Amphiphilic cationic drugs and phospholipids influence the activities of beta-galactosidase and beta-glucosidase from liver lysosomal fraction of untreated rats.
The influence of amphiphilic drugs and phospholipids on the activities of beta-galactosidase and beta-glucosidase from liver lysosomal fractions of untreated rats, isolated by affinity chromatography using castor bean lectins, was studied in vitro. Chloroquine (93 microM) inhibited beta-galactosidase activity by about 30%, while O,O'-bis(diethylaminoethyl)hexestrol showed no inhibitory effect. Neutral phospholipids (phosphatidylcholine, phosphatidylethanolamine, sphingomyelin) inhibited the enzyme slightly, while the enzyme activity was drastically reduced in the presence of acidic phospholipids (phosphatidylinositol, phosphatidylserine, bis-(monoacylglycero)phosphate). Lysosomal beta-glucosidase was strongly inhibited by chloroquine and O,O'-bis(diethylaminoethyl)-hexestrol. The neutral phospholipids showed only a moderate inhibitory effect, whereas the acidic phospholipids were stimulators. Bis(monoacylglycero)phosphate was by far the best stimulating compound.
Harder
A
A
Dodt
G
G
Debuch
H
H
D000818:Animals; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002738:Chloroquine / Q000494:pharmacology; D002846:Chromatography, Affinity; D005260:Female; D005696:Galactosidases / Q000037:antagonists & inhibitors*; D005959:Glucosidases / Q000037:antagonists & inhibitors*; D006589:Hexestrol / Q000031:analogs & derivatives / Q000494:pharmacology; D066298:In Vitro Techniques; D008099:Liver / Q000201:enzymology*; D008246:Lysophospholipids; D008247:Lysosomes / Q000201:enzymology*; D050178:Monoglycerides; D010712:Phosphatidic Acids; D010743:Phospholipids / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D001616:beta-Galactosidase / Q000037:antagonists & inhibitors*; D001617:beta-Glucosidase / Q000037:antagonists & inhibitors*
D008246:Lysophospholipids; D050178:Monoglycerides; D010712:Phosphatidic Acids; D010743:Phospholipids; C012786:bis(monoacylglyceryl)phosphate; D006589:Hexestrol; D002738:Chloroquine; D005696:Galactosidases; D005959:Glucosidases; D001617:beta-Glucosidase; D001616:beta-Galactosidase; C100116:hexestrol bis(diethylaminoethyl ether)