• Archives of Pharmacal Research
• /
• 제23권4호
• /
• pp.315-323
• /
• 2000

Syntheses of new analogues of oxathiin carboxanilide (UC84) and their antiviral activities were described. The heterocyclic carboxylic acids including oxathiins (4), thiazines (9) and dithiins (13) in which the methyl was replaced either by lipophilic trifluoromethyl- or bulky phenylgroup were synthesized starting from $\beta$-keto esters (5). Reaction of 4, 9 and 13 with thionyl chloride followed by treatment of the substituted aniline 22 gave the corresponding carboxanilides (24a~24f). The carboxanilides were subjected to Laweson's reagent the corresponding thiocarboxanilides (24g~24k). The antiviral activities of the synthesized compounds against human immunodeficiency virus type 1 (HIV-1), poliovirus type 1 (PV-1 ), coxsackie B virus type 3 (CoxB-3), vesicular stomatitis virus (VSV) and herpes simplex virus type 1 (HSV-1) were presented. The antiviral activity against HIV-1 of dithiin carboxanilide (24e) was similar with that of UC84 (24a). The corresponding thiocarboxanilides (24g~24k) showed higher inhibitory activity against HIV-1 than the carboxanilides (24a, 24b, 24d, 24e). The compounds in which ether the lipophilic trifluorormethyl substituents (24d, 24f, 24i ,24k) or bulky phenyl substituent is present in the heterocyclic compounds showed lower inhibitory activity than that of the methyl substituents is present in the compounds against the HIV-1. But the trifluoromethylated dithiin (24f) showed higher inhibitory activity against PV-1 and CoxB-3 virus than commercial antiviral agents, ribavirin (RV).

• Preventive Nutrition and Food Science
• /
• 제8권2호
• /
• pp.130-136
• /
• 2003

The protective effects of onion extract (OE), onion powder extracted in ethanol for 2 days. on carbon tetrachloride ($CCl_4$)-induced hepatotoxicities and the possible mechanisms involved in this protection were investigated in mice. Pretreatment with OE prior to the administration of $CCl_4$ significantly reduced the increase in serum alanine and aspartate aminotransferase activities and hepatic lipid peroxidation in a dose-dependent manner. In addition, pretreatment with OE significantly prevented the depletion of reduced glutathione content in the liver of $CCl_4$-intoxicated mice. $CCl_4$-induced hepatotoxicity was also prevented, as indicated by a liver histopathologic findings. The effects of OE on the cytochrome P450 (P450) 2E1, the major isozyme involved in $CCl_4$ biotransformation were investigated. Treatment of mice with OE resulted in a significant decrease in P450 2E1-dependent p-nitrophenol and aniline hydroxylation in a dose-dependent manner. Consistent with these observations, the P450 2E1 expressions were also decreased, as determined by immunoblot analysis. OE also exhibited antioxidant effects in FeCl$_2$-ascorbate induced lipid peroxidation in rat liver homogenates and in superoxide radical scavenging activity. These results show that the protective effects of OE against the $CCl_4$-induced hepatotoxicity may be due to its ability to block bioactivation of $CCl_4$, mainly tty inhibiting the expression and activities of P450 2E1 and by scavenging free radicals.

