• The Korean Journal of Pesticide Science
• /
• v.12 no.3
• /
• pp.295-301
• /
• 2008

Phenylformamidines are well known as insecticides for their specific activity against the insects. It has now been established that they show insecticidal activity as agonists on the octopamine receptor which is located in the synapse membrane. In this study we tried to test the effect of fluorine substituted aromatic formamidines and 1,3,5-triazapenta-1,4-dienes. Among the compounds, 2h, 2k, 21, 3g, 3h, 3k showed good activity against mite and aphid and 4f and 4g showed high activity against mite.

• Journal of Nutrition and Health
• /
• v.34 no.8
• /
• pp.833-842
• /
• 2001

The purpose of this study is to determine the effect of dietary proteins and fats on the hepatic histological changes, membrane stability, and drug-metabolizing enzyme activities during chemically induced rat hepatocarcinogenesis. Weanling Sprague-Dawley rats were fed the diet containing 20% casein or soy protein isolate and 15% perilla or corn oil for 10 weeks. Hepatocarcinogensis was initiated with diethylnitrosamine(DEN), and the rats were fed diets containing 0.02% 2-acetylaminofluorene(AAF) followed by 0.05% phenobarbital (PB). The scores of histological changes were decreased in treated rats fed soy protein diet compared to those find casein diet. Liver weights were significantly increased by AAF and PB treatment in rats fed casein diets in both oil groups. Glucose 6-phosphatase(G6Pase) activities, an index of membrane stability, were significantly reduced by AAF and PB treatment in rats find casein diets, and were lower in casein diet compared to soy protein diet groups. Especially, the activities were the highest in the rats fed soy protein-perilla oil diet. Lipid peroxide values also were increased by AAF and PB treatment in rats fed casein diet. Aniline hydroxylase activities were not influenced by protein and fat sources. Glutathione-dependent enzyme activities were increased by AAF and PB treatment. Linoleic and arachidonic acid content were increased in rats fed corn oil diet, and linolenic and eicosapentaenoic acid contents were increased in rats fed perilla oil diet. Our results suggest that soy protein isolate inhibit the abnormal histological changes in liver, possibly by maintaining the membrane stability during chemically induced rat hepatocarcinogenesis. Soy protein may be protective against the hepatocarcinogenesis induced by chemical carcinogen.

• The Korean Journal of Pesticide Science
• /
• v.10 no.1
• /
• pp.1-6
• /
• 2006

A methodology for the syntheses of carboxanilides using solid support of 4-chloro-3-nitorbenzophenone oxime resin 5 was developed. Condensation of 4-chloro-3-nitorbenzophenone resin 6 with hydroxylamine hydrochloride salt gave oxime resin 5. The reaction of oxime resin 5 with dioxin and oxathiin derivatives 7a-d afforded the corresponding polymer-bound dioxin and oxathiin derivatives 9a-d. These polymer-bound resins 9a-d were treated respectively with aniline in the presence of acetic acid resulted in the corresponding dioxin carboxanilides 10a-d (yield, 5%-quantitative).

• YAKHAK HOEJI
• /
• v.52 no.4
• /
• pp.316-321
• /
• 2008

The hepatoprotection by the methanol extract of Oenanthe javanica DC (water dropwort) (OJME) was investigated in Sprague Dawley rats with inducing liver damage by acetaminophen. After OJME administration for 1 week, the increase of hepatic lipid peroxide level by acetaminophen-induced hepatotoxicity was significantly reduced. In case of phase I microsomal enzyme systems including cytochrome P-450, aminopyrine N-demethylase and aniline hydroxylase, any significant differences between in control and in OJME-pretreated group was observed after acetaminophen treatment. However, the pretreatment of OJME maintained the hepatic glutathione level and the activity of liver cytosolic glutathione S-transferase, which was significantly decreased by the acetaminophen intoxication. Among the glutathione-generating system, glutathione reductase was more responsible for its biosynthesis rather than ${\gamma}-glutamylcystein$ synthetase. OJME itself showed the strong inhibition activity on DPPH radical generation. In conclusion, OJME administration maintains the liver glutathione pool and hepatic glutathione S-transferase activity, in addition with its high anti-oxidative capability, to show hepatoprotective effect from acetaminophen intoxication.

