Renin inhibition activity by chitooligosaccharides

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2471-4. doi: 10.1016/j.bmcl.2008.02.041. Epub 2008 Feb 19.

Abstract

Six kinds of chitooligosaccharides (COSs) with different molecular weight (MW) and degree of deacetylation (DD) were prepared using ultrafiltration membrane reactor, and their renin inhibition modes were evaluated. All the COSs showed the renin-inhibitory activities with dose-dependent manner, and 90-COSs had the potent renin-inhibitory activity than that of 50-COSs. Among them, 90-MMWCOS (1000-5000Da) exhibits the highest activity with IC(50) value of 0.51mg/mL and acts as competitive inhibitor with K(i) value of 0.28mg/mL by Lineweaver-Burk and Dixon plots. These results indicated that DD value and MW of COSs are important factors affecting renin-inhibitory activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation
  • Angiotensin-Converting Enzyme Inhibitors / chemical synthesis
  • Angiotensin-Converting Enzyme Inhibitors / pharmacology*
  • Chitin / analogs & derivatives
  • Chitin / chemical synthesis
  • Chitin / pharmacology*
  • Dose-Response Relationship, Drug
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Molecular Weight
  • Oligosaccharides / chemical synthesis
  • Oligosaccharides / pharmacology*
  • Renin / antagonists & inhibitors*

Substances

  • Angiotensin-Converting Enzyme Inhibitors
  • Oligosaccharides
  • Chitin
  • Renin