• Title/Summary/Keyword: ${\alpha}$-LA

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Cinnamaldehyde Derivatives Inhibit Coxsackievirus B3-Induced Viral Myocarditis

  • Li, Xiao-Qiang;Liu, Xiao-Xiao;Wang, Xue-Ying;Xie, Yan-Hua;Yang, Qian;Liu, Xin-Xin;Ding, Yuan-Yuan;Cao, Wei;Wang, Si-Wang
    • Biomolecules & Therapeutics
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    • v.25 no.3
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    • pp.279-287
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    • 2017
  • The chemical property of cinnamaldehyde is unstable in vivo, although early experiments have shown its obvious therapeutic effects on viral myocarditis (VMC). To overcome this problem, we used cinnamaldehyde as a leading compound to synthesize derivatives. Five derivatives of cinnamaldehyde were synthesized: 4-methylcinnamaldehyde (1), 4-chlorocinnamaldehyde (2), 4-methoxycinnamaldehyde (3), ${\alpha}$-bromo-4-methylcinnamaldehyde (4), and ${\alpha}$-bromo-4-chlorocinnamaldehyde (5). Neonatal rat cardiomyocytes and HeLa cells infected by coxsackievirus B3 (CVB3) were used to evaluate their antiviral and cytotoxic effects. In vivo BALB/c mice were infected with CVB3 for establishing VMC models. Among the derivatives, compound 4 and 5 inhibited the CVB3 in HeLa cells with the half-maximal inhibitory concentrations values of $11.38{\pm}2.22{\mu}M$ and $2.12{\pm}0.37{\mu}M$, respectively. The 50% toxic concentrations of compound 4 and 5-treated cells were 39-fold and 87-fold higher than in the cinnamaldehyde group. Compound 4 and 5 effectively reduced the viral titers and cardiac pathological changes in a dose-dependent manner. In addition, compound 4 and 5 significantly inhibited the secretion, mRNA and protein expressions of inflammatory cytokines TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 in CVB3-infected cardiomyocytes, indicating that brominated cinnamaldehyde not only improved the anti-vital activities for VMC, but also had potent anti-inflammatory effects in cardiomyocytes induced by CVB3.

Resonant Properties of Modified $PvTiO_3$System Ceramics for High frequency Resonator (고주파 레조네이터용 변성 $PvTiO_3$계 세라믹스의 공진특성)

  • 민석규;류주현;박창엽;김종선;윤현상;정회승
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2001.07a
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    • pp.976-980
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    • 2001
  • In this study, P $b_{0.88}$(L $a_{a}$N $d_{l-a}$)$_{0.08}$(M $n_{1}$3/S $b_{2}$3/)$_{0.02}$ $Ti_{0.98}$ $O_3$system ceramics were manufactured for 20 MHz class resonator application. Electromechanical coupling factor, mechanical quality factor and dynamic range of 3rd overtone thickness vibration mode were measured as the variations of La and Nd molar ratio. Mechanical quality factor and dynamic range at $\alpha$=0.6 composition ceramics showed the highest value of 2, 691 and 52.37 dB, respectively. The tempearture coefficient of resonant frequency measured from -2$0^{\circ}C$ to 8$0^{\circ}C$ showed an excellent value of 5ppm/$^{\circ}C$ at $\alpha$ = 1 composition ceramics. ceramics.s.

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Activities of E6 Protein of Human Papillomavirus 16 Asian Variant on miR-21 Up-regulation and Expression of Human Immune Response Genes

  • Chopjitt, Peechanika;Pientong, Chamsai;Bumrungthai, Sureewan;Kongyingyoes, Bunkerd;Ekalaksananan, Tipaya
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.9
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    • pp.3961-3968
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    • 2015
  • Background: Variants of human papillomavirus (HPV) show more oncogenicity than do prototypes. The HPV16 Asian variant (HPV16As) plays a major role in cervical cancer of Asian populations. Some amino acid changes in the E6 protein of HPV16 variants affect E6 functions such as p53 interaction and host immune surveillance. This study aimed to investigate activities of HPV16As E6 protein on modulation of expression of miRNA-21 as well as interferon regulatory factors (IRFs) 1, 3, 7 and c-fos. Materials and Methods: Vectors expressing E6 protein of HPV16As (E6D25E) or HPV16 prototype (E6Pro) were constructed and transfected into C33A cells. HCK1T cells expressing E6D25E or E6Pro were established by transducing retrovirus-containing E6D25E or 16E6Pro. The E6AP-binding activity of E6 and proliferation of the transfected C33A cells were determined. MiR-21 and mRNA of interesting genes were detected in the transfected C33A cells and/or the HCK1T cells, with or without treatment by culture medium from HeLa cells (HeLa-CM). Results: E6D25E showed binding activity with E6AP similar to that of E6Pro. Interestingly, E6D25E showed a higher activity of miR-21 induction than did E6Pro in C33A cells expressing E6 protein. This result was similar to the HCK1T cells expressing E6 protein, with HeLa-CM treatment. The miR-21 up-regulation significantly corresponded to its target expression. Different levels of expression of IRFs were also observed in the HCK1T cells expressing E6 protein. Interestingly, when treated with HeLa-CM, IRFs 1, 3 and 7 as well as c-fos were significantly suppressed in the HCK1T cells expressing E6D25E, whereas those in the HCK1T cells expressing E6Pro were induced. A similar situation was seen for IFN-${\alpha}$ and IFN-${\beta}$. Conclusions: E6D25E of the HPV16As variant differed from the E6 prototype in its activities on epigenetic modulation and immune surveillance and this might be a key factor for the important role of this variant in cervical cancer progression.

