• Archives of Pharmacal Research
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• 제17권6호
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• pp.443-451
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• 1994

The binding characteristics of pirenzepine and oxomemazine to muscarinic receptor were studied to evaluate the selectivity of oxomemazine for the muscarinic receptor subtypes in rat cerebral microsomes. Equililbrium dissociation constant $(K_D){\;}of{\;}(-)[^3H]$quinuclidinyl benzilate$([^3H)QNB)$ determined from saturation isotherms was 64-pM. Analysis of the pirenzepine inghibition curve of [$^3H$]QNB binding to cerebral microsome indicatd the presence of two receptor subtypes with high $(K_1 = 16 nM, M_1 receptor)$two receptor subypes with about 20-fold difference in the affinity for high $(k_1 = 84nM, {\;} O_H receptor){\;} and {\;}low{\;} (K_1{\;} ={\;} 1.65\muM, {\;} O_L receptor$) affinity sites. The percentage populations of $M_1{\;} and M_3$, /TEX> receptors to the total receptors were 61 : 39, and those of $O_H{\;} and{\;} O_L$ receptors 39 : 61, resepectively. Both pirenzepine and oxomemazine increaed the $K_D$ value for $[^3H]QNB$ without affecting the binding site concentrations and Hii coefficient for the $[^3H]QNB$ without affecting the binding site concentractions and Hill coefficient for the [$^{3}$H]QNB binding. Oxomemazine had a 10-fold higher affinity at $M_1$ receptors than at $M_3$ receptors, and pirenzepine a 8-fold higher affinity at $O_H$ receptors were of $O_H$ receptors and 71% of $M_3$ receptors. However, $M_3$for oxomemazine and $O_H$for pirenzepine were composed of a uniform population. These results suggest that oxomemazine could be classified as a selective drug for $M_1$ receptors and also demonstrate that rat cerebral microsomes contain three different subtypes of $M_1{\;} M_3$ and the other site which is different from $M_1, {\;} M_2$, /TEX> receptors.

• 약학회지
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• 제37권6호
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• pp.647-658
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• 1993

The susceptibilities of aldehyde dehydrogenase (AldDH) and alcohol dehydrogenase (ADH) to active oxygen generated by xanthine-xanthine oxidase (XOD) system were studied. Incubation of AldDH with 2$\times$10$^{-3}$ units of XOD for 30 min at $25^{\circ}C$ resulted in the decrease of enzyme activity to 30% and it was inactivated completely when incubated with 5$\times$10$^{-3}$ units of XOD. Whereas 70% of ADH activity was retained after exposure to 5$\times$10$^{-3}$ units of XOD for 30 min, 40% of ADH activity was retained after exposure to 5$\times$10$^{-2}$ unit of XOD for 30 min. This inhibition effect by the active oxygen was preventable by catalase and glutathione, but not by SOD. The rates of the NADPH-dependent oxygen consumption by the liver S-9 mixture and microsomes were also determined in this study. Rate of oxygen consumption is increased in the liver S-9 mix and microsomes from phenobarbital-treated rat, and it was consistent with increased lipid peroxidation. In the presense of ethanol as a substrate, the oxygen consumption rates were increased. It is reported that hepatic AldDH activity is depressed in alcoholic liver diseases, however there is few report that explains the reason of depressed AldDH activity. These results are supportive of the theory that the increase in hepatic ethanol oxidation through the induced ME activity after chronic ethanol feeding generate oxygen radical at elevated rates and it leads to the depression of AldDH activity.

• Journal of Nutrition and Health
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• 제40권2호
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• pp.111-117
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• 2007

