Abstract
To develop angiotensin I converting enzyme (ACE) inhibitory chitin derivatives based on the properties of ACE inhibitors, chitins with different degree of deacetylation were chemically modified by grafting 2‐chloroethylamino hydrochloride onto chitin at the C‐6 position. Three kinds of chitin derivatives were prepared and designated as aminoethyl‐chitin (AEC) with 10% degree of deacetylation, aminoethyl‐chitin with 50% degree of deacetylation (AEC50), and aminoethyl‐chitin with 90% degree of deacetylation (AEC90). IC~50~ values of three chitin derivatives on ACE were 0.064 μ__M__ (AEC), 0.038 μ__M__ (AEC50), and 0.103 μ__M__ (AEC90). The results of Dixon plots revealed that AEC50 was a competitive inhibitor, and the inhibition constant (K~i~) value was 0.021 μ__M__. In addition, the antihypertensive effect of AEC50 on spontaneously hypertensive rats (SHR) was evaluated, and the result showed that it effectively decreased systolic blood pressure (SBP) in a dose‐dependent manner. © 2006 Wiley Periodicals, Inc. Biopolymers 83: 250–254, 2006
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