• Title/Summary/Keyword: chemical-based agent

Search Result 348, Processing Time 0.036 seconds

Neuroprotective effect of caffeic acid phenethyl ester in 3-nitropropionic acid-induced striatal neurotoxicity

  • Bak, Jia;Kim, Hee Jung;Kim, Seong Yun;Choi, Yun-Sik
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.20 no.3
    • /
    • pp.279-286
    • /
    • 2016
  • Caffeic acid phenethyl ester (CAPE), derived from honeybee hives, is a bioactive compound with strong antioxidant activity. This study was designed to test the neuroprotective effect of CAPE in 3-nitropropionic acid (3NP)-induced striatal neurotoxicity, a chemical model of Huntington's disease (HD). Initially, to test CAPE's antioxidant activity, a 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulfonic acid (ABTS) antioxidant assay was employed, and CAPE showed a strong direct radical-scavenging effect. In addition, CAPE provided protection from 3NP-induced neuronal cell death in cultured striatal neurons. Based on these observations, the in vivo therapeutic potential of CAPE in 3NP-induced HD was tested. For this purpose, male C57BL/6 mice were repeatedly given 3NP to induce HD-like pathogenesis, and 30 mg/kg of CAPE or vehicle (5% dimethyl sulfoxide and 95% peanut oil) was administered daily. CAPE did not cause changes in body weight, but it reduced mortality by 29%. In addition, compared to the vehicle-treated group, robustly reduced striatal damage was observed in the CAPE-treated animals, and the 3NP-induced behavioral deficits on the rotarod test were significantly rescued after the CAPE treatment. Furthermore, immunohistochemical data showed that immunoreactivity to glial fibrillary acidic protein (GFAP) and CD45, markers for astrocyte and microglia activation, respectively, were strikingly reduced. Combined, these data unequivocally indicate that CAPE has a strong antioxidant effect and can be used as a potential therapeutic agent against HD.

Mutagenicity and Antimutagenicity of Hydrophilic and Lipophilic Extracts of Thai Northern Purple Rice

  • Punvittayagul, Charatda;Sringarm, Korawan;Chaiyasut, Chaiyawat;Wongpoomchai, Rawiwan
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.15 no.21
    • /
    • pp.9517-9522
    • /
    • 2014
  • Purple rice (Oryza sativa L. var. indica) cv. Kum Doisaket is cultivated in northern Thailand. This study evaluated the mutagenic and antimutagenic properties of hydrophilic and lipophilic components of purple rice using the Ames test. The seed and hull of purple rice were extracted with hexane, methanol, ethanol, and water. The methanol extracts had the highest amounts of phenolic acids and flavonoids, while the hexane extracts contained large amount of tocols and ${\gamma}$-oryzanol. None of the extracts were mutagenic in Salmonella typhimurium strains TA98 and TA100. The hexane extract of rice hull and the methanol extract of rice seed were strongly effective against aflatoxin B1- and 2-amino-3, 4 dimethylimidazo (4, 5-f) quinoline-induced mutagenesis, while aqueous extracts showed weakly antimutagenic properties. All extracts with the exception of aqueous extracts enhanced the number of revertant colonies from benzo (a) pyrene induced-mutagenesis. None of the extracts inhibited mutagenesis induced by the direct mutagens 2-(2-furyl)-3-(5-nitro-2-furyl)-acrylamide and sodium azide. The hull extracts showed more potent antimutagenicity than the seed extracts. Based on a chemical analysis, ${\gamma}$-oryzanol and ${\gamma}$-tocotrienol in the hull and cyanidin-3-glucoside and peonidin-3-glucoside in the seed are candidate antimutagens in purple rice. The antimutagenic mechanisms of purple rice might be related to either modulation of mutagen metabolizing enzymes or direct attack on electrophiles. These findings supported the use of Thai purple rice as a cancer chemopreventive agent.

