• YAKHAK HOEJI
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• v.39 no.6
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• pp.622-630
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• 1995

Inoculation of Friend anemia virus, which was a Kind of retro virus such as HIV, results splenomegaly, anemia, the increase of WBC counts and reverse transcriptase activity in serum. These results were due to the inhibition of the differentiation of erythroid progenitor cell by the FVA at the spleen. Using these as index of antiviral effects, we pursued the establishment of in vivo screening method for the new anti-ADS drugs. Among zidovudine, didanosine and zalcitabine, which were already approved as anti-AIDS drugs, treatment of zidovudine for 18 days in BALB/c mice inoculated with Friend anemia virus resulted the most potent inhibitory effects on the splenomegaly, the increase of WBC counts and reverse transcriptase activity, but did not recovered the anemia due to the tomcity of zidovudhie itself on the bone marrow. The antiviral effects of zidovudine was reduced in case of zidovudine treatment 7 days after Friend anemia virus inoculation. These results suggested that the sooner treatment of zidovudine would be better improved when the virus was inoculated. Human recombinant interferon itself .alpha. did not showed the antiviral activity against Friend anemia virus and did not also affected the antiviral activity of zidovudine. These results suggested that Friend anemia virus would be used as a tool in vivo screening method for the Lobster of reverse transcriptase.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.11
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• pp.4853-4856
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• 2016

Objective: Gimatecan is a new camptothecin (CPT) analogue that inhibits tumor growth by targeting DNA topoisomerase I (TOP I) and introducing strong and persistent DNA cleavage. Anti-tumor activity has been demonstrated with a wide range of solid tumors in previous preclinical and clinical studies. Here, we investigated for the first time the effects of gimatecan on the proliferation of hepatocellular carcinoma (HCC) cells both in vitro and in vivo. Methods: Anticancer efficacy of gimatecan were evaluated in a panel of HCC cell lines and corresponding mouse xenograft models. Inhibition of cell proliferation was measured by CellTiter-Glo cell viability assay. In vivo, gimatecan and control preparations were orally administered every four days, for a total of four times. Tumor volume and body weights of the mice were measured twice weekly. Results: In vitro cytotoxicity evaluation showed that gimatecan inhibited the proliferation of a large panel of HCC cell lines in a dose dependent manner, with IC50 values ranging between 12.1~1085.0 nM. In vivo evaluation in mouse xenograft models showed significant antitumor effects of gimatecan at 0.8mg/kg and 0.4mg/kg as compared to the control group. Conclusion: This study suggested that gimatecan may have the potential to be used as a chemotherapeutic agent for the treatment of HCC.

• Journal of the Korean Society of Food Science and Nutrition
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• v.26 no.2
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• pp.254-260
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• 1997

Effects of kimchi extracts on the immune response related to its antitumor activity in vitro and in vivo were investigated. The extracts of kimchi fermented for 0(fresh) and 3 weeks at $5^{\circ}C$ showed a direct cytotoxic effect on sarcoma-180 cells, tumor cells in vitro. Methanol extract(4mg/ml), MSF(methanol soluble fraction : 3mg/ml) and hexane extract(fresh : 2.0mg/ml, 3 weeks : 0.3mg/ml) of the kimchi(3 weeks, $5^{\circ}C$) markedly decreased the total numbers of sarcoma-180 cells, but not their viability. The phagocytic activity of peritoneal macrophage of mice was significantly augmented by these extracts of the kimchi compared with that of control in vitro and in vivo. These extracts also raised the phagocytic index, indicating that the number of phagocytized microbes per macrophage increased. Thus, kimchi might show a anti-tumor activity by enhancing the phagocytic cell activities.