Evaluation of Estrogenic Activity of Extract from the Herbal Mixture Cynanchum wilfordii Hemsley, Phlomis umbrosa Turczaninow, and Angelica gigas Nakai

  • Kim, Se Jong;Jin, Sun Woo;Lee, Gi-Ho;Kim, Yong An;Jeong, Hye Gwang
    • Toxicological Research
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    • v.33 no.1
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    • pp.71-77
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    • 2017
  • Hormone replacement therapy (HRT) consists of highly effective prescription medications for treating menopausal symptoms; however, these agents have exhibited side effects including the risk of estrogen-induced carcinogenesis. Therefore, interest in phytotherapy-based materials as a natural source of alternatives to estrogen therapy has increased. However, some of these herbal medicines have been reported to increase the risk of estrogen-induced cancer. Herbal formulations composed of a combination of Cynanchum wilfordii Hemsley (CW), Phlomis umbrosa Turczaninow (PU), and Angelica gigas Nakai (AG) extracts (CPAE) have been used for treating menopausal symptoms. Therefore, in this study, we aimed to examine the safety of CPAE by determining its potential adverse estrogenic activity using the Organization for Economic Cooperation and Development (OECD) test guideline 455 (TG455) in a stably transfected transcriptionally activated human estrogen receptor ${\alpha}$ ($hER{\alpha}$)-HeLa9903 cell model. We found that CPAE did not how any estrogenic activity or stimulate promoters containing estrogen response elements in MCF-7 cells. In addition, CPAE showed no significant selective activity against $hER{\alpha}$ and $hER{\beta}$, non-selective activity against the ER, or effects on ER target gene expression. Furthermore, CPAE did not significantly induce MCF-7 cell proliferation and uterine weight increase in ovariectomized rats. These results demonstrate that CPAE can be used as beneficial herbal drug for prevention and therapeutic intervention of estrogen carcinogenesis in menopausal women.

Compositions of Defensive Cells and Assay of Prostaglandins in Human Colostrum (초유내 방어 세포의 구성과 프로스타글라딘 함량 분석)

  • 박란숙
    • Journal of Nutrition and Health
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    • v.27 no.7
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    • pp.752-759
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    • 1994
  • It is accepted that colostral macrophages have protective effects on gastrointestinal tract of the neonates. Macrophages act as a major defensive cells in colostrum and serve as a main source of colostral prostaglandins which are known to exert cytoprotection for gastrointestinal tract of neonates against infectious agents and drugs such as aspirin. This study was conducted to evaluate the total cell numbers and differential counts for macrophages, neutrophils and lymphocytes in colostrum of Korean mothers. To compare the level of PGE2, 6-keto-PGF1$\alpha$, and TXB2 between colostrum and serum of postpartum mothers, radioimmunoassay adopting eicosanoids-antibody complex method was applied instead of charcoal method. The results were as follows : 1) Total defensive cell count was 7.6$\pm$2,37$\times$106 cells/ml, differential counts of macrophages, neutrophils and lymphocytes were 57.49$\pm$4.14%, 37.98$\pm$4.43% and 4.29$\pm$0.73% respectively. 2) The order of prostaglandin level in colostrum which are known to enhance development and cytoprotection of gastrointestinal tract, was 6-keto-PGF1$\alpha$, TXB2 and PGE2. Colostral PGE2 level was 584.6$\pm$72.3 pg/ml, higher than that of serum(p<0.01). 6-keto-PGF1$\alpha$, the most abundant prostaglandin in colostrum was higher than in serum level, too (p<0.01). Serum TXB2 level of postpartum mothers(n=42) was higher nine times than that of colostrum(p<0.01), which seems to cause vasoconstriction of uterus in postpartum period. 3) In preterm mothers, serum level of TXB2 level in both groups.

