Effects of manidipine on DNA and protein syntheses in cultured vascular smooth muscle and endothelial cells and on proto-oncogene expression

Blood Press Suppl. 1992:3:30-5.

Abstract

To elucidate the importance of Ca2+ influx via voltage-dependent Ca2+ channels in the mechanism of vascular remodeling, we investigated effects of a new Ca2+ channel blocker manidipine on DNA and protein syntheses stimulated by several mitogens in cultured rat vascular smooth muscle cells (VSMC) and bovine endothelial cells (EC), and growth-related immediate early proto-oncogenes expression in VSMC. Endothelin-1 (ET-1) induced receptor-mediated phosphoinositide breakdown and increased cytosolic free Ca2+ levels in rat VSMC, with concomitant increases in proto-oncogenes (c-fos c-myc) mRNA levels as well as DNA and protein syntheses. Manidipine dose-dependently (10(-9) M to 10(-6) M) inhibited DNA, and protein syntheses stimulated by 10(-7) M ET-1 in rat VSMC; manidipine was a more potent inhibitor for protein synthesis (IC50: 10(-8) M) than for DNA synthesis (IC50: 10(-7) M). Manidipine also inhibited DNA synthesis stimulated by 10 ng/mL bFGF and 2.5% FCS in rat VSMC and bovine EC; manidipine was more potent in inhibiting DNA synthesis stimulated by bFGF than that by FCS in both cells. The expression of ET-1-induced c-fos and c-myc mRNAs levels was unaffected by manidipine. These results suggest that manidipine has potent inhibitory effects on the ET-1-induced hyperplasia and/or hypertrophy of VSMC, as well as on the bFGF-induced hyperplasias of VSMC and EC, thus implicating its potential usefulness for preventing abnormal VSMC proliferation and angiogenesis associated with hypertension and atherosclerosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Northern
  • Calcium Channel Blockers / pharmacology*
  • Cattle
  • Cells, Cultured
  • DNA / biosynthesis*
  • DNA / drug effects
  • Dihydropyridines / pharmacology*
  • Endothelins / pharmacology
  • Endothelium, Vascular / drug effects*
  • Endothelium, Vascular / metabolism
  • Endothelium, Vascular / physiology
  • Gene Expression / drug effects*
  • Genes, fos / drug effects*
  • Genes, fos / genetics*
  • Genes, myc / drug effects*
  • Genes, myc / genetics*
  • Inositol 1,4,5-Trisphosphate / biosynthesis
  • Kinetics
  • Mitogens / pharmacology
  • Muscle Proteins / biosynthesis*
  • Muscle, Smooth, Vascular / drug effects*
  • Muscle, Smooth, Vascular / metabolism
  • Muscle, Smooth, Vascular / physiology
  • Nitrobenzenes
  • Piperazines
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Rats
  • Stimulation, Chemical

Substances

  • Calcium Channel Blockers
  • Dihydropyridines
  • Endothelins
  • Mitogens
  • Muscle Proteins
  • Nitrobenzenes
  • Piperazines
  • RNA, Messenger
  • manidipine
  • Inositol 1,4,5-Trisphosphate
  • DNA