• Microbiology and Biotechnology Letters
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• v.30 no.1
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• pp.51-56
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• 2002

An antitumor substance was purified from the culture filtrate of phytopathogenic fungus Alternaria brassicicola SW-3 isolated from soil of a chinese cabbage patch, and its characteristics were investigated. Antitumor activity of A. brassicicola SW-3 was measured by MTT assay. The cytotoxic activity against human cancer cell line was detected in the culture filtrate of A. brassicicola SW-3, but no activity found in mycelium. Antitumor substance was isolated from the culture broth by ethyl acetate extraction and purified by silica gel column chromatography. Structure of the purified compound was analyzed by the instrumental analysis such as $^1$H-NMR, $^{13}$ C-NMR and IR spectroscopy. The purified fungal metabolite of an A. brassicicola SW-3, consists of 11 carbon chain with two hydroxyl groups and two epoxides which is identical to depudecin. The $IC_{50}$/ values of the active compound identified as depudecin were $69\mu$g/mL and $57\mu$g/mL against mouse melanoma B16BL6 cell line, and human hepatoma SK-HEP1 cell line, respectively.

• The Korea Journal of Herbology
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• v.28 no.4
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• pp.93-100
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• 2013

Objectives : This study was to evaluate the anti-inflammatory and anti-pruritic effects of WSY-1075 composited with Corni Fructus, Angelica gigantis Radix, Lycii Fructus, Ginseng Radix, Cervi parvum Cornu and Cinnamomi Cortex in rat peritoneal mast cells (RPMCs) and scratching mouse model. Methods : WSY-1075 was prepared by extracting with 30% ethanol. In the present study, we investigated the effect of WSY-1075 on the production of tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-$1{\beta}$ (IL-$1{\beta}$) and histamine in rat peritoneal mast cells (RPMCs) activated with phorbol 12-myristate 13-acetate (PMA) plus calcium ionophore A23187, and on the scratching behavior in mice treated with pruriogens. Results : WSY-1075 was not cytotoxic effect in used all concentration. PMA plus A23187 treatment significantly increased TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 production compared with media control in RPMCs. However, TNF-${\alpha}$, $IL1{\beta}$ and IL-6 production increased by PMA plus A23187 treatment were significantly inhibited by WSY-1075 (200 ${\mu}g/mL$ and 400 ${\mu}g/mL$). WSY-1075 also inhibited the histamine release from RPMCs stimulated by compound 48/80, which promotes histamine release. Moreover, WSY-1075 administration had an inhibitory effects on the scratching behavior induced by pruritogen (compound 48/80, histamine, serotonin and substence P) in ICR mice. Conclusion : These results suggest that WSY-1075 administration (200 mg/kg or 400 mg/kg) has the anti-inflammatory and anti-pruritic effects on the activated rat peritoneal mast cell and mouse pruritus. WSY-1075 has a potential use as a composition of medicinal plants for treatment against inflammation- and pruritus-related disease.

• Journal of Microbiology and Biotechnology
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• v.18 no.10
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• pp.1621-1629
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• 2008

Harmful algal blooms (HABs), commonly called red tides, are caused by some toxic phytoplanktons, and have made massive economic losses as well as marine environmental disturbances. As an effective and environment-friendly strategy to control HAB outbreaks, biological methods using marine bacteria capable of killing the harmful algae or algicidal extracellular compounds from them have been given attention. A new member of the $\gamma$-Proteobacteria, Hahella chejuensis KCTC 2396, was originally isolated from the Korean seashore for its ability to secrete industrially useful polysaccharides, and was characterized to produce a red pigment. This pigment later was identified as an alkaloid compound, prodigiosin. During the past several decades, prodigiosin has been extensively studied for its medical potential as immunosuppressants and antitumor agents, owing to its antibiotic and cytotoxic activities. The lytic activity of this marvelous molecule against Cochlodinium polykrikoides cells at very low concentrations ($\sim$l ppb) was serendipitously detected, making H. chejuensis a strong candidate among the biological agents for HAB control. This review provides a brief overview of algicidal marine bacteria and their products, and describes in detail the algicidal characteristics, biosynthetic process, and genetic regulation of prodigiosin as a model among the compounds active against red-tide organisms from the biochemical and genetic viewpoints.

