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Prolyl endopeptidase inhibitors from caryophylli flos

Archives of Pharmacal Research volume 21, pages 207–211 (1998)Cite this article

Abstract

Three prolyl endopeptidase inhibitors were isolated and identified as luteolin, quercetin and β-sitosterol-3-O-β-D-glucopyranoside with IC50 of 0.17, 0.19 and 27.5 ppm, respectively. The inhibition of two flavonoids were non-competitive with substrate. Twenty authentic flavonoids were tested in order to investigate structure-activity relationship. No significant relationship was found in them, however, catechol moiety of B-ring and 7-OH group in flavonoid skeleton were seemed to be responsible for the stronger activity.

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Author notes

  1. Jong Hwan Kwak

    Present address: Division of Applied Science, Korea Institute of Science and Technology, 136-650, Seoul, Korea

Affiliations

  1. Department of Agricultural Chemistry, College of Agriculture, Kyungpook National University, 1370 Sankyuk-Dong, 702-701, Taegu, Korea

    Kyung-Hee Lee & Kyung-Sik Song

  2. College of Pharmacy, SungKyunKwan University, 440-746, Suwon, Korea

    Jong Hwan Kwak

  3. Department of Chemistry, KonYang University, 320-800, Nonsan, Chungnam, Korea

    Kyung-Bok Lee

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  1. Kyung-Hee Lee
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  2. Jong Hwan Kwak
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  3. Kyung-Bok Lee
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  4. Kyung-Sik Song
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Lee, KH., Kwak, J.H., Lee, KB. et al. Prolyl endopeptidase inhibitors from caryophylli flos. Arch. Pharm. Res. 21, 207–211 (1998). https://doi.org/10.1007/BF02974029

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  • DOI: https://doi.org/10.1007/BF02974029

Key words

  • Prolyl endopeptidase inhibitor
  • Eugenia caryophyllata
  • Caryophylli Flos
  • Luteolin
  • Quercetin
  • Flavonoids
  • β-sitosterol-3-O-β-D-glucopyranoside