Human neutrophil elastase inhibitory dihydrobenzoxanthones and alkylated flavones from the Artocarpus elasticus root barksopen access
- Ban, Yeong Jun; Baiseitova, Aizhamal; Nafiah, Mohd Azlan; Kim, Jeong Yoon; Park, Ki Hun
- Issue Date
- SPRINGER SINGAPORE PTE LTD
- Alkylated flavones; Artocarpus elasticus; Dihydrobenzoxanthones; Fluorescence quenching; Human neutrophil elastase inhibition (HNE)
- APPLIED BIOLOGICAL CHEMISTRY, v.63, no.1
- Journal Title
- APPLIED BIOLOGICAL CHEMISTRY
- Neutrophil elastases are deposited in azurophilic granules interspace of neutrophils and tightly associated with inflammatory ailments. The root barks ofArtocarpus elasticushad a strong inhibitory potential against human neutrophil elastase (HNE). The responsible components for HNE inhibition were confirmed as alkylated flavones (2-4, IC50 = 14.8 similar to 18.1 mu M) and dihydrobenzoxanthones (5-8, IC50 = 9.8 similar to 28.7 mu M). Alkyl groups on flavone were found to be crucial functionalities for HNE inhibition. For instance, alkylated flavone2(IC50 = 14.8 mu M) was 20-fold potent than mother compound norartocarpetin (1, IC50 > 300 mu M). The kinetic analysis showed that alkylated flavones (2-4) were noncompetitive inhibition, while dihydrobenzoxanthones (5-8) were a mixed type I (K-I < K-IS) inhibitors, which usually binds with free enzyme better than to complex of enzyme-substrate. Inhibitors and HNE enzyme binding affinities were examined by fluorescence quenching effect. In the result, the binding affinity constants (K-SV) had a significant correlation with inhibitory potencies (IC50).
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- 자연과학대학 > Department of Pharmaceutical Engineering > Journal Articles
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