시판 목초액 A (원액 35%)을 사용하여 음용수에 0%, 1.0%, 25.0%, 50.0%, 75.0%가 되도록 조제한 다음, CD계 수컷 흰쥐 (150 ${\pm}$ 10 g)에 2개월 동안 조제사료와 함께 자유 음용케 하여 간조직 중의 활성산소로서 수퍼옥시드 라디칼(O$_{2}\;^-$), 히디록시 라디칼, 과산화수소 및 제거효소로서 수퍼옥시드 디스무타아제 (SOD), 글루타치온 퍼옥시다아제 (GPx) 및 카탈라아제 (CAT)에 미치는 영향을 평가하였다. 목초액 PL-25 및 PL-50 투여군의 간조직의 미토콘드리아 획분에서는 O$_{2}\;^-$의 생성량은 대조군 대비 12${\sim}$14%의 O$_{2}\;^-$의 생성량 억제효과가 나타났고, 간조직의 마이크로솜획분에서는 대조군 대비 각각 11.0${\sim}$15.0의 O$_{2}\;^-$의 생성량 억제효과가 나타났다. 간조직 미토콘드리아획분에서 ${\cdot}$OH 생성량이 목초액 PL-25 및 PL-50 투여군에서 대조군 대비 12${\sim}$20%의 ${\cdot}$OH 생성 억제효과가 나타났고, 간조직의 마이크로솜획분에서는 대조군 대비 17${\sim}$20%의 ${\cdot}$OH 생성 억제효과가 나타났다. 목초액 PL-25 및 PL-50 투여군의 간조직의 미토콘드리아획분에서는 대조군 대비 12${\sim}$15%의 유의적인 H$_{2}$O$_{2}$의 생성 억제효과가 나타났고, 간조직의 마이크로솜획분에서는 대조군 대비 20${\sim}$22%의 상당히 유의적인 H$_{2}$O$_{2}$의 생성 억제효과가 나타났다. 목초액 PL-25 및 PL-50 투여군의 간조직의 Mn-SOD 활성은 대조군 대비 15${\sim}$25%나 유의적인 활성 증가효과가 인정되었고, 간조직의 Cu/Zn-SOD 활성은 대조군 대비 11${\sim}$16%의 유의적인 SOD활성 증가효과가 인정되었다. 목초액 PL-25 및 PL-50 투여군의 간조직의 미토콘드리아획분의 GPx 활성은 대조군 대비 10${\sim}$17%의 GPx 활성 증가효과가 인정되었고, 간조직의 마이크로솜획분의 GPx 활성 증가효과가 인정되었다. 목초액 PL-25 및 PL-50 투여군의 간조직의 미트콘드리아획분의 CAT 활성은 대조군 대비 12${\sim}$14%의 유의적인 CAT 활성 증가효과가 나타났고, 간조직의 시토졸 1획분에서는 대조군 대비 15${\sim}$27%의 CAT 활성 증가효과가 인정되었다. 이상의 결과에서 목초액의 장기간 투여는 간조직 중의 활성산소의 억제효과뿐만 아니라 방어시스템으로서 활성산소 제거효소의 역할도 충실히 수행하여 노화를 효과적으로 예방하고 억제할 수 있을 것으로 기대된다.

• 한국수산과학회지
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• 제33권2호
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• pp.87-92
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• 2000

간장중의 활성산소 및 제거효소의 활성에 미치는 영향을 평가하기 위하여 미역의 건조분말을 $10{\%},\;20{\%},\;40{\%}$-첨가 조제한 미역국수 ($10{\%},\;20{\%},\;40{\%}\;FBA-noodle$)를 4주동안 SD계 흰쥐에 투여하여 미역국수의 생리작용을 평가하였다. $10{\%},\;20{\%},\;40{\%}$ FBA-noodle의 투여그룹의 mitochondria의 ${\cdot}OH$ 생성은 대조그룹 대비 각각 $20{\%},\;25{\%},\;35{\%}$의 현저한 OH 생성 억제효과가 인정되었다. 또한 $10{\%},\;20{\%},\;40{\%}$ FBA-noodle의 투여그룹의 microsome의 ${\cdot}OH$ 생성도 대조그룹 대비 $12{\~}20{\%}$의 유의적인 ${\cdot}OH$ 생성 억제효과가 인정되었다. $10{\%},\;20{\%},\;40{\%}$ FBA-noodle의 microsome의 $H_2O_2$의 생성은 유의적인 억제효과를 인정할 수 없었지만, cytosol중의 $O_2^({\cdot}-)$ 생성은 $20{\%},\;40{\%}$ FBA-noodle에서 $10{\%}$의 $O_2^({\cdot}-)$의 생성 억제효과가 인정되었다. $10{\%},\;20{\%},\;40{\%}$ FBA-noodle 투여그룹의 간장 mitochondria의 Mn-SOD 활성은 대조그룹 대비 $10{\~}15{\%}$의 Mn-SOD 활성의 증가효과가 인정되었다. 간장 microsome의 Mn-SOD 활성은 $10{\%} 및 20{\%}$ FBA-noodle 투여그룹은 Mn-SOD 활성의 유의적인 증가 효과를 인정할 수 없었지만, $40{\%}$ FBA-noodle 투여그룹은 $12{\%}$의 유의적인 Mn-SOD 활성 증가효과가 인정되었다. 또한 $10{\%},\;20{\%},\;40{\%}$ FBA-noodle의 투여그룹의 간장 cytosol의 Cu, Zn-SOD 활성은 대조그룹 대비 $10{\~}20{\%}$의 Cu, Zn-SOD 활성의 유의적인 증가효과가 인정되었다. 한편 간장 cytosol의 글루타치온 퍼옥시다아제 (GSHPx) 활성을 평가하여 보면 $10{\%}, 20{\%}, 40{\%}$ FBA-noodle 투여그룹의 cytosol의 GSHPx 활성은 대조그룹 대비 $20{\~}40{\%}$의 매우 효과적인 GSHPx활성의 증가효과가 인정되었다. $10{\%}, 20{\%}, 40{\%}$ FBA-noodle 투여그룹의 mitochondria의 LPO의 함량을 비교하여 보면 $10{\%}$ FBA-noodle은 유의적인 LPO의 생성 억제효과를 인정할 수 없었지만, $20{\%},\;40{\%}$ FBA-noodle은 $10{\%}$의 유의적인 LPO 생성 억제효과가 인정되었다. $10{\%},\;20{\%},\;40{\%}$ FBA-noodle 투여그룹의 microsome의 LPO의 함량은 $10{\%}$ FBA-noodle은 유의적인 LPO의 생성 억제효과를 인정할 수 없었지만, $20{\%} 및 40{\%}$ FBA-noodle은 약 $10{\~}12{\%}$의 유의적인 LPO 생성 억제효과가 인정되었다.

