• Title/Summary/Keyword: leading compound

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Inhibition of Proliferation of Human Fibroblast by δ-Aminolevulinic Acid (ALA) Derivatives through the Induction of Mitochondria Membrane Depolarization (δ-Aminolevulinic acid (ALA) 유도체들의 미토콘드리아 탈분극 유도에 의한 인간 섬유아세포의 세포분열 억제)

  • Jun, Yong-woo;Han, Du-Gyeong;Lee, Jin-A;Jo, Su-Yeon;Jang, Deok-Jin
    • KSBB Journal
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    • v.30 no.6
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    • pp.313-318
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    • 2015
  • ${\delta}$-Aminolevulinic acid (ALA) is an endogenous metabolite formed in the mitochondria from succinyl-CoA and glycine, and plays a key role in the living body as an intermediate of the compound in the porphyrin biosynthesis pathway. ALA has been commonly used in photodynamic therapy for several years, because ALA is of interest as a biodegradable mediator, a growth regulator, and an effective agent used in dermatology. Here, we determined which ALA derivatives were the most effective for the inhibition of the cell proliferation and growth of human fibroblast. As a result, we found that the treatment of ALA derivatives including ALA, ALAP (ALA phosphate salt), MAL (Methyl 5-aminolevulinate hydrochloride salt), PBGL (phophobilinogen lactam) and PBGH (phophobilinogen-HCl) could attenuate cell proliferation of human fibroblast cells. Among them, PBGH was the most effective derivative. In addition, PBGH treatment could induce mitochondrial membrane depolarization, leading to cell death of human fibroblast. These results suggest that mitochondrial membrane depolarization induced by ALA and PBGH treatment might be responsible for inhibition of cell proliferation and death. Taken together, our results propose the possibility that PBGH can be used as one of the effective drugs in human skin disease, psoriasis.

An Experimental Study on the Effect of Maltol against Oxygen Toxicity (산소중독에 대한 MALTOL의 보호효과에 관한 실험적 연구)

  • Hwang, Sung-Joo;Cho, Soo-Hon;Yon, Dork-Ro
    • Journal of Preventive Medicine and Public Health
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    • v.26 no.4 s.44
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    • pp.551-564
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    • 1993
  • Since the widespread application of hyperbaric oxygenation in clinical medicine, the problems of oxygen toxicity have been attracting a deep interest from the researchers on hyperbaric medicine as a practical issue. Among extensive research trials, the study on the protective agents oxygen toxicity occupied one of the most challenging field. As the mechanisms of oxygen toxicity, the role of the oxygen free radicals produced by peroxidation process are strongly accepted by the leading researchers on oxygen toxicity, the probable protective effects of antioxidant against oxygen toxicity are sustaining a sufficient rational. Maltol ($2-methyl-3-hydroxy-{\gamma}-pyrone$) which is known to be a component of Korean red ginseng has been reporting to have an antioxidant action. But, further study is needed to provide definite evidence for this compound to be an antioxidant, since the action was based on the results which were obtained under in vitro experiment. In this study, the author attempted to evaluate the effect of maltol as protective agent against oxygen toxicity through the observation of death rate, convulsion rate, time to convulsion and microscopic pathological changes in some organs of experimental rats exposed to various conditions. The findings observed are as follows : 1) The death rate, convulsion rate, time to convulsion, lung/weight ratio and microscopic pathological finding of lung were identified as reliable objective and quantitative indices for oxygen toxicity. 2) Maltol showed excellent protective effect against pulmonary oxygen toxicity as an antioxidant.

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Inhibitory Effects of Total Saponin Korean Red Ginseng on Thromboxane A2 Production and P-Selectin Expression via Suppressing Mitogen-Activated Protein Kinases

