• Bulletin of the Korean Chemical Society
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• v.30 no.11
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• pp.2707-2712
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• 2009

5-$HT_{3}$ receptor;5-$HT_{3A}$ receptor channel activity;Novel 5-$HT_{3}$ receptor channel current blockers;Chlorophenyl substituted piperazinylethylaminomethylpyrazoles; The 5-$HT_{3A}$ receptors are one of ligand-gated ion channels and are known to be involved in visceral pain, anxiety, or anticancer agent-induced nausea and vomiting. In present study, we designed novel skeletons based on the developed 5-$HT_{3}$ receptor antagonists and evaluated their effects on 5-$HT_{3A}$ receptor channel currents ($I_{5-HT}$) of a series of pyrazole derivatives having N-chlorophenylpiperazine functionality (6-9). We found that most of N-p-chlorophenyl substituted piperazinyl-pyrazole derivatives (7b, 7c, 7e and 7h) exhibited the high potency for the inhibition of $I_{5-HT}$, whereas the compound without chloride (6) or with m-chlorophenyl group (a serious of 8 and 9) showed the low potency. These result indicate that p-chlorophenyl group is might play an important role for increasing the inhibitory potency on $I_{5-HT}$.

• Journal of Microbiology and Biotechnology
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• v.8 no.3
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• pp.197-202
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• 1998

Aliphatic alkenals having 6 to 13 carbons were evaluated for antifungal activity against Saccharomyces cerevisiae. The activity was gradually increased with chain length, e.g., (E)-2-decenal and (E)-2-undecenal exhibited maximum potency, while (E)-2-dodecenal and (E)-2-tridecenal were completely inactive. Alkenals showed increasing inhibitory activity with chain length, as in the case of antifungal activity, towards glucose-induced medium acidification by the plasma membrane $H^+$-ATPase of S. cerevisiae. The group including (E)-2-nonenal, (E)-2-decenal, and (E)-2-undecenal exhibited maximum potency, but the potency of (E)-2-dodecenal and (E)-2-tridecenal demonstrated a sudden drop with respect to the former group. (E)-2-Nonenal revealed dose-responsive inhibition to the medium acidification and inhibited over 90% at a concentration of 1.25 mM ($175.3{\mu}g$/ml). In contrast to (E)-2-undecenal whose inhibitory efficiency increased with incubation time, inhibition by (E)-2-dodecenal was reversed with time. Of the tested alkenals, (E)-2-heptenal and (E)-2-octenal most highly inhibited ATP hydrolytic activity by the plasma membrane $H^+$ ATPase, while (E)-2-heptenal at 10 mM ($1121.8{\mu}g$/ml) showed an inhibitory efficacy of 93.2%.

• The Korean Journal of Physiology and Pharmacology
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• v.11 no.1
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• pp.9-13
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• 2007

Antioxidant properties have been proposed as a mechanism for the putative anti-inflammatory effects of phenolic compounds. To reveal the relationship between antioxidant activity and anti-inflammatory effects of various antioxidants, we measured 1, 1-diphenyl-2-picryhydrazyl(DPPH)-reducing activity and examined the inhibitory effects on LPS-induced inflammation-related gene expression in the BV2 microglial cell line. Lipopolysaccharide(LPS)(0.2 ${\mu}g/ml$) was used with or without antioxidants to treat cells, and the regulation of iNOS and cytokine gene expression was monitored using an RNase protection assay(RPA). Although, all tested antioxidants had similar DPPH-reducing activity and inhibited nitrite production, but the curcuminoid antioxidants(ferulic acid, caffeic acid, and curcumin) inhibited LPS-induced gene expression(iNOS, $TNF-\alpha,\;IL-1{\beta}$, IL-6, and IL-1 Ra) in a concentration-dependent manner. Other tested antioxidants did not exhibit the same effects; N-acetylcysteine(NAC) only began to suppress $IL-1{\beta}$ gene expression just below the concentration at which cytotoxicity occurred. Moreover, the antioxidant potency of curcuminoids appeared to have no correlation with anti-inflammatory potency. Only curcumin could inhibit LPS-induced microglial activation at a micromolar level. These data suggest that curcumin may be a safe antioxidant possessing anti-inflammatory activity.

