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Dec 29, 2001 - The extract of Digitalis purpurea enhanced pNA formation, and digitoxin, the active compound, was isolate

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Table of Contents

A Neutrophil Multitarget Functional Bioassay to Detect Anti-inflammatory Natural Products Senia Johansson,Ulf Göransson,Teus Luijendijk,Anders Backlund,Per Claeson, andLars Bohlin* Division of Pharmacognosy, Department of Medicinal Chemistry, Biomedical Centre, Uppsala University, PO Box 574, S751 23 Uppsala, Sweden

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J. Nat. Prod., 2002, 65 (1), pp 32–41 DOI: 10.1021/np010323o Publication Date (Web): December 29, 2001 Copyright © 2002 American Chemical Society and American Society of Pharmacognosy

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A multitarget functional bioassay was optimized as a method for detecting substances

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interacting with the inflammatory process of activated neutrophil granulocytes, mainly to release

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elastase detected by p-nitroanilide (pNA) formation. Using this bioassay, 100 fractionated

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extracts of 96 plants were screened, with results presented in a manner that links recorded

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biological activity to phylogenetic information. The plants were selected to represent a major part

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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

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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

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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. Retrieve Detailed Record of this Article

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

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extract of Reseda luteola was high (97%). Orders such as Lamiales and Brassicales were shown

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to include a comparably high proportion of plants with inhibitory extracts.

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