• Journal of Microbiology and Biotechnology
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• v.26 no.2
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• pp.337-346
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• 2016

Three combinations of molecular chaperones from Escherichia coli (i.e., DnaK-DnaJ-GrpE-GroEL-GroES, GroEL-GroES, and DnaK-DnaJ-GrpE) were overproduced in E. coli BL21, and their in vitro stabilizing effects on a nitrile hydratase (NHase) were assessed. The optimal gene combination, E. coli groEL-groES (ecgroEL-ES), was introduced into Rhodococcus ruber TH3. A novel engineered strain, R. ruber TH3G was constructed with the native NHase gene on its chromosome and the heterologous ecgroEL-ES genes in a shuttle plasmid. In R. ruber TH3G, NHase activity was enhanced 37.3% compared with the control, TH3. The in vivo stabilizing effect of ecGroEL-ES on the NHase was assessed using both acrylamide immersion and heat shock experiments. The inactivation behavior of the in vivo NHase after immersion in a solution of dynamically increased concentrations of acrylamide was particularly evident. When the acrylamide concentration was increased to 500 g/l (50%), the remaining NHase activity in TH3G was 38%, but in TH3, activity was reduced to 10%. Reactivation of the in vivo NHases after varying degrees of inactivation was further assessed. The activity of the reactivated NHase was more than 2-fold greater in TH3G than in TH3. The hydration synthesis of acrylamide catalyzed by the in vivo NHase was performed with continuous acrylonitrile feeding. The final concentration of acrylamide was 640 g/l when catalyzed by TH3G, compared with 490 g/l acrylamide by TH3. This study is the first to show that the chaperones ecGroEL-ES work well in Rhodococcus and simultaneously possess protein-folding assistance functions and the ability to stabilize and reactivate the native NHases.

• The Korean Journal of Pharmacology
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• v.27 no.1
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• pp.1-5
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• 1991

We studied changes in the hypothalamic norepinephrine(NE) metabolism in streptozotocin (STZ)-induced diabetic rats by measuring basal NE levels, turnover rate of NE, and in vivo tyrosine hydroxylase activities. Basal NE level did not change significantly upto 4 weeks after the establishment of diabetes with STZ(60 mg/kg, iv). But turnover rate of NE decreased to 62% of control rate(P<0.01), and in vivo tyrosine hydroxylase activities decreased to 32% of control level(P<0.05) at one week of diabetes. From these results, we concluded that, of the three parameters measured, in vive tyrosine hydroxylase activity is the most sensitive index of altered hypothalamic NE metabloism in STZ-induced diabetic rats.

• The Journal of Korean Medicine
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• v.25 no.1
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• pp.152-160
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• 2004

Backgrounds : Androgenetic alopecia is a relatively common disorder, but its precise mechanism is not elucidated. There are two commercial drugs approved by FDA. One(finasteride) has an inhibition activity of 5$\alpha$-reductase(type 2) and the other(minoxidil) has a vasodilation activity. Objectives : A verified herbal remedy for baldness is needed for medicinal treatment or preventing alopecia, which could be demonstrated by alopecia-related in vitro & in vivo tests Methods : On the basis of oriental pharmacognosy, we classified many herbal medicines into four groups (malnutrition, aging, alopecia and gray hair) according to its effect. The mitosis induction of hairy dermal papillae cell and the metabolic inhibition for type 2 $5{\alpha}-reductase$ were tested with five herbal extracts. Also, five herbal extracts were added to the normal essence formulation (HHRHG0202-80) in ranges of 0.1~0.3%, which was applied two-mouse models to validate each hair growing activity in vivo. Results : Stimulation of follicular papillae cell proliferation was observed in treatment of three herbal extracts (Glycyrrhizae radix:159.7%, Corni fructus : 144.7%, and Coicis semen : 136.6%) at a dose of $10\mu\textrm{g}/ml$. Three herbal extracts (Biotae semen. Glycyrrhizae radix and Coicis semen) showed inhibitory activity for $5{\alpha}-reductase$(type 2) at 93.18%, 73.36% and 47.6%, respectively at the same dose. We observed the enhancement of hair growth activity in C57b1/6 mouse and the inhibition of alopecia in AGA mouse after topical administration of the hair essence. Conclusions : Hair essence product, which contains five medicinal plants, would be used for the remedy for male pattern baldness (MPB) and the other alopecia diseases.

