• Applied Microscopy
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• 제17권2호
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• pp.41-54
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• 1987

This experiment was performed to investigate the acute and chronic effects of lead on cerebral cortex. In acute treatment, mouse were injected with lead acetate at dose of 0.3 mmole/kg body weight, and in chronic treatment, mouse were supplied 0.03 M lead acetate sol. in the place of water. After treatment, mouse were sacrificed at time intervals of 24, 48, 72, and 96 hours in acute treatment and at time intervals of 4 weeks and 8 weeks in chronic treatment. In acute treatment, acetylcholinesterase activity is reduced at 72 hours and recovered at 96 hours in homogenate, and reduced at 24 hours and recovered at 72 hours in crude synaptosomes. In chronic treatment, acetylcholinesterase activity is increased in young mouse but reduced in mother mouse. Ultrastructural changes were composed of swelling of Golgi apparatus, nerve terminals with diminished synaptic vesicles, and vacuolated myeline lamellae of myelinated axon.

• Journal of Pharmaceutical Investigation
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• 제18권2호
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• pp.49-53
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• 1988

Pivaloyloxymethyl ester of piperacillin was synthesized by reacting sodium piperacillin with chloromethyl pivalate, and its chemical structure was determined by infrared and $^1H$ nuclear magnetic resonance spectroscopic methods. The pharmaceutical properties of the ester were investigated to assess its potential as a novel prodrug of piperacillin. The interface transfer of piperacillin and the ester was studied in a two-phase in vitro system composed of aqueous pH buffers and n-octanol. The ester was more lipophilic, and less water soluble above pH 4.0 than piperacillin. Significant antibacterial activity was not observed in the ester in vitro, but the ester was hydrolyzed into the parent drug in the rat liver homogenate. The serum levels of orally administered ester suspension containing 0.1% Tween 80 were measured in rabbits. It was found that the ester showed higher blood level, comparing with no observation of piperacillin in serum, but the time reaching the maximum serum concentration was 5 hr.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1996년도 춘계학술대회
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• pp.287-287
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• 1996

Long-circulating liposomes have prompted interests in using them as a drug delivery system. This improvements in delivery has been thought to be the results from sustained action of liposomes in plasma without RES uptake. Although methotrexate(MTX) has been one of the most widely used antineoplastc drug, its use was limited by prompt RES uptake. The purpose of this study was to prepare long-circulating liposomes for MTX using highly water-soluble polymer (PEG-PE). In vitro, release of MTX from liposomes in phosphate buffer (pH 7.4), rat liver homogenate, and rat plasma was investigated. The pharmacokinetics and organ distribution of fee drug, conventional and long-circulating liposomes were also compared with one another after intravenous administration to rats.

• Advances in Traditional Medicine
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• 제4권3호
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• pp.211-214
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• 2004

The inhibitory effect of dl-puerol A as but-2-enolide isolated from Sophora japonica was investigated on copper ion-induced protein oxidative modification in vitro. It inhibited copper-induced protein oxidative modification. However, its inhibitory effect was a little weaker than that of $dl-{\alpha}-tocopherol$ as an antioxidant. The results demonstrated that dl-puerol A, one of but-2-enolides, might be of use in the oxidative stress.

• Archives of Pharmacal Research
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• 제14권2호
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• pp.109-113
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• 1991

Two types of aggressive behavior were produced by selective breeding in ICR mimce. NC900 line mice exhibited high level of species-typical, isolation-induced aggression, conversely, NC100 line mice exhibited little aggression. The present study tested the hypothesis that these differences involved brain monoamine systems. Comparisons of microdissected samples from various brain regions showed that NC100 line mice had significantly lower concentrations of dopamine. DOPAC and HVA in the nucleus accumbens (NAB) and caudate nucleus (NCU) than NC900 line. Homogenate binding studies demonstrated that NC100 mice had significantly increased density of $D_1$ dopamine receptor, but not $D_2$ dopamine receptor in the caudate nucleus. These results support the hypothesis that central dopamine pathways play an important role in modulating the genetically selected differences in aggressive behavior, and of which intensity differs from TEX>$D_1$\;and\;$D_2$ dopamine receptors.

