• Asian Pacific Journal of Cancer Prevention
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• 제13권11호
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• pp.5903-5908
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• 2012

Objective: The purpose of this study is to investigate the combined effects of exemestane and aspirin on MCF-7 human breast cancer cells. Methods: Antiproliferative effects of exemestane and aspirin, alone and in combination, on growth of MCF-7 human breast cancer cells were assessed using the MTT assay. Synergistic interaction between the two drugs was evaluated in vitro using the combination index (CI) method. The cell cycle distribution was analyzed by flow cytometry and Western blotting was used to investigate the expression of cyclooxygenase-1, cyclooxygenase-2 and Bcl-2. Results: MTT assays indicated that combination treatment obviously decreased the viability of MCF-7 human breast cancer cells compared to individual drug treatment (CI<1). In addition, the combination of exemestane and aspirin exhibited a synergistic inhibition of cell proliferation, significantly arrested the cell cycle in the $G_0/G_1$ phase and produced a stronger inhibitory effect on COX-1 and Bcl-2 expression than control or individual drug treatment. Conclusion: These results indicate that the combination of exemestane and aspirin might become a useful method to the treatment of hormone-dependent breast cancer. The combination of the two inhibitors significantly increased the response as compared to single agent treatment, suggesting that combination treatment could become a highly effective approach for breast cancer.

• Asian Pacific Journal of Cancer Prevention
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• 제15권11호
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• pp.4651-4657
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• 2014

The development of chemopreventive approaches using a concoction of phytochemicals is potentially viable for combating many types of cancer including colon carcinogenesis. This study evaluated the anti-proliferative effects of ginger and Gelam honey and its efficacy in enhancing the anti-cancer effects of 5-FU (5-fluorouracil) against a colorectal cancer cell line, HCT 116. Cell viability was measured via MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulphenyl)-2H-tetrazolium) assay showing ginger inhibiting the growth of HCT 116 cells more potently ($IC_{50}$ of 3mg/mL) in comparison to Gelam honey ($IC_{50}$ of 75mg/mL). Combined treatment of the two compounds (3mg/mL ginger+75mg/mL Gelam honey) synergistically lowered the $IC_{50}$ of Gelam honey to 22mg/mL. Combination with 35 mg/mL Gelam honey markedly enhanced 5-FU inhibiting effects on the growth of HCT 116 cells. Subsequent analysis on the induction of cellular apoptosis suggested that individual treatment of ginger and Gelam honey produced higher apoptosis than 5-FU alone. In addition, treatment with the combination of two natural compounds increased the apoptotic rate of HCT 116 cells dose-dependently while treatment of either ginger or Gelam honey combined with 5-FU only showed modest changes. Combination index analysis showed the combination effect of both natural compounds to be synergistic in their inhibitory action against HCT 116 colon cancer cells (CI 0.96 < 1). In conclusion, combined treatment of Gelam honey and ginger extract could potentially enhance the chemotherapeutic effect of 5-FU against colorectal cancer.

• Journal of Microbiology and Biotechnology
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• 제27권4호
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• pp.785-790
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• 2017

Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an $IC_{50}$ value of $1.21{\mu}M$; in addition, it was found to be highly effective against MAO-A, with an $IC_{50}$ value of $6.47{\mu}M$. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B ($IC_{50}=14.50{\mu}M$) but not for MAO-A ($IC_{50}$ > $80{\mu}M$). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with $K_i$ values of 0.573 and $0.248{\mu}M$, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.

• 대한수의학회지
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• 제47권3호
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• pp.265-271
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• 2007

