• Journal of Physiology & Pathology in Korean Medicine
• /
• v.17 no.4
• /
• pp.952-957
• /
• 2003

To certify the protective effect of herbal medicine against oxygen free radical-induced myocardiotoxicity, cytotoxicity was measured using LDH activity and TBARS assay in the presence of Jisilhaebaekgyejitang(JHGT) extracts or single constituents of this prescription, In the present study, xanthine oxidase/hypoxanthine (XO/HX) resulted in a cell damage such as increases in LDH activity in culture medium and lipid peroxidation in cultured myocardial cells. In the effect of JHGT extract and its single constituents, which are Fructus Ponciri Seu Aurantii Immaturus (FPSAI), Cortex Magnoliae Officinalis (CMO), Bulbus Allii Macrostemi (BAM), Ramulus Cinnamomi (RC) and Fructus Trichosanthis (FT), they showed the prevention from the XO/HX-induced cardiotoxicity by the decrease of LDH activity and lipid peroxidation. From these results, they show that XO/HX is cardiotoxic in cultured myocardial cells derived from neonatal rat, and it suggests that JHGT, FPSAI, PT, CMO, BAM, RC and FT extracts are positively effective in the blocking in XO/HX-induced cardiotoxicity.

• Biomolecules & Therapeutics
• /
• v.28 no.5
• /
• pp.423-430
• /
• 2020

Telmisartan is an angiotensin-II receptor blocker and acts as a selective modulator of peroxisome proliferator-activated receptor gamma (PPARγ). Several studies have demonstrated that telmisartan ameliorates depression and memory dysfunction and reduces brain inflammation. We hypothesized that the beneficial effects of telmisartan on brain could be due to modulation of the blood-brain barrier (BBB) function. Here, we examined the effect of telmisartan on tumor necrosis factor alpha (TNF-α)-induced expression of intercellular adhesion molecule 1 (ICAM-1) which plays an important role in leukocyte transcytosis through the BBB. Telmisartan blocked TNF-α-induced ICAM-1 expression and leukocyte adhesion in U87MG human glioma cells but showed no effect on human brain microvascular endothelial cells. In U87MG cells, a PPAR antagonist, GW9662 did not block the effect of telmisartan on ICAM1 expression but rather potentiated. Moreover, GW9662 caused no change in TNF-α-induced ICAM-1 expression, suggesting no implication of PPARγ in the telmisartan effect. Further studies showed that telmisartan blocked TNF-α-induced activation of c-Jun N-terminal kinase (JNK), extracellular signal-regulated kinase 1/2 (ERK1/2), p38, and nuclear factorkappa B (NF-κB). In contrast, inhibitors of JNK, ERK1/2 and NF-κB but not p38, blocked ICAM-1 expression induced by TNF-α. Thus, our findings suggest that the beneficial effect of telmisartan is likely due to the reduction of astrocytic ICAM1 expression and leukocytes adhesion to astrocytes, and that this response was mediated by the inhibition of JNK/ERK1/2/NF-κB activation and in the PPAR-independent manner. In conclusion, this study enhances our understanding of the mechanism by which telmisartan exerts the beneficial brain function.

• Proceedings of the Korea Technical Association of the Pulp and Paper Industry Conference
• /
• 2006.06b
• /
• pp.337-347
• /
• 2006

Papers made from unbleached and bleached bagasse chemimechanical pulp were chemically modified by acetylation. The effects of irradiation on unbleached and bleached also reduced papers of bagasse chemimechanical pulp before and after acetylation were investigated in this study. Chemimechanical pulp was prepared from bagasse and then bleached with hydrogen peroxide. Unbleached and hydrogen bleached pulps were reduced by Sodium borohydride in different procedures. Paper sheets were prepared from pulps and then acetylated using a technical grade of acetic anhydride. Accelerated photo-aging was run on the samples using fluorescent lamps to verify photo-stability of paper sheets before and after pretreatments. Brightness reversion (as Post-color number) and other optical properties of the paper sheets were measured. Efficient inhibition of photo-yellowing of papers made from bagasse CMP was achieved by acetylation. The acetylated unbleached CMP was noticeably photo-bleached during irradiation. Sodium borohydride reduction followed by acetylation had the same effect as acetylation alone at the same degree of reaction time and reductive treatment did not affect the yellowing rate to any great extent. The pre-reduced, acetylated unbleached papers were, however, not brightened during irradiation. Calculation done by Kubelka-Munk equation showed that reductive treatment had little effect in reducing the photo-yellowing of paper made from CMP pulp; a small stabilization effect was observed in the case of bleached CMP, while unbleached CMP was slightly more prone to discolor in the later phase of photo-reversion. The improved stability towards light may was closely related to the decrease in the phenolic hydroxyl content as a result of blocking by acetyl groups during treatment with acetic anhydride. The results support the hypothesis that phenolic hydroxyl has an important role in the process of photo-reversion of high-yield pulps. The results obtained in this study demonstrate that the acetylation of paper manufactured from peroxide bleached Bagasse CMP significantly retards light-induced discoloration. The inhibition of yellowing is connected with a decrease in the phenolic hydroxyl content of both unbleached and peroxide bleached papers.

