• YAKHAK HOEJI
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• v.45 no.5
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• pp.494-499
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• 2001

Houttuynia cordata (Saururaceae) has pungent smell and taste. It has been regarded as detoxicant, antipyretic, antiinflammantory and diuretic agents. In order to evaluate antioxidative and antilipidperoxidative efficacies, its fractions ($H_2O$, 20% MeOH, 40% MeOH, 60% MeOH, 170% MeOH) were measured by DPPH method and TBARS assay on rat liver homogenate. It was revealed that 60% MeOH fractions had potential antioxidative activity and inhibited lipid peroxidation significantly: In active fractions, we isolated rutin, hyperin, quercitrin and quercetin.

• YAKHAK HOEJI
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• v.44 no.4
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• pp.354-357
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• 2000

Two ellagitannins, pedunculagin and 2,3-(S)-Hexahydroxydiphenoyl (HHDP)-D -glucose and three condensed tannins, (+)-catechin, (-)-epicatechin and procyanidin B-4 which were isolated from Rubus coreanum were evaluated for their antioxidative effects with 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and lipid peroxidation generation system mediated by addition of $H_2O$$_2$to rat liver homogenate (TBARS). The ellagitannins, 2,3-(S)-HHDP-D-glucose and pedunculagin, showed more potent antioxidative activities by DPPH and TBARS than condensed tannins.

• YAKHAK HOEJI
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• v.39 no.5
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• pp.506-510
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• 1995

The 5-(2'-(N-(1-methyl-3'-carbamylphenyl)-n-propyl))aminoethyl)-8- hydroxy-4-methyl-carbostyril derivatives which have isoelectronic and isosteric structural similarity with dobutamine without having the Catechol-O-Methyltransferase (COMT) vulnerable m-hydroxy group were synthesized via 7 synthetic steps, and their stabilities in phosphate buffer solution(pH=7.4), human blood. 80% human plasma and 20% rat liver homogenate were determined in vitro condition.

• YAKHAK HOEJI
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• v.38 no.1
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• pp.12-19
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• 1994

Capsaicin(8-methyl-N-vanillyl-6-nonenamide) is the principal pungent component of Capsicum fruits. This work is directed to the capsaicin-hydrolyzing enzyme playing a key role in the rate limiting and critical step of capsaicin metabolism. In order to get precise information on the enzyme's subcellular location, rat liver homogenate was divided into six subcellular fractions by differential centrifugation technique: crude nuclear pellet, PNS(post nuclear supernatant) fraction, lysosomal pellet, cytosol, Tris wash fraction, micrisomes. Capsaicin-hydrolysing enzyme activity was analysed by high performance liquid chromatography(HPLC). This enzyme was found at the highest specific activity in the microsomal fraction and co-distributed with marker enzymes of the endoplasmic reticulum, NADPH-cytochrome c reductase and nucleoside diphosphatase. This is compatible with the result of ninhydrin color reaction of vanillylamine, primary metabolite of capsaicin hydrolysis, on thin layer chromatography(TLC). This enzyme is most active at pH $8.0{\sim}9.0$. Definite subcellular location of this enzyme will make it easy to proceed with further study.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.133-133
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• 1993

DA-125의 rat blood중 분해반감기는 4.28분으로, DA-125는 정맥 투여후 신속히 M1으로 분해되었으며, DA-125는 투여 10분 후부터 검출되지 않았다. Mouse에 25mg/kg 정맥주사 한 후의 M1의 phamacokinetic parameter는 terminal t$\frac{1}{2}$ 344분, MRT 371분, Vss 25.7 $\ell$/kg, CL$_{total}$ 69.3 ml/min/kg이었으며 투여 2hr후에 M1및 대사체가 폐, 위, 신장등에는 다량 존재하였으나 심장에서는 검출되지 않았다. Rat에 10 mg/kg 정맥주사한 후의 혈장농도는 terminal phase에 도달하지 못하고 혈장농도가 변동을 나타내었다. 담즙으로의 배설은 주로 M2의 형태로 이루어졌으며 M1이 소량 차지하고 M3와 M4는 검출되지 않았다. DA-125는 rat 및 mouse liver homogenate에 의해 대사되어 FT-ADM(M1) ,13-dihy-dro FT-ADM(M2), 7-deoxy-adriamycinone(M3) 및 7-deoxy-13-dihydro adriamyci-none(M4)를 형성하였다. DA-125는 혐기, 호기 및 보효소, 종차에 관계얼이 반응개시 30분후에 약 90%가 분해되었으나 각 대사체의 생성여부 및 속도는 조건에 따라 변화하였다.

• Journal of Ginseng Research
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• v.9 no.2
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• pp.213-220
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• 1985

It was attempted to observe the effects of ginseng saponin, one of the major components of the roots of Panax ginseng, on androgen biosynthesis from cholesterol in vitro as well as in vivo in rat testis. Ginseng saponin was administered by stomach tubing prior to intraperitoneal injection of cholesterol containing (4-14C)-cholesteroll into adult male rats and the liver, testis and blood serum were analyzed. The first high radioactivity of the liver and blood serum of test animal was observed at 6 hours after radioactive cholesterol injection, while that of control appeared at 12 hours after the injection. In the case of testis, the first high radioactivity of test group appeared between 4 and 6 hours after the radioactive cholesterol injection, while that of control appeared at 10-14 hours. Analysis of radioactivity distribution of cholesterol, androstenedione and testosterone in the testis of rats fed with/without ginseng saponin piror to (4-14C)-cholesterol injection showed that the saponin stmulated the synthesis of androgens from cholesterol. This was confirmed again by in vitro experiment using testis homogenate as an enzyme source. From the above experimental results, it was suggested that the ginseng saponin stimulates both cholesterol transport and the biosynthesis of androgens from cholesterol in rat testis.

