• Archives of Pharmacal Research
• /
• v.27 no.3
• /
• pp.278-282
• /
• 2004

A number of 8-arylflavones have been synthesized as congeners of wogonin and evaluated for their inhibitory activities of $PGE_2$ production. 8-Arylflavones were obtained from commercially available chrysin via two different synthetic pathways. Most 8-arylflavones exhibited much reduced inhibitory activities against COX-2 catalyzed $PGE_2$ production compared to that of wogonin. Functional group replacement at the 8-position of wogonin from methoxy to aryl group caused loss of inhibitory activity. Our present results imply that the functional group at the 8-position of flavones seems to play very important roles for bioactivity.

• Bulletin of the Korean Space Science Society
• /
• 2009.10a
• /
• pp.38.2-38.2
• /
• 2009

The ionosphere displays variations on a wide variety of time-scales, ranging from few hours to days and up to solar cycles and even more. In this paper, we examine the ionospheric F2-layer variability in mid latitude by analyzing the foF2 and hmF2 from the Anyang ionosonde. Especially, we investigate how ionospheric semi-annual and seasonal anomalies vary with local time and solar activity. In addition to the characterization of the ionospheric semi-annual an seasonal anomalies, our study extends to the investigation of the relationship between ionospheric variability and geomagnetic activity. Finally we also discuss the coupling between ionospheric F2-layer variability and thermospheric neutral composition.

• Bulletin of the Korean Chemical Society
• /
• v.33 no.6
• /
• pp.1939-1944
• /
• 2012

Benzoyloxy benzophenone derivatives were prepared in 3 steps including DCC coupling, Fries rearrangement and esterification from benzoic acids in 24-89% total yields. Among the prepared 12 benzophenone analogues 1a-1l, the compound 1b having three chloro groups at the para position showed maximum inhibitory effects of ICAM-1 expression but, 1a which have no substituents at all showed no inhibitory activity. This study provides the evidences that benzoyloxy benzophenone derivative, 1b may exert its anti-inflammatory activity by suppressing IFN-${\gamma}$-induced ICAM-1 expression.

• Bulletin of the Korean Chemical Society
• /
• v.30 no.11
• /
• pp.2626-2630
• /
• 2009

2'($\beta$)-Hydroxymethylated adenosine is a potent and selective inhibitor of hepatitis C virus (HCV) replication. It targets the RNA-dependent RNA polymerase of HCV, NS5B. Synthesis and antiviral evaluation of carbocyclic versions are described. The cyclopentene intermediate ($9\beta$) was successfully synthesized through sequential Johnson-Claisen orthoester rearrangement and ring-closing metathesis (RCM). Coupling of bases via a Pd(0) catalyst, selective dihydroxylation, and desilylation yielded the target nucleoside analogues. The compounds 17 and 18 were assayed for their ability to inhibit HCV RNA replication in a subgenomic replicon Huh7 cell line and showed moderate antiviral activity with toxicity up to 20.0 and 24.7 ${\mu}g/mL$, respectively.

• YAKHAK HOEJI
• /
• v.39 no.1
• /
• pp.48-54
• /
• 1995

Coupling of tetracycline(Tc) to dithiocarbamate chitosan(DTCC) via chelate bond was investigated varying reaction time, concentration, temperature, pH, and Ca(II)/Tc ratio. The amount of Tc bound to matrix increased to give a maximum and decreased as the reaction proceeded. The degree and rate of dissociation of Tc complex were affected by the reaction temperature, and pH. By running the reaction at low temperature and pH, the degree of dissociation was greatly diminished. Properties of drug-release from DTCC-Ca(II)-Tc complex were studied by batch- and flow-method and release of Tc and CA(II) by flow method followed nearly zero-order. DTCC-Ca(II)-Tc showed very prolonged antimicrobial activity compared to that of free Tc.

• YAKHAK HOEJI
• /
• v.51 no.2
• /
• pp.103-107
• /
• 2007

In these study novel 1,4-disubstituted carbocyclic nucleoside analogues were synthesized as potential antiviral agents. The coupling reaction of the alcohol 8${\alpha}$ with natural bases using Mitsunobu reaction afforded the target nucleosides 13, 14. The synthesized compounds were evaluated for their antiviral activity against various viruses such as HIV-1, HSV-1, HSV-2 and HCMV. Cytosine derivative 13 exhibited moderate antiviral activity against HIV-1 (EC$_{50}$=16.4 ${\mu}$M).