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Peptide Analysis and the Bioactivity of Whey Protein Hydrolysates from Cheese Whey with Several Enzymes

  • Jeewanthi, Renda Kankanamge Chaturika;Kim, Myeong Hee;Lee, Na-Kyoung;Yoon, Yoh Chang;Paik, Hyun-Dong
    • Food Science of Animal Resources
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    • v.37 no.1
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    • pp.62-70
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    • 2017
  • The aim of this study was identifying a suitable food grade enzymes to hydrolyze whey protein concentrates (WPCs), to give the highest bioactivity. WPCs from ultrafiltration retentate were adjusted to 35% protein (WPC-35) and hydrolyzed by enzymes, alcalase, ${\alpha}-chymotrypsin$, pepsin, protease M, protease S, and trypsin at different hydrolysis times (0, 0.5, 1, 2, 3, 4, and 5 h). These 36 types of hydrolysates were analyzed for their prominent peptides ${\beta}-lactoglobulin$ (${\beta}-Lg$) and ${\alpha}-lactalbumin$ (${\alpha}-La$), to identify the proteolytic activity of each enzyme. Protease S showed the highest proteolytic activity and angiotensin converting enzyme inhibitory activity of IC50, 0.099 mg/mL (91.55%) while trypsin showed the weakest effect. Antihypertensive and antioxidative peptides associated with ${\beta}-Lg$ hydrolysates were identified in WPC-35 hydrolysates (WPH-35) that hydrolyzed by the enzymes, trypsin and protease S. WPH-35 treated with protease S in 0.5 h, responded positively to usage as a bioactive component in different applications of pharmaceutical or related industries.

Antioxidant and α-glucosidase inhibition activity of seaweed extracts (해조류 추출물의 항산화 및 α-glucosidase 저해 활성)

  • Kim, Jin-Hak;Kang, Hye-Min;Lee, Shin-Ho;Lee, Ju-Young;Park, La-Young
    • Food Science and Preservation
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    • v.22 no.2
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    • pp.290-296
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    • 2015
  • The antioxidant and ${\alpha}$-glucosidase inhibition activities of 10 kinds of seaweeds Ecklonia cava (EC), Ecklonia stolonifera (ES), Eisenia bicyclis (EB), Capsosiphon fulvescens (CF), Sargassum fulvellum (SF), Undaria pinnatifida (UP), Sargassum thunbergii (ST), Codium fragile (CFr), Hizikia fusiformis (HF), and Enteromorpha prolifera (EP) were investigated. Among all the tested seaweed extracts, the total polyphenol and flavonoid contents of the EB extract were highest 150.81 mg/g and 77.02 mg/g, respectively. The DPPH and ABTS radical scavenging abilities of the EB ethanol extract (1 mg/mL) were 86.26% and 99.71%, respectively, and its SOD-like activity and reducing power were 21.34% and 1.710 ($OD_{700}$). The ${\alpha}$-glucosidase inhibition activities of the EC, EB, and ST were above 98% at the 0.1 mg/mL concentration. These results suggest that seaweed extracts effectively prevent the what of antioxidants and decrease the blood glucose level, and may be used to develop various functional products.

Thymosin Beta-4, Actin-Sequestering Protein Regulates Vascular Endothelial Growth Factor Expression via Hypoxia-Inducible Nitric Oxide Production in HeLa Cervical Cancer Cells

  • Ryu, Yun-Kyoung;Lee, Jae-Wook;Moon, Eun-Yi
    • Biomolecules & Therapeutics
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    • v.23 no.1
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    • pp.19-25
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    • 2015
  • Vascular endothelial growth factor (VEGF) is an important regulator of neovascularization. Hypoxia inducible nitric oxide (NO) enhanced the expression of VEGF and thymosin beta-4 ($T{\beta}4$), actin sequestering protein. Here, we investigated whether NO-mediated VEGF expression could be regulated by $T{\beta}4$ expression in HeLa cervical cancer cells. Hypoxia inducible NO production and VEGF expression were reduced by small interference (si) RNA of $T{\beta}4$. Hypoxia response element (HRE)-luciferase activity and VEGF expression were increased by the treatment with N-(${\beta}$-D-Glucopyranosyl)-N2-acetyl-S-nitroso-D, L-penicillaminamide (SNAP-1), to generate NO, which was inhibited by the inhibition of $T{\beta}4$ expression with $T{\beta}4$-siRNA. In hypoxic condition, HRE-luciferase activity and VEGF expression were inhibited by the treatment with $N^G$-monomethyl-L-arginine (L-NMMA), an inhibitor to nitric oxide synthase (NOS), which is accompanied with a decrease in $T{\beta}4$ expression. VEGF expression inhibited by L-NMMA treatment was restored by the transfection with pCMV-$T{\beta}4$ plasmids for $T{\beta}4$ overexpression. Taken together, these results suggest that $T{\beta}4$ could be a regulator for the expression of VEGF via the maintenance of NOS activity.