• Archives of Pharmacal Research
• /
• v.29 no.4
• /
• pp.310-317
• /
• 2006

We investigated the effects of trinitrobenzene sulfonic acid (TNBS), an amino-group reagent, on the human ether-a-go-go-related gene (HERG) $K^+$ channels expressed in Xenopus oocytes. TNBS neutralizes the positively charged amino-groups of peptide N-terminal and lysine residues. External application of TNBS at 10 mM for 5 min irreversibly shifted the curves for currents at the end of the pulse and tail currents of HERG to a more negative potential and decreased the maximal amplitude of the $I_{tail}$ curve $(I_{tail,max})$. TNBS had little effect on either the activated current-voltage relationship or the reversal potential of HERG current, indicating that TNBS did not change ion selectivity properties. TNBS shifted the time constant curves of both activation and deactivation of the HERG current to a more hyperpolarized potential; TNBS's effect was greater on channel opening than channel closing. External $H^+$ is known to inhibit HERG current by shifting $V_{1/2}$ to the right and decreasing $I_{tail,max}$. TNBS enhanced the blockade of external $H^+$ by exaggerating the effect of $H^+$ on $I_{tail,max}$, not on $V_{1/2}$. Our data provide evidence for the presence of essential amino-groups that are associated with the normal functioning of the HERG channel and evidence that these groups modify the blocking effect of external $H^+$ on the current.

• Genomics & Informatics
• /
• v.19 no.1
• /
• pp.6.1-6.10
• /
• 2021

Vascular endothelial growth factor (VEGF) is expressed at elevated levels by most cancer cells, which can stimulate vascular endothelial cell growth, survival, proliferation as well as trigger angiogenesis modulated by VEGF and VEGFR (a tyrosine kinase receptor) signaling. The angiogenic effects of the VEGF family are thought to be primarily mediated through the interaction of VEGF with VEGFR-2. Targeting this signaling molecule and its receptor is a novel approach for blocking angiogenesis. In recent years virtual high throughput screening has emerged as a widely accepted powerful technique in the identification of novel and diverse leads. The high resolution X-ray structure of VEGF has paved the way to introduce new small molecular inhibitors by structure-based virtual screening. In this study using different alkaloid molecules as potential novel inhibitors of VEGF, we proposed three alkaloid candidates for inhibiting VEGF and VEGFR mediated angiogenesis. As these three alkaloid compounds exhibited high scoring functions, which also highlights their high binding ability, it is evident that these alkaloids can be taken to further drug development pipelines for use as novel lead compounds to design new and effective drugs against cancer.

• Fire Science and Engineering
• /
• v.33 no.2
• /
• pp.20-29
• /
• 2019

In this paper, the effect of spontaneous combustion inhibitor on the surface of coal stockpile in coal yard was investigated by numerical analysis. First, the numerical analysis method of the present study was compared with the results of the previous study by analyzing the case where the spontaneous combustion inhibitor was not applied, and the effect of preventing spontaneous combustion by various areas and positions for spraying spontaneous combustion inhibitor was analyzed. As a result, the larger the application area of the spontaneous combustion inhibitor, the more the effect of preventing spontaneous combustion by blocking the oxygen inflow into the coal stockpile, and the greater the effect of the spontaneous combustion prevention when spraying spontaneous combustion inhibitor from the bottom of the coal stockpile. Spontaneous combustion inhibitor should be sprayed effectively, considering the economic aspects, such as manufacturing cost etc.

• The Korean Journal of Physiology and Pharmacology
• /
• v.23 no.1
• /
• pp.21-28
• /
• 2019

Swertiamarin (STM) is an iridoid compound that is present in the Gentianaceae swertia genus. Here we investigated antiapoptotic effects of STM on carbon tetrachloride ($CCl_4$)-induced liver injury and its possible mechanisms. Adult male Sprague Dawley rats were randomly divided into a control group, an STM 200 mg/kg group, a $CCl_4$ group, a $CCl_4+STM$ 100 mg/kg group, and a $CCl_4+STM$ 200 mg/kg group. Rats in experimental groups were subcutaneously injected with 40% $CCl_4$ twice weekly for 8 weeks. STM (100 and 200 mg/kg per day) was orally given to experimental rats by gavage for 8 consecutive weeks. Hepatocyte apoptosis was determined by TUNEL assay and the expression levels of Bcl-2, Bax, and cleaved caspase-3 proteins were evaluated by western blot analysis. The expression of $TGF-{\beta}1$, collagen I, collagen III, CTGF and fibronectin mRNA were estimated by qRT-PCR. The results showed that STM significantly reduced the number of TUNEL-positive cells compared with the $CCl_4$ group. The levels of Bax and cleaved caspase-3 proteins, and $TGF-{\beta}1$, collagen I, collagen III, CTGF, and fibronectin mRNA were significantly reduced by STM compared with the $CCl_4$ group. In addition, STM markedly abrogated the repression of Bcl-2 by $CCl_4$. STM also attenuated the activation of the PI3K/Akt pathway in the liver. These results suggested that STM ameliorated $CCl_4$-induced hepatocyte apoptosis in rats.

• Journal of Microbiology and Biotechnology
• /
• v.29 no.9
• /
• pp.1349-1360
• /
• 2019

Chronic exposure to ultraviolet (UV) radiation, regarded as a major cause of extrinsic aging or photoaging characterized by wrinkle formation and skin dehydration, exerts adverse effects on skin by causing the overproduction of reactive oxygen species. Agastache rugosa Kuntze, known as Korean mint, possesses a wide spectrum of biological properties including anti-oxidation, anti-inflammation, and anti-atherosclerosis. Previous studies have reported that A. rugosa protected human keratinocytes against UVB irradiation by restoring the anti-oxidant defense system. However, the anti-photoaging effect of A. rugosa extract (ARE) in animal models has not yet been evaluated. ARE was orally administered to hairless mice at doses of 100 or 250 mg/kg/day along with UVB exposure for 12 weeks. ARE histologically improved UVB-induced wrinkle formation, epidermal thickening, erythema, and hyperpigmentation. In addition, ARE recovered skin moisture by improving skin hydration and transepidermal