• Journal of Acupuncture Research
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• v.15 no.2
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• pp.135-145
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• 1998

Bupleury radix has been used for the treatment of fever, liver disease, inflammation in traditional medicine. The present study was carried out to evaluate the antioxidant effects of Bupleury radix aqua-acupuncture solution (BRAS) in vitro. Oxygen derived free radicals produced in the course of normal aerobic life, such as superoxide anion radical($O_2^-$ ), hydroxyl radicaI( OH), hydrogen peroxide($H_2O_2$) and singlet oxygen($^1O_2$) can attack polyunsaturated fatty acid in cell membranes, enzymes, other cell compounds, and give rise to lipid peroxidation, DNA damage, lipofuscin accumulation, structure alteration of cell membrane and cell death. In this study, antioxidant effects of BRAS on lipid peroxidation were determined according to the method of TBA. BRAS inhibited markedly peroxidation of linoleic acid during the autoxidation, and also inhibited lipid peroxidation induced by hydroxyl radical derived from $H_2O_2-Fe^{2+}$ in rat liver homogenate. And BRAS showed 30% scavenging effect on DPPH radical, also exhibited a 30% inhibitory effect on superoxide generation from xanthine-xanthine oxidase system. In addition, BRAS protected the cell death induced by tert-butyl hydroperoxide(t-BHP) and significantly increased cell viability in the normal rat liver cell(Ac2F).

• Journal of Pharmaceutical Investigation
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• v.27 no.1
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• pp.1-10
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• 1997

For the purpose of improving the chemotherapeutic index of acyclovir(ACV), it was conjugated with asialofetuin(AF), which has been reported to enter into hepatocytes. When $[H^3]$ acyclovir in itself or its conjugate were administered to rats, the latter was taken up more selectively by the liver than any other tissues. The stability of ACVMP-AF conjugate in phosphate buffer (pH 5.0) and rat liver homogenate showed a pseudo-first order profile. ACVMP-AF, however, was relatively stable in pH7.4 phosphate buffer and rat plasma. The conjugate was added to the isolated rat hepatocyte and cellular uptake was monitored by scintillation counting for up to 6 hours at $37^{\circ}C$. Hepatocytes incubated with the conjugate exhibited radioactivities significantly enhanced over control levels dose-dependently, i.e., a 3-40 fold increase in radioactivities was observed over controls at the conjugate concentrations of $0.1-10\;{\mu}g/ml$. The AUQ in the liver, kidney, spleen, intestine and lung was higher in treatment with ACVMP-AF than that in treatment with ACV. In treatment with ACVMP-AF, the weighted-average overall drug targeting efficiency(Te) for the liver was higher than in treatment with ACV(57.00 vs 13.31 %), and the weighted-average tissue exposure(Re) was 5.03 for the liver. These results indicated that ACVMP-AF conjugate was rapidly taken up by hepatocytes and could be an efficient and selective hepatic targeting system.

• Journal of Life Science
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• v.16 no.1
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• pp.95-100
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• 2006

This study was carried out to investigate the effects of Salicornia herbacea L. (SH) on carbon tetrachloride $(CCl_4)-induced$ hepatotoxicity. Sprague-Dawley rats were intraperitoneally administered the SH at 100 mg/kg per day for two weeks. Then single dose of $CCl_4$ (3.3 ml/kg) was injected into rats. Twelve hours later, they were anesthesized with ether and dissected. $SH-CCl_4-administered$ group showed $65.56\%\;and\;59.04\%$ of inhibitory effects in aspartate aminotransferase (AST) and alanine aminotransferase (ALT) activities, compared to $CCl_4-treated$ group (p<0.05). Malonedialdehyde (MDA) levels of $SH-CCl_4-administered$ group in liver homogenate and mitochondria were significantly inhibited by $53.74\%,\;89.86\%$, and respectively, compared to $CCl_4-treated$ group (p<0.05). Superoxide dismutase (SOD) activities of $SH-CCl_4-administered$ group in liver homogenate and mitochondria were significantly inhibited by $42.51\%,\;and\;38.42\%$, respectively, compared to $CCl_4-treated$ group (p<0.05). The histological examinations showed that the liver cell necrosis and centrilobular congestive aggregation induced by $CCl_4$ were clearly eliminated by the administration of SH. These results suggest that SH could have the protective effects against hepatotoxicity.

• Journal of Pharmaceutical Investigation
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• v.22 no.3
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• pp.185-196
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• 1992

To assess its suitability as a prodrug of 5-fluorouracil (5-FU), 1-glycyloxymethyl-5-FU HCl (GFU), a 5-fluorouracil derivative having a glycyloxymethyl group at the N-l position was synthetized. Its physicochemical properties and hydrolysis kinetics, in aqueous solution of pH $1{\sim}10$ and in the presence of human plasma or rat liver homogenate were studied. Its acute toxicity and antitumor activity against sarcoma 180 were also examined, GFU showed higher lipid/water partition coefficient than 5-FU. The calculated $pK_{\alpha}$ values of 5-FU and GFU were 8.02 and 7,20, respectively. The decomposition rates of GFU in aqueous solution showed a pH-dependence over the pH range used, which could be ascribed to solvent catalysed hydrolysis reaction at pH lower than 4,16 and to specific hydroxide ion hydrolysis reaction at pH higher than 4,16, The half-life of GFU was 6,9 min in 80% human plasma solution and less than 3 min in rat liver homogenate at $37^{\circ}C$, The $LD_{50}$ value of 5-FU was 240 mg/kg while that of GFU was 440.6 mg/kg (226 mg as 5-FU). Both of 5FU and GFU showed a strong antitumor activity, Therapeutic ratios of 5-FU and GFU were 3.07 and 3.55, respectively.