• Food Science and Preservation
• /
• v.8 no.4
• /
• pp.481-487
• /
• 2001

Grifola umbellatus was extracted using methanol, and the extract was further fractionated by water and ethyl acetate. Assay of each fraction with MTT [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium-bromide] revealed significant cytotoxicity effect of the methanol extract of Grifola umbellatus against human gastric cancer cell but not normal human lymphocytes. The methanol extract showed the highest antioxidant activity as well. Antimicrobial activity of Grifola umbellants against Helicobacter pylori was higher in method extract than in other fractions. Grifola umbellatus had a significant inhibitory effect on Helicobacter pylori reducing both its growth and urease activity. These results show that the methanol extract of Grifola umbellatus possesses therapeutic potential on gastric diseases.

• Archives of Pharmacal Research
• /
• v.25 no.5
• /
• pp.655-663
• /
• 2002

Liver fibrosis is a prepathological state wherein damaged liver tissues in chronic liver diseases, such as hepatitis, are not repaired to normal tissues, but converted to fibrous tissue. 5-(2-Pyrazinyl)-4-methyl-1,2-dithiol-3-thione (oltipraz), a cancer chemopreventive agent, is effective against a wide variety of chemical carcinogens. Recently, we reported that oltipraz inhibits liver fibrogenesis (Kang et al., 2002). In the present study, the effects of oltipraz in combination with dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethylene dioxybiphenyl-2,2'-dicarboxylate (DDb) on dimethylnitrosamine (DMN)-induced liver fibrogenesis were assessed in rats. Oltipraz (30 mg/kg body weight, po, 3 times per week for 4 weeks) was found to inhibit the increases in plasma ALT, AST and bilirubin by DMN, whereas DDB (30 mg/kg body weight, po, 3 times per week for 4 weeks) attenuated the increases in the plasma ALT and bilirubin. The lowered plasma protein and albumin contents in DMN-treated rats were completely restored by oltipraz, but not by DDB. DDB decreases liver cell injury and inflammation through inhibition of nuclear factor-kB. DMN increased the accumulation of liver collagen, as indicated by the increase in the 4-hydroxyproline content in liver homogenates, which was reduced by treatment with oltipraz, but not by DDB. Given the differential effect between oltipraz and DDB, the potential enhancement of antifibrotic efficacy by the drugs was assessed in the animal model. Despite the minimal effect of DDB on DMN-induced fibrogenesis, DDB (5-25 mg/kg), administered together with oltipraz (25-5 mg/kg), showed an additive protective effect against hepatotoxicity and fibrosis induced by DMN, which was shown by the blood chemistry parameters and histopathological analysis. The adequate composition ratio of oltipraz to DDB was 5:1. These results provide information on the pharmaceutical composition, comprising of oltipraz and DDB as the active components, for the treatment and/or prevention of liver fibrosis and cirrhosis.

• Journal of Life Science
• /
• v.24 no.3
• /
• pp.219-226
• /
• 2014

The immune system protects the body from bacterial infection and disease, as well as cancer that develops following the mutation of cells. Aging exerts adverse effects on the immune system, such as chronic inflammation, resulting in rheumatoid arthritis. The purpose of this study was to investigate the anti-inflammatory effectiveness of Scutellaria baicalensis, which contains baicalin. HPLC analysis showed that S. baicalensis hot water extracts (SBWE) contained 42.2 mg/g of baicalin. To evaluate the cytotoxicity of SBWE, an MTT assay was carried out in Raw264.7 cells. No cytotoxicity was observed below 160 ${\mu}g/ml$ of SBWE. SBWE at 40 ${\mu}g/ml$ reduced the amount of nitric oxide produced by macrophages stimulated with lipopolysaccharide by 40%. In addition, SBWE inhibited phagocytosis stimulated with zymosan. Furthermore, the content of tumor necrosis factor-alpha ($TNF-{\alpha}$) produced by the macrophages was decreased in the presence of SBWE in a dose-dependent manner. SBWE also inhibited the production of interleukin-1 beta ($IL-1{\beta}$) in a time course experiment. Moreover, treatment with 20 ${\mu}g/ml$ of SBWE remarkably decreased the expression level of cyclooxynase-2. The results provide evidence that SBWE may exert an anti-inflammatory effect through modulation of the immune system.

