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      • SCOPUS

        Synergistic Effects of Leflunomide and Benazepril in Streptozotocin-Induced Diabetic Nephropathy

        Jin, Hua,Piao, Shang Guo,Jin, Ji Zhe,Jin, Ying Shun,Cui, Zhen Hua,Jin, Hai Feng,Zheng, Hai Lan,Li, Jin Ji,Jiang, Yu Ji,Yang, Chul Woo,Li, Can S.Karger 2014 The Nephron Journals Vol.126 No.3

        <P>Abstract</P><P><B><I>Background:</I></B> Leflunomide (LEF) and benazepril have renoprotective effects on diabetic nephropathy (DN) through their anti-inflammatory and anti-fibrotic activities. This study investigated whether combined treatment using LEF and benazepril affords superior protection compared with the respective monotherapies. <B><I>Methods:</I></B> Diabetes was induced with streptozotocin (STZ, 65 mg/kg) by intraperitoneal injection in male Wistar rats. Two weeks after STZ injection, diabetic rats were treated daily for 12 weeks with LEF (10 mg/kg), benazepril (10 mg/kg), or a combination of both. Basic parameters (body weight, fasting blood glucose level, and 24 h urinary protein excretion), histopathology, inflammatory [inflammatory cell infiltration (ED-1), monocyte chemoattractant protein-1 (MCP-1), and Toll-like receptor-2 (TLR-2)] and glomerulosclerotic factors [transforming growth factor-β<SUB>1</SUB> (TGF-β<SUB>1</SUB>) and connective tissue growth factor (CTGF)], and oxidative stress (8-hydroxy-2'-deoxyguanosine, 8-OHdG) were studied. <B><I>Results:</I></B> Benazepril or LEF treatment significantly prevented body weight loss and 24 h urinary protein excretion induced by diabetes; combined treatment with LEF and benazepril further improved these parameters compared with giving each drug alone (all p < 0.01). Increased expression of inflammatory (MCP-1 and TLR-2) and glomerulosclerotic (TGF-β<SUB>1</SUB> and CTGF) factors in diabetic rat kidney was reduced by treatment with either LEF or benazepril and was further reduced by the combined administration of the two drugs (p < 0.01). These effects were accompanied by suppression of urinary 8-OHdG excretion. There was no significant between-group difference in blood glucose level. <B><I>Conclusions:</I></B> LEF treatment lessens DN, and combined treatment with LEF and benazepril provides synergistic effects in preventing DN.</P><P>© 2014 S. Karger AG, Basel</P>

      • SCIESCOPUSKCI등재

        Purification and Characterization of β-N-Acetylhexosaminidase from Rice Seeds

        (Yu Lan Jin),(Yu Young Jo),(Kil Yong Kim),(Jae Han Shim),(Yong Woong Kim),(Ro Dong Park) 생화학분자생물학회 2002 BMB Reports Vol.35 No.3

        N-Acetyl-β-D-hexosaminidase (β-HexNAc’ase) (EC 3.2.1.52)was purified from rice seeds (Oryza sativa L. var. Dongjin)using ammonium sulfate (80%) precipitation, Sephadex G-150, CM-Sephadex, and DEAE-Sephadex chromatography, sequentially. The activities were separated into 7 fractions(F1-F7) by CM-Sephadex chromatography. Among them, F6 was further purified to homogeneity with a 13.0% yield and 123.3 purification-fold. The molecular mass was estimated to be about 52 kDa on SDS-PAGE and 37.4 kDa on Sephacryl S-300 gel filtration. The enzyme catalyzed the hydrolysis of both p-nitrophenyl-N-acetyl-β-D-glucosaminide (pNP-GlcNAc) and p-nitrophenyl-N-acetyl-β-D-galactosaminide (pNPGalNAc) as substrates, which are typical properties of β-HexNAc’ase. The ratio of the pNP-GlcNAc’ase activity to the pNP-GalNAc’ase activity was 4.0. However, it could not hydrolyze chitin, chitosan, pNP-β-glucopyranoside, or pNP-β-galactopyranoside. The enzyme showed Km, Vmax and Kcat for pNP-GlcNAc of 1.65mM, 79.49mM min?1, and 4.79 × 10^6 min^-1, respectively. The comparison of kinetic values for pNPGlcNAc and pNP-GalNAc revealed that the two enzyme activities are associated with a single binding site. The purified enzyme exhibited optimum pH and temperature for pNPGlcNAc of 5.0 and 50oC, respectively. The enzyme activity for pNP-GlcNAc was stable at pH 5.0-5.5 and 20-40oC. The enzyme activity was completely inhibited at a concentration of 0.1 mM HgCl2 and AgNO_3, suggesting that the intact thiol group is essential for activity. Chloramine T completely inhibited the activity, indicating the possible involvement of methionines in the mechanism of the enzyme.

