Sodium houttuyfonate alleviates monocrotaline-induced pulmonary hypertension by regulating canonical transient receptor potential channel proteins

Eur J Pharmacol. 2026 Jan 30:1013:178507. doi: 10.1016/j.ejphar.2025.178507. Epub 2025 Dec 25.

Abstract

Elevated intracellular Ca2+ concentration ([Ca2+]i), resulting from store-operated calcium entry (SOCE), serves as a pivotal trigger for the proliferation of pulmonary arterial smooth muscle cells (PASMCs) and plays a crucial role in the pathogenesis of pulmonary hypertension (PH). As the crucial constituents of the store-operated Ca2+ channel (SOCC), canonical transient receptor potential channel (TRPC) proteins, particularly TRPC1, TRPC4, and TRPC6 are upregulated in monocrotaline-induced PH (MCT-PH). Sodium houttuyfonate (SH) is a compound derived from the combination of sodium bisulfite and houttuynin, and has been scientifically proven to possess a wide range of antibacterial, anti-inflammatory, and cardiovascular protective properties. In this study, we investigated the contributions of TRPC1, TRPC4, and TRPC6 to MCT-enhanced SOCE-[Ca2+]i and PASMC proliferation. Furthermore, based on the actions of TRPC1, TRPC4 and TRPC6, we explored the mechanism by which SH mitigates MCT-PH. The results revealed that: 1) TRPC1, TRPC4, and TRPC6 played significant roles in MCT-induced enhancement of SOCE-[Ca2+]i and PASMC proliferation; 2) SH exhibited suppressive effects on the expression levels of TRPC1, TRPC4, TRPC6 and NF-κB in distal pulmonary arteries (PAs) and cultured PASMCs. 3) Overexpression of either TRPC1, TRPC4 or TRPC6 attenuated the inhibitory effect of SH on MCT-elevated SOCE-[Ca2+]i and PASMC proliferation. 4) SH down-regulated the interaction between STIM1 and TRPC1, TRPC4 or TRPC6 in distal PAs and cultured PASMCs from MCT-PH model rats. The present findings provide compelling evidence that SH effectively mitigates MCT-PH by inhibiting PASMC proliferation through the TRPC1,4,6-SOCE-[Ca2+]i pathway, likely mediated by NF-κB and STIM1.

Keywords: MCT-PH; PASMCs; SOCE; Sodium houttuyfonate; [Ca(2+)](i).

MeSH terms

  • Alkanes
  • Animals
  • Calcium / metabolism
  • Cell Proliferation / drug effects
  • Hypertension, Pulmonary* / chemically induced
  • Hypertension, Pulmonary* / drug therapy
  • Hypertension, Pulmonary* / metabolism
  • Hypertension, Pulmonary* / pathology
  • Male
  • Monocrotaline*
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / metabolism
  • Myocytes, Smooth Muscle / drug effects
  • Myocytes, Smooth Muscle / metabolism
  • Myocytes, Smooth Muscle / pathology
  • NF-kappa B / metabolism
  • Pulmonary Artery / drug effects
  • Pulmonary Artery / metabolism
  • Pulmonary Artery / pathology
  • Rats
  • Rats, Sprague-Dawley
  • Sulfites* / pharmacology
  • Sulfites* / therapeutic use
  • TRPC Cation Channels* / genetics
  • TRPC Cation Channels* / metabolism
  • TRPC6 Cation Channel / metabolism

Substances

  • Monocrotaline
  • TRPC Cation Channels
  • sodium houttuyfonate
  • Sulfites
  • NF-kappa B
  • transient receptor potential cation channel, subfamily C, member 1
  • Calcium
  • Trpc6 protein, rat
  • TRPC6 Cation Channel
  • Alkanes