• 한국환경보건학회지
• /
• 제36권3호
• /
• pp.236-246
• /
• 2010

In preparative anti-corrosive coating experiments, polyaniline was obtained by reacting an oxidizing agent with the monomer aniline. Further, the primer coating was prepared using a variety of widely-used materials such as urethane resin. For the top coating, epoxy resin and acrylic urethane resin were used. Characteristics of the coatings were assessed according to KS and ASTM specifications, and the structure of the polyaniline was characterized using FT-IR and TGA. For analysis of anti-corrosive properties in salt-spray experiments, measurements of the oxidation state of iron and surface atomic analysis were conducted using XPS and SEM-EDX. Unlike general anti-corrosive coatings which exhibit anti-corrosive effects only as a primer coating, the anti-corrosive coatings using polyaniline as the anti-corrosive pigment showed a marked synergistic effect with the top coatings. In other words, the top coatings not only produce a fine view effect, but also increase, through interaction with the primer coatings, the resistance to diffusion of corrosive factors from the external environment. It was also found that, unlike the heavy metal oxide-forming layer of the passive barrier alone, the polyaniline anti-corrosive pigment oxidized iron at the interface with the iron substrate to form a passive barrier in the oxidic layer, and itself formed a potential barrier layer with anti-corrosive factors from the external environment. Although the passive layer was damaged, the damaged area did not become completely oxidized iron; on the contrary, it showed a tendency to reduction. This can be interpreted such that a passive layer is formed again on the damaged area, and that at the same time there is a tendency to self-healing.

• 대한화학회지
• /
• 제41권2호
• /
• pp.69-76
• /
• 1997

메탄올-아세토니트릴 혼합용매에서 벤조산 무수물의 아닐린에 의한 친핵성 치환반응을$35.0{\circ}C$에서 속도론적으로 연구하여 반응 메카니즘을 밝혔다. 벤조산 무수물에 있는 두 개의 카르보닐 탄소에서 경쟁적으로 치환반응이 일어나므로 반응 생성물의 비율로부터 각각의 반응속도$k_{XY}$와$k_{XZ}$를 구하였다. Hammett$p_i$값과 교차작용상수$p_{ij}$를 이용하여 전이상태구조 및 반응메카니즘을 규명하였다. 현저히 큰$p_X,\;p_{XY},\;p_{XZ}$및 양의값을 갖는$p_Y$의 크기로부터, 본 반응이 사각고리 전이상태를 갖는 전면공격$SN_2$메카니즘으로 진행됨을 알았다.

• 혜화의학회지
• /
• 제8권1호
• /
• pp.711-726
• /
• 1999

Aging in the life form occurs due to a gradual progression of the body growth and degeneration. Morphological and functional changes in the body decreases the adaptation and prevention capacity leading into the decline of a life force. Various studies have been released to examine the anti-aging effects of herbal prescriptions. This experiment has chosen Boganhwan which is used for the deficiency of the liver function and studied the anti-aging factors by examining the biotransformation enzymes. The following results were obtained in this study: 1. Hepatic lipid peroxide activity was significantly suppressed in the experimental group treated with Boganhwan for 2 weeks at the dosage of 350mg/kg, while other dosage groups did not present much changes. 2. Insignificant changes were shown for the cytochrome P-450 level, aminopyrine demethylase, and aniline hydroxylase (AH) activities. Cytochrome P-450 do not appears to be a part of the detoxification scheme. 3. Boganhwan decoction treated group showed most significant increase of superoxide dismutase (SOD), catalase, superoxide, and glutathione activities at the concentration of 350mg/kg and 500mg/kg. 4. Glutathione S-transferase and glutathione made most significant increase at the decoction concentration of 350mg/kg and 500mg/kg compared to the control group. 5. Hepatic glutathione concentration, protein bound-SH, and nonprotein bound-SH made most significant increase at the decoction concentration of 350mg/kg and 500mg/kg compared to the control group. From the above results, Boganhwan decoction played an important role in eliminating foreign substances in the body excluding cytochrome P-450 enzyme system. Thus, Boganhwan decoction can provide substantial aid in preventing and treating senile related illnesses.

