• Bulletin of the Korean Chemical Society
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• v.32 no.9
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• pp.3219-3222
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• 2011

Three types of ${\beta}$-ketoacyl acyl carrier protein synthase (KAS) are important for overcoming the bacterial resistance problem. Recently, we reported the discovery of a antimicrobial flavonoid, YKAF01 (3,6-dihydroxyflavone), which exhibits antibacterial activity against Gram-positive bacteria through inhibition of ${\beta}$-ketoacyl acyl carrier protein synthase III (KAS III). In this report, we suggested that YKAF01 can be an inhibitor ${\beta}$-ketoacyl acyl carrier protein synthase I (KAS I) with dual inhibitory activity for KAS I as well as KAS III. KAS I is related to the elongation of unsaturated fatty acids in bacterial fatty acid synthesis and can be a good therapeutic target of designing novel antibiotics. We performed docking study of Escherichia coli KAS I (ecKAS I) and YKAF01, and determined their binding model. YKAF01 binds to KAS I with high binding affinity ($2.12{\times}10^6$) and exhibited an antimicrobial activity against the multidrug-resistant E. coli with minimal inhibitory concentration (MIC) value of 512 ${\mu}g$/mL. Further optimization of this compound will be carried out to improve its antimicrobial activity and membrane permeability against bacterial cell membrane.

• Korean Journal of Plant Tissue Culture
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• v.27 no.5
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• pp.375-377
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• 2000

It is now generally accepted that a phosphoinositide cycle is involved in the transduction of a variety of signals in plant cells. In animal cells, the hydrolysis of phosphatidyl-4,5-bisphosphate catalysed by phosphatidylinositol - specific phospholipase C yields to D-myo-inositol - 1,4,5-trisphosphate and diacylglycerol, which are well known second messengers. The binding of InsP$_3$to a receptor located on the endoplasmic reticulum triggers a calcium release from the endoplasmic reticulum. We have detected and partially characterised key components of phosphoinositide signaling. First, tobacco microsomal fraction and plasma membrane PI-PLC. Consecutively, using a radioligand binding assay we have identified a $Ca^{2+}$ -dependent high affinity InsP$_3$binding site in microsomal membrane fraction vesicle preparation and then we have measured inositol-1,4,5-trisphosphate induced calcium release from tobacco microsomal fraction. These findings suggest that phosphoinositide signaling system is present and operates in the tobacco suspension culture.e.

• Journal of Ginseng Research
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• v.26 no.4
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• pp.187-190
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• 2002

Crude synaptic membrane fractions from the frontal cortex, striatum, brain stem and whole brain of rat were prepared to assay the effects of ginseng total saponin (GTS) on [$^3$H]DAGO bindings of the opioid $\mu$-receptors. Scatchard plots analysis binding data demonstrated that GTS (0.1 mg/ml) decreased the affinity of specific [$^3$H]DAGO bindings without changes in B$\_$max/ in the frontal cortex and striatum. On the other hand, GTS did not affect the [$^3$H]DAGO bindings iii the brain stem and whole brain. These results suggest that the regulation of [$^3$H]DAGO bindings by GTS may play roles in the change of the pharmacological responses of $\mu$-opioids.

• BMB Reports
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• v.41 no.7
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• pp.555-560
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• 2008

The interaction of the rod GTP binding protein, Transducin ($G_t$), with bleached Rhodopsin ($R^*$) was investigated by measuring radiolabeled guanine nucleotide binding to and release from soluble and/or membrane-bound Gt by reconstituting $G_t$ containing bound GDP ($G_t$-GDP) or the hydrolysis-resistant GTP analog guanylyl imidodiphosphate ($G_t$-p[NH]ppG) with $R^*$ under physiological conditions. Release of GDP and p[NH]ppG from $G_t$ occurred to the same extent and with the same light sensitivity both in the presence and absence of added GTP. Significant amounts of $G_t$ without bound nucleotide ($G_{t^-}$) were generated. When ROS containing bleached rhodopsin ($R^*$) were centrifuged in low ionic strength buffer, $G_{t^-}$ remained associated with the membrane fraction, whereas $G_t$-GDP remained in the soluble fraction. These results suggest that $G_t$-GDP and $G_t$-p[NH]ppG have similar affinities for $R^*$. The results also suggest that $G_{t^-}$, rather than $G_t$-GDP, is the moiety which exhibits tight, "light-induced" binding to rhodopsin.

