Simvastatin induces degradation of the extracellular matrix in human leiomyomata: novel in vitro, in vivo, and patient level evidence of matrix metalloproteinase involvement

F S Sci. 2024 Feb;5(1):80-91. doi: 10.1016/j.xfss.2023.11.005. Epub 2023 Dec 2.

Abstract

Objectives: To assess the effect of simvastatin on uterine leiomyoma growth and extracellular matrix (ECM) deposition.

Design: Laboratory analysis of human leiomyoma cell culture, xenograft in a mouse model, and patient tissue from a clinical trial.

Setting: Academic research center.

Patient(s): Tissue culture from human leiomyoma tissue and surgical leiomyoma tissue sections from a placebo-controlled randomized clinical trial.

Intervention(s): Simvastatin treatment.

Main outcome measure(s): Serum concentrations, xenograft volumes, and protein expression.

Results: Mice xenografted with 3-dimensional human leiomyoma cultures were divided as follows: 7 untreated controls; 12 treated with activated simvastatin at 10 mg/kg body weight; and 15 at 20 mg/kg body weight. Simvastatin was detected in the serum of mice injected at the highest dose. Xenograft volumes were significantly smaller (mean 53% smaller at the highest concentration). There was dissolution of compact ECM, decreased ECM formation, and lower collagen protein expression in xenografts. Membrane type 1 matrix metalloproteinase was increased in vitro and in vivo. Matrix metalloproteinase 2 and low-density lipoprotein receptor-related protein 1 were increased in vitro.

Conclusions: Simvastatin exhibited antitumoral activity with ECM degradation and decreased leiomyoma tumor volume in vivo. Activation of the matrix metalloproteinase 2, membrane type 1 matrix metalloproteinase, and low-density lipoprotein receptor-related protein 1 pathway may explain these findings.

Trial registration: ClinicalTrials.gov NCT03400826.

Keywords: Simvastatin; collagen; extracellular matrix; uterine leiomyoma; xenograft.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Body Weight
  • Extracellular Matrix / metabolism
  • Extracellular Matrix / pathology
  • Female
  • Humans
  • Leiomyoma* / drug therapy
  • Lipoproteins, LDL / metabolism
  • Lipoproteins, LDL / pharmacology
  • Lipoproteins, LDL / therapeutic use
  • Matrix Metalloproteinase 14 / metabolism
  • Matrix Metalloproteinase 14 / pharmacology
  • Matrix Metalloproteinase 2 / metabolism
  • Matrix Metalloproteinase 2 / pharmacology
  • Mice
  • Simvastatin / metabolism
  • Simvastatin / pharmacology
  • Simvastatin / therapeutic use
  • Uterine Neoplasms* / drug therapy
  • Uterine Neoplasms* / metabolism
  • Uterine Neoplasms* / pathology

Substances

  • Matrix Metalloproteinase 2
  • Simvastatin
  • Matrix Metalloproteinase 14
  • Lipoproteins, LDL

Associated data

  • ClinicalTrials.gov/NCT03400826