ABSTRACT
The hypotensive effects of Vaccinium ashei reade (blueberry) leaves were studied in vitro and in vivo. Blueberry leaf showed a strong inhibitory effect on angiotensin-converting enzyme activity in vitro. Additionally, feeding of blueberry leaf suppressed the development of essential hypertension in spontaneously hypertensive rats in vivo. These results promise the use of blueberry leaf as a source of dietary hypotensive components.
Subject(s)
Angiotensin-Converting Enzyme Inhibitors/chemistry , Angiotensin-Converting Enzyme Inhibitors/pharmacology , Blood Pressure/drug effects , Blueberry Plants/chemistry , Peptidyl-Dipeptidase A/metabolism , Animals , Body Weight/drug effects , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , RatsABSTRACT
The acyl group of an alpha-aryl-beta-keto ester was readily transferred to N-, O-, and S-nucleophiles. The transacylation from arylated diethyl 3-oxoglutarate to amines led to unsymmetrical malonic acid amide esters in high yields. The present reaction proceeded under mild conditions without formation of detectable byproducts. Only simple experimental manipulations were required. This reaction was also found to be sensitive to steric factors, which enabled the chemoselective monoacylation of diamines and amino alcohols without any modifications such as protection.