• Archives of Pharmacal Research
• /
• v.29 no.10
• /
• pp.911-920
• /
• 2006

Phenolic antioxidant butylated hydroxyanisole (BHA) is a commonly used food preservative with broad biological activities, including protection against chemical-induced carcinogenesis, acute toxicity of chemicals, modulation of macromolecule synthesis and immune response, induction of phase II detoxifying enzymes, as well as its undesirable potential tumor-promoting activities. Understanding the molecular basis underlying these diverse biological actions of BHA is thus of great importance. Here we studied the pharmacokinetics, activation of signaling kinases and induction of phase II/III drug metabolizing enzymes/transporter gene expression by BHA in the mice. The peak plasma concentration of BHA achieved in our current study after oral administration of 200 mg/kg BHA was around $10\;{\mu}M$. This in vivo concentration might offer some insights for the many in vitro cell culture studies on signal transduction and induction of phase II genes using similar concentrations. The oral bioavailability (F) of BHA was about 43% in the mice. In the mouse liver, BHA induced the expression of phase II genes including NQO-1, HO-1, ${\gamma}-GCS$, GST-pi and UGT 1A6, as well as some of the phase III transporter genes, such as MRP1 and Slco1b2. In addition, BHA activated distinct mitogen-activated protein kinases (MAPKs), c-Jun N-terminal kinase (JNK), extracellular signal-regulated protein kinase (ERK), as well as p38, suggesting that the MAPK pathways may play an important role in early signaling events leading to the regulation of gene expression including phase II drug metabolizing and some phase III drug transporter genes. This is the first study to demonstrate the in vivo pharmacokinetics of BHA, the in vivo activation of MAPK signaling proteins, as well as the in vivo induction of Phase II/III drug metabolizing enzymes/transporters in the mouse livers.

• Korean Journal of Veterinary Research
• /
• v.45 no.1
• /
• pp.85-91
• /
• 2005

Much of the interest on the chemopreventive properties of herbs and plants has been raised, whereas little is regarding to anti-tumor effect of farming and aquatic products. In the present study, the anti-tumor effect of hot-water extract of a seaweed, BLC (Sargassum fulvellum) and BLC/HEN egg was investigated using MCF-7 cells in vitro and in vivo systems. We found that the BLC extract and BLC/HEN egg inhibited cell proliferation in a dose-dependent manner, which might be mediated through up-regulation of p53. Furthermore, this test compound can directly induce apoptosis in MCF-7 cells, which might be mediated through up-regulation of a pro-apoptotic Bax protein and down-regulation of a anti-apoptotic Bcl-2 protein, not by immune system. Nude mice bearing established breast tumors (with exogenous estradiol) were treated with BLC extract and BLC/HEN egg. Treatment BLC extract and BLC/HEN egg caused a 42% and 71% inhibition of tumor growth, respectively. Both agents caused a significant inhibition of volume and weight growth of estrogen independent human breast tumors established from MCF-7 cells. Our results suggested that BLC extract and BLC/HEN egg have the efficacious effect of human breast cancer not only in vitro but also in vivo.

• Environmental Mutagens and Carcinogens
• /
• v.24 no.4
• /
• pp.198-205
• /
• 2004

Cytochrome P4501B1(CYP1B1) is known to be inducible by xenobiotic compounds such as policyclic aromatic hydrocarbon(PAH) and dioxins such as 2,3,7,8-tetrachloro-dibenzo-p-dioxin(TCDD). And these induction of CYP1B1 is also regulated by many categories of chemicals. In order to investigate the effects of several chemicals on CYP1B1 gene expression in Hepa-I and MCF-7 cells, 5' flanking DNA of human CYP1B1 was cloned into pGL3 basic vector containing luciferase gene, and then transfected into these cells. After treatment of chemicals, the luciferase activity was measured. CYP1B1 enzyme metabolize PAHs and estradiol. CYP1B1 metabolize estradiol to 4-hydrozyestradiol that is considered as carcinogenic metabolite. Recent industrialized industrialized society, human has been widely been exposed to widespread environmental contaminants such as PAHs(polycyclic aromatic hydrocarbon) that are originated from the imcomplete combustion of hydrocarbons. PAHs are known to be ligands of the AhR(aryl hydrocarbon receptor). Induction of cytochrome P4501B1(CYP1B1) in cell culture is widely used as a biomarker for PAHs. Therefore we have studied the effect of PAHs in the human breast cancer cells MCF-7 to evaluate bioactivity of PAHs. We have used the United State of America EPA selected 13 different PAHs, PAHs mixtures and extracts from environmental samples to evaluate the bioassay system. We examined effects of PAHs on the CYP1B1-luciferase reporter gene and CYP1B1 mRNA level. Benzo(k)fluoranthene and dibenzo(a, h)anthracene showed strong response to CYP1B1 promoter activity stimulation, and also CYP1B1 mRNAs increase in MCF-7 cells in a concentration-dependent manner. RT-PCR analysis indicated that PAHs significantly up-regulate the level of CYP1B1 mRNA. Some flavonoids such as genistein, daidzein, chrysin, naringenin and morin were also investigeted. These flavonoids decreased B(k)F infuced luciferase activity at low concentration. But, these flavonoids exhibited stimulatory effect at high concentration.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.43 no.1
• /
• pp.86-92
• /
• 2014