• Journal of Microbiology and Biotechnology
• /
• v.8 no.3
• /
• pp.251-257
• /
• 1998

Cycloinulooligosaccharide fructanotransferase (CFTase) which produces cyclofructan from inulin was purified 332-fold from a culture broth of Bacillus macerans CFCl. The molecular mass of the CFTase was estimated to be 110 kDa by SDS-polyacrylamide gel electrophoresis and gel filtration, indicating that the enzyme has a monomer structure. The maximal level of enzyme activity was observed at pH 7.5 and $45^{\circ}C$. The enzyme was stable in the pH range 6.0 to 9.5, and at temperatures up to $45^{\circ}C$ for 1 h. The enzyme activity was completely inhibited in the presence of 0.5 mM $Ag^+\;or\;Cu^2+$ ion. None of sucrose (GF), l-kestose (GF2), or nystose (GF3) were found to be substrates for the CFTase, but inulooligosaccharides larger than nystose were attacked by the enzyme. The CFTase catalyzes not only the cyclization as the major reaction, but also disproportionation and coupling reactions involving intermolecular transfructosylation in the same manner as cyclodextrin glucanotransferase (CGTase) (EC 2.4.1.19).

• Korean Journal of Pharmacognosy
• /
• v.11 no.1
• /
• pp.15-23
• /
• 1980

A new iridoid glucoside was isolated from the whole plant of Ajuga spectabilis Nakai (Jaran-cho; Labiatae). This compound was obtained as white plate-like crystal and named as Jaranidoside. It has a molecular formula $C_{17}H_{26}O_{12}$ and mp $128{\sim}130^{\circ}C$. The structure of the Jaranidoside was assumed from data of chemical reactions and PMR specturum of the compound. To determine the most favorable conformation, informations on the proton coupling and chemical shift were used. Jaranidoside exhibited a stimulating activity on smooth muscle and cardiac muscle. No antimicrobial activity on five microorganism strains was observed.

• Journal of Life Science
• /
• v.16 no.3 s.76
• /
• pp.505-509
• /
• 2006

Membranes prepared from Bacillus cereus KCTC 3674, grown aerobically on a complex medium, oxidized NADH exclusively, whereas deamino-NADH was little oxidized. The respiratory chain-linkedNADH oxidase system exhibited an apparent $K_m$ value of about $65\;{\mu}M$ for NADH. Interestingly, the activity of NADH:DCIP oxidoreductase on NADH oxidase system was decreased remarkably by $Na^+$ or $K^+$, and its optimal pH was 5.5. The activity of NADH:DCIP oxidoreductase was very resistant to the respiratory chain inhibitors such as rotenone, capsaicin, and $AgNO_3$, whereas it was inhibited by about 40% with $40{\mu}M$ 2-heptyl-4-hydroxyquinoline-N-oxide (HQNO). From the results, we suggest the possibility that the aerobic respiratory chain-linked NADH oxidase system of B. cereus KCTC 3674 may possess the HQNO-sensitive NADH:DCIP oxidoreductase lacking an energy coupling site.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1996.04a
• /
• pp.208-208
• /
• 1996

In this work we investigated coupling of the m2 and m4 subtypes of muscarinic acetylcholine receptors expressed in chinese hamster ovary (CHO) cells to activation of neuronal nitric oxide synthase (nNOS). Stimulation of guanylate cyclase activity in detector neuroblastoma cells was used as an index of generation of nitric oxide (NO) in CHO cells. The agonist carbachol induced marked time and concentration-dependent enhancement of the activity of nNOS at m2 receptors. In sharp contrast, the response in CHO cells transfected with the m4 receptor gene was similar in magnitude to that observed in non-transfected cells, suggesting lack of significant coupling of m4 muscarinic receptors to NO signaling. This novel observation of functional divergence of the two muscarinic receptor subtypes at the level of activation of nNOS is quite intriguing, in light of the currently accepted dogma that they belong to the same functional class. This functional selectivity was not due to differential effects on intracellular Ca$\^$2+/ concentration, since activation of both subtypes of muscarinic receptors produced a comparable, albeit quite small, Ca$\^$2+/ signal. Taken together, our present data strongly suggest that the generally assumed functional equivalence of m2 and m4 muscarinic receptors should be carefully reexamined. These data also suggest the presence of alternate mechanisms of activation of nNOS, which might be operative in the absence of large changes in the concentration of cellular Ca$\^$2+/. The latter mechanisms are expected to be activated by m2, but not m4 muscarinic receptors. Both sets of findings are quits important in regards to refining the functional classification of muscarinic receptor subtypes and the cellular mechanisms of activation of NOS.