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<p>Peptides from natural sources have often served as valuable leads in drug discovery. Plant-derived protease inhibitors are a notable class, yet their distribution, diversity, and targets remain underexplored. Here, eleven tropical Psychotria species were screened for cyclic cysteine-rich peptides, with extracts showing concentration-dependent inhibition of human prolyl oligopeptidase (POP). Peptidomics combining mass spectrometry and transcriptome mining revealed multiple inhibitory peptides. From <i>Psychotria solitudinum</i>, which contained 37 peptides, a novel peptide (psysol 3) was purified and sequenced. Its synthetic analogue inhibited POP with an IC<sub>50</sub> of ~ 1.3&#xa0;µM. Sequence analysis and synthetic probes identified loop 3 as the inhibitory motif. Psysol 3 is a new probe for POP pharmacology and future structure–activity studies.</p>

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Tropical psychotria plants are a rich source for peptide inhibitors of human prolyl oligopeptidase

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年4月14日

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  • Roland Hellinger,
  • Paula Schwarz,
  • Jonathan Dieringer,
  • Carina Ebermann,
  • Kirtikumar B. Jadhav,
  • Markus Muttenthaler,
  • Christian W. Gruber

摘要

Peptides from natural sources have often served as valuable leads in drug discovery. Plant-derived protease inhibitors are a notable class, yet their distribution, diversity, and targets remain underexplored. Here, eleven tropical Psychotria species were screened for cyclic cysteine-rich peptides, with extracts showing concentration-dependent inhibition of human prolyl oligopeptidase (POP). Peptidomics combining mass spectrometry and transcriptome mining revealed multiple inhibitory peptides. From Psychotria solitudinum, which contained 37 peptides, a novel peptide (psysol 3) was purified and sequenced. Its synthetic analogue inhibited POP with an IC50 of ~ 1.3 µM. Sequence analysis and synthetic probes identified loop 3 as the inhibitory motif. Psysol 3 is a new probe for POP pharmacology and future structure–activity studies.