• Clinical and Experimental Pediatrics
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• v.48 no.6
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• pp.594-598
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• 2005

Purpose : Phimosis is the inability to retract the foreskin of the penis over the glans of the penis. Even though phimosis is not pathogenic, the presence of phimosis is known to increase the risk of urinary tract infection in infancy. The use of topical steroids has been advocated as a safe and economical alternative to surgical intervention. The purpose of the study was to assess the effectiveness of topical steroids for the treatment of phimosis in young boys. Methods : A total of 53 boys with phimosis were divided into two groups to distinguish between the efficacy of low-potency topical steroid(group 1, 27 cases) and of high-potency topical steroid (group 2, 26 cases). Results : The success rate increased in the process of time. After 6 weeks, the success rate was 21 cases in group 1 and 22 cases in group 2. There was no significant differences in treatment outcomes between the two groups. The age of the boys, the appearance of prepuce prior to treatment, and the presence of previous symptoms, including symptoms of UTI, and ballooning of the prepuce at micturation had no significant difference on treatment outcomes. Conclusion : Topical steroid was effective in treatment of phimosis in boys younger than 4 years old. Although treatment outcomes between low- and high-potency topical steroids were not significantly different, those treated with a high-potency steroid cream showed more fast improvement. Further studies are necessary to assess systemic side effects of steroid treatment, duration of treatment and prevention of genitourinary tract infection in male infants.

• Korean journal of applied entomology
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• v.31 no.2
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• pp.122-132
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• 1992

Experiments were conducted to establish an in vitro AChE inhibition test system to evaluate the potency of AChE inhibition of new chemical compounds. For a fixed time inhibition test, optimal inhibition (incubation) time to evaluate their AChE inhibition potency was 10 min. for AChE inhibitors such as DFP, DDVP, and paraoxon. The concentration of new chemical compounds with an ester group for evaluation of their inhibition potency was 10 $\mu$M under 10 min. preincubation conditions. However, the stepwise inhibition test with higher concentrations seemed to be needed for other chemical compounds. For a progressive inhibition test to calculate inhibition constants such as $K_d$, $K_3$ and $K_i$, extremely low $K_d(1.3\times10-^85.6\times10^{-7})$ and $K_3$(0. 21-0.27 $min^{-1}$) were observed under lagged preincubation time (0.8-13.3 min) and low in¬hibitor concentrations $(1\times10-^92\times10-^6M)$. However, this method seemed to be useful for comparison of AChE inhibition potency among inhibitors. Differences in inhibition potency among DFP, paraoxon, and KH501 were due to the differences in $K_d$, in other words, differences in affinities between inhibitors and AChEs. Therefore, AntiChE screening should consist of two steps. The first step is to evaluate the potency of AChE inhibition based on $I_50$ valuse obtained from fixed time inhibition tests. The second step is to study inhibition patterns and characteristics of chemical compounds selected in the first step.

• Current Research on Agriculture and Life Sciences
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• v.5
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• pp.173-184
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• 1987

Anethole, eugenol, isoeugenol, safrole and isosafrole are ingredients of refined oils which are obtained from some plants and their chemical structures are very similar. They are mainly used as a flavoring agent, food additive, dental analgesics and for many drugs. But, there is no report about their effect on the intestinal motility. The result of examining the effect, potency and mode of action of anethole, eugenol, isoeugenol, safrole and isosafrole on motility of isolated rabbit jejunum segment, are as follows : 1. Single administration of anethole, eugenol, isoeugenol, safrole and isosafrole showed the inhibition of motility of isolated rabbit jejunum segment, degree of which was various. The $pD_2$ values of isoeugenol, isosafrole, eugenol, safrole and anethole in isolated rabbit jejunum segment were 4.22, 4.18, 4.17, 4.15 and 3.82 (in the descending order of potency). 2. The contracted rabbit jejunum segment : by carbachol, pilocarpine, barium chloride and histarmine were relaxed by five essential oil. 3. The relaxed rabbit jejunum segment by anethole was not recovered by carbachol, pilocarpine, barium chloride and histamine. The relaxed rabbit jejunum segment by eugenol, isoeugenol, safrole and isosafrole were recovered by carbachol, pilocarpine and barium chloride but partially recovered by histamine. 4. Judging from the facts above, it is thought that five essential oil are inhibit the motility of isolated rabbit jejunum segment by neurotropic and musculotropic action.

