Improvement of ACE inhibitory activity of chitooligosaccharides (COS) by carboxyl modification.
In the present research, chitooligosaccharides (COS) were carboxylated with -COCH(2)CH(2)COO(-) groups to obtain specific structural features similar to Captopril. Angiotensin I converting enzyme (ACE) inhibitory activity of carboxylated COS was studied and observed to enhance its activity with increased substitution degree. Further, Lineweaver-Burk plot analysis revealed that inhibition was competitive via obligatory binding site of the enzyme. This was accompanied with substitution of positively charged quarternized amino groups to COS with different substitution degrees, in which negative impact on ACE inhibition was observed.
Huang
Ronghua
R
Department of Chemistry, Pukyong National University, Busan 608-737, South Korea.
Mendis
Eresha
E
Kim
Se-Kwon
SK
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology*; D048271:Chitosan / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D009844:Oligosaccharides / Q000737:chemistry / Q000494:pharmacology*
D000806:Angiotensin-Converting Enzyme Inhibitors; D009844:Oligosaccharides; D048271:Chitosan