ACE inhibition by astilbin isolated from Erythroxylum gonocladum (Mart.) O.E. Schulz.
Erythroxylum species have several traditional uses in different countries, including the treatment of hypertension. The ethanol extract from E. gonocladum aerial parts, a species endemic to the Brazilian cerrado, elicited a concentration-dependent inhibition of angiotensin converting enzyme (ACE) (pIC(50)=4.53+/-0.05). Extract fractionation led to the isolation of two compounds, whose structures were assigned by spectrometric data as astilbin and beta-sitosterol, along with a mixture of palmitic, stearic and linolenic acids. This is the first report on the occurrence of these compounds on E. gonocladum. Astilbin promoted significant ACE inhibition in vitro (pIC(50)=5.86+/-0.33) and its activity did not differ from captopril, when both compounds were assayed at 10 microM concentration.
Lucas-Filho
M D
MD
School of Pharmacy, Universidade Federal de Ouro Preto, Ouro Preto, Brazil.
Silva
G C
GC
Cortes
S F
SF
Mares-Guia
T R
TR
Perpétua Ferraz
V
V
Serra
C P
CP
Braga
F C
FC
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000959:Antihypertensive Agents / Q000302:isolation & purification / Q000494:pharmacology*; D001938:Brazil; D002216:Captopril; D004305:Dose-Response Relationship, Drug; D030921:Erythroxylaceae / Q000737:chemistry*; D005227:Fatty Acids / Q000302:isolation & purification; D044948:Flavonols / Q000302:isolation & purification / Q000494:pharmacology*; D007703:Peptidyl-Dipeptidase A / Q000378:metabolism*; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D012855:Sitosterols / Q000302:isolation & purification
D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D005227:Fatty Acids; D044948:Flavonols; D010936:Plant Extracts; D012855:Sitosterols; C099069:astilbin; C025473:gamma-sitosterol; D002216:Captopril; D007703:Peptidyl-Dipeptidase A