• 혜화의학회지
• /
• 제8권1호
• /
• pp.689-710
• /
• 1999

Bobitang(BBT) is one of the most important prescription that has been used in oriental medicine(dongyibogam) for recovering spleen condition. The study was done to evaluate effects of BBT water extract on the spleen lipid peroxide content and metabolic enzyme system changes. After pretreatment of BBT I (100mg/kg), BBT II(250mg/kg), BBT III(350mg/kg), BBT IV(500mg/kg) for 1 week, lipid peroxide content and metabolic enzyme system changes of the spleen was measured in 8 months rats. The results were obtained as follows : 1. The content of spleen lipid peroxide was significantly decreased in all experimental groups as compared with control, and best in BBT III IV treated groups. 2. The activity of spleen superoxide generation was significantly decreased in all experimental groups as compared with control, and best in BBT IV III treated groups. 3. The activity of cytochrome P-450 and aminopyrine demethylase wasn't significant change. 4. The activity of aniline hydroxylase was significantly decreased in BBT IV II treated groups, xanthine oxidase was significantly decreased in all experimental groups, aldehyde oxidase was significantly decreased in BBT IV treated group as compared with control. 5. The activity of antioxidant enzymes as superoxide dismutase, catalase, glutathione peroxidase was significantly increased in all experimental groups as compared with control. 6. The activity of glutathion S-transferase was significantly increased in all experimental groups, the concentration of spleen glutathione was significantly increased in BBT IV treated group as compared with control. 7. The activity of ${\gamma}$ -glutamylcystein synthetase was significantly increased in BBT III IV I treated groups as compared with control, the activity of glutathione reductase wasn't significant change. From the above results, BBT is cosidered to have effect of remove peroxide content and free radical that was made during ageing process. It is expected that treatment of BBT can be applied in future clinical study of delaying the ageing process.

• 대한의생명과학회지
• /
• 제9권2호
• /
• pp.75-84
• /
• 2003

To evaluate the influence of hepatic oxygen free radical systems on liver injury by topical p-phenylenediamine (PPD) application on rat skin, PPD (25 mg/16.5 $\textrm{cm}^2$) was topically applied to the abdominal region 5 times every other day and sacrificed. By PPD treatment, increasing rate of liver weight/body weight (%), serum activities of alanine aminotransferase and aspartate aminotransferase and decreasing rate of microsomal glucose-6-phosphatase activity were higher in the rats fed tungstate supplemented diet than those fed a standard diet. These findings indicate that group fed tungstate supplemented diet have more severe liver injury compared with group fed standard diet on topical PPD application. However, the activities of oxygen free radical generating enzymes such as xanthine oxidase (XO) and cytochrome P450 dependent aniline hydroxylase and those of oxygen free radical scavenging enzymes were not found to be different between these two animal groups. In the present study, a novel monitoring method to detect the generating of oxygen free radicals in liver extract was devised. Throughout this method, the oxidized PPD produced by oxygen free radicals was determined colorimetrically. The increasing rate of PPD oxidation by liver homogenate was higher in tungstate fed animals than in standard diet fed ones. Among the fractionations of liver extract, the mitochondrial and postmitochondrial fractions in the liver extract of tungstate fed animals led to a higher availability of PPD oxidation by PPD treatment compared with standard diet fed ones. In conclusion, these results suggest that an enhanced liver injury in tungstate fed animals treated with PPD may be due to oxygen free radicals produced in other systems except oxygen free radicals generating from cytosolic XO system. Especially, oxidative availability by PPD can be used for oxygen free radical detection in some tissue.

• Journal of Ginseng Research
• /
• 제32권2호
• /
• pp.161-170
• /
• 2008

The aim of this meta-analysis was to systematically investigate the anti-hepatotoxic effect of ginseng in rats induced toxicity which damage to liver. Primary researches were gained on the ScienceDirect database, the DBpia, and the KISS, and the data about the effect factors in plasma and in enzyme were listed as many as possible. The effect factors were alanine transaminase (ALT), aspartate transaminase (AST), liver aminopyrine N-demethylase (AD), liver aniline hydroxylase (AH), liver 3,4-Methylenedioxyamphetamine (liver MDA), cytochrome P450 (P450), serum alkaline phosphatase (ALP), serum lactate dehydrogenase (LDH), cytochrome b5 (Cyto b5), glutathione reductase (GR), Liver glutathione S-transferase (GST), liver glutamyltransferase (GT), Liver (${\gamma}-GCS$), serum liver 3,4-Methylenedioxyamphetamine (serum MDA), serum sorbitol dehydrogenase (SDH), serum total protein (TP), serum ${\gamma}-glutamyltransferase$ (${\gamma}-GT$). To investigate the effect of ginseng, the mean difference (MD) between the group of rats induced by toxicity (RH) and the group of rats induced by toxicity with ginseng (RHG) were combined, and the significance of MDs were tested. The combined MDs were checked the biases caused by heterogeneity among studies and the publication biases, and adjusted by using random effect model and trim and fill method, respectively. The effect about ALT, AST, ALP, LDH, SDH, TP and ${\gamma}-GT$ in plasma factors were significant, and about AD, liver MDA, P450, Cyto b5, GR, GST, GT and ${\gamma}-GCS$ in enzyme factors were significant. The treatment with ginseng supplementation was significantly effected on plasma and enzyme factors of damaged-rats.