  • Shin, Jung-Hae;Kwon, Hyuk-Woo;Rhee, Man Hee;Park, Hwa-Jin
    • Biomedical Science Letters
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    • v.23 no.4
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    • pp.310-320
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    • 2017
  • Ginseng has been widely used for traditional medicine in eastern Asia and is known to have inhibitory effects on cardiovascular disease (CVD) such as thrombosis, atherosclerosis, and myocardial infarction. Because, platelet is a crucial mediator of CVD, many studies are focusing on inhibitory mechanism of platelet functions. Among platelet activating molecules, thromboxane $A_2$ ($TXA_2$) and P-selectin play a central role in CVD. $TXA_2$ leads to intracellular signaling cascades and P-selectin plays an important role in platelet-neutrophil and platelet-monocyte interactions leading to the inflammatory response. In this study, we investigated the inhibitory mechanisms of total saponin fraction from Korean red ginseng (KRG-TS) on $TXA_2$ production and P-selectin expression. Thrombin-elevated $TXA_2$ production and arachidonic acid release were decreased by KRG-TS dose (25 to $150{\mu}g/mL$)-dependently via down regulation of microsomal cyclooxygenase-1 (COX-1), $TXA_2$ synthase (TXAS) activity and dephosphorylation of cytosolic phospholipase $A_2$ ($cPLA_2$). In addition, KRG-TS suppressed thrombin-activated P-selectin expression, an indicator of granule release via dephosphorylation of mitogen-activated protein kinases (MAPK). Taken together, we revealed that KRG-TS is a beneficial novel compound inhibiting $TXA_2$ production and P-selectin expression, which may prevent platelet aggregation-mediated thrombotic disease.

Nickel Silicide Nanowire Growth and Applications

  • Kim, Joondong
    • Proceedings of the Korean Vacuum Society Conference
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    • 2013.02a
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    • pp.215-216
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    • 2013
  • The silicide is a compound of Si with an electropositive component. Silicides are commonly used in silicon-based microelectronics to reduce resistivity of gate and local interconnect metallization. The popular silicide candidates, CoSi2 and TiSi2, have some limitations. TiSi2 showed line width dependent sheet resistance and has difficulty in transformation of the C49 phase to the low resistive C54. CoSi2 consumes more Si than TiSi2. Nickel silicide is a promising material to substitute for those silicide materials providing several advantages; low resistivity, lower Si consumption and lower formation temperature. Nickel silicide (NiSi) nanowire (NW) has features of a geometrically tiny size in terms of diameter and significantly long directional length, with an excellent electrical conductivity. According to these advantages, NiSi NWs have been applied to various nanoscale applications, such as interconnects [1,2], field emitters [3], and functional microscopy tips [4]. Beside its tiny geometric feature, NW can provide a large surface area at a fixed volume. This makes the material viable for photovoltaic architecture, allowing it to be used to enhance the light-active region [5]. Additionally, a recent report has suggested that an effective antireflection coating-layer can be made with by NiSi NW arrays [6]. A unique growth mechanism of nickel silicide (NiSi) nanowires (NWs) was thermodynamically investigated. The reaction between Ni and Si primarily determines NiSi phases according to the deposition condition. Optimum growth conditions were found at $375^{\circ}C$ leading long and high-density NiSi NWs. The ignition of NiSi NWs is determined by the grain size due to the nucleation limited silicide reaction. A successive Ni diffusion through a silicide layer was traced from a NW grown sample. Otherwise Ni-rich or Si-rich phase induces a film type growth. This work demonstrates specific existence of NiSi NW growth [7].

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Identification of Proteins Binding to Decursinol by Chemical Proteomics

  • Kang, Hyo-Jin;Yoon, Tae-Sung;Jeong, Dae-Gwin;Kim, Yong-Mo;Chung, Jin-Woong;Ha, Jong-Seong;Park, Sung-Sup;Ryu, Seong-Eon;Kim, Sang-Hee;Bae, Kwang-Hee;Chung, Sang-J.
    • Journal of Microbiology and Biotechnology
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    • v.18 no.8
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    • pp.1427-1430
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    • 2008
  • Decursinol, found in the roots of Angelica gigas Nakai, has been traditionally used to treat anemia and other various diseases. Recently, numerous biological activities such as cytotoxic effect on leukemia cells, and antitumor, neuroprotection, and antibacterial activities have been reported for this compound. Although a number of proteins including protein kinase C, androgen receptor, and acetylcholinesterase were proposed as molecular targets responsible for the activities of decursinol, they are not enough to explain such a diverse biological activity mentioned above. In this study, we employed a chemical proteomic approach, leading to identification of seven proteins as potential proteins interacting with decursinol. Most of the proteins contain a defined ATP or nucleic acid binding domain and have been implied to be involved in the pathogenesis and progression of various human diseases including cancer, autoimmune disorders, or neurodegenerative diseases. The present results may provide clues to understand the molecular mechanism of the biological activities shown by decursinol, an anticancer natural product.