Application of Statistical Experimental Design to Improve the Quality of Fresh-Cut Apple Cubes by Edible Coating with Alginate

  • Zuo, Li;Lee, Jun-Ho
    • Food Science and Biotechnology
    • /
    • v.15 no.6
    • /
    • pp.825-832
    • /
    • 2006
  • The effect of alginate coating in combination with an anti-browning agent on increasing the post-cutting shelf life and improving the quality of minimally processed apple cubes was studied during storage at room temperature for 5 days. A simple coating technique involving the chemical cross-linkage of alginate by calcium was used. Statistical-based experimental designs were applied to improve the quality of the alginate-coated apple cubes (ACAC). Plackett-Burman design was first used to determine the main factors influencing the preservation of the original weight, color, and texture of ACAC. Among these variables, alginate concentration ($X_1$), dipping time ($X_2$), and dipping temperature ($X_3$) significantly influenced the ACAC weight and color (confidence levels above 90%). Subsequently, the effects of the 3 main factors were further investigated by a central composite design. The polynomial models developed by response surface methodology were adequate to describe the relationships between the studied factors and the responses. Overall optimization conducted by superimposing the curves of the responses enabled the determination of an optimal range of the independent variables in which the five responses were simultaneously optimized. The point chosen as representative of this optimal area corresponded to $X_1=2.98%$, $X_2=0.85\;min$, and $X_3=55^{\circ}C$ and under these conditions the model predicted weight loss=0.522%, relative hardness=1.517, ${\Delta}E=1.423$, browning inhibition=93.403%, and ${\Delta}L=0.158$.

Biological Screening of Novel Derivatives of Valproic Acid for Anticancer and Antiangiogenic Properties

  • Farooq, Muhammad;El-Faham, Ayman;Khattab, Sherine N.;Elkayal, Ahmed M.;Ibrahim, Mahmoud F.;Taha, Nael Abu;Baabbad, Almohannad;Wadaan, Mohammad A.M.;Hamed, Ezaat A.
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.15 no.18
    • /
    • pp.7785-7792
    • /
    • 2014
  • Background: Valproic acid (VPA) is a potent anticancer and antiangiogenic agent. However, design and synthesis of chemical derivatives with improved antiangiogenic and anticancer activities are still necessary. In this study a library of novel derivatives of VPA was synthesized and tested. Methods: A human liver cancer cell line (HepG2) and a human normal embryonic kidney cell line (HEK 293) were exposed to various concentrations of VPA derivatives for 24 hours and cell viability was checked by MTT colorimetric assay. Anti-angiogenic properties were evaluated in transgenic zebrafish embryos. Results: N-valproylglycine derivatives suppressed survival almost 70% (p value 0.001) in HepG2 cells but only 10-12% in HEK 293 cells (p value 0.133). They also suppressed angiogenic blood vessel formation by 80% when used between $2-20{\mu}M$ in zebrafish embryos. Valproic acid hydrazides showed moderate level of anticancer activity by affecting 30-50% (p value 0.001) of cell viability in HepG2 cells and 8-10% in HEK293 cells (p value 0.034). Conclusion: The majority of compounds in this study showed potent and stronger antiangiogenic and anticancer activity than VPA. They proved selectively toxic to cancer cells and safer for normal cells. Moreover, these compounds inhibited developmental angiogenesis in zebrafish embryos. Based on the fact that liver is a highly vascularized organ, in case of liver carcinoma these compounds have the potential to target the pathological angiogenesis and could be an effective strategy to treat hepatocellular carcinoma.

Altered Gene Profiles using KISTCHIP-400 in MCF-7 cells after Exposure to Di(2-ethylhexyl) Phthalate (DEHP) and Dibutyl Phthalate (DBP)

  • Yun, Hye-Jung;Kim, Youn-Jung;Kim, Eun-Young;Ryu, Jae-Chun
    • Proceedings of the Korea Society of Environmental Toocicology Conference
    • /
    • 2003.10a
    • /
    • pp.174-174
    • /
    • 2003
  • There are many synthetic chemicals, such as di(2-ethylhexyl) phthalate (DEHP) and dibutyl phthalate (DBP), used in chemical reaction processes in industry. The establishment of toxicity and detection of synthetic chemicals that may pose a genetic hazard in our enviornment is subjects of great concern at present DEHP, a ubiquitous phthalate plasticizer, induces a wide range of developmental and reproductive toxicities in mammals. DEHP belongs to the large diverse class of peroxisome proliferator compounds, which include herbicides, hypolipidemic drugs. DBP is a plasticizer used to products containing nitrocellulose, polyvinyl acetate, and polyvinyl chloride such as food wraps and blood bags. DBP is also used in cosmetics as a solvent and fixative for perfumes, a suspension agent for solids, an antifoamer, a skin emollient, and hair spray The present study was performed to examine patterns of gene expression in MCF-7 cells following DEHP and DBP exposure. Changes in gene expression were determined by microarray analysis using KISTCHIP-400 including 401 endocrine related genes based on public database and research papers. Of the genes analysis, we determined that genes detected by array showed a 2-fold or greater change in their expression level(increase or decrease). The results of this study demonstrate that a number of genes were differentially expressed in MCF-7 cells but these changes were not significant. Therefore, we keep going this study using microarray analysis and future studies will examine changes of gene expression on time-course and does treatment in variable cell lines.

