• YAKHAK HOEJI
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• v.34 no.4
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• pp.224-237
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• 1990

A single uniform population of specific, saturable, high affinity binding site of $[^3H]QNB$ guinuclidinyl benzilate(QNB) was identified in the rat cerebral microsomes. The Kd value(37.2 pM) for $[^3H]QNB$ calculated from the kinetically derived rate constants was in agreement with the Kd value(48.9 pM) determined by analysis of saturation isotherms at various receptor concentrations. Dimenhydrinate(DMH), histamine $H_1-blocker$, increased Kd value for $[^3H]QNB$ QNB without affecting the binding site concentrations and this effect resulted from the ability of DMH to slow $[^3H]QNB-receptor$ association. Pirenzepine inhibition curve of $[^3H]QNB$ binding was shallow(nH = 0.52) indicating the presence of two receptor subtypes with high ($M_1-site$) and low($M_2-site$) affinity for pirenzepine. Analysis of these inhibition curves yielded that 68% of the total receptor populations were of the $M_1-subtype$ and the remaining 32% of the $M_2-subtype$. Ki values for the $M_1-$ and $M_2-subtypes$ were 2.42 nM and 629.3 nM, respectively. Ki values for $H_1-blockers$ that inhibited $[^3H]QNB$ binding varied with a wide range ($0.02-2.5\;{\mu}M$). The Pseudo-Hill coefficients for inhibition of $[^3H]QNB$ binding by most of $H_1-blockers$ examined except for oxomemazine inhibition of $[^3H]QNB$ binding were close to one. The inhibition curve for oxomemazine in competition with $[^3H]QNB$ was shallow(nH = 0.74) indicating the presence of two receptor populations with different affinities for this drug. The proportion of high and low affinity was 33:67. The Ki values for oxomemazine were $0.045{\pm}0.016\;{\mu}M$ for high affinity and $1.145{\pm}0.232\;{\mu}M$ for low affinity sites. These data indicate that muscarinic receptor blocking potency of $H_1-blockers$ varies widely between different drugs and that most of $H_1-blockers$ examined are nonselective antagonist for the muscarinic receptor subtypes, whereas oxomemazine might be capable of distinguishing between subclasses of muscarinic receptor.

• Korean Journal of Food Science and Technology
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• v.32 no.3
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• pp.726-735
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• 2000

This study was conducted to investigate the biological activities of polysaccharide extracted from the fruit body and cultured mycelia of Phellinus linteus IY001. All fractions were extracted by hot water, in the next, Fr. I, Fr. II, Fr. III and Fr. IV were polysaccharide obtained by ethanol precipitation or ultrafiltration. The highest antitumor activity against sarcoma 180 in ICR mice was observed in Fr. III and Fr. IV at the level 85%, but the antitumor activity had no connection with their anticomplementary activity in vitro, it might probably be due to extraction of hot water. All fractions promoted the production of nitric oxide and $TNF-{\alpha}$ in macrophage, addition of Fr. I and Fr. II resulted in production of nitric oxide$3(5.9{\sim}37.6\;{\mu}M)$ and of the $TNF-{\alpha}$ production($8,696.2{\sim}9,420pg/ml)$. All fractions inhibited the lipid peroxidation induced by $AsA/Fe^{2+}$, $ADP/NADPH/Fe^{3+}\;and\;CCl_4/NADPH$ in rat liver microsomes, and Fr. III showed the electron donating ability stronger than tocopherol in assay system using DPPH. From these results, it is suggested that all fractions contain immunoregulatory components which may protect cellular materials from the oxidative damages by their radical scavenging activities.

• Korean Journal of Community Nutrition
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• v.2 no.5
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• pp.735-744
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• 1997

The effect of green tea drinking on the hepatocellular chemical cacinogenesis have been studied. Placental glutathione S-transferase(GST-P) positive foci area in a liver tissue, contents of thiobarbituric acid reactive substances(TBARS), total cytochrome P450 and glucose 6-phospphatase(G6P) activity in hepatic microsomes were investigated. Weaning Sprague-Dawley male rats were fed AIN-76A diet with deionized water or green tea infusion, Rats of CTR and CTR+ groups were provided deionized water while GTI and GTI+ groups were provided green tea instead of deionized water for the entire experimental period of 13weeks. Rats of GTP and GTP + groups had deionized water for the first 6 weeks and switched to green tea for the last 7weeks of the experimental period. CTR+, GTI +, and GTP + groups were carcinogen treated groups, Diethylnitrosamine(DEN) was injected as a single dose of 200mg/kg body weight intraperitoneally after 4 weeks of feeding. 2-Acetyla-minofluorene(AAF) was used as a carcinogen proliferater and suppled in the diets of carcinogen treated rats as 0.02% content for the last 6weeks starting from 2weeks after DEN injection. Rats were sacrificed after 13week weeks of feeding. The area and number of GST-P positive foci detected in carcinogen treated rats were decreased by green tea ingestion but when timing and duration of green tea ingestion was delayed after promotion period as in GTP + group, GST-P positive foci were not decreased as much as in GTI+ group. TBARS contents of carcinogen treated rats decreased by 13weeks of green tea ingestion but GTP groups did not show statiscally significant differences. G6P activities tended to decrease by carcinogen treatment but changes were not statiscally significant by green tea ingestion. Total cytochrome P450 contents were increased by carcinogen treatment. Thirteen weeks of green tea ingestion (GTI) also increased to total cytochrome P450 contents while 7weeks of green tea ingestion(GTP) did show any effects. These results suggest that green tea has suppressive effects on hepatocellular chemical carcinogenesis probably through the activities of antioxidant compounds. (Korean J Community utrition 2(5) : 735∼744, 1997)