Inhibitory Effects of Panduratin A on Periodontitis-Induced Inflammation and Osteoclastogenesis through Inhibition of MAPK Pathways In Vitro

  • Kim, Haebom;Kim, Mi-Bo;Kim, Changhee;Hwang, Jae-Kwan
    • Journal of Microbiology and Biotechnology
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    • v.28 no.2
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    • pp.190-198
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    • 2018
  • Periodontitis is an inflammatory disease caused by microbial lipopolysaccharide (LPS), destroying gingival tissues and alveolar bone in the periodontium. In the present study, we evaluated the anti-inflammatory and anti-osteoclastic effects of panduratin A, a chalcone compound isolated from Boesenbergia pandurata, in human gingival fibroblast-1 (HGF-1) and RAW 264.7 cells. Treatment of panduratin A to LPS-stimulated HGF-1 significantly reduced the expression of interleukin-$1{\beta}$ and nuclear factor-kappa B (NF-${\kappa}B$), subsequently leading to the inhibition of matrix metalloproteinase-2 (MMP-2) and MMP-8 compared with that in the LPS control ($^{**}p$ < 0.01). These anti-inflammatory responses were mediated by suppressing the mitogen-activated protein kinase (MAPK) signaling and activator protein-1 complex formation pathways. Moreover, receptor activator of NF-${\kappa}B$ ligand (RANKL)-stimulated RAW 264.7 cells treated with panduratin A showed significant inhibition of osteoclastic transcription factors such as nuclear factor of activated T-cells c1 and c-Fos as well as osteoclastic enzymes such as tartrate-resistant acid phosphatase and cathepsin K compared with those in the RANKL control ($^{**}p$ < 0.01). Similar to HGF-1, panduratin A suppressed osteoclastogenesis by controlling MAPK signaling pathways. Taken together, these results suggest that panduratin A could be a potential candidate for development as a natural anti-periodontitis agent.

Isorhamnetin Attenuates Staphylococcus aureus-Induced Lung Cell Injury by Inhibiting Alpha-Hemolysin Expression

  • Jiang, Lanxiang;Li, Hongen;Wang, Laiying;Song, Zexin;Shi, Lei;Li, Wenhua;Deng, Xuming;Wang, Jianfeng
    • Journal of Microbiology and Biotechnology
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    • v.26 no.3
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    • pp.596-602
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    • 2016
  • Staphylococcus aureus, like other gram-positive pathogens, has evolved a large repertoire of virulence factors as a powerful weapon to subvert the host immune system, among which alpha-hemolysin (Hla), a secreted pore-forming cytotoxin, plays a preeminent role. We observed a concentration-dependent reduction in Hla production by S. aureus in the presence of sub-inhibitory concentrations of isorhamnetin, a flavonoid from the fruits of Hippophae rhamnoides L., which has little antibacterial activity. We further evaluate the effect of isorhamnetin on the transcription of the Hla-encoding gene hla and RNAIII, an effector molecule in the agr system. Isorhamnetin significantly down-regulated RNAIII expression and subsequently inhibited hla transcription. In a co-culture of S. aureus and lung cells, topical isorhamnetin treatment protected against S. aureus-induced cell injury. Isorhamnetin may represent a leading compound for the development of anti-virulence drugs against S. aureus infections.

Effect of OQ21 and Melatonin on Lipopolysaccharide-Induced Oxidative Stress in Rat Brain (흰쥐 뇌에서의 Lipopolysaccharide-유도 산화적 스트레스에 대한 OQ21과 Melatonin의 작용)

  • Bae Mee Kyung;Choi Shinkyu;Ko Moon-Jeong;Ha Hun-Joo;Kim Hwa-Jung
    • YAKHAK HOEJI
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    • v.49 no.4
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    • pp.347-354
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    • 2005
  • Lipopolysaccharide (LPS) induces synthesis of several inflammatory cytokines and nitric oxide (NO). NO in brain is involved not only in the regulation of important metabolic pathways via intracellular cyclic GMP-dependent path­ways, but also in neurotoxic damage by reacting with superoxide ion leading to form peroxynitrite radical. Oxidative stress has suggested to be related to the inhibition of NO synthase/cyclic GMP pathway. OQ21 is a new fluorinated quinone compound that is recently known to have inhibitory effects on both NO synthase (NOS) and guanylyl cyclase (GC). In this study, we examined effects of OQ21, other known NOS or GC inhibitors, or an antioxidant, melatonin, on the oxidative stress produced by LPS in rat brain. Oxidative stress was observed by using the 2',7'-dichlorofluorescin diacetate to measure intra-cellular reactive oxygen species (ROS) production and by measuring the formation of thiobarbituric acid reactive substances to measure lipid peroxidation. LPS induced significant increase in both ROS produdction and lipid peroxidation in all brain regions tested (striatum, hippocampus and cortex), which were dissected 6hr after intraperitoneal administration of LPS to rats. Direct striatal injection of two NOS inhibitors, N-nitro-L-arginine methyl ester and diphenyleneiodonium, or a GC inhibitor, IH-[1,2,4]oxadiazolo[4,3-a]quinoxaline-l-one, produced no significant ROS increase. However, OQ21 enhanced ROS formation in striatal tissues from LPS-treated rats. Melatonin decreased LPS-induced ROS formation and decreased ROS formation increased by OQ21 in striatum of LPS-treated rats.

