Anti-inflammatory and analgesic properties of Polyphyllin VI revealed by network pharmacology and RNA sequencing

Purinergic Signal. 2024 Aug;20(4):449-463. doi: 10.1007/s11302-023-09979-2. Epub 2023 Nov 20.

Abstract

Inflammatory pain, sustained by a complex network of inflammatory mediators, is a severe and persistent illness affecting many of the general population. We explore possible anti-inflammatory pathways of Polyphyllin VI (PPVI) based on our prior study, which showed that PPVI reduces inflammation in mice to reduce pain. Network pharmacology and RNA-Seq identified the contribution of the MAPK signaling pathway to inflammatory pain. In the LPS/ATP-induced RAW264.7 cell model, pretreatment with PPVI for 1 h inhibited the release of IL-6 and IL-8, down-regulated expression of the P2X7 receptor(P2X7R), and decreased phosphorylation of p38 and ERK1/2 components of the MAPK pathway. Moreover, PPVI decreased expression of IL-6 and IL-8 was observed in the serum of the inflammatory pain mice model and reduced phosphorylation of p38 and ERK1/2 in the dorsal root ganglia while the reductions of expression of IL-6 and phosphorylation of ERK1/2 were not observed after the pre-treatment with A740003 (an antagonist of the P2X7R). These results suggest that PPVI may inhibit the release of IL-8 by regulating P2X7R to reduce the phosphorylation of p38. However, the modulation of PPVI on the release of IL-6 and phosphorylation of ERK1/2 may mediated by other P2X7R-independent signals.

Keywords: Inflammatory pain; Network pharmacology; P2X7 receptor; Polyphyllin VI; RNA sequencing.

MeSH terms

  • Analgesics* / pharmacology
  • Animals
  • Anti-Inflammatory Agents* / pharmacology
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • MAP Kinase Signaling System / drug effects
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Network Pharmacology*
  • Pain / drug therapy
  • Pain / metabolism
  • RAW 264.7 Cells
  • Receptors, Purinergic P2X7 / drug effects
  • Receptors, Purinergic P2X7 / metabolism
  • Sequence Analysis, RNA / methods

Substances

  • Anti-Inflammatory Agents
  • Analgesics
  • Receptors, Purinergic P2X7