, compound 1 was assigned to mixed type I and exhibited the greatest binding to the free enzyme (KI = 11.7 μM, KIS = 40.9 μM)

🔖

Cite This Article

PARK, K. H., LEE, S. M., SONG, Y. H., UDDİN, Z., BAN, Y. J. (2017). Prenylated Flavonoids from Epimedium koreanum Nakai and their Human Neutrophil Elastase Inhibitory Effects. Records of Natural Products, Cilt: 11 - Sayı: 6, 514–536. https://ajindex.com/articles/308600

📄 Full Text PDF Viewer

📄

PDF görüntüleyici hazırlanıyor...

References (15)

  1. V. Brinkmann, U. Reichard, C. Goosmann, B. Faule, Y. Uhlemann, D. S. Weiss, Y. Weinrach and A. Zychlinsky (2004). Neutrophil extracellular traps kill bacteria, Science 303, 1532-1535
  2. P. M. Fitch, A. Roghanian, S. E. M. Howie and J. M. Sallenave (2006). Human neutrophil elastase inhibitors in innate and adaptive immunity, Biochem. Soc. Trans. 34, 279-282
  3. G. Doring (1999). Serine protease inhibitor therapy in α1-antitrypsin inhibitor deficiency and cystic fibrosis, Pediatr. Pulmonol. 28, 364-375
  4. C. T. Pham (2006). Neutrophil serine protease: specific regulators of inflammation, Nat. Rev. Immunol. 6, 541-550
  5. S. E. Wiliams, T. I. Brown, A. Roghanian and J. M. Sallnave (2006). SLPI and elafin: One glove, many fingers, Clin. Sci. (lond). 110, 21-35
  6. O. Wiedow and U. Meyer-Hoffert (2005). Neutrophil serine protease: potential key regulators of cell signaling during inflammation, J. Intern. Med. 257, 319-328
  7. I. Patel, T. Seemungal, M. Wilks, S. Lloyd-Owen, G. Donaldson and J. Wedzicha (2002). Relationship between bacterial colonization and the frequency, character and severity of COPD exacerbations, Thorax 57, 759-764
  8. W. L. Lee and G. P. Downey (2001). Leukocyte elastase physiological functions and role in acute lung injury, Am. J. Respir. Crit. Care Med. 164, 896-904
  9. H. Takeuchi, T. Gomi, M. Shishido, H. Watanabe and N. Suenobu (2010). Neutrophil elastase contributes to extracellular matrix damage induced by chronic low-dose UV irradiation in a hairless mouse photoaging model, J. Dermatol. Sci. 60, 151-158
  10. G. H. Xu, Y. H. Kim, S. J. Choo, I. J. Ryoo, J. K. Yoo, J. S. Ahn and I. D. Yoo (2009). Chemical constituents from the leaves of Ilex paraguariensis inhibit human neutrophil elastase, Arch. Pharm. Res. 32, 1215-1220
  11. H. Ma, X. He, Y. Yang, M. Li, D. Hao and Z. Jia (2011). The genus Epimedium: an ethnopharmacological and phytochemical review, J. Ethnopharmacol. 134, 519-541
  12. C. Yin, Y. Deng, J. Gao, X. Li, Y. Liu and Q. Gong (2016). Icariside II, a novel phosphodiesterase-5 inhibitor, attenuates streptozotocin-induced cognitive deficits in rats, Neuroscience 328, 69-79
  13. B. Y. Ahn (2009). Free radical scavenging effect of ethanol exract from Areca catechu, J. Korean Soc. Appl. Biol. Chem. 52, 92-95
  14. J. Zhang, C. Zhou, H. Li and R. Li (2014). A new furan flavonol glycoside from Epimedium koreanum, Chin. Herb. Med. 6, 168-170
  15. J. Y. Kim, J. H. Lee, Y. H. Song, W. M. Jeong, X. Tan, Z. Uddin an