• Title/Summary/Keyword: Inhibiting activity

Search Result 1,343, Processing Time 0.034 seconds

Hydrogenation and Electrochemical Characteristics of Amorphous-nanostructured Mg-based Alloys

  • Gebert, A.;Khorkounov, B.;Schultz, L.
    • Journal of Powder Materials
    • /
    • v.13 no.5 s.58
    • /
    • pp.327-335
    • /
    • 2006
  • In the development of new hydrogen absorbing materials for a next generation of metal hydride electrodes for rechargeable batteries, metastable Mg-Ni-based compounds find currently special attention. Amor phous-nanocrystalline $Mg_{63}Ni_{30}Y_7$ and $Mg_{50}Ni_{30}Y_{20}$ alloys were produced by mechanical alloying and melt-spinning and characterized by means of XRD, TEM and DSC. On basis of mechanically alloyed Mg-Ni-Y powders, complex hydride electrodes were fabricated and their electrochemical behaviour in 6M KOH (pH=14,8) was investigated. The electrodes made from $Mg_{63}Ni_{30}Y_7$ powders, which were prepared under use of a SPEX shaker mill, with a major fraction of nanocrystalline phase reveal a higher electrochemical activity far hydrogen reduction and a higher maximum discharge capacity (247 mAh/g) than the electrodes from alloy powder with predominantly amorphous microstructure (216 mAh/g) obtained when using a Retsch planetary ball mill at low temperatures. Those discharge capacities are higher that those fur nanocrystalline $Mg_2Ni$ electrodes. However, the cyclic stability of those alloy powder electrodes was low. Therefore, fundamental stability studies were performed on $Mg_{63}Ni_{30}Y_7$ and $Mg_{50}Ni_{30}Y_{20}$ ribbon samples in the as-quenched state and after cathodic hydrogen charging by means of anodic and cathodic polarisation measurements. Gradual oxidation and dissolution of nickel governs the anodic behaviour before a passive state is attained. A stabilizing effect of higher fractions of yttrium in the alloy on the passivation was detected. During the cathodic hydrogen charging process the alloys exhibit a change in the surface state chemistry, i.e. an enrichment of nickel-species, causing preferential oxidation and dissolution during subsequent anodization. The effect of chemical pre-treatments in 1% HF and in $10\;mg/l\;YCl_3/1%\;H_2O_2$ solution on the surface degradation processes was investigated. A HF treatment can improve their anodic passivation behavior by inhibiting a preferential nickel oxidation-dissolution at low polarisation, whereas a $YCl_3/H_2O_2$ treatment has the opposite effect. Both pre-treatment methods lead to an enhancement of cathodically induced surface degradation processes.

Physicochemical Properties of Fermented Milk Supplemented with Helianthus tuberosus Powder (돼지감자 분말 첨가 발효유의 이화학적 특성)

  • Park, Byung Bae;Renchinkhand, Gereltuya;Nam, Myoung Soo
    • Journal of Dairy Science and Biotechnology
    • /
    • v.37 no.3
    • /
    • pp.196-205
    • /
    • 2019
  • Helianthus tuberosus is a perennial plant in the genus, Asteraceae. Pork potato has various pharmacological functions such as improving constipation, preventing bowel disease, inhibiting colon cancer, reducing serum cholesterol, lowering blood lipids, and enhancing blood sugar. This study investigated the physicochemical properties of fermented milk by adding Helianthus tuberosus powder. During the fermentation process, the pH of the fermented milk with added Helianthus tuberosus was higher after 16 hours of fermentation. At 48 hours of fermentation, the pH decreased to 3.70, 3.65, 3.63, and 3.59 with 0% (the control group), 1%, 3%, and 5% Helianthus tuberosus added, respectively. In the last 48 hours of fermentation, the acidity increased to 2.35%, 2.57%, and 3.17% with 0% (the control group), 1%, 3%, and 5% Helianthus tuberosus added, respectively. The number of lactic acid bacteria increased as the quantity of Helianthus tuberosus added increased. The highest number of lactic acid bacteria was 9.96 log CFU/g after 16 hours of fermentation with a 5% addition of Helianthus tuberosus . After 48 hours of fermentation, the amount of lactic acid bacteria decreased to 7.84 log CFU/g and 7.88 log CFU/g in the control group and the 1% added Helianthus tuberosus group, respectively. The addition of 3% and 5% Helianthus tuberosus increased the lactic acid bacteria count to 9.48 log CFU/ g and 9.81 log CFU/g, respectively. As the fermentation time increased, oxalic acid and tartaric acid decreased but lactic acid increased. Lactose degraded galactose and glucose over time. After 48 hours of fermentation, the viscosity in the control, 1%, 3%, 5% added Helianthus tuberosus groups increased to 1,006 cP, 1,026 cP, 1,040 cP, and 1,106 cP, respectively. The antioxidant effect was higher in the 5% added Helianthus tuberosus group (84.14%) than in the control group (80.39%) at 48 hours of fermentation. The concentration of polyphenol was 1.6 mg/g and antimicrobial activity was strong against E. coli and Staphylococcus aureus.