• Membrane Journal
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• v.30 no.1
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• pp.46-56
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• 2020

In this study, poly (ether-block-amide) (PEBAX)/poly (ethylene) glycoldiacrylate (PEGDA)/zeolitic imidazolate framework-8 (ZIF-8)-polyethersulfone (PES) composite membranes were prepared. The gas permeation properties of N₂ and CO₂ were investigated for each composite membrane. First, the gas permeability in the PEBAX/PEGDA-PES composite membrane decreased with increasing PEGDA content for each molecular weight at PEGDA250, PEGDA575, and PEGDA-700 g/mol. The CO₂/N₂ selectivity showed a constant value and gradually increased with increasing PEGDA content after 30 wt% PEGDA, and PEBAX/PEGDA250 50 wt%-PES prepared by adding PEGDA250 g/mol 50 wt% showed a selectivity of 15.1. This is because as the PEGDA content increases, the number of diacrylate groups increases, and the CO₂ affinity due to the ether structure of PEGDA increases. Gas permeation properties according to ZIF-8 were investigated for composite membranes of PEGDA 0 to 30 wt%, with CO₂/N₂ selectivity almost constant for each molecular weight. The permeability of N₂ and CO₂ gradually increased with increasing ZIF-8 content, and CO₂/N₂ selectivity was the highest at 3.4 in PEBAX/PEGDA250 g/mol 30 wt%/ZIF-8 20 wt%-PES composite membrane.

• Membrane Journal
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• v.21 no.4
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• pp.389-397
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• 2011

In this study, polymer composite membranes based on sulfonated poly(arylene ether sulfone) (SPAES) were prepared using a solution casting method with different amount of vermiculite (VMT) content. The dispersion of VMT particles in the SPAES matrix was confirmed by means of a scanning electron microscopy observation. The composite membrane containing less than 1 wt% of VMT has a smooth skin on the top and bottom, which means there is a good dispersion of VMT in the matrix. The water uptake of the composite membranes gradually increases as the temperature increases, and the results confirm that all the adsorbed water is bound water because VMT has a strong water affinity on account of its high cation exchange value. A composite membrane with a VMT content of less than 1 wt% increases the proton conductivity and reduces the methanol permeability. Of all the composite membranes, the membrane SPAES/VMT 1.0 has the best fuel cell performance in terms of membrane selectivity. The performance value of SPAES/VMT 1.0 is double that of Nafion 112, which suggests that SPAES/VMT1.0 could be an excellent candidate for direct methanol fuel cells.

• Membrane Journal
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• v.30 no.6
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• pp.409-419
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• 2020

In this study, PEBAX/ZIF-8 and PEBAX/amineZIF-8 composite membranes were prepared according to the content of zeolitic imidazolate framework-8 (ZIF-8), amine-modified ZIF-8 (amineZIF-8), the gas permeability properties of N2 and CO2 were investigated for each composite membrane. In the case of the PEBAX/ZIF-8 composite membrane, the permeability of N2 and CO2 increased as the ZIF-8 content increased, and in the case of the PEBAX/amineZIF-8 composite membrane, the permeability of N2 and CO2 increased up to 20 wt% of amineZIF-8, but decreased at the higher content. CO2/N2 ideal selectivity increased up to 20 wt% of ZIF-8 and amineZIF-8 contents in both PEBAX/ZIF-8 and PEBAX/ amineZIF-8 composite membranes, and then decreased thereafter, in the case of PEBAX/amineZIF-8 composite membrane was less decreased. The reason for the highest CO2/N2 ideal selectivity at 20 wt% of amineZIF-8 is that amine modification improved the compatibility between PEBAX and amineZIF-8, and thus amineZIF-8 was evenly dispersed in PEBAX, resulting in the greatest effect of the porous ZIF-8 with a 3.4 Å pore size and the amine with affinity for CO2.

