Skip to main content
U.S. Department of Energy
Office of Scientific and Technical Information

Potential candidate genomic biomarkers of drug induced vascular injury in the rat

Journal Article · · Toxicology and Applied Pharmacology
 [1];  [1];  [2];  [2]
  1. Department of Safety Assessment, King of Prussia, PA 19406 (United States)
  2. Department of Quantitative Sciences GlaxoSmithKline, King of Prussia, PA 19406 (United States)

Drug-induced vascular injury is frequently observed in rats but the relevance and translation to humans present a hurdle for drug development. Numerous structurally diverse pharmacologic agents have been shown to induce mesenteric arterial medial necrosis in rats, but no consistent biomarkers have been identified. To address this need, a novel strategy was developed in rats to identify genes associated with the development of drug-induced mesenteric arterial medial necrosis. Separate groups (n = 6/group) of male rats were given 28 different toxicants (30 different treatments) for 1 or 4 days with each toxicant given at 3 different doses (low, mid and high) plus corresponding vehicle (912 total rats). Mesentery was collected, frozen and endothelial and vascular smooth muscle cells were microdissected from each artery. RNA was isolated, amplified and Affymetrix GeneChip Registered-Sign analysis was performed on selectively enriched samples and a novel panel of genes representing those which showed a dose responsive pattern for all treatments in which mesenteric arterial medial necrosis was histologically observed, was developed and verified in individual endothelial cell- and vascular smooth muscle cell-enriched samples. Data were confirmed in samples containing mesentery using quantitative real-time RT-PCR (TaqMan Trade-Mark-Sign ) gene expression profiling. In addition, the performance of the panel was also confirmed using similarly collected samples obtained from a timecourse study in rats given a well established vascular toxicant (Fenoldopam). Although further validation is still required, a novel gene panel has been developed that represents a strategic opportunity that can potentially be used to help predict the occurrence of drug-induced mesenteric arterial medial necrosis in rats at an early stage in drug development. -- Highlights: Black-Right-Pointing-Pointer A gene panel was developed to help predict rat drug-induced mesenteric MAN. Black-Right-Pointing-Pointer A gene panel was identified following treatment of rats with 28 different toxicants. Black-Right-Pointing-Pointer There was a strong correlation of genes and histologic evidence of mesenteric MAN. Black-Right-Pointing-Pointer Many genes were also regulated prior to histologic evidence of arterial effects.

OSTI ID:
22212574
Journal Information:
Toxicology and Applied Pharmacology, Journal Name: Toxicology and Applied Pharmacology Journal Issue: 2 Vol. 257; ISSN TXAPA9; ISSN 0041-008X
Country of Publication:
United States
Language:
English

Similar Records

A novel adipocytokine, chemerin exerts anti-inflammatory roles in human vascular endothelial cells
Journal Article · Fri Jun 22 00:00:00 EDT 2012 · Biochemical and Biophysical Research Communications · OSTI ID:22207907

All-trans retinoic acid protects against arsenic-induced uterine toxicity in female Sprague-Dawley rats
Journal Article · Wed Dec 14 23:00:00 EST 2011 · Toxicology and Applied Pharmacology · OSTI ID:22212571

MicroRNA changes in rat mesentery and serum associated with drug-induced vascular injury
Journal Article · Wed Aug 01 00:00:00 EDT 2012 · Toxicology and Applied Pharmacology · OSTI ID:22215868