  • PDF

Quantitative Analysis of Chemical Composition and In Vitro Anti-oxidant and Anti-inflammatory Properties of Asparagus oligoclonos (방울비짜루 지표성분의 함량분석과 항산화·항염증 활성)

  • Lee, Hyun Joo;Jeong, Da Eun;Gang, Ju Eun;Sim, Mi-Ok;Seong, Tae Kyoung;Woo, Kyeong Wan;An, Byeongkwan;Jung, Ho Kyung;Cho, Hyun Woo
    • Korean Journal of Pharmacognosy
    • /
    • v.49 no.2
    • /
    • pp.138-144
    • /
    • 2018
  • Asparagus oligoclonos is one of the endemic halophytes used folk medicine in Korea. We isolated the main compound rutin from methanol extracts of A. oligoclonos based on nuclear magnetic resonance and TOF ESI-MS data. We have investigated the quantitative analysis method of main compound using HPLC and the results exhibit that rutin content of A.oligoclonos were 1.816%. To explore anti-oxidant from A. oligoclonos ethanol extracts (AOE), we investigated the antioxidant effects of AOE on $H_2O_2$-induced oxidative stress in RAW 264.7 cell. AOE were reduced $H_2O_2$-induced oxidative stress via enhancement of cell viability, and AOE significantly decreased ROS production depending on concentration. Next, to screen for anti-inflammatory activity of AOE, we investigated the inhibitory effects of AOE in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. AOE had no effect on cell viability at a concentration of $500{\mu}g/mL$. Nitric oxide (NO) production inhibited in a dose-dependent manner. These results suggest that AOE may be a useful antioxidant and anti-inflammatory agent.

Morphological optimization of process parameters of randomly oriented carbon/carbon composite

  • Raunija, Thakur Sudesh Kumar;Manwatkar, Sushant Krunal;Sharma, Sharad Chandra;Verma, Anil
    • Carbon letters
    • /
    • v.15 no.1
    • /
    • pp.25-31
    • /
    • 2014
  • A microstructure analysis is carried out to optimize the process parameters of a randomly oriented discrete length hybrid carbon fiber reinforced carbon matrix composite. The composite is fabricated by moulding of a slurry into a preform, followed by hot-pressing and carbonization. Heating rates of 0.1, 0.2, 0.3, 0.5, 1, and $3.3^{\circ}C/min$ and pressures of 5, 10, 15, and 20 MPa are applied during hot-pressing. Matrix precursor to reinforcement weight ratios of 70:30, 50:50, and 30:70 are also considered. A microstructure analysis of the carbon/carbon compacts is performed for each variant. Higher heating rates give bloated compacts whereas low heating rates give bloating-free, fine microstructure compacts. The compacts fabricated at higher pressure have displayed side oozing of molten pitch and discrete length carbon fibers. The microstructure of the compacts fabricated at low pressure shows a lack of densification. The compacts with low matrix precursor to reinforcement weight ratios have insufficient bonding agent to bind the reinforcement whereas the higher matrix precursor to reinforcement weight ratio results in a plaster-like structure. Based on the microstructure analysis, a heating rate of $0.2^{\circ}C/min$, pressure of 15 MPa, and a matrix precursor to reinforcement ratio of 50:50 are found to be optimum w.r.t attaining bloating-free densification and processing time.

Influence of Essential Oil in 'Shiranuhi' Immature Fruit on Antioxidant and Antimicrobial Activities (부지화 미숙과 에센셜 오일의 항산화 및 항균 활성 효과)