Cordycepin is the major functional component of Cordyceps species and is widely used in traditional oriental medicine. Cordycepin has been shown to possess many pharmacological properties, such as enhancement of immune function along with anti-inflammatory, antioxidant, anti-aging, and anti-cancer effects. Here, we investigated the inhibitory effects of cordycepin on cell migration and invasion, which are two critical cellular processes that are often deregulated during metastasis, using HCT116 human colorectal carcinoma cells. According to our data, cordycepin at non-cytotoxic concentrations markedly inhibited the motility and invasiveness of HCT116 cells in a time-dependent manner. RT-PCR and Western blotting results indicated that cordycepin reduced the levels of claudin proteins, which are major components of tight junctions (TJs), and induced tightening of TJs. Cordycepin also attenuated the expression and activities of matrix metalloproteinases (MMPs)-2 and -9, whereas levels of tissue inhibitor of metalloproteinases (TIMPs)-1 and -2 were simultaneously elevated. These findings suggest that cordycepin reduces the migration and invasion of HCT116 cells by modulating the activities of TJs and MMPs.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.34 no.7
• /
• pp.937-941
• /
• 2005

The antioxidant and anticancer activities of Styela plicata extracts were evaluated. When extracts were prepared with fresh Styela plicata (FR), extraction yield was in the order of methanol > ethanol = acetone > water among treated solvents. However, the extraction order was methanol > water > ethanol > acetate in freeze dried Styela plicata (FD). Radical scavenging activity was the highest in acetone extracts $(37.39\%)$ from FR, while in ethanol extracts $(78.40\%)$ from FD. Reducing power of FR was the greatest in methanol extracts (1.076), and that of FD in ethanol extracts (1.360). The acetone extracts from FD showed significant anticancer activity when revealed with human colon cancer cell line HT-29. These results indicated that extraction yields and properties of extracts from Styela plicata were variable depending on solvent and/or physicochemical state, and appropriate extraction process could provide some valuable bioactive materials from Styela plicata.

• Food Science and Preservation
• /
• v.13 no.5
• /
• pp.649-654
• /
• 2006

To enhance beneficial effects of citron fruits, anticancer and antioxidant activities of citron fruits extracts were assessed with or without ascorbic acid. Total phenolic acids and flavonoids of fruits peels and flesh extracts were determined. Fruits peels contained more phenolic acids and flavonoids than those detected in flesh extracts. Scavenging activities of 1,1-diphenyl-2-picrylhydrazyl radicals and reducing powers were increased depending on the concentration. The antioxidant activities on oxidation of linoleic acid emulsion incubated at $50^{\circ}C$ were increased but the effect was small to that of butylated hydroxy toluene and ascorbic acid. The anti-tumorigenic effect of these compounds were investigated. They were shown to inhibit the in vitro proliferation of four human tumorigenic cell lines, HT-29, MCF-7, DU-145 and HepG2, in a doso-dependent manner. This study demonstrated that the antioxidant and anticancer activities of citron fruits extracts were derived from their phenols and flavonoids.

• Food Science and Preservation
• /
• v.18 no.4
• /
• pp.590-596
• /
• 2011

Pimpinella brachycarpa, called as cham-na-mul in Korea, is an edible popular herb. However, the study of biological activity of P. brachycarpa is still rudimentary in worldwide. In this study, from the cultivated P. brachycarpa, we prepared the methanol extract and its subsequent solvent fractions, and their antimicrobial, antioxidation, and anti-proliferative activities were evaluated. The fraction yields of n-hexane (H), methylene chloride (EC), ethylacetate (EA), butanol (B), and water residue (W) from the methanol extract were 18.71, 0.7, 0.56, 4.57, and 71.51%, respectively. Analysis of total flavonoid and total polyphenol showed that the EA fraction contained the highest contents (89.23 and 200 mg/g), and the W residue has the lowest contents (19.6 and 2.27 mg/g) among the factions. In antimicrobial activity assay, the EA fraction showed a broad-range antibacterial activity, while the H fraction is effective against gram positive bacteria. In antioxidation activity assay, EA and B fraction showed strong DPPH anion and ABTS cation scavenging activities including reducing power, and Hand MC fraction showed effective nitrite scavenging activity (71.43~83.82 ${\mu}g$/mL of $IC_{50}$). In a while, only B fraction showed strong anti-proliferative activity against human colorectal cancer HCT-116 (166 ${\mu}g$/mL of $IC_{50}$) as a dose-dependent manner up to 200 ${\mu}g$/mL. These results suggest that the EA and B fraction of P. brachycarpa could be developed as functional food ingredients.