• The Korean Journal of Physiology and Pharmacology
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• v.20 no.2
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• pp.221-228
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• 2016

We investigated whether prunetin affects the proteolytic activity, secretion, and gene expression of matrix metalloproteinase-3 (MMP-3) in primary cultured rabbit articular chondrocytes, as well as in vivo production of MMP-3 in the rat knee joint to evaluate the potential chondroprotective effect of prunetin. Rabbit articular chondrocytes were cultured in a monolayer, and reverse transcriptionpolymerase chain reaction (RT-PCR) was used to measure interleukin-$1{\beta}$ (IL-$1{\beta}$)-induced expression of MMP-3, MMP-1, MMP-13, a disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4), and ADAMTS-5. In rabbit articular chondrocytes, the effects of prunetin on IL-$1{\beta}$-induced secretion and proteolytic activity of MMP-3 were investigated using western blot analysis and casein zymography, respectively. The effect of prunetin on MMP-3 protein production was also examined in vivo. The results were as follows: (1) prunetin inhibited the gene expression of MMP-3, MMP-1, MMP-13, ADAMTS-4, and ADAMTS-5; (2) prunetin inhibited the secretion and proteolytic activity of MMP-3; (3) prunetin suppressed the production of MMP-3 protein in vivo. These results suggest that prunetin can regulate the gene expression, secretion, and proteolytic activity of MMP-3, by directly acting on articular chondrocytes.

• The Korean Journal of Physiology and Pharmacology
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• v.26 no.3
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• pp.157-164
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• 2022

Disulfiram (DSF) is an aldehyde dehydrogenase inhibitor. DSF has potent anti-cancer activity for solid and hematological malignancies. Although the effects on cancer cells have been proven, there have been few studies on DSF toxicity in bone marrow cells (BMs). DSF reduces the metabolic activity and the mitochondrial membrane potential of BMs. In subset analyses, we confirmed that DSF does not affect the proportion of BMs. In addition, DSF significantly impaired the metabolic activity and differentiation of BMs treated with granulocyte macrophage-colony stimulating factor, an essential growth and differentiation factor for BMs. To measure DSF toxicity in BMs in vivo, mice were injected with 50 mg/kg, a dose used for anti-cancer effects. DSF did not significantly induce BM toxicity in mice and may be tolerated by antioxidant defense mechanisms. This is the first study on the effects of DSF on BMs in vitro and in vivo. DSF has been widely studied as an anti-cancer drug candidate, and many anti-cancer drugs lead to myelosuppression. In this regard, this study can provide useful information to basic science and clinical researchers.

• The Korean Journal of Pesticide Science
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• v.8 no.3
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• pp.168-174
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• 2004

In a course of the process for a lead optimization of 2-imino-l,3-thiazolines 1 which show a selective in vivo antifungal activity against rice blast, new compounds 2 in which C-5 was substituted by methyl group of the lead compound were synthesized and tested for the biological activity. Bromination of $\beta$-keto ester 7 followed by the reaction with thiourea and hydrolysis gave 2-imino-5-methyl-l,3-thiazoline carboxylic acid 3. Coupling reactions of 3 with aniline derivatives afforded 17 kinds of the corresponding 2-imino-5-methyl-l,3-thiazoline carboxanilides 2. Their in vivo antifungal activity against rice blast was weaker than that of 1, indicating that the in vivo antifungal activity of 2-imino-l,3-thiazolines was affected by the substituent at C-5. These results would be an important data for the molecular design in the lead optimization process of this series.

• Archives of Pharmacal Research
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• v.11 no.3
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• pp.213-217
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• 1988

The effects of ethanol and acetaldehyde on monoamine oxidase activity in mouse liver mitochondrial fraction were studied. In vivo, a single dose of ethanol increased the hepatic monoamine oxidase activity compared to control group, and chronic ethanol consumption also increased the enzyme activity using tyramine, benzylamine or serotonin as substrate. Acetaldehyde, the metabolite of ethanol, significantly increased monoamine oxidase activity more than ethanol did. In contrast to the in vivo results, it was found that the monoamine oxidase activity was inhibited in vitro by ethanol or acetaldehyde in the dose-dependent manner.