This study investigated the protective effects of ethylene glycol-bis(${\beta}$-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA), an extracellular calcium chelator, and ethylenediaminetetraacetic acid (EDTA), which chelates calcium and most metal ions, against carbon tetrachloride ($CCl_4$)-induced acute hepatotoxicity in mice. Mice were treated with EGTA or EDTA at a dose of 20 (low) or 100 mg/kg (high) subcutaneously 1h before $CCl_4$ administration. The mice were fasted and sacrificed 18h after $CCl_4$ treatment. Blood samples were collected from the carotid artery by decapitation under light ether anesthesia. Serum alkaline phosphatase (ALP), aspartate aminotransferase (AST), alanine aminotransferase (ALT), triglyceride (TG), and cholesterol levels were measured. Malondialdehyde (MDA) production was determined as an index of lipid peroxidation in the liver. The liver, kidneys, and spleen were weighed. We also evaluated the histopathological changes in the liver in each group. The relative weights of the liver were significantly higher in the $CCl_4$-treatment group than in the normal group, except in the high-EDTA treatment group. EGTA and EDTA treatment caused a significant decrease in serum ALP, ALT, and AST levels. Of all of the doses of EGTA and EDTA tested, the high-EDTA dose resulted in the most remarkable inhibitory action. The protective effect in the high-EDTA-treatment group was confirmed histopathologically. The low-EGTA-treatment group showed a significant decrease in serum TG and cholesterol levels. Liver MDA levels were significantly decreased in the EGTA (20 mg/kg) and EDTA (20, 100 mg/kg) groups. These results suggest that EDTA, which chelates both calcium and metal ions, confers better protection in $CCl_4$-induced acute liver damage than does EGTA, a calcium chelator.

• 한국작물학회지
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• 제45권4호
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• pp.261-266
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• 2000

This study was to investigate antioxidative activity of rice grain using 1, 1-Diphenyl-2-picrylhydrazyl(DPPH) and thiobarbituric acid (TBA) method and germination ability for screening rice varieties with high antioxidative activities on korean native and foreign rice varieties harvested in 1998 and 1999. The average antioxidative activity of foreign rice varieties (DPPH 63.5% and TBA 55.2%) was significantly higher than that of native rice varieties (DPPH 47.2% and TBA 45.6%) on varieties harvested in 1999. The promptness index (PI) of native rice varieties was higher in stored rices for three months (mean PI=160.7) than that of stored rices for a year (mean PI=141.6). On the other hand, the PI of foreign rice varieties was higher in stored rices stored for a year (mean PI=176.7) than that of stored rices for three months (mean PI=157.5). Varieties with high redness of hulled rice (a-value) showed significant lipid peroxidation inhibitory activity to DPPH in a stored rices for a year (r=${0.5744}^**$) and stored rices for three months (r=${0.5630}^**$) . These results indicate that the pigments of hulled rice varieties may play important antioxidative roles and colored rice varieties with higher antioxidative potentials can be developed and also may provide information with rice breeder to breed rice variety with a high antioxidative activity for a rapid screening of a small amounts of a large number of samples using color value.

• 대한본초학회지
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• 제25권4호
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• pp.103-112
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• 2010

Objective : The aim of this study was to determine whether methanol extract of Do-Ki-Tang (DKT) inhibit free radical generation and production of nitrite an index of NO, $PGE_2$, iNOS, COX-2 and pro-inflammatory cytokines such as TNF-${\alpha}$, IL-$1{\beta}$, IL-6 and MCP-1 in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Methods : Cytotoxic activity of extract on RAW 264.7 cells was measured using 5-(3-caroboxymeth-oxyphenyl)-2H-tetra-zolium inner salt (MTS) assay. The expression level of inflammatory response-related proteins was confirmed by western blot. The production of proinflammatory cytokines was measured by ELISA. Results : Our results indicated that DKT scavenged DPPH radical and nitric oxide in vitro. Moreover, DKT significantly inhibited the LPS-induced NO, $PGE_2$ production and iNOS, COX-2 expression accompanied by an attenuation of TNF-${\alpha}$, IL-$1{\beta}$, IL-6 and MCP-1 formation in macrophages. Furthermore, DKT treatment also blocked LPS-induced intracellular ROS production and the activation of NF-${\kappa}B$ and MAPKs. Conclusion : Our data suggest that the anti-inflammatory effect of DKT is mediated through down-modulation of pro-inflammatory mediators and cytokines by blocking the signaling pathways of NF-${\kappa}B$ and MAPKs. These inhibitory effects by DKT represent a potential therapeutic approach to the treatment of inflammatory diseases.

• Journal of Pharmaceutical Investigation
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• 제41권4호
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• pp.227-232
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• 2011

Alnus japonica has been known to exert antioxidative, anti-inflammatory, anti-cancer and immune response inhibitory effects. The aim of this study was to figure out the characteristics of extracts obtained with different extraction solvent such as water, 100% ethanol, 70% ethanol or 70% methanol because characteristic components such as oregonin and hirsutanone extracted from Alnus japonica might be essential for the biological activity. For this purpose, oregonin and hirsutanon of four extracts, index ingredient of Alnus japonica, were analyzed with HPLC and physicochemical studies such as SEM, particle size and zeta potential were conducted. In cell cytotoxicity study, extract of water showed the highest cytotoxicity among four extracts. In case of oregonin, 70% MeOH and water extracts showed high contents and in case of hirsutanone, all extracts showed similar contents except 70% EtOH extracts. The extract of 70% MeOH from Alnus japonica for both oregonin and hirsutanone appeared to have the highest content. Both oregonin and hirsutanone extracted from Alnus japonica using 70% methanol showed stability in pH 1.2.