Methoxychlor Produces Many Adverse Effects on Male Reproductive System, Kidney and Liver by Binding to Oestrogen Receptors

  • Kim, Dae Young
    • Journal of Embryo Transfer
    • /
    • v.28 no.2
    • /
    • pp.157-162
    • /
    • 2013
  • Methoxychlor (MXC) was developed to be a replacement for the banned pesticide DDT. HPTE [2,2-bis (p-hydroxyphenyl)-1,1,1-trichloroethane], which is an in vivo metabolite of MXC, has strong oestrogenic and anti-androgenic effects. MXC and HPTE are thought to produce potentially adverse effects by acting through oestrogen and androgen receptors. Of the two, HPTE binds to sex-steroid receptors with greater affinity, and it inhibits testosterone biosynthesis in Leydig cells by inhibiting cholesterol side-chain cleavage enzyme activity and cholesterol utilisation. In a previous study, MXC was shown to induce Leydig cell apoptosis by decreasing testosterone concentrations. I focused on the effects of MXC on male mice that resulted from interactions with sex-steroid hormone receptors. Sex-steroid hormones affect other organs including the kidney and liver. Accordingly, I hypothesised that MXC can act through sex-steroid receptors to produce adverse effects on the testis, kidney and liver, and I designed our experiments to confirm the different effects of MXC exposure on the male reproductive system, kidney and liver. In these experiments, I used pre-pubescent ICR mice; the puberty period in ICR mice is from postnatal day (PND) 45 to PND60. I treated the experimental group with 0, 100, 200, 400 mg MXC/kg b.w. delivered by an intra-peritoneal injection with sesame oil used as vehicle for 4 weeks. At the end of the experiment, the mice were sacrificed under anaesthesia. The testes and accessory reproductive organs were collected, weighed and prepared for histological investigation. I performed a chemiluminescence immune assay to observe the serum levels of testosterone, LH and FSH. Blood biochemical determination was also performed to check for other effects. There were no significant differences in our histological observations or relative organ weights. Serum testosterone levels were decreased in a dose-dependent manner; a greater dose resulted in the production of less testosterone. Compared to the control group, testosterone concentrations differed in the 200 and 400 mg/kg dosage groups. In conclusion, I observed markedly negative effects of MXC exposure on testosterone concentrations in pre-pubescent male mice. From our biochemical determinations, I observed some changes that indicate renal and hepatic failure. Together, these data suggest that MXC produces adverse effects on the reproductive system, kidney and liver.

Antimicrobial activity of epigallocatechin gallate from green tea (Camellia sinensis) on pathogenic Salmonella Enteritidis in braised quail eggs (메추리알 장조림에서 녹차 Epigallocatechin gallate (EGCG)의 Salmonella Enteritidis에 대한 저장 온도에 따른 항미생물 활성)

  • Kim, Kwang-Yeop;Kim, Young-Ji;Kim, Hong-Seok;Song, Kwang-Young;Kim, Dong-Hyeon;Lee, Mi-Young;Kim, Eui-Su;Jeong, Heon-Sang;Seo, Kun-Ho
    • Korean Journal of Food Science and Technology
    • /
    • v.48 no.4
    • /
    • pp.329-334
    • /
    • 2016
  • The inhibitory effect of epigallocatechin gallate (EGCG), one of the antioxidants in green tea (Camellia sinensis), against Salmonella Enteritidis was evaluated in commercial braised quail eggs at two temperatures (4 and $25^{\circ}C$). Although S. Enteritidis was dose-dependently suppressed by EGCG in pure culture at $25^{\circ}C$, it was not inhibited in the sauce or eggs at this temperature. At low temperature ($4^{\circ}C$), S. Enteritidis was inhibited in both the sauce and eggs by $400{\mu}g/mL$ EGCG. Thus, EGCG at an appropriate concentration could be a useful food additive for inhibiting S. Enteritidis in braised quail eggs at low temperatures.