The Study of Malodor Reduction after Periodontal Treatment (치주질환 치료 후 구취 감소에 대한 연구)

  • Lee, Jae-Myung;Lim, Sung-Bin;Chung, Chin-Hyung;Hong, Ki-Seok
    • Journal of Periodontal and Implant Science
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    • v.34 no.2
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    • pp.449-459
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    • 2004
  • Bacterial byproducts and volatile sulfur compounds(VSC) have been found to be the leading intra-oral agents, specifically, the byproducts of gram negative anaerobic bacteria have been implicated as primary factors of halitosis in patients presenting with periodontal disease. The objective of this study was to determine the correlation between periodontal treatment and the subsequent reduction in the level of halitosis. Forty-three subjects presenting with periodontal disease were examined before periodontal treatment, one week after treatment, one month after treatment, and finally, two months after treatment, using a portable sulfide monitoring $Halimeter^{(R)}$ to measure the VSC concentrations at the prescribed intervals. The results of the study were as follows: 1. Significant decreases in the mean VSC concentration were observed at the one week, one month, and two month post-op intervals relative to the pre-op measurement. (p<0.05) 2. Significant decreases in the mean VSC concentration were observed in subjects after completion of flap operations. Significant decreases in the mean VSC concentration were observed at the one and two month post-flap operation measurement relative to the VSC concentration at one week (p<0.05), but no significant differences between the one month and two month VSC concentrations were found. (p<0.05) 3. Significant decreases in the mean VSC concentration were observed in subjects after completion of subgingival curettage (p<0,05). Significant decreases were found between the one week and one month measurements and between the one month and two month measurements, but significant differences were not observed between the one week and two month measurements. (p<0.05) The results of this study show significant decreases in VSC concentration in test subjects after periodontal treatment. It can be inferred from the results above, that periodontal disease is a significant contributing factor of halitosis, and that treatment of periodontal disease can been an effective means of reducing VSC concentration in patients presenting with halitosis concurrent with periodontal disease.

Effect of L-carnitine on the expression of the apoptotic genes Bcl-2 and Bax

  • Vardiyan, Reyhane;Ezati, Daniyal;Anvari, Morteza;Ghasemi, Nasrin;Talebi, Alireza
    • Clinical and Experimental Reproductive Medicine
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    • v.47 no.3
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    • pp.155-160
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    • 2020
  • Objective: The genes Bcl-2 and Bax play important roles in apoptosis. Many studies have shown that formalin has a strong deleterious effect on male fertility and can induce apoptosis. L-carnitine has been reported to potentially reverse the negative effects of formalin, leading to improved spermatogenesis. In this study, we examined the levels of expression of Bcl-2 and Bax in mice treated with formalin and L-carnitine. Methods: Thirty adult BALB/c mice were categorized into three groups. The mice in the control group (n = 10) were not injected with any substance. The mice in the second group (n = 10) received 10 mg/kg of formalin daily via an intraperitoneal injection, while those in the final group (n = 10) were intraperitoneally injected daily with a dose of 10 mg/kg of formalin and 100 mg/kg of L-carnitine. All mice were kept in isolated cages for 31 days. Results: The expression of Bax was significantly higher in the formalin-treated mice than in the mice of the control group, while the expression of Bcl-2 was significantly lower in the formalin-treated mice than in the control mice. Additionally, relative to control mice, Bcl-2 expression increased and Bax expression decreased in the mice administered both formalin and L-carnitine. Conclusion: In this study, L-carnitine was shown to augment Bcl-2 expression and to reduce Bax expression, indicating that this compound may inhibit apoptosis. Due to its positive effects, L-carnitine can be used as a prophylactic treatment for people who routinely come into direct contact with formalin as an occupational hazard.