• International Journal of Industrial Entomology and Biomaterials
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• v.26 no.2
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• pp.89-94
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• 2013

Entomopathogenic fungal species have been investigated for their potential use as biological control agents owing to their natural role as insect pathogens. These fungi produce a wide range of secondary metabolites with high therapeutic values, such as antibiotics and cytotoxic substances. To evaluate the antibacterial activity of entomopathogenic fungi, 10 isolates from Korean soil were selected and tested for their activity against Escherichia coli by using fungal culture filtrates. Antibacterial activity was assessed using a two-step process: (1) a screening assay for the selection of fungal isolates and (2) a quantitative assay to evaluate the activity of select fungi. Although 4 fungal isolates were selected through the screening assay, only 3 fungal isolates, from Beauveria bassiana and Metarhizium anisopliae, showed high antibacterial activity according to the quantitative assay. The antibacterial activity of selected fungal culture filtrates was stable when exposed to heat and proteolytic enzyme treatments, which indicated that the antibacterial compound is not a protein. These entomopathogenic fungal metabolites might be useful as a source for bacterial control and in the pharmaceutical industry.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.6
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• pp.517-523
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• 2013

Naphthyridine compounds are important, because they exhibit various biological activities including anticancer, antimicrobial, and anti-inflammatory activity. Some naphthyridines have antimitotic effects or demonstrate anticancer activity by inhibiting topoisomerase II. These compounds have been investigated as potential anticancer agents, and several compounds are now part of clinical trials. A series of naphthyridine derivatives were evaluated for their in vitro cytotoxic activities against human cervical cancer (HeLa), leukemia (HL-60), and prostate cancer (PC-3) cell lines using an MTT assay. Some compounds (14, 15, and 16) were more potent than colchicine against all three human cancer cell lines and compound (16) demonstrated potency with $IC_{50}$ values of 0.7, 0.1, and $5.1{\mu}M$, respectively. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used for quantitative structure-activity relationship (QSAR) molecular modeling of these compounds. We obtained accurate and predictive three-dimensional QSAR (3D-QSAR) models as indicated by the high PLS parameters of the HeLa ($q^2$, 0.857; $r^2$, 0.984; $r^2\;_{pred}$, 0.966), HL-60 ($q^2$, 0.777; $q^2$, 0.937; $r^2\;_{pred}$, 0.913), and PC-3 ($q^2$, 0.702; $q^2$, 0.983; $r^2\;_{pred}$, 0.974) cell lines. The 3D-QSAR contour maps suggested that the C-1 NH and C-4 carbonyl group of the naphthyridine ring and the C-2 naphthyl ring were important for cytotoxicity in all three human cancer cell lines.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.6
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• pp.3449-3453
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• 2013

Background: Telomerase has been considered as an attractive molecular target for breast cancer therapy. The main objective of this work is to assess the inhibitory effects of silibinin and curcumin, two herbal substances, on telomerase gene expression in breast cancer cells. Materials and Methods: For determination of cell viability tetrazolium-based assays were conducted after 24, 48, and 72 h exposure times and expression of human telomerase reverse transcriptase gene was measured with real-time PCR. Results: Each compound exerted cytotoxic effects on T47D cells and inhibited telomerase gene expression, both in a time-and dose-dependent manner. The mixture of curcumin and silibinin showed relatively more inhibitory effect on growth of T47D cells and hTERT gene expression as compared with either agent alone. Conclusions: These findings suggest that cell viability along with hTERT gene expression in breast cancer cells could be reduced by curcumin and silibinin.

• International Journal of Oral Biology
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• v.36 no.1
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• pp.7-11
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• 2011

Ursolic acid is a triterpenoid compound present in many plants. This study examined the antimicrobial activity of ursolic acid against mutans streptococci (MS) isolated from the Korean population. The antimicrobial activity was evaluated by the minimum inhibitory concentration (MIC) and time kill curves of MS. The cytotoxicity of ursolic acid against KB cells was tested using an MTT assay. The $MIC_{90}$ values of ursolic acid for Streptococcus mutans and Streptococcus sobrinus isolated from the Korean population were $2 {\mu}g$/ml and $4 {\mu}g$/ml, respectively. Ursolic acid had a bactericidal effect on S. mutans ATCC $25175^T$ and S. sobrinus ATCC $33478^T$ at > $2 \;{\times}\; MIC (4 {\mu}g$/ml) and $4 \;{\times}\; MIC (8 {\mu}g$/ml), respectively. Ursolic acid had no cytotoxic effect on KB cells at concentrations at which it exerted antimicrobial effects. The results suggest that ursolic acid can be used in the development of oral hygiene products for the prevention of dental caries.

