Byong-Gon Park

Kwandong University, Gangneung, Gangwon, South Korea

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Publications (7)14.81 Total impact

  • [Show abstract] [Hide abstract]
    ABSTRACT: A newly designed curcumin mimic library (11a-11k) with 2-ethylamino groups in a chalcone structure and variously substituted triazole groups as side chains was synthesized using the Huisgen 1,3-cycloaddition reaction between various alkynes (a-k) and an intermediate (10), with CuSO4 and sodium ascorbate in a solution mixture of chloroform, ethanol, and water (5:3:1) at room temperature for 5h. In the lactate dehydrogenase (LDH) release assay involving co-treatment with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) and/or synthetic curcumin derivatives using TRAIL-resistant human CRT-MG astroglioma cells, the novel curcumin mimic library was found to effectively stimulate the cytotoxicity of TRAIL, causing mild cytotoxicity when administered alone. In particular, 11a and 11j are promising candidates for TRAIL-sensitizers with potential use in combination chemotherapy for brain tumors.
    Bioorganic & medicinal chemistry letters. 06/2014;
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    ABSTRACT: A specific blocker of L-type Ca2+ channels may be useful in decreasing arterial tone by reducing the open-state probability of L-type Ca2+ channels. The aim of the present study was to evaluate the farnesylacetones, which are major active constituents of Sargassum siliquastrum, regarding their vasodilatation efficacies, selectivities toward L-type Ca2+ channels, and in vivo antihypertensive activities. The application of 5E-(farnesylacetone 311) or 5Z-farnesylacetone (farnesylacetone 312) induced concentration-dependent vasodilatation effects on the basilar artery that was pre-contracted with depolarization and showed an ignorable potential role of endothelial-derived nitric oxide. We also tested farnesylacetone 311 or 312 to determine their pharmacological profiles for the blockade of native L-type Ca2+ channels in basilar arterial smooth muscle cells (BASMCs) and ventricular myocytes (VMCs), cloned L- (α1C/β2a/α2δ), N- (α1B/β1b/α2δ), and T-type Ca2+ channels (α1G, α1H, and α1I). Farnesylacetone 311 or 312 showed greater selectivity toward the L-type Ca2+ channels among the tested voltage-gated Ca2+ channels. The ranked order of the potency for farnesylacetone 311 was cloned α1C≒L-type (BASMC)≒L-type (VMCs)>α1B>α1H>α1I>α1G and that for farnesylacetone 312 was cloned α1C≒L-type (BASMCs)≒L-type (VMCs)>α1H>α1G>α1B>α1I. The oral administration of the farnesylacetone 311 (80mg/kg) conferred potent, long-lasting antihypertensive activity in spontaneous hypertensive rats, but it did not alter the heart rate.
    Vascular Pharmacology 02/2013; · 3.21 Impact Factor
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    ABSTRACT: Ulcerative colitis is an inflammatory bowel disease (IBD) characterized by recurrent episodes of colonic inflammation and tissue degeneration in human or animal models. The contractile force generated by the smooth muscle is significantly attenuated, resulting in altered motility leading to diarrhea or constipation in IBD. The aim of this study is to clarify the altered contractility of circular and longitudinal smooth muscle layers in proximal colon of trinitrobenzen sulfonic acid (TNBS)-induced colitis mouse. Colitis was induced by direct injection of TNBS (120 mg/kg, 50% ethanol) in proximal colon of ICR mouse using a 30 G needle anesthetized with ketamin (50 mg/kg), whereas animals in the control group were injected of 50% ethanol alone. In TNBS-induced colitis, the wall of the proximal colon is diffusely thickened with loss of haustration, and showed mucosal and mucular edema with inflammatory infiltration. The colonic inflammation is significantly induced the reduction of colonic contractile activity including spontaneous contractile activity, depolarization-induced contractility, and muscarinic acetylcholine receptor-mediated contractile response in circular muscle layer compared to the longitudinal muscle layer. The inward rectification of currents, especially, important to Ca(2+) and Na(+) influx-induced depolarization and contraction, was markedly reduced in the TNBS-induced colitis compared to the control. The muscarinic acetylcholine-mediated contractile responses were significantly attenuated in the circular and longitudinal smooth muscle strips induced by the reduction of membrane expression of canonical transient receptor potential (TRPC) channel isoforms from the proximal colon of the TNBS-induced colitis mouse than the control.
    Korean Journal of Physiology and Pharmacology 12/2012; 16(6):437-46. · 1.00 Impact Factor
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    ABSTRACT: We have synthesized novel vasodilatation farnesylacetones 1 and 2, which are major active constituents of Sargassum siliquastrum collected from the coast of the East Sea in Korea, in 9 steps. A test of the vasodilatation effect of synthetic intermediates and their deprotected compounds on the basilar arteries of rabbits revealed that 14 and 14-1 have a similar dilation effect as their target marine natural products 1 and 2.
    Bioorganic & medicinal chemistry letters 07/2010; 20(14):4206-9. · 2.65 Impact Factor
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    ABSTRACT: In order to discover novel small vasodilatory molecules for potential use in the treatment of vascular disease, we tested the vasodilatation effect of two types of synthetic curcumin mimics, amide type (3) and sulfonyl amide type (4), upon the basilar artery of rabbits. In general, the sulfonyl amide type mimic (4) is more potent than the amide type (3). Curcumin (1) and compounds 12 and 20 effectively dilated the basilar artery of white rabbits.
    Bioorganic & medicinal chemistry letters 02/2009; 19(5):1481-3. · 2.65 Impact Factor
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    ABSTRACT: Two farnesylacetones, 311 and 312, major active constituents of Sargassum siliquastrum collected from the coast of the East Sea in Korea, showed a moderate vasodilatation effect on the basilar arteries of rabbits. Therefore, treatment with farnesylacetones 311 and 312 may selectively accelerate cerebral blood flow through dilatation of the basilar artery.
    Bioorganic & medicinal chemistry letters 01/2009; 18(24):6324-6. · 2.65 Impact Factor
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    ABSTRACT: Sargahydroquinoic acid (2), a major active constituent of Sargassum micracanthum collected from the coast of the East Sea in Korea, showed a selective vasodilatation effect on the basilar arteries of rabbits. Therefore, treatment with sargahydroquinoic acid may selectively accelerate cerebral blood flow through dilatation of the basilar artery without lowering systemic blood pressure.
    Bioorganic & medicinal chemistry letters 05/2008; 18(8):2624-7. · 2.65 Impact Factor

Publication Stats

19 Citations
14.81 Total Impact Points

Institutions

  • 2008–2014
    • Kwandong University
      • College of Medicine
      Gangneung, Gangwon, South Korea
  • 2012
    • Asan Medical Center
      • Department of Gastroenterology
      Seoul, Seoul, South Korea
  • 2009
    • Yonsei University
      • The Institute of Genetic Science
      Seoul, Seoul, South Korea