• Bulletin of the Korean Chemical Society
• /
• 제28권11호
• /
• pp.1985-1992
• /
• 2007

Ordered mesoporous silica (MCM-41) materials with different textural properties were prepared using alkyl (dodecyl, cetyl, eicosane) trimethyl ammonium bromide (DTAB, CTAB, ETAB, respectively) as structure directing surfactants, functionalized with amine groups and used as adsorbent for the toxic metal ions, Cr (VI), As (V), Pb (II) and Hg (II). Amino functionalization of mesoporous MCM-41 was achieved by cocondensation of N-[3-(trimethoxysilyl)-propyl] aniline with tetraethyl orthosilicate. Adsorption isotherm and adsorption capacity of the amine functionalized materials for Cr (VI), As (V), Pb (II) and Hg (II) ions were followed by inductively coupled plasma mass spectrometry (ICP-MS). Results demonstrate that amine functionalized MCM-41 prepared with ETAB showed higher adsorption capacity for Cr (VI), As (V), Pb (II) and Hg (II) ions in comparison to MCM-41 prepared with CTAB and DTAB. The higher adsorption capacity for MCM-41(ETAB) was correlated with amine content in the material (determined by CHN analysis) and relative decrease in pore volume and pore diameter. X-ray diffraction (XRD) analysis, nitrogen adsorptiondesorption measurements and Fourier Transform infrared spectrometry (FTIR) were used to follow the changes in the textural parameters and surface properties of the mesoporous materials as a result of amine functionalization to correlate with the adsorption characteristics. The adsorption process was found to depend on the pH of the medium.

• Clinical and Experimental Reproductive Medicine
• /
• 제47권2호
• /
• pp.101-107
• /
• 2020

Objective: The present study investigated sperm chromatin quality and testosterone levels in acrylamide-treated mice and the possible protective effects of vitamin E on the fertility potential of spermatozoa. Methods: Thirty-two adult male mice were divided equally into four groups. Group 1 was the control, group 2 received acrylamide (10 mg/kg, water solution), group 3 received vitamin E (100 mg/kg, intraperitoneal), and group 4 received both acrylamide and vitamin E. After 35 days, spermatozoa from the right cauda epididymis were analyzed in terms of count, motility, morphology, and viability. Sperm DNA integrity and chromatin condensation were assessed by acridine orange (AO), aniline blue (AB), toluidine blue (TB), and chromomycin A3 (CMA3) staining. Results: In acrylamide-treated mice, significantly lower sperm concentration, viability, motility, and testosterone levels were found in comparison with the control and acrylamide+vitamin E groups (p< 0.05). In the vitamin E group, significantly more favorable sperm parameters and testosterone levels were found than in the other groups (p< 0.05). There were also significantly more spermatozoa with less condensed chromatin in the acrylamide-treated mice than in the other groups. Moreover, significantly more spermatozoa with mature nuclei (assessed by AB, CMA3, AO, and TB staining) were present in the vitamin E group than in the control and acrylamide+vitamin E groups. Conclusion: This study revealed the deleterious effects of acrylamide on sperm parameters and sperm chromatin quality. Vitamin E can not only compensate for the toxic effects of acrylamide, but also improve sperm chromatin quality in mice.