Inhibition of Candida rugosa lipase by berberine and structurally related alkaloids, evaluated by high-performance liquid chromatography.
It is known that certain microorganisms produce extracellular lipase to better colonize the skin and mucosal surfaces. Since different extracts from medicinal plants have anti-lipase activity (Shimura et al., Biosci. Biotechnol. Biochem., 56: 1478-1479, 1992), we examined the effects of selected natural substances on Candida rugosa lipase. In the presence of the compounds under examination, the enzyme was incubated with beta-naphthyl laurate, and beta-naphthol, produced by the enzymatic reaction, was extracted with ethyl acetate and analyzed by reversed phase HPLC, using a C-18 column. Thus, the inhibitory activity was calculated by a proper formula based on the variations of the area under the chromatographic peak of beta-naphthol. The method was validated by analyzing substances with known anti-lipase activity such as saturated fatty acids (C10-16) and tetracycline. Berberine and a number of structurally related alkaloids such as chelidonine, chelerythrine, and sanguinarine appeared active. This property of berberine and sanguinarine is of interest because they are used in pathological conditions in which microbial lipases could play a pathogenic role.
Grippa
E
E
Department of Pharmacology of Natural Substances and General Physiology, University of Rome La Sapienza, Italy.
Valla
R
R
Battinelli
L
L
Mazzanti
G
G
Saso
L
L
Silvestrini
B
B
D000470:Alkaloids / Q000737:chemistry / Q000494:pharmacology*; D000890:Anti-Infective Agents / Q000494:pharmacology; D001599:Berberine / Q000737:chemistry / Q000494:pharmacology*; D002175:Candida / Q000201:enzymology* / Q000472:pathogenicity; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005227:Fatty Acids / Q000494:pharmacology; D006801:Humans; D008049:Lipase / Q000032:analysis / Q000037:antagonists & inhibitors*; D012867:Skin / Q000382:microbiology
D000470:Alkaloids; D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; D005227:Fatty Acids; D001599:Berberine; D008049:Lipase