• Food Science and Biotechnology
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• v.17 no.5
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• pp.983-989
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• 2008

Two flavonoids, isorhamnetin 3-O-$\beta$-D-glucopyranoside (1) and quercetin 3-O-$\beta$-D-glucopyranoside (2), from slander glasswort (Salicornia herbacea, Korean name hamcho) were isolated. Antioxidative and matrix metalloproteinase-9(MMP-9) inhibitory effects of these compounds were investigated in HT 1080 cell lines. These compounds suppressed the electron spin resonance (ESR) signal intensity on generation of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical in a free-cellular system. Their scavenging effects on generation of intercellular reactive oxygen species (ROS) also exhibited similar trends with DPPH radical in the free cellular system. Also, a control group combined only with Fe(II)-$H_{2}O_2$ resulted in DNA apoptosis by oxidative stress, whereas treatments with these compounds suppressed radical-mediated DNA damage. Intracellular glutathione (GSH) levels were slightly increased in the presence of compound 1 and 2. Moreover, these compounds led to the reduction of the expression levels of MMP-9 without cytotoxic influence. These results suggest that these compounds have a potential as a valuable natural antioxidant and MMP inhibitor related to oxidative stress. Therefore, these compounds not only can be developed as a candidate for a therapeutic potential but also a source for use as ingredients of health foods or functional foods to prevent metastasis involving MMP-9, closely related to ROS.

• Journal of the Korean Applied Science and Technology
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• v.28 no.1
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• pp.75-84
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• 2011

Atopic dermatitis is a chronic inflammatory skin disease associated with cutaneous hyper-reactivity to environmental triggers. In order to develop effective therapeutic herbal extracts for atopic dermatitis, cytotoxicity, antioxidant, anti-inflammatory and anti-allergic activities were investigated for various herbal extracts. Among candidate extracts, we selected Aloe vera L. (AV), Viola mandshurica W. Becker (VM), Punica granatum L. (PG), Dendrobium nobile L. (DN) and mixture of the above extracts (MX) for further investigations. All of them did not show cytotoxic activities to macrophage RAW264.7 cells below the concentration of 100 ppm. All showed antioxidant, anti-inflammatory and anti-allergic effects, although to various extents. In antioxidant effects, AV showed the highest effect, followed by PG and VM, while DN did the lowest. In evaluation for anti-inflammatory activities in macrophage RAW264.7 cells, AV and DN inhibited almost completely the LPS-induced production of nitric oxide, while AV, DN and VM showed strong inhibitory activities on the LPS-induced production of TNF-${\alpha}$. In anti-allergy effect in mast cell HMC-1, DN showed the highest effect, followed by AV and PG, while VM did the lowest. In the topical allergy reaction induced by compound 48/80 in Sprague-Dawley rat, DN exhibited significant anti-allergic effect, while PG, VM and AV did slight effect. These results suggest that AV, VM, PG and DN have antioxidant, anti-inflammatory and anti-allergic activities, and thus have the potential to reduce and alleviate the symptoms of atopic dermatitis.

• YAKHAK HOEJI
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• v.40 no.2
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• pp.218-224
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• 1996

This laboratory has recently reported the synthesis and in vitro antitumor activity of PT(II) complexes containing ethylenediamine and diphosphine. In view of the reports of others, cisplatin is toxic to the kidney since the kidney's vulnerability to PT(II) complexes may originate in its ability to accumulate and retain platinum to a greater degree than other organs. The in vitro cytotoxicity of these synthetic PT(II) complexes on the primary cultured proximal tubular cells of rabbit kidney and renal cortical cells of human kidney was investigated. Three endpoints for cytotoxicity tests were evaluated:3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT), $^3H$-thymidine uptake and the glucose consumption tests. The rank order of sensitivity exhibited $^3H$-thymidine uptake>MTT>glucose consumption test. The agents with diphosphine leaving group were significantly less cytotoxic than cisplatin. Moreover, 1,2-bis(diphenylphosphino)ethane (DPPE) exhibited less cytotoxicity than 1.3-bis (diphenylphosphino)propane (DPPP) against on rabbit and human cultured kidney cells. Based on these results, the decreased nephrotoxicity of these new complexes over cisplatin appeared to be partially attributable to a leaving group of DPPP and DPPE. This novel class of platinum compound represents a valuable lead in the development of a "third-generation" agent.