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Ban Yeong Jun,Baiseitova Aizhamal,Nafiah Mohd Azlan,Kim Jeong Yoon,Park Ki Hun 한국응용생명화학회 2020 Applied Biological Chemistry (Appl Biol Chem) Vol.63 No.5
Neutrophil elastases are deposited in azurophilic granules interspace of neutrophils and tightly associated with inflammatory ailments. The root barks of Artocarpus elasticus had 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 ~ 18.1 μM) and dihydrobenzoxanthones (5–8, IC50 = 9.8 ~ 28.7 μM). Alkyl groups on flavone were found to be crucial functionalities for HNE inhibition. For instance, alkylated flavone 2 ( IC50 = 14.8 μM) was 20-fold potent than mother compound norartocarpetin (1, IC50 > 300 μM). The kinetic analysis showed that alkylated flavones (2–4) were noncompetitive inhibition, while dihydrobenzoxanthones (5–8) were a mixed type I (KI < KIS) 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 (KSV) had a significant correlation with inhibitory potencies ( IC50).
Wang, Yan,Kim, Jeong Yoon,Song, Yeong Hun,Li, Zuo Peng,Yoon, Sang Hwa,Uddin, Zia,Ban, Yeong Jun,Lee, Keun Woo,Park, Ki Hun Elsevier 2019 INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES Vol.128 No.-
<P><B>Abstract</B></P> <P>The chromenone derivatives (<B>1</B>–<B>4</B>) from the root part of <I>Flemingia philippinensis</I> showed a significant inhibition against bacterial neuraminidase (NA) which plays a pivotal role in a cellular interaction including pathogenesis of bacterial infection and subsequent inflammation. The compounds <B>1</B> and <B>2</B> were the new compounds, philippin D (<B>1</B>) and philippin E (<B>2</B>). In particular, compounds (<B>1</B>–<B>3</B>) exhibited sub micromolar levels of IC<SUB>50</SUB> values with 0.75, 0.54, and 0.07 μM. This is the first report that chromenone skeleton emerged as a lead structure of bacterial NA inhibition. In kinetic study, 8,8-diprenyl compounds displayed competitive inhibitory mode, whereas 4a,8-diprenyl ones showed noncompetitive behavior. It was manifested that all competitive inhibitors (<B>1</B> and <B>2</B>) were simple reversible slow-binding against bacterial NA. The binding affinities (<I>K</I> <SUB>SV</SUB>) of inhibitors to enzyme were agreement with their respective inhibitory potencies. Molecular docking data confirmed that the position of 3-methyl-2-butenyl substituent affects inhibitory mechanism against <I>Cp</I>NanI. The tri-arginyl cluster of R266, R555, and R615 and D291 in NanI tightly interact with the competitive inhibitors.</P>
Li, Zuo Peng,Kim, Jeong Yoon,Ban, Yeong Jun,Park, Ki Hun Elsevier 2019 Bioorganic chemistry Vol.90 No.-
<P><B>Abstract</B></P> <P>In the course of an investigation of human neutrophil elastase (HNE) associated with inflammation, the extract of the flower parts of <I>Hypericum ascyron</I> showed a significant influence to HNE. The responsible metabolites to HNE inhibition were found to be eight polyprenylated acylphloroglucinols, PPAPs (<B>1</B>–<B>8</B>) which showed IC<SUB>50</SUB> ranges between 2.4 and 19.9 μM. This is the first report to demonstrate that PPAP skeleton exhibits potent HNE inhibition. The compounds <B>1</B>–<B>3</B> were characterized and newly named as ascyronone E (IC<SUB>50</SUB> = 4.3 μM), ascyronone F (IC<SUB>50</SUB> = 19.9 μM), ascyronone G (IC<SUB>50</SUB> = 4.5 μM) based on 2D-NMR spectroscopic data. In the kinetic analysis of double reciprocal plots, all the compounds showed noncompetitive behaviors to HNE enzyme with the remaining of <I>K</I> <SUB>m</SUB> and the increase of <I>V</I> <SUB>max</SUB>. The binding affinity levels (<I>K</I> <SUB>SV</SUB>) by using fluorescence were sufficient to be able to prove that PPAPs (<B>1</B>–<B>8</B>) had compliant interaction with inhibitory potencies.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Eight human neutrophil elastase (HNE) inhibitors were isolated from the flowers of <I>Hypericum ascyron.</I> </LI> <LI> Ascyronones E-G were identified as new polycyclic polyprenylated acylphloroglucinols (PPAPs). </LI> <LI> The isolated acylphloroglucinols showed a significant HNE inhibition with noncompetitive behavior. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Effect of Photopolymerization on the Rate of Photocrosslink in Chalcone-based Oligomeric Compounds
최동훈,오상준,반시영,오광용,Choe, Dong Hun,O, Sang Jun,Ban, Si Yeong,O, Gwang Yong Korean Chemical Society 2001 Bulletin of the Korean Chemical Society Vol.22 No.11
A new photochemically bifunctional epoxy and dimethacrylate compounds were synthesized for investigating the photosensitivity under UV irradiation. Photosensitivity of the synthesized chalcone-based compounds was investigated by using UV-visible absorption and Fourier transformed infrared (FT-IR) spectroscopies. The result of spectroscopic analysis substantiated that the two chalcone-based compounds have functions of both photocrosslinking and photopolymerization by UV exposure in the presence of photoinitiator. Two kinds of photochemical reactions proceeded competitively during UV exposure. Particularly, we studied the effect of photopolymerization on the rate of photocrosslink due to cycloaddition in the two oligomeric compounds.