• Membrane Journal
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• v.31 no.6
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• pp.404-416
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• 2021

In this study, a mixed matrix membrane was prepared by varying the contents of GO and PEI-GO synthesized in PEBAX2533, and the permeation characteristics of N₂ and CO₂ were studied. The N₂ and CO₂ permeability of the PEBAX/GO mixed membrane decreased as the GO content increased, and showed the highest CO₂/N₂ selectivity of 58.9 at GO 0.3 wt%. For the PEBAX/PEI-GO mixed membrane, the N₂ permeability decreased as the PEI-GO content increased, and the CO₂ permeability showed a different trend according to the PEI-GO content. Overall, the CO₂/N₂ selectivity was higher than that of the PEBAX/GO mixed membrane. In particular, PEI-GO 0.3 wt% showed the highest CO₂/N₂ selectivity of 73.5 among the mixed membranes, and a positive result was obtained as it was located above the Robeson upper bound. This is believed to be due to the molecular sieving channel effect resulting from the original GO structure, the functional groups present in the structure of GO having affinity for CO₂, and the effect of amine bound to PEI by modifying GO into PEI.

• Biomolecules & Therapeutics
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• v.7 no.4
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• pp.307-314
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• 1999

The human muscarinic acetylcholine receptor (mAChR) subtypes Hml, Hm2 and Hm3 have been expressed in insect cells (Spodoptera frugiperda, Sf9) using the baculovirus expression system. Expression of relevant DNA, transcript and receptor proteins was identified by PCR, Northern blotting and [$^{3}H$]QNB binding, respectively. As assessed by [$^{3}H$]QNB binding sites, yields of muscarinic receptors in membrane preparations in this study were as about 5-20 times high as those in mammalian cells reported in previous studies. The [$^{3}H$]QNB competition binding studies with well-known subtype-selective mAChR antagonists showed that the receptors expressed in Sf9 cells retain the pharmacological characteristics expected for the ml , m2 and m3 muscarinic receptors. The ml-selective antagonist, pirenzepine, displayed a considerably higher affinity for Hml by 110-fold and 35-fold than for Hm2 and Hm3, respectively, The m2-selective methoctramine displayed a significantly higher affinity for Hm2 than for Hml and Hm3 (10- and 26-fold, respectively). p-F-HHSiD exhibited high affinity for Hm3 that is not significantly different from those for Hml, but 66-fold higher than its affinity for Hm2. The functional coupling of the recombinant receptors to second messenger systems was also examined. While both Hml and Hm3 stimulated phosphoinositide hydrolysis upon activation by carba-chol, Hm2 produced no response. On the other hand, activation of mAChRs induced the inhibition of forsko-lin-stimulated cyclic AMP formation in Hm2-expressing cells, whereas the significant dose-dependent increase in or poor response on cyclic AMP formation were produced in Hml or Hm3-expressing cells, respectively. These results indicate the differential coupling of recombinant Hml, Hm2 and Hm3 receptors expressed in SF9 cells to intracellular signalling system.

• Journal of fish pathology
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• v.14 no.1
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• pp.31-36
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• 2001

A novel clonidine binding sites were characterized in the intestinal membrane isolated from seawater eels, Anguilla japonica. The specific clonidine binding sites consisted of at least two classes, high affinity ($K_d=1.4{\pm}0.3$ nM n = 5) and low affinity ($K_d=175{\pm}34$ nM n = 5) sites. The specific binding of 2 nM [$^3H$]clonidine was most enhanced at $20^{\circ}C$ and pH 7.5, and reversed by unlabelled clonidine. Such binding was hardly inhibited by adrenaline, yohimbine or rauwolscine, indicating that most binding sites are distinct from $\alpha_2$-adrenoceptor. The specific clonidine binding sites was inhibited by various imidazoline/guanidinium drugs, indicating existence of imidazoline/guanidinium receptive sites (IGRS) or imidazoline receptors in the eel intestine. Competition experiments revealed that rank order to displace 2 nM [$^3H$]clonidine from their binding sites was as follows : guanabenz > cirazoline = naphazoline = UK14,304 = ST587 $\geq$ clonidine $\geq$ idazoxan = RX821002 = tolazoline > ST93 = oxymetazoline = amiloride = ST91 > yohimbine = efaroxan = rauwolscine $\geq$ adrenaline = ST567 = histamine = agmatine. Although physiological role of IGRS is not clear yet even in mammalian cell/tissues, eel intestine may be a good model to elucidate how the IGRS act in the cell and to decide what is the endogenous ligand for the IGRS.