      • SCIESCOPUSKCI등재

        Structural Requirements of 2',4',6'-Tris(methoxymethoxy) chalcone Derivatives for Anti-inflammatory Activity: The Importance of a 2'-Hydroxy Moiety

        Jin, Feng,Jin, Xing Yu,Jin, Ying Lan,Sohn, Dae-Won,Kim, Soon-Ai,Sohn, Dong-Hwan,Kim, Youn-Chul,Kim, Hak-Sung 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.11

        Butein, a natural chalcone, has anti-inflammatory and hepatoprotective activity. One synthetic derivative of butein, 2',4',6'-tris(methoxymethoxy)chalcone (TMMC), has potent anti-inflammatory activity via an HO-1 (heme oxygenase 1) dependent pathway. The ${\alpha},{\beta}-unsaturated$ ketone moiety in both TMMC and chalcones could be important in mediating this effect. To investigate the structural requirements of TMMC derivatives for anti-inflammatory effects, we modified the ${\alpha},{\beta}-unsaturated$ ketone moiety through catalytic hydrogenation, hydride reduction, or introduction of a triple bond. In addition, we performed structural modifications such as converting the -OMOM group to an -OMe or -OH group. Generally, modifications in the a,_-unsaturated ketone caused a significant decrease or loss of anti-inflammatory activity, which is consistent with the role of the a,_-unsaturated ketone group acting as a Michael acceptor of nucleophilic species like glutathione or cysteine residues on proteins. Chemically, the electron-donating substituents could make the thiol-adduct more stable by decreasing the acidity of the ${\alpha}-hydrogen$ and slowing the speed of the retro-Michael reaction. Also, like previous studies, the 2'-hydroxy group was crucial in increasing the anti-inflammatory effect. The 2'-hydroxy group produced potent anti-inflammatory effects by increasing the electrophilic properties of ${\alpha},{\beta}-unsaturated$ ketones due to hydrogen bonding between the 2'-hydroxy group and the ketone moiety.

      • SCIESCOPUSKCI등재

        Structure Activity Relationship Studies of Anti-inflammatory TMMC Derivatives: 4-Dimethylamino Group on the B Ring Responsible for Lowering the Potency

        Jin, Ying Lan,Jin, Xing Yu,Jin, Feng,Sohn, Dong-Hwan,Kim, Hak-Sung 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.9

        We previously synthesized 2', 4', 6'-tris(methoxymethoxy)chalcone (TMMC) derivatives with various substituents on the A ring that showed potent anti-inflammatory effects by inhibiting NO production in RAW 264.7 cells. The 2'-hydroxy group on the A ring could elevate the electrophilicity of Michael addition of GSH and electron donating groups on the A ring could stabilize the GSH adduct by decreasing the acidity of the $\alpha$-hydrogen. Using this interpretation, we tested various substituents on the B ring and established a proper balance between biological activity and the position of the electron donating or electron withdrawing groups on the B ring. In this case, the 2'-hydroxy group was excluded because it could cause the formation of GSSG through a phenoxy radical and can confuse the interpretation of the biological results. Chalcone derivatives without 2'-hydroxy are likely to deplete cellular GSH levels by a Michael addition process. Strong electron donating groups on the B ring, such as 4-dimethylamino group, gave the weakest inhibition of NO production. A 4-dimethyamino group on the B ring could decrease the stability of the GSH adduct by weakening the C-S bond strength through movement of an electron pair on nitrogen via an aromatic ring.

      • SCIESCOPUSKCI등재
      • Purification and Characterization of β-N-Acetylhexosaminidase from Rice Seeds

        Jin, Yu-Lan,Jo, Yu-Young,Kim, Kil-Yong,Shim, Jae-Han,Kim, Yong-Woong,Park, Ro-Dong 생화학분자생물학회 2002 Journal of biochemistry and molecular biology Vol.35 No.3