• Biomedical Science Letters
• /
• v.5 no.1
• /
• pp.51-58
• /
• 1999

To evaluate an effect of liver damage on the dermal oxygen free radical metabolizing enzyme activities, the $CCl_4$ (0.1 ml/ 100 g body wt., 50% $CCl_4$ in olive oil) was intraperitoneally given to the rats every other day for 2 weeks. Based on the histopathological findings, liver weight (%), serum alanine aminotransferase, xanthine oxidase activities and hepatic lipid peroxide contents, the animals were induced severe liver damage. In the present liver damaged animal, all the activities of dermal scavenging enzymes such as superoxide dismutase, catalase and glutathione peroxidase were significantly decreased compared with central. And under the cytochemical electron microscopy the more coarse granules of cerrous perhydroxide were found compared with the control. In conclusion, the $CCl_4$-induced liver damage may influence upon the activities of some dermal oxygen free radical scavenging enzymes.

• Biomedical Science Letters
• /
• v.12 no.4
• /
• pp.361-370
• /
• 2006

To evaluate an effect of pathological liver damage on the conjugation of cyclohexane metabolites, rats were pretreated with 50% $CCl_4$ dissolved in olive oil (0.1 ml/100 g body weight) 10 or 17 times intraperitoneally at intervals of every other day. On the basis of liver function, the animals pretreated with $CCl_4$ 10 times were identified as acutely liver damaged ones and the animals pretreated with $CCl_4$ 17 times were identified as severly liver damaged ones. To these liver damaged animals, cyclohexane (a single dose of 1.56 g/kg body weight, i.p.) was administered at 48 hr after the last injection of $CCl_4$. The rats were sacrificed at 4 or 8 hr after injection of cyclohexane. The cyclohexane metabolites, cyclohexanol (CH-ol), cyclohexane-1,2-diol (CH-1,2-diol), cyclohexane-1,4-diol (CH-1,4-diol), and their glucuronyl conjugates and cyclohexanone were detected in the urine of cyclohexane treated rats. The urinary concentration of cyclohexane metabolites was generally more increased in liver damaged animals than normal ones, and the increasing rate was higher in $CCl_4$ 17 times injected rats than 10 times injected ones. And liver damaged.ats, especially $CCl_4$ 17 times treated ones, had an enhanced ability of glucuronyl conjugation to CH-ol analogues compared with normal group. Futhermore, CH-1,2 and 1,4-diol were all conjugated with glucuronic acid in $CCl_4$ 17 times injected animals. On the other hand, the increasing rate of activities of hepatic cytochrome P450 dependent aniline hydroxylase, alcohol dehydrogenase and urine diphosphate glucuronyl transferase was higher in 17 times $CCl_4$-treated rats compared with normal and $CCl_4$ 10 times injected animals. Taken all together, it is assumed that an increased urinary excretion amount of cyclohexane metabolites in liver damaged rats might be caused by an increase in the activities of cyclohexane metabolizing enzymes. And enhanced conjugating ability of CH-ol in liver damaged animals and novel finding of conjugating form of CH-1,2 and 1,4-diol might be caused by increase in the activity of hepatic diphosphouridine glucuronyltransferase.

• BMB Reports
• /
• v.45 no.10
• /
• pp.560-564
• /
• 2012

The role of peroxiredoxin (Prx) I as an erythrocyte antioxidant defense in red blood cells (RBCs) is controversial. Here we investigated the function of Prx I by using Prx $I^{-/-}$ and Prx I/$II^{-/-}$ mice. Prx $I^{-/-}$ mice exhibited a normal blood profile. However, Prx I/$II^{-/-}$ mice showed more significantly increased Heinz body formation as compared with Prx $II^{-/-}$ mice. The clearance rate of Heinz body-containing RBCs in Prx $I^{-/-}$ mice decreased significantly through the treatment of aniline hydrochloride (AH) compared with wild-type mice. Prx I deficiency decreased the phagocytic capacity of macrophage in clearing Heinz body-containing RBCs. Our data demonstrate that Prx I deficiency did not cause hemolytic anemia, but showed that further increased hemolytic anemia symptoms in Prx $II^{-/-}$ mice by attenuating phagocytic capacity of macrophage in oxidative stress damaged RBCs, suggesting a novel role of Prx I in phagocytosis of macrophage.

