Structure-activity relationships of gagaminine and its derivatives on the inhibition of hepatic aldehyde oxidase activity and lipid peroxidation.
In order to determine the structure-activity relationships for antioxidative effects of gagaminine, a steroidal alkaloid isolated from the roots of Cynanchum wilfordi (Asclepiadaceae), two derivatives identified as sarcostin and penupogenin were prepared from gagaminine by hydrolysis and reduction. These compounds were evaluated for the inhibitory effects on the aldehyde oxidase activity and on lipid peroxidation in vitro. Furthermore, their effects were compared with those of gagaminine and the related compounds, cinnamic acid and nicotinic acid. The results of this study prove that the cinnamoyl group in the structure of gagaminine is critical in inhibition of the aldehyde oxidase activity while the nicotinoyl group may be necessary for anti-lipid peroxidation of the compound.
Lee
D U
DU
Department of Biochemistry, College of Natural Science, Dongguk University, Kyongju, Korea.
Shin
U S
US
Huh
K
K
D000445:Aldehyde Oxidoreductases / Q000302:isolation & purification / Q000378:metabolism*; D000818:Animals; D000975:Antioxidants / Q000494:pharmacology*; D002934:Cinnamates / Q000494:pharmacology*; D015227:Lipid Peroxidation / Q000187:drug effects*; D008099:Liver / Q000187:drug effects / Q000201:enzymology*; D008297:Male; D011283:Pregnenes / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D000975:Antioxidants; D002934:Cinnamates; D011283:Pregnenes; C116955:sarcostin; C116953:penupogenin; C116954:gagaminine; D000445:Aldehyde Oxidoreductases