  • Kim, Sang Suk;Hyun, Ju Mi;Kim, Kwang Sik;Park, Kyung Jin;Park, Suk Man;Choi, Young Hun
    • Korean Journal of Medicinal Crop Science
    • /
    • v.21 no.6
    • /
    • pp.493-497
    • /
    • 2013
  • This study was designed to analyze the chemical composition of essential oil in 'Shiranuhi' immature fruit and to test their biological activities. 'Shiranuhi' immature essential oils (SIEO) were obtained by steam distillation from fruits collected from Jeju Island and were analyzed using gas chromatograph (GC)-flame ionization detectors (FID) and GC-MS. Fourteen components were identified in the essential oil. Limonene (75.21%) and terpineol (8.68%) were the major components in SIEO. Since acne vulgaris is the combined result of a bacterial infection and the inflammatory response to that infection, we examined whether SIEO possessed antibacterial against skin pathogens. As a result, SIEO showed excellent antibacterial activities against drug-susceptible and -resistant Propionibacterium acnes and Staphylococcus epidermidis, which are acne-causing bacteria. In this study, SIEO was examined on DPPH radical scavenging activities, which showed moderate antioxidant activity ($SC_{50}$, $15.36{\mu}L/mL$). In order to determined whether SIEO can be safely applied to human skin, the cytotoxicity effects of SIEO were determined by colorimetric MTT assays in normal human fibroblasts and keratinocyte HaCaT cells. They exhibited low cytotoxicity at $0.5{\mu}L/mL$ in both celllines. Based on these results, we suggest the possibility that essential oil of 'Shiranuhi' maybe considered as an antibacterial and antioxidant agent.

Potent Inhibition of Human Cytochrome P450 1 Enzymes by Dimethoxyphenylvinyl Thiophene

  • Lee, Sang-Kwang;Kim, Yongmo;Kim, Mie-Young;Kim, Sanghee;Chun, Young-Jin
    • Archives of Pharmacal Research
    • /
    • v.27 no.2
    • /
    • pp.199-205
    • /
    • 2004
  • Cytochrome P450 (P450) 1 enzymes such as P450 1A1, 1A2, and 181 are known to be involved in the oxidative metabolism of various procarcinogens and are regarded as important target enzymes for cancer chemoprevention. Previously, several hydroxystilbene compounds were reported to inhibit P450 1 enzymes and were rated as candidate chemopreventive agents. In this study, we investigated the inhibitory effect of 2-[2-(3,5-dimethoxyphenyl)vinyl]-thiophene (DMPVT), produced from the chemical modification of oxyresveratrol, on the activities of P450 1 enzymes. The inhibitory potential by DMPVT on the P450 1 enzyme activity was evaluated with the Escherichia coli membranes of the recombinant human cytochrome P450 1A1, 1A2, or 1B1 coexpressed with human NADPH-P450 reductase. DMPVT significantly inhibited ethoxyresorufin O-deethylation (EROD) activities with $IC_{50}$ values of 61, 11, and 2 nM for 1A1, 1A2, and 1B1, respectively. The EROO activity in OMBA-treated rat lung microsomes was also significantly inhibited by OMPVT in a dose-dependent manner. The modes of inhibition by DMPVT were non-competitive for all three P450 enzymes. The inhibition of P450 1B1-mediated EROD activity by OMPVT did not show the irreversible mechanism-based effect. The loss of EROD activity in P450 1B1 with OMPVT incubation was not blocked by treatment with the trapping agents such as glutathione, N-acetylcysteine, or dithiothreitol. Taken together, the results suggested DMPVT to be a strong noncompetitive inhibitor of human P450 1 enzymes that should be considered as a good candidate for a cancer chemopreventive agent in humans.

A Study on the Engineering Properties of Micro Fine Hybrid Silicate Grout Materials (마이크로 복합실리카 그라우트재의 공학적 특성에 관한 연구)

  • Chun, Byung-Sik;Kim, Jin-Chun;Choi, Young-Chul;Jung, Jong-Ju;Yoon, Nam-Sik;Shin, Sang-Jae
    • Journal of the Korean GEO-environmental Society
    • /
    • v.2 no.1
    • /
    • pp.67-79
    • /
    • 2001
  • The objective of this study is to determine the engineering properties of micro fine hybrid silicate grout materials that were developed recently. In this study, MSG-N type was mainly used as grout materials, and the chemical components, grain size distribution, mineral characteristics were analyzed. Moreover, the properties of active silica and ordinary portland cement acting as coagulating agent were analyzed and compared with each other. To determine the engineering properties, the bleeding test, viscosity test, coagulation test, examination with naked eye, photographing by using SEM, uniaxial compression test and in-situ application test for reclaimed ground were carried out. A series of test results showed that the strength of micro fine hybrid silicate grout materials was about twice that of ordinary sodium silicate grout materials, and alkali leakage decreased dramatically when MSG method was utilized. Especially, based on the evaluation of the application of the MSG method to field, this method would be very effective in reducing coefficient of permeability due to its excelent permeability.

  • PDF