Inhibition of Microbial Quorum Sensing Mediated Virulence Factors by Pestalotiopsis sydowiana

  • Parasuraman, Paramanantham;Devadatha, B;Sarma, V. Venkateswara;Ranganathan, Sampathkumar;Ampasala, Dinakara Rao;Reddy, Dhanasekhar;Kumavath, Ranjith;Kim, In-Won;Patel, Sanjay K.S.;Kalia, Vipin Chandra;Lee, Jung-Kul;Siddhardha, Busi
    • Journal of Microbiology and Biotechnology
    • /
    • v.30 no.4
    • /
    • pp.571-582
    • /
    • 2020
  • Quorum sensing (QS)-mediated infections cause severe diseases in human beings. The control of infectious diseases by inhibiting QS using antipathogenic drugs is a promising approach as antibiotics are proving inefficient in treating these diseases. Marine fungal (Pestalotiopsis sydowiana PPR) extract was found to possess effective antipathogenic characteristics. The minimum inhibitory concentration (MIC) of the fungal extract against test pathogen Pseudomonas aeruginosa PAO1 was 1,000 ㎍/ml. Sub-MIC concentrations (250 and 500 ㎍/ml) of fungal extract reduced QS-regulated virulence phenotypes such as the production of pyocyanin, chitinase, protease, elastase, and staphylolytic activity in P. aeruginosa PAO1 by 84.15%, 73.15%, 67.37%, 62.37%, and 33.65%, respectively. Moreover, it also reduced the production of exopolysaccharides (74.99%), rhamnolipids (68.01%), and alginate (54.98%), and inhibited the biofilm formation of the bacteria by 90.54%. In silico analysis revealed that the metabolite of P. sydowiana PPR binds to the bacterial QS receptor proteins (LasR and RhlR) similar to their respective natural signaling molecules. Cyclo(-Leu-Pro) (CLP) and 4-Hydroxyphenylacetamide (4-HPA) were identified as potent bioactive compounds among the metabolites of P. sydowiana PPR using in silico approaches. The MIC values of CLP and 4-HPA against P. aeruginosa PAO1 were determined as 250 and 125 ㎍/ml, respectively. All the antivirulence assays were conducted at sub-MIC concentrations of CLP (125 ㎍/ml) and 4-HPA (62.5 ㎍/ml), which resulted in marked reduction in all the investigated virulence factors. This was further supported by gene expression studies. The findings suggest that the metabolites of P. sydowiana PPR can be employed as promising QS inhibitors that target pathogenic bacteria.

The Effect of Laminaria japonica Diet on the Pharmacokinetics of Glipizide in Rats (다시마 식이가 흰쥐에서 글리피지드의 체내동태에 미치는 영향)

  • Choi, Han-Gon;Jang, Bo-Hyun;Rhee, Jong-Dal;Yu, Bong-Kyu;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
    • /
    • v.33 no.2
    • /
    • pp.113-120
    • /
    • 2003
  • Drug interactions with food, on occasion, lead to serious nutritional and functional changes in the body as well as alternations of pharmacological effect. It, therefore, should be necessary to take drug interactions with food into consideration for effective and safe therapeutics. Diabetes mellitus is a heterogeneous group of disorders characterized by abnormal glucose homeostasis, resulting in hyperglycemia, and is associated with increased risk of micovascular, macrovascular, and neuropathic complications. However, the precise mechanism of diabetes mellitus remains unclear. Three basic objectives in the care of diabetic patients are maintaining optimal nutrition, avoiding hypo- or hyperglycemia and preventing complications. The purpose of this study was to investigate thε effect of Laminaria japonica diet on the absorption, distribution, metabolism and excretion of glipizide which are frequently used in the treatment of diabetes. Diabetic rats induced by streptozotocin were employed in this study. Blood concentrations of oral hypoglycemic agents were measured by HPLC and resultant pharmacokinetic parameters were calculated by RSTRIP. The mechanisms of drug interaction with food were evaluated on the basis of pharmacokinetic parameters such as $k_{a},\;t_{1/2},\;C_{max},\;t_{max}$ and AUC. Administration of glipizide in normal rats treated with Laminaria japonica diet showed significant increase in AUC, $k_{a},\;t_{1/2},\;t_{max}$ and decrease in $C_{max}$, compared to those without Laminaria japonica diet. This might result from adsorption of glipizide on components of Laminaria japonica, causing delayed absorption. Administration of glipizide in diabetic rats treated with Laminaria japonica diet showed significant increase in $t_{1/2}\;and\;t_{max}$, and decrease in $C_{max}$, compared to those without Laminaria japonica diet. This might also result from adsorption of glipizide on components of Laminaria japonica, causing delayed absorption and flattened blood concentration of glipizide. The oral glucose test showed that Laminaria japonica diet could lower blood glucose level probably through either inhibiting the activity of disaccharidases, intestinal digestive enzymes, or delaying the absorption of glucose. More studies should be followed to fully understand pharmacokinetic changes of glipizide caused by long-term Laminaria japonica diet.