• Korean Journal of Acupuncture
• /
• v.23 no.4
• /
• pp.177-186
• /
• 2006

목적 : 약침액(藥鐵液)의 지질과산화 예방 및 cytocome P450과의 상호 작용에 있어서 대계의 역할은 과거 연구가 거의 없었다. 따라서 본 실험에서는 대계 약침액이 지질과산화를 예방하고, 심혈관계질환 유발에 밀접한 연관이 있는 cytochrome P450의 직접적인 저해 효과를 검토 하고자 한다. 방법 : 대계 약침액이 지질과산화를 억제하는 정도를 평가하기 위하여 세포막을 구성하는 불포화지방산의 일종인 linoleic acid를 대상으로 지질과산화 진행 시간과 대계 약침액의 농도에 의존적인 저해 효과를 실험하였다. 또한 실험쥐의 간조직을 이용하여, 강제적인 과산화를 유도한 후 이를 방어하는 효능을 검토하였다. 그리고 cytochrome P450을 구성하는 그룹의 1A1, 1A2 및 2E1의 활성을 각각 EROD, MROD, p-nitrophenol, aniline 방법으로 측정하였다. 결과 및 결론 : 대계 약침액은 세포막 구성의 불포화 지방산인 linoleic acid의 산화를 시간 및 처리 농도에 의존적으로 억제하였고, 실험쥐의 조직 과산화를 유의성 있게 저해하였다. 또한 aryl hydrocarbon receptor (AHR)을 활성화 시켜 polycyclic aromatic hydrocarbons (PAHs)에 의한 심혈관계 질환 유발 인자로 알려진 cytochrome P450 1A1 및 1A2의 발현을 일부 저해하였으며, 특히 체내에 흡수된 알콜 대사에 관여하는 P450 2E1을 강하게 억제 시켰다.

• Journal of the Korean Chemical Society
• /
• v.45 no.6
• /
• pp.549-554
• /
• 2001

For the development of new COX-2 inhibitor, novel compound were synthesized through induction an arylsulfonyl group to 1-position, an arylcarboxamidyl group to 2-position and an alkyl group to 4-position of L-proline. We started from 4-hydroxy-L-proline, the 4-methylphenylsulfonyl of 1-position was introduced through N-tosylation and the carboxylic acid group was protected by esterification. We sucessfully converted to a various derivatives 4b-d for O-alkyl-(or aralkyl)ation of 4-position using silver oxide as catalysis. The 4-alkyloxy-1-tosyl L-prolines 5b-d were synthesized through base-hydrolysis for the deprotection of carboxylic acid. Final compound 1,2,4-substituted pyrrolidines, 4-alkyloxy-2-phenylcarboxamidyl-1-tosyl pyrrolidines 6a-d were synthesized through the condensation of arylamine with 3 and 5b-d using DCC.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.17 no.5
• /
• pp.1177-1181
• /
• 2003

Chinese cabbage is a vegetable of Cruciferous family. It was usually consumed as Kimchi. It was known to have amount of vitamin c. Recently the trend for the development of functional food combined with oriental herbs. For this aim the study was performed to evaluate the hepatoprotective effect via antioxidant activity of leaf and root of Sanchon Chinese cabbage(Brassica campetris L.) comparatively. The methanol extracts of Chinese cabbage were tested for investigating the effects on the formation of lipid peroxide and the activities of free radical generating enzyme in vitro in bromobenzene-treated rats. The methanol extracts of chinese cabbage reduced bromobenzene-induced hepatic lipid peroxidation and inhibited the activity of xanthine oxidase. The methanol extracts of chinese cabbage did not activate amionopyrine N-demethylase, aniline hydroxylase and glutathione S-transferase. Epoxide hydrolase activity was decreased by bromobenzene, which was restored by pretreatment of the methanol extracts of chinese cabbage. The results suggest that the methanol extracts of Chinese cabbage is reduced by enhancing the activity of epoxide hydrolase.