A neutrophil multitarget functional bioassay to detect anti-inflammatory natural products
2002 (English)In: Journal of natural products (Print), ISSN 0163-3864, E-ISSN 1520-6025, Vol. 65, no 1, 32-41 p.Article in journal (Refereed) Published
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 Digitalbis 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.
Place, publisher, year, edition, pages
2002. Vol. 65, no 1, 32-41 p.
IdentifiersURN: urn:nbn:se:uu:diva-63205DOI: 10.1021/np010323oISI: 000173618200009PubMedID: 11809061OAI: oai:DiVA.org:uu-63205DiVA: diva2:91116