Inhibition of Angiotensin II-Induced Vascular Smooth Muscle Cell Hypertrophy by Different Catechins

  • Zheng, Ying;Song, Hye-Jin;Yun, Seok-Hee;Chae, Yeon-Jeong;Jia, Hao;Kim, Chan-Hyung;Ha, Tae-Sun;Sachinidis, Agapios;Ahn, Hee-Yul;Davidge, Sandra T.
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.9 no.2
    • /
    • pp.117-123
    • /
    • 2005
  • A cumulative evidence indicates that consumption of tea catechin, flavan-3-ol derived from green tea leaves, lowers the risk of cardiovascular diseases. However, a precise mechanism for this cardiovascular action has not yet been fully understood. In the present study, we investigated the effects of different green tea catechins, such as epigallocatechin-3 gallate (EGCG), epigallocatechin (EGC), epicatechin-3 gallate (ECG), and epicatechin (EC), on angiotensin II (Ang II)-induced hypertrophy in primary cultured rat aortic vascular smooth muscle cell (VSMC). [$^3H$]-leucine incorporation was used to assess VSMC hypertrophy, protein kinase assay, and western blot analysis were used to assess mitogen-activated protein kinase (MAPK) activity, and RT-PCR was used to assess c-jun or c-fos transcription. Ang II increased [$^3H$]-leucine incorporation into VSMC. However, EGCG and ECG, but not EGC or EC, inhibited [$^3H$]-leucine incorporation increased by Ang II. Ang II increased phosphorylation of c-Jun, extracellular-signal regulated kinase (ERK) 1/2 and p38 MAPK in VSMC, however, EGCG and ECG , but not EGC or EC, attenuated c-Jun phosphorylation increased by Ang II. ERK 1/2 and p38 MAPK phosphorylation induced by Ang II were not affected by any catechins. Ang II increased c-jun and c-fos mRNA expression in VSMC, however, EGCG inhibited c-jun but not c-fos mRNA expression induced by Ang II. ECG, EGC and EC did not affect c-jun or c-fos mRNA expression induced by Ang II. Our findings indicate that the galloyl group in the position 3 of the catechin structure of EGCG or ECG is essential for inhibiting VSMC hypertrophy induced by Ang II via the specific inhibition of JNK signaling pathway, which may explain the beneficial effects of green tea catechin on the pathogenesis of cardiovascular diseases observed in several epidemiological studies.

Enhanced Pathogenicity of Baculovirus Using Immunosuppressive Genes Derived From Cotesia plutellae Bracovirus (폴리드나바이러스(CpBV) 유래 면역억제 유전자를 이용한 베큘로바이러스 병원력 제고 기술)

  • Kim, Yong-Gyun;Kwon, Bo-Won;Bae, Sung-Woo;Choi, Jai-Young;Je, Yeon-Ho
    • The Korean Journal of Pesticide Science
    • /
    • v.12 no.3
    • /
    • pp.283-290
    • /
    • 2008
  • Baculoviruses have been used to control some serious lepidopteran pests. However, their narrow target insect spectrum and slow efficacy are main limitations to be used in various applications. This study introduces a technique to overcome these limitations by inhibiting insect immune defence to enhance the viral pathogenicity. Polydnaviruses are an insect DNA virus group and symbiotic to some ichneumonid and braconid endoparasitoids. Cotesia plutellae bracovirus (CpBV) is a braconid polydnavirus and encodes several immunosuppressive genes. We selected seven CpBV genes and recombined them to wild type Autographa California multiple nucleopolyhedrovirus (AcNPV). A bioassay of these seven recombinants indicated that most recombinants had similar or superior efficacy to wild type AcNPV against beet armyworm, Spodoptera exigua, and diamondback moth, Plutella xylostella. Recombinant AcNPV with CpBV-ELP was the most potent in terms of lethal time by shortening more than 2 days compared to wild type AcNPV. This recombinant was further proved in its dose-dependent pathogenicity and its efficacy by spray application on S. exigua infesting cabbage cultivated in pots. We discussed the efficacy of CpBV-ELP recombinant AcNPV in terms of suppressing antiviral activity of target insects.