• YAKHAK HOEJI
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• v.8 no.1
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• pp.1-5
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• 1964

Present experiment in vivo shows that some conversions of active groups in chloramphenicol residue of ester, that is hydrolytic cleavage of dichloracetamide and glucuronide formation, seem to take place prior to hydrolysis. This result suggest that the enzymatic hydrolysis rate in vitro, is not available as an index for the evaluation of the chlorampherical ester potency.

• Proceedings of the Korean Society of Toxicology Conference
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• 2003.10b
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• pp.94-94
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• 2003

Tea is the most popular beverage in the world, especially green tea (Camellia sinensis) is daily taken by Asian people including Japanese. In last two decades, a variety of biological effects of tea components such as antioxidative, antimutagenic, anticarcinogenic, antibacterial and radical scavenging activities on bacteria, cultured cells and mammals have been elucidated.(omitted)

• Toxicological Research
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• v.16 no.2
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• pp.141-146
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• 2000

Phthalate esters are used extensively as a plasticizer in the manufacture of plastic products such as PVC bags and medical devices. Recently, phthalate esters have been shown to induce endocrine system mediated responses. However. only a Jew studies have been conducted for estrogenic activity of phthalate esters. In this study estrogenic activities of seven phthalate esters. butyl benzyl phthalate (BBP), di(2-ethylhexyl) phthalate (DEHP), di-n-butylphthalate (DBP), diethylphthalate (DEP), di-n-pentylphthalate (DPP), di-n-propylphthalate (DPrP) and dicyclohexylphthalate (DCHP), were examined in vitro using E-screen assay and competitive binding assay. From the E-screen assay, BBP. DEHP. DBP and DEP showed weak estrogenic activity at the concentration of 5 $\mu\textrm{M}$. The relative proliferative effect (RPE) and the relative proliferative potency (RPP) were 50~70% and 0.01%. respectively, when compared with 500 pM of 17$\beta$-estradiol (E2). In competitive binding assay with the rat uterine estrogen receptor (ER), BBP and DEP showed weak binding potency ［(l/$10^4$~1/$10^5$ of E2］ while DEHP and DBP scarcely bound to ER. These results suggest that some phthalate esters have weak estrogenic activities in vitro.

• The Korean Journal of Physiology and Pharmacology
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• v.2 no.2
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• pp.201-207
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• 1998

To evaluate the possibility that the ginseng saponins could be developed as an anti-arteriosclerotic agent, we examined the inhibitory effects of ginseng saponins (total saponin[TS], panaxatriol[PT], panaxadiol[PD]) on the expression of c-fos mRNA and the proliferation of cultured rat aortic vascular smooth muscle cells (VSMCs) stimulated by angiotensin II (Ang II). TS and PT (1.0 mg/ml) suppressed c-fos mRNA induction in VSMCs stimulated by $10^{-5}$ M Ang II. The order of inhibitory potency was PT>TS. Ginseng saponins ($0.01{\sim}1.0$ mg/ml) inhibited the proliferation of VSMCs stimulated by Ang II in a concentration dependent manner, the inhibitory potency was TS＞PT＞PD at $0.1{\sim}1.0$ mg/ml. These results suggest that ginseng saponins may suppress Ang II-stimulated proliferation of aortic VSMCs which can be seen in atherosclerosis, hypertension and restenosis.