Abstract
A multitarget functional bioassay was optimized as a method for detecting substances interacting with the inflammatory process of activated neutrophil granulocytes, mainly to release elastase detected by p-nitroanilide (pNA) formation. Using this bioassay, 100 fractionated extracts of 96 plants were screened, with results presented in a manner that links recorded biological activity to phylogenetic information. The plants were selected to represent a major part of the angiosperms, with emphasis on medicinal plants, Swedish anti-inflammatory plants, and plants known to contain peptides. Of the tested extracts, 41% inhibited pNA formation more than 60%, and 3% stimulated formation. The extract of Digitalis purpurea enhanced pNA formation, and digitoxin, the active compound, was isolated and identified. Plant extracts that exhibited potent nonselective inhibition (>80% inhibition) were evaluated further for direct inhibition of isolated elastase and trypsin enzyme. The inhibitory effect of most tested extracts on the isolated enzyme elastase was similar to that of PAF- and fMLP-induced pNA formation. Compared to trypsin, inhibition of elastase by extracts of Rubus idaeus and Tabernaemontana dichotoma was significantly higher (80% and 99%, respectively). Inhibition of trypsin by the extract of Reseda luteola was high (97%). Orders such as Lamiales and Brassicales were shown to include a comparably high proportion of plants with inhibitory extracts.
Publication types
-
Comparative Study
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Anti-Inflammatory Agents / chemistry
-
Anti-Inflammatory Agents / isolation & purification
-
Anti-Inflammatory Agents / pharmacology*
-
Benzoylarginine Nitroanilide / analysis
-
Biological Assay / methods*
-
Biological Products / chemistry
-
Biological Products / isolation & purification
-
Biological Products / pharmacology*
-
Cytochalasin B
-
Digitalis / chemistry
-
Digitonin / chemistry
-
Digitonin / pharmacology
-
Digitoxin / chemistry
-
Digitoxin / isolation & purification
-
Digitoxin / pharmacology
-
Dose-Response Relationship, Immunologic
-
Hemolysis
-
Humans
-
Lamiaceae / chemistry
-
Leukocyte Elastase / analysis*
-
Leukocyte Elastase / antagonists & inhibitors
-
Leukocyte Elastase / metabolism
-
Magnoliopsida / chemistry*
-
N-Formylmethionine Leucyl-Phenylalanine
-
Neutrophil Activation* / drug effects
-
Neutrophils* / drug effects
-
Neutrophils* / enzymology
-
Peptides
-
Plant Proteins / analysis
-
Plant Proteins / chemistry
-
Plant Proteins / pharmacology
-
Plants, Medicinal / chemistry*
-
Plants, Medicinal / classification*
-
Platelet Activating Factor
-
Superoxides / pharmacology
-
Sweden
-
Tabernaemontana / chemistry
-
Trypsin Inhibitors
-
Violaceae / chemistry
-
alpha-Amylases / antagonists & inhibitors
Substances
-
Anti-Inflammatory Agents
-
Biological Products
-
Peptides
-
Plant Proteins
-
Platelet Activating Factor
-
Trypsin Inhibitors
-
Superoxides
-
Cytochalasin B
-
N-Formylmethionine Leucyl-Phenylalanine
-
Benzoylarginine Nitroanilide
-
Digitoxin
-
alpha-Amylases
-
Leukocyte Elastase
-
Digitonin