Effect of Conjugated Linoleic Acid on the Proliferation of the Human Colon Cancer Cell Line, HT-29 (Conjugated Linoleic Acid가 대장암 세포인 HT-29의 증식에 미치는 영향)

  • 김은지;조한진;김석종;강영희;하영래;윤정한
    • Journal of Nutrition and Health
    • /
    • v.34 no.8
    • /
    • pp.896-904
    • /
    • 2001
  • Conjugated linoleic acid(CLA) is a group of positional and geometric isomers of linoleic acid(LA) and exhibits anticarcinogenic activity in multiple experimental animal models. Cis-9,trns-11(c9t11) and trans-10,cis-12(t10c12) CLA are the principal isomers found in foods. The present study was performed to determine whether CLA and the two isomers inhibits HT-29 cell proliferation and to assess whether such an effect was related to changes in secretion of eicosanoids. Cells were incubated in serum-free medium with various concentrations(0 to 20$\mu$M) of CLA or LA. CLA inhibited cell proliferation in a dose-dependent manner, with maximal inhibition(70 $\pm$ 1%) observed at 20$\mu$M concentration after 96 hours. However, LA had no effect at the same concentration range. To compare the ability of c9f11 and t10c12 to inhibit cell proliferation, cells were incubated with increasing concentrations(0 to 4$\mu$M) of these isomers. T10c12 inhibited cell proliferation in a dose-dependent manner. A 66 $\pm$ 2% decrease in cell number was observed within 96 hours after addition of 4$\mu$M t10c12. By contrast, c9t11 had no effect. The concentrations of CLA and the two isomers in the plasma membrane were increased when they were added to the incubation medium. However, they did not alter the levels of arachidonic acid in plasma membrane. To assess whether the proliferation inhibiting effect of CLA was related to changes in eicosanoid production, prostaglandin E$_2$(PGE$_2$) and leukotriene B$_4$(LTB$_4$) concentrations in conditioned media were estimated by a competitive enzyme immunoassay. Both CLA and t10c12 increased the production of materials reactive to PGE$_2$ and LTB$_4$ antibodies in a dose-dependent manner. By contrast, c9t11 had no effect. These results indicate that inhibition of HT-29 cell proliferation by CLA is attributed to the effect of the t10v12 isomer. The materials reactive to PGE$_2$ and LTB$_4$ antibodies may inhibit growth stimulatory effect of arachidonic acid-derived eicosanoids on HT-29 cell proliferation.

  • PDF

Anti-tumor Effects of Penfluridol through Dysregulation of Cholesterol Homeostasis

  • Wu, Lu;Liu, Yan-Yang;Li, Zhi-Xi;Zhao, Qian;Wang, Xia;Yu, Yang;Wang, Yu-Yi;Wang, Yi-Qin;Luo, Feng
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.15 no.1
    • /
    • pp.489-494
    • /
    • 2014
  • Background: Psychiatric patients appear to be at lower risk of cancer. Some antipsychotic drugs might have inhibitory effects on tumor growth, including penfluridol, a strong agent. To test this, we conducted a study to determine whether penfluridol exerts cytotoxic effects on tumor cells and, if so, to explore its anti-tumor mechanisms. Methods: Growth inhibition of mouse cancer cell lines by penfluridol was determined using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Cytotoxic activity was determined by clonogenic cell survival and trypan blue assays. Animal tumor models of these cancer cells were established and to evaluate penfluridol for its anti-tumor efficacy in vivo. Unesterified cholesterol in cancer cells was examined by filipin staining. Serum total cholesterol and tumor total cholesterol were detected using the cholesterol oxidase/p-aminophenazone (CHOD-PAP) method. Results: Penfluridol inhibited the proliferation of B16 melanoma (B16/F10), LL/2 lung carcinoma (LL/2), CT26 colon carcinoma (CT26) and 4T1 breast cancer (4T1) cells in vitro. In vivo penfluridol was particularly effective at inhibiting LL/2 lung tumor growth, and obviously prolonged the survival time of mice bearing LL/2 lung tumors implanted subcutaneously. Accumulated unesterified cholesterol was found in all of the cancer cells treated with penfluridol, and this effect was most evident in LL/2, 4T1 and CT26 cells. No significant difference in serum cholesterol levels was found between the normal saline-treated mice and the penfluridol-treated mice. However, a dose-dependent decrease of total cholesterol in tumor tissues was observed in penfluridol-treated mice, which was most evident in B16/F10-, LL/2-, and 4T1-tumor-bearing mice. Conclusion: Our results suggested that penfluridol is not only cytotoxic to cancer cells in vitro but can also inhibit tumor growth in vivo. Dysregulation of cholesterol homeostasis by penfluridol may be involved in its anti-tumor mechanisms.