• Archives of Pharmacal Research
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• 제26권7호
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• pp.535-539
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• 2003

The EtOAc soluble fraction from the stem of Sorghum bicolor showed a strong free radical scavenging activity. Five major compounds were isolated from this fraction. They were identified by spectral data as methyl ferulate (1), methyl p-hydroxycinnamate (2), p-hydroxybenzaldehyde (3), tricin (4), and quercetin 3,4 -dimethyl ether (5). Among these compounds, 1 exhibited a strong, free radical scavenging activity on 1, 1-diphenyl-2-picrylhydrazyl (DPPH) with an $IC_50$ value of 0.7 $\mu$M. We further studied the effects of these isolated compounds on the lipid peroxidation in rat liver microsomes induced by non-enzymatic method. All five compounds showed anti-lipid peroxidation activity ($IC_50$ values of 0.5, 0.4, 0.3 and 0.3 $\mu$ M, respectively).

• 생명과학회지
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• 제10권5호
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• pp.467-474
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• 2000

Male mice (ddY strain) were fed a laboratory chow diet containing the water extract from stem bark of Rhus verniciflua Stokes (RVS) for 14 days. There were no significant difference in body weight gain, feed intake, the hepatic lipid profile and serum total cholesterol and phodpholipid concentrations. The concentration of triglyceride in serum was significantly lower in the RVS group than that in the control group. The concentration of high-density-lipoprotein cholestrol in serum was significantly higher in the RVS group than that in the control group. The methanol extract from RVS stem bark effectively inhibited the formation of thiobarbituric acid-reactive substances as a marker of lipid peroxidation of liver microsomes in a concentration-dependent manner. This study showed that the water extract from stem bark of RVS decreased the serum triglyceride concentration and methanol extract has an antioxidative activity.

• 한국연초학회지
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• 제9권2호
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• pp.87-93
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• 1987

The mutagenic activities of the pyrolyzates (300, 600, 750 and 85$0^{\circ}C$ ) of extracts from three saponeous expectorants (Platicodi Radix, Polygalae Radix and Asiasari Radix) and two nonalkaloidal antitussives (Lirionis Tuber and Codonopsis lanceolata Radix), medicinal plants, were studied in the Ames Salmonella/microsomes test system. The pyrolysates of Codonopsis lanceolata Radix and Asiasari Radix extracts at 85$0^{\circ}C$ were slightly mutagenic to tester strain TA98( frame shift ) and TA100(base-pair substitution) of Salmonella typhimurium, and the mutagens in these pyrolyzates required the metabolic activation by a liver microsomal fraction However, the extracts and pyrolyzates of all medicinal plants tasted except the above two results dud not show the significant increase in revertant colonies.

• 한국연초학회지
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• 제10권1호
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• pp.57-63
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• 1988

The mutagenic activities of the pyrolysates(300, 600, 750 and 85$0^{\circ}C$) of extracts from four antitussive or expectorant medicinal plants(Daturae Folios, Scopoliae Rhizoma, Acori Rhisoma, and Schigandrae Fructus) were studied in the Ames Salmonella/microsomes test system. The pyrolyzate of Schizandrae Fructus did not show the mutagenicity to tester strain TA98 of Salmonella typhinurium. However, those of other medicinal Plants, Daturae Folium, Scopoliae Rhigoma and Acori Rhizoma, exhibited the mutagenic activity to this strain and the mutagenicity of them were decreased gradually to 70% of the initial activity according to time course after the preparation of the samples with DMSO.

• BMB Reports
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• 제30권2호
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• pp.157-161
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• 1997

The present paper reports characteristics and specificity of the inhibitory action of $N^{\alpha}-tosyl-L-lysine-chloromethyl\;ketone$ (TLCK) and $N^{\alpha}-tosyl-L-phenylalanine-chloromethyl\;ketone$ (TPCK) on the glucose6-phosphate transporter of rat liver microsomes. The TLCK-induced inhibition was pH dependent. The inhibition constants for TPCK were determined by following pseudo-Lst order reaction mechanism. The inhibition was protected by preincubation with excess amount of glucose-6-phosphate. The results proved that (a) TLCK inactivates the microsomal glucose-6-phosphate transporter, (b) the inhibition results from the modification of sulfhydryl groups of the transporter.

• BMB Reports
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• 제36권3호
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• pp.332-335
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• 2003

Cytochrome P450 in microsomes can be quantitated using the characteristic 450 nm absorption peak of the CO adduct of reduced cytochrome P450. We developed a simple microplate assay method that is superior to previous methods. Our method is less laborious, suitable for analyzing many samples, and less sensitive to sample aggregation. Microsome samples in microplate wells were incubated in a CO chamber rather than bubbled with CO gas, and then reduced with sodium hydrosulfite solution. This modification allowed a reliable and reproducible assay by effectively eliminating variations between estimations.