• Journal of the Korean Society of Food Science and Nutrition
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• v.32 no.1
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• pp.124-130
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• 2003

Effect of Korean red ginseng (KRG) on the level of serum and liver lipids and lipid peroxidation was investigated in the rats fed high fat diet. Content of serum total cholesterol was significantly decreased (P<0.05) in KRG I group and KRG II group. Content of HDL-cholesterol was significantly increased by 69.75% and 39.15% in KRG I and KRG II group compared to control group, respectively. Atherogenic index (hi) was also significantly decreased by 74.76% and 37.38% in KRG I and KRG II groups compared to control group, respectively. Serum triglyceride content was significantly decreased (p<0.05) in only KRG II group. Antioxidative activity of KRG on the lipid peroxidation of serum and tissues in rats was also studied in vivo by measuring the formation of thiobarbituric acid reactive substances (TBARS). Contents of TBARS in the serum of both KRG groups were significantly decreased (p<0.05) and that of nonheme iron in serum was significantly increased (p<0.05) in a dose-dependent manner, which suggested that lipid peroxidation contents are inversely correlated with serum nonheme iron content. Content of TBARS in liver was significantly decreased (p<0.05) in KRG I and KRG II groups, without any influence in other tissues. Content of TBIARS in liver microsomal fractions stimulated by Fe$^{2+}$/ascorbate was significantly decreased (p<0.05) in KRG I and KRG II groups, whereas this observation did not occur in liver mitochondrial fractions. When the effect of KRG on TBARS content in the liver fractions of homogenates, microsomes, and mitochodria stimulated by Fe$^{2+}$/ascorbate was tested in vitro experimental model, TBARS of liver three fractions was significantly decreased at 6 mg/mL KRG compared with those of control. These results suggested that KRG powder have hypocholesterolemic effect as well as antioxidative effect in the serum and liver of the rats fed high fat diet.

• Journal of Life Science
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• v.15 no.5 s.72
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• pp.819-825
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• 2005

The Antioxidative accvities of the cell free extracts containing high glutathione by Saccharomyces cerevisiae FF-8 were tested in vitro experimental models : DPPH method for radical scavenging activity, ferric TBA method and ferric thiocyanate method using linoleic acid and tissue microsome for lipid peroxidation inhibitions. The concentration of intercellular glutathione by cultivating S. cerevisiae FF-8 in the YM optimal medium obtained $204\mug/ml$, which was increased by 2.76-fold from $74\mug/ml$ in the YM basal medium. A comparition between the YM basal medium and the YM optimal medium on antioxidative substance produced by S. cerevisiae FF-8 was investigated. In DPPH ($\alpha, \alpha-diphenyl-\beta-picrylhydrazyl$) method, the electron donating activity of the glutathione produced by S. cerevisiae FF-8 cultured in the YM optimal medium was as high as that of BHT ($ 0.05\%w/v $). The antioxidative a.tivity was measured by inhibition against lipid peroxidation of rat tissues' microsomes. The results of anti-oxidant activity of the cell free extracts by S. rerevisiae FF-8 cultured in the YM optimal medium was shown in the following order . $ liver 60.98\% > kidney 56.43\% > heart 52.91\% > brain 52.13\% > testis 45.57\% > spleen 42.95\% $. In antioxidative activities determined by ferric thiocyanate method and TBA methods against lipid peroxidation, the lipid peroxidation in the control mixture increased more rapidly than the typical peroxidation curve of linoleic acid from one day. The antioxidative activity of the cell free extracts by cultivating S. cerevisine FF-8 in the YM optimal medium were higher than that of the YM basal medium. These data indicate that the cell free extracts containing a high intercellular glutathione of S. cerevisiae FF-8 cultured in YM optimal medium showed strong antioxidative capacities by DPPH radical scavenging activity and ferric thiocyanate and TBARS measurements.