• Bulletin of the Korean Chemical Society
• /
• 제22권11호
• /
• pp.1217-1223
• /
• 2001

A series of benzimidazole derivatives containing oxycyclic pyridine was prepared and evaluated for their gastric H+ /K+ -ATPase inhibitory activity. Several of the synthesized compound exhibited potent antisecretion in pylorus-ligated rats when administered intradoudenally. Their inhibitory activities were equivalent or comparable to omeprazole.

• Archives of Pharmacal Research
• /
• 제26권9호
• /
• pp.735-738
• /
• 2003

The methanolic extract of the twigs of Celtis chinensis was found to show inhibitory activity on acetylcholinesterase (AChE), an enzyme that plays a role in the metabolic hydrolysis of ACh. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of N-p-coumaroyl tyramine. as an inhibitor on AChE. This compound inhibited AChE activity in a dose-dependent manner, and the $IC_50$ value of trans-N-p-coumaroyl tyramine was 34.5 $\mu$g/mL (122 $\mu$M).

• Bulletin of the Korean Chemical Society
• /
• 제33권5호
• /
• pp.1571-1576
• /
• 2012

A diarylurea compound 1 possessing pyrrolo[3,2-$c$]pyridine nucleus was designed and synthesized with structure similarity to Sorafenib. Compound 1 was tested over 60-cancer cell line panel at a single dose concentration of 10 ${\mu}M$ and showed high activity. It was further tested in a five-dose mode to determine its $IC_{50}$, TGI, and $LC_{50}$ values over the 60 cell lines. Compound 1 showed high potency and good efficacy, and was accordingly tested at a single dose concentration of 10 ${\mu}M$ over a panel of 40 kinases. At this concentration, it completely inhibited the enzymatic activities of a number of oncogenic kinases, including ABL, ALK, c-RAF, FLT3, KDR, and TrkB. The target compound was subsequently tested over these 6 kinases in 10-dose testing mode in order to determine its $IC_{50}$ values.

• Journal of Microbiology and Biotechnology
• /
• 제25권12호
• /
• pp.2007-2010
• /
• 2015

A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC₅₀ values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 μM concentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.

• 약학회지
• /
• 제41권2호
• /
• pp.268-272
• /
• 1997

We studied the action of methyleugenol on immediate hypersensitivity. Methyleugenol completely inhibited systemic anaphylaxis induced by compound 48/80 in mice. Methyleugenol al so inhibited local anaphylaxis induced by anti-dinitrophenyl (DNP) IgE. Moreover, methyleugenol dose-dependently inhibited histamine release in peritoneal mast cells activated by compound 48/80 or anti-DNP IgE. These results suggest that the inhibitory effect of methyleugenol on anaphylaxis induced by compound 48/80 or anti-DNP IgE is due to, in part at least, the membrane stabilization of mast cells.

• Journal of Microbiology and Biotechnology
• /
• 제25권8호
• /
• pp.1257-1264
• /
• 2015

Trichoderma strain T-33 has been demonstrated to have inhibitory effect on the fungus species Cytospora chrysosperma. Here, an active antifungal compound was obtained from Trichoderma strain T-33 extract via combined separation technologies, including organic solvent extraction, liquid chromatography, and thin-layer chromatography. The purified compound was further characterized by advanced analytical technologies to elucidate its chemical structure. Results indicated that the active antifungal compound in Trichoderma strain T-33 extract is 2,5-cyclohexadiene-1,4-dione-2,6-bis (1,1-dimethylethyl).

• Bulletin of the Korean Chemical Society
• /
• 제27권9호
• /
• pp.1353-1358
• /
• 2006

We investigated in vitro T-cell inhibitory activity and bioavailability of small chemical inhibitors for Lck SH2 domain, which had a different scaffold such as an amide bond, reduced amide bond, N-methyl amide bond, thioamide bond, and urethane bond. Each of these compounds, with its particular scaffold, showed a different logP value, stability against serum enzyme, stability in buffer solution, and in vitro T-cell inhibitory activity. Overall results indicated that the SH2 inhibitor containing urethane bond can be a new lead compound because of its superior bioavailability, potent in vitro T-cell inhibitory activity, and facile synthesis.

• Natural Product Sciences
• /
• 제20권1호
• /
• pp.13-16
• /
• 2014

Five compounds were isolated from the stem of Zea mays. Based on spectral data, they were identified as 4-hydroxybenzaldehyde (1), N-trans-p-coumaryl tyramine (2), N-trans-ferulyl tryptamine (3), N-(p-coumaryl) serotonine (4), and N-(p-coumaryl)-tryptamine (5). All isolates were evaluated in vitro for their inhibitory activity on acetylcholinesterase. Among tested compounds, compounds 2 - 5 exhibited acetylcholinesterase inhibitory activity, with $IC_{50}$ values of 125, 60.4, 183.5 and 53.3 ${\mu}M$, respectively. Compound 1 did not show acetylcholinesterase inhibitory activity in the present study.

• Applied Biological Chemistry
• /
• 제29권2호
• /
• pp.207-211
• /
• 1986

김치 발효 경과에 따라 젖산균을 분리하여 E. coli와 Streptococcus faecalis, Lactobacillus bulgaricus에 대해 생육 저해능력이 있는 균주를 screening하였다. 젖산균중 생육 저해균의 비율을 조사한 결과 이들은 2주의 발효기간 중 중기에 가장 많이 나타났으며 대부분 Pediococcus cerevisiae로 동정하였다. 이 P. cerevisiae의 생육억제 작용은 열에 불안정하고 단백분해 효소의 작용을 받지 않는 물질에 의한 것이며 이 물질은 배지의 pH를 중성으로 유지했을 때는 산성인 경우보다 생성이 저하되는 것으로 나타났다.

• Natural Product Sciences
• /
• 제18권1호
• /
• pp.22-25
• /
• 2012

Five triterpenoids, epifriedelanol (1), friedelin (2), lupeol (3), ${\beta}$-sitosterol (4), daucosterol (5), and one phenyl propanoids ester, trans-docosanoyl ferulate (6) were isolated from the whole parts of Portulaca oleracea. They were determined using a combination of spectroscopic analyses ($^1H-$, $^{13}C$-NMR, and MS data) and evaluated for their cyclooxygenase inhibitory activity. Compound 6 exhibited inhibitory effect with $IC_{50}$ values of $40.2{\mu}M$ and 1.6 mM on COX-1 and COX-2 activities, respectively.