• 대한한방내과학회지
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• 제1권1호
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• pp.92-97
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• 1976

Upon feeding dried Ginseng to rats of either low-protein or high protein diet ethanol was administered intraperitoneally and disappearance rate blood alcohol was enzymatically measure. In terms of residual blood alcohol after a time lapse of 3.5 hours between intraperitonial administration and blood withdrawal neither ginseng nor ginseng plus 40% casein did improve the rate, of alcohol clearance but sexual difference was clearly demonstrated in favor of female rats. In the case of blood withdrawn only 2 hours after intraperitoneal injection of alcohol, the tendency of female superiority in alcohol clearance rate is demonstrated when a comparison is made among the groups fed with ginseng and this was particularly true is groups of rats fed with basal diet plus 1 percent ginseng residual blood ethanol being 15.4 mg/ml vs. 8.8 mg/ml. Liver homogenate alcohol dehydrogenase activity measured in terms of residual ethanol content after in vitro reaction on which a known amount of alcohol was added clearly demonstrated a male superiority in alcohol clearance.

• 한국식품과학회지
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• 제31권4호
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• pp.1096-1100
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• 1999

The protective effect of Bifidobacterium breve K-110, K-111 and B. infantis K-525 on carbon tetrachloride induced hepatotoxicity in rats was investigated. Among them, B. infantis K-525 had the most potent hepatoprotective activity. It reduced serum aspartate aminotransferase and alanine aminotransferase levels to 51% and 80% of the $CCl_{4}-treated$ groups, respectively. In rat liver homogenate intoxificated with $CCl_{4}$, B. infantis K-525 inhibited in vitro as well as in vivo lipid peroxidation more than the other Bifidobacteria.

• 생약학회지
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• 제28권3호
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• pp.156-161
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• 1997

For the search of hepatoprotective compounds from the folk medicines, 14 natural products which have been traditionally used as hepatoprotective drugs in Korea were extracted with methanol. The extracts were screened for the antioxidant activity on lipid peroxidation induced by Fenton reaction in rat homogenate and Ac2F cell toxicity by t-hydroperoxide. Dendrobium moniliforme and Castanea crenata were chosen for the further investigation and its therapeutic effects on the liver damage induced by carbon tetrachloride in rats were evaluated. Oral administration of the extracts reduced the aspartate aminotransferase(AST) and alanine aminotransferase(ALT) activities in the serum of the carbon tetrachloride intoxicated rat. And the treatment of the extracts prevented the decrease of aminopyrine N-demethylation and aniline hydroxylation activities of the carbon tetrachloride-intoxicated rat liver. These results suggest that oral administration of Dendrobium moniliforme and Castanea crenata is effective in recovering the liver function in $CCl_4-treated$ rats.

• Archives of Pharmacal Research
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• 제22권1호
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• pp.18-24
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• 1999

Various flavonoid derivatives were previously reported to possess the inhibitory activity on cyclooxygenase/lipoxygenase. And these properties of flavonoids might contribute to their anti-inflammatory activity in vivo. In this study, several polyhydroxylated/methoxylated flavonoid derivatives such as oroxylin A. wogonin, skullcapflavone II, tectorigenin and iristectorigenin A were isolated from the medicinal plants. these compounds were evaluated fro their inhibitory effects on cyclooxygenase/lipoxygenase from the homogenate of human platelets in vitro. It was found that isoflavones including daidzein and tectorigenin possessed the inhibitory activity on cycloooxygenase, although the potency of inhibition was far less than that of indomethacin. In addition, oroxylin A, baicalein and wogonin inhibited 12-lipoxygenase activity without affecting cyclooxygenase, which suggested that 5,6,7- or 5,7,8-trisubstitutions of A-ring of flavone gave favorable results. The IC50 values of oroxylin A and NDGA against 12-lipoxygenase were found to be 100 and 1.5 uM, respectively.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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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.