        N-Acetyl-$\beta$-D-hexosaminidase ($\beta$-HexNAc'ase) (EC 3.2.1.52) was purified from rice seeds (Oryza sative L. var. Dongjin) using ammonium sulfate (80%) precipitation, Sephadex G-150, CM-Sephadex, and DEAE-Sephadex chromatography, sequentially. The activities were separated into 7 fractions($F_1-F_7$) by CM-Sephadex chromatography. Among them, F6 was further purified to homogeneity with a 13.0% yield and 123.3 purification-fold. The molecular mass was estimated to be about 52 kDa on SDS-PAGE and 37.4 kDa on Sephacryl S-300 gel filtration. The enzyme catalyzed the hydrolysis of both p-nitrophenyl-N-acetyl-$\beta$-D-hexosaminide (pNP-GlcNAc) and p-nitrophenyl-N-acetyl-$\beta$-D-hexosaminide (pNP-GalNAc) as substrates, which are typical properties of $\beta$-HexNAc'ase. The ratio of the pNP-GlcNAc'ase activity to the pNP-GalNAc'ase activity was 4.0. However, it could not hydrolyze chitin, chitosan, pNP-$\beta$-glucopyranoside, or pNP-$\beta$-glucopyranoside. The enzyme showed $K_m$, $V_{max}$ and $K_{cat}$ for pNP-GlcNAc of 1.65 mM, $79.49\;mM\;min^{-1}$, and $4.79{\times}10^6\;min^{-1}$, respectively. The comparison of kinetic values for pNP-GlcNAc and pNP-GalNAc revealed that the two enzyme activities are associated with a single binding site. The purified enzyme exhibited optimum pH and temperature for pNP-GlcNAc of 5.0 and $50^{\circ}C$, respectively. The enzyme activity for pNP-GlcNAc was stable at pH 5.0-5.5 and $20-40^{\circ}C$. The enzyme activity was completely inhibited at a concentration of 0.1 mM $HgCl_$ and $AgNO_3$, suggesting that the intact thiol group is essential for activity. Chloramine T completely inhibited the activity, indicating the possible involvement of methionines in the mechanism of the enzyme.

      • KCI등재

        The Influence of a Second Metal on the Ni/SiC Catalyst for the Methanation of Syngas

        ( Lan Lan Song ),( Yue Yu ),( Xiao Xiao Wang ),( Guoq Jang Jin ),( Ying Yong Wang ),( Xiang Yun Guo ) 한국화학공학회 2014 Korean Chemical Engineering Research(HWAHAK KONGHA Vol.52 No.5

        The catalytic performance of silicon carbide supported nickel catalysts modified with or without secondmetal (Co, Cu and Zn) for the methanation of CO has been investigated in a fixed-bed reactor using a feed consisting of25% CO and 75% H2 without any diluent gas. It has been found that the introduction of Co species can clearly improvethe catalytic activity of Ni/SiC catalyst, whereas the addition of Cu or Zn can result in a significant decrease in the catalyticactivity. The characterizations by means of XRD, TEM, XPS, CO-TPD and H2-TPR indicate that the addition ofCo could decrease the particle size of active metal, increase active sites on the surface of methanation catalyst, improvethe chemisorption of CO and enhance the reducibility of methanation catalysts. Additionally, the special interaction betweenCo species and Ni species is likely favorable for the dissociation of adsorbed CO on the surface of catalyst, and this mayalso contribute to the high activity of 5Co-Ni/SiC catalyst for CO methanation reaction. For 5Cu-Ni/SiC catalyst and 5Zn-Ni/SiC catalyst, Cu and Zn species could cover partial nickel particles and decrease the chemisorption amount of CO. These could be responsible for the low methanation activity. In addition, a 150h stability test under 2 MPa and 300 oCshowed that 5Co-Ni/SiC catalyst was very stable for CO methanation reaction.

      • KCI등재

        A New Steroidal Saponin, Yuccalan, from the Leaves of Yucca smalliana

        Yu-Lan Jin,Ju-Hee Kuk,Kyung-Taek Oh,Young-Ju Kim,Xiang Lan Piao,박노동 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.5

        An extract of the leaves of Yucca smalliana Fern. (Agavaceae) showed potential antimicrobial activity. Employing a bioassay linked fractionation method, one of the active principles, namely yuccalan, was isolated as a new steroidal saponin. The structure of the new steroidal saponin was elucidated as 3-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl-(3β, 5α, 6α, 25S)- spirostan-3,6,27-triol (1) using various spectroscopic techniques, including IR, MS, 1D and 2D 1H-NMR, and 13C-NMR. The purified yuccalan showed antifungal activities against both Rhizoctonia solani and Fusarium oxysporum.

      • SCIESCOPUSKCI등재

        A New Steroidal Saponin, Yuccalan, from the Leaves of yucca smalliana

        Jin, Yu-Lan,Kuk, Ju-Hee,Oh, Kyung-Taek,Kim, Young-Ju,Piao, Xiang-Lan,Park, Ro-Dong 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.5

        An extract of the leaves of Yucca smalliana Fern. (Agavaceae) showed potential antimicrobial activity. Employing a bioassay linked fractionation method, one of the active principles, namely yuccalan, was isolated as a new stroidal saponin. Thn structure of the new steroidal saponin was elucidated as 3-0-${\beta}$-D-glucopyranosyl-(1${\longrightarrow}$6)-${\beta}$-D-glucopyranosyl-(3${\beta}$, 5${\alpha}$, 6${\alpha}$, 25S)-spirostan-3,6,27-triol (1) using various spectroscopic techniques, including IR, MS, ID and 2D $^1$H-NMR, and $^{13}$C-NMR. The purified yuccalan showed antifungal activities against both Rhizoctonia silani and Fusarium oxysporum.

      • SCOPUSKCI등재

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