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Exploring Multifunctional Bioactive Components from Podophyllum sinense Using Multi-Target Ultrafiltration.

Huixia Feng1,2,3,4, Guilin Chen1,3,4, Yongli Zhang1,3,4

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|November 11, 2021
PubMed
Summary
This summary is machine-generated.

This study identifies key bioactive compounds in Podophyllum sinense using a novel UF-HPLC/MS method. These compounds show potential for developing new multi-target drugs from traditional herbal medicines.

Keywords:
Podophyllum sinenseanti-inflammatoryantiproliferativemulti-targetultrafiltration-LC/MS

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Area of Science:

  • Phytochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Podophyllum sinense (P. sinense) is a traditional herbal medicine with diverse pharmaceutical activities.
  • Identifying specific bioactive constituents and their targets for P. sinense's antiproliferative, anti-inflammatory, and antiviral effects is challenging due to complex chemical composition.

Purpose of the Study:

  • To develop and apply an affinity ultrafiltration with multiple drug targets coupled with high-performance liquid chromatography/mass spectrometry (UF-HPLC/MS) strategy.
  • To rapidly screen and identify bioactive compounds from P. sinense interacting with Topo I, Topo II, COX-2, and ACE2 drug targets.
  • To validate the antiproliferative and COX-2 inhibitory activities of identified compounds.

Main Methods:

  • Affinity ultrafiltration with multiple drug targets combined with UF-HPLC/MS.
  • In vitro antiproliferative assays against A549 and HT-29 cancer cell lines.
  • In vitro COX-2 inhibitory assays.
  • Molecular docking analysis.

Main Results:

  • 7, 10, 6, and 7 phytochemicals were identified as potential ligands for Topo I, Topo II, COX-2, and ACE2, respectively.
  • Diphyllin and podophyllotoxin showed significant antiproliferative activity against A549 and HT-29 cells, outperforming 5-FU and etoposide.
  • Diphyllin demonstrated potent COX-2 inhibitory activity (IC50 = 1.29 ± 0.14 μM), comparable to indomethacin.
  • Molecular docking validated the affinity of compounds like diphyllin and podophyllotoxin for the targeted enzymes.

Conclusions:

  • The integrated UF-HPLC/MS method effectively identifies multi-target bioactive components from P. sinense.
  • The study elucidates potential mechanisms of action for P. sinense's pharmacological effects.
  • Findings provide valuable insights for developing new multi-target drugs derived from natural sources.