• 생약학회지
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• 제34권1호통권132호
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• pp.45-54
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• 2003

We have conducted to characterize the physico-chemical change and pharmacological transformation of traditional herbal medicines by means of processing. Processed Gardeniae Fructus was prepared by heating of fruit of Gardenia jasminoides(GF) for $30{\sim}50\;minute$ in the roster designed for herb processing. The contents of drying loss, water extract, diluted ethanol extract, ether extract and geniposide in non-processed GF and processed GF were examined. The contents of drying loss, water extract and geniposide in processed GF showed a decrease as compared with those of non-processed GF, however the contents of dilute ethanol and ether extract showed a increase as compared with those of non-processed GF. The rate of decrease/increase of those index were in proportion to heating time. And, biological activities of methanol extract of non-processed GF and processed GF were investigated. DPPH scavenging effects and inhibitory effect of xanthine oxidate and hemolysis of processed GF exhibited more effective than those of non-processed GF in vitro. Accelerating effect of large intestinal transport and purgative action of non- processed GF were discriminated by processing of GF. Methanol extracts of non-pro- cessed GF and processed GF showed the protective effects against the hepatotoxicity induced by ${\alpha}-naphthylisothiocyanate$ in rats. These results suggested that the transformation of biological activities of GF by means of processing may be due to the physico-chemical change of the constituents in GF by heating.

• 동의생리병리학회지
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• 제27권4호
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• pp.409-415
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• 2013

We attempted to determine the action target of Shiitake mushroom extract with a known anti-hyperlipidemic effect in poloxamer(P) 407-induced hyperlipidemia model. We investigated the anti-hyperlipidemic effects of the water extract from Shiitake mushroom on the progress of high fat diet for 4 weeks. Experimental rats were divided into 5 different experimental groups including an normal group (normal diet; n=10), control group (hyperlipidemia; n=10), Experimental group I (hyperlipidemic rats treated with Shiitake mushroom extract (100 mg/kg, PO), n=10), Experimental group II (hyperlipidemic rats treated with Shiitake mushroom extract (300 mg/kg, PO), n=10), and Experimental group III (hyperlipidemic rats treated with Shiitake mushroom extract (500 mg/kg, PO), n=10). It is to analysis changes in body weight, visceral fat weight, blood lipid profiles, HMG-CoA reductase and histological findings. Body weight and epididymal fat weight was not significantly change in experimental groups (p>0.05). The level of total cholesterol, TG, arthrogenic index, and HMG-CoA reductase were significantly lower in experimental groups than control group (p<0.05). These results suggested that the Shiitake mushroom extract administration may act by inhibitory the release of cholesterol related factors and HMG-CoA from the hepatocyte without liver and kidney cell damage in hyperlipidemia rats.

• Journal of Microbiology and Biotechnology
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• 제19권12호
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• pp.1576-1581
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• 2009

The emergence of methicillin-resistant Staphylococcus aureus (MRSA) has led to an urgent need for the discovery and development of new antibacterial agents. As part of an ongoing investigation into the antibacterial properties of natural products, 20-hydroxyecdysone (20E), isolated from the roots of Achyranthes japonica Nakai, was found to be active against MRSA, either alone or in combination with ampicillin (AM) or gentamicin (GM), via checkerboard assay. This study investigated the antibacterial activity of 20E, which exhibited poor antibacterial activity ($MIC=250-500\;{\mu}g/ml$) against MRSA tested. The combined activity of AM or GE plus 20E against MRSA resulted in fractional inhibitory concentractions (FICs) ranging from 4.00 to $0.031\;{\mu}g/ml$, respectively. Meanwhile, the FIC index ranged from 0.16-4.50, indicating a marked synergistic relationship between AM, GE, and 20E against MRSA. Time-kill assays also showed a remarkable decrease between the combination and the more active compound. Therefore, this study demonstrated that AM, GE, and 20E can act synergistically in inhibiting MRSA in vitro.