• Title/Summary/Keyword: Stereospecificity

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Protective effect of ginsenoside Rh3 against anticancer drug-induced apoptosis in LLC-PK1 kidney cells

  • Lee, Hye Lim;Kang, Ki Sung
    • Journal of Ginseng Research
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    • v.41 no.2
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    • pp.227-231
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    • 2017
  • Background: Ginsenosides are active components of Panax ginseng that exert various health benefits including kidney protection effect. The medicinal activity of ginsenosides can be enhanced by modulating their stereospecificity by heat processing. Ginsenosides Rk2 and Rh3 represent positional isomers of the double bond at C-20(21) or C-20(22). Methods: The present study investigated the kidney-protective effects of ginsenosides Rk2 and Rh3 against cisplatin, a platinum based anticancer drug, induced apoptotic damage in renal proximal LLC-PK1 cells. Results: As a result, ginsenoside Rh3 shows a stronger protective effect than that shown by Rk2. Cisplatin-induced elevated protein levels of phosphorylated c-Jun N-terminal kinase (JNK), extracellular signal-regulated kinase (ERK), p38, and cleaved caspase-3 decreased after cotreatment with ginsenoside Rh3. The increase in the percentage of apoptotic LLC-PK1 cells induced by cisplatin treatment also significantly reduced after cotreatment with ginsenoside Rh3. Conclusion: These results demonstrate that inhibition of the JNK and ERK mitogen-activated protein kinase signaling cascade plays a critical role in mediating the renoprotective effect of ginsenoside Rh3.

Molecular Cloning and Characterization of a cis-Epoxysuccinate Hydrolase from Bordetella sp. BK-52

  • Pan, Hai Feng;Bao, Wen Na;Xie, Zhi Peng;Zhang, Jian Guo;Li, Yongquan
    • Journal of Microbiology and Biotechnology
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    • v.20 no.4
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    • pp.659-665
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    • 2010
  • A cis-epoxysuccinate hydrolase (CESH) from Bordetella sp. BK-52 was purified 51.4-fold with a yield of 27.1% using ammonium sulfate precipitation, ionic exchange, hydrophobic interaction, molecular sieve chromatography and an additional anion-exchange chromatography. The CESH was stable in a broad range of temperature (up to $50^{\circ}C$) and pH (4.0-10.0) with optima of $40^{\circ}C$ and pH 6.5, respectively. It could be partially inhibited by EDTA-$Na_2$, $Ag^+$, SDS, and DTT, and slightly enhanced by $Ba^{2+}$ and $Ca^{2+}$. The enzyme exhibited high stereospecificity in D(-)-tartaric acid (enantiomeric excess value higher than 99%) with $K_m$ and $V_max$ values of 18.67 mM and $94.34\;{\mu}M$/min/mg for disodium cis-epoxysuccinate, respectively. The Bordetella sp. BK-52 CESH gene, which contained 885 nucleotides (open reading frame) encoding 294 amino acids with a molecular mass of about 32 kDa, was successfully overexpressed in Escherichia coli using a T7/lac promoter vector and the enzyme activity was increased 42-times compared with the original strain. It may be an industrial biocatalyst for the preparation of D(-)-tartaric acid.

Ginsentology III;Identifications of Ginsenoside Interaction Sites for Ion Channel Regulation

  • Choi, Sun-Hye;Shin, Tae-Joon;Lee, Byung-Hwan;Lee, Jun-Ho;Hwang, Sung-Hee;Pyo, Mi-Kyung;Nah, Seung-Yeol
    • Journal of Ginseng Research
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    • v.32 no.2
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    • pp.99-106
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    • 2008
  • A ligand - whether an endogenous hormone, neurotransmitter, exogenous toxin or synthetic drug - binds to plasma membrane proteins (e.g., ion channels, receptors or other functional proteins) to exert its physiological or pharmacological effects. Ligands can also have functional groups, showing stereospecificity for interaction sites on their counterpart plasma membrane proteins. Previous reports have shown that the ginsenoside Rg$_3$, a bioactive ginsenoside, meets these criteria in that: 1) an aliphatic side chain of $Rg_3$ plays a role as a functional group, 2) Rg$_3$ regulates voltage- and ligand-gated ion channels in a stereospecific manner with respect to carbon-20, and 3) $Rg_3$ regulates subsets of ligand-gated and voltage-gated ion channels through specific interactions with identified amino acid residues inside the channel pore, in the outer pore entryway, or in toxin binding sites. Rg$_3$, therefore, could be a candidate for a novel ginseng-derived glycosidic ligand regulating ion channels and receptors. This review will examine how Rg$_3$ regulates voltage-gated and ligand-gated ion channels through interactions with its target proteins in the plasma membrane. Hopefully, this review will advance understanding of ginseng pharmacology at the cellular and molecular levels.

Synthesis and Characterization of trans-Dichlorocobalt(Ⅲ) Complex Containing N,N'-bis-[2(S)-pyrrolidinylmethyl]ethane-1,2-diamine (N,N'-bis-[2(S)-pyrrolidinylmethyl]ethane-1,2-diamine이 배위된 trans-Dichlorocobalt(Ⅲ) 착물의 합성과 특성)

  • Kim, Dong Yeup;Kim, Nam Jin;Son, Byung Sam;Lee, Dong Jin;Oh, Chang Eon;Doh, Myung Ki
    • Journal of the Korean Chemical Society
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    • v.39 no.12
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    • pp.940-945
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    • 1995
  • The SS-epm(N,N '-bis-[2(S)-pyrrolidinylmethyl]ethane-1,2-diamine) ligand having stereospecificity has been prepared and reacted with $CoCl_2{\cdot}6H_2O$ or trans-$[Co(pyridine)_4Cl_2]Cl.$ The resultants are green crystals, both of which are identified to be trans-$[Co(SS-epm)Cl_2]_2(COCl_4)$ by elemental analysis and absorption spectra. CD spectrum of trans complex shows negative (-) cotton effect at long wavelength due to the vicinal effect of the stereospecifically chelated ligands. The conformation of SS-epm in trans complex is ${\delta}{\lambda}{\delta}$(SRRS) for each of the five membered chelated ring. $Co(II)Cl_4^{2-}$ as counter ion plays an importance role in the ionic association of the formation of trans complex with SS-epm. Furthermore, according to orientation of secondary amine, total strain energy on each isomers was calculated by molecular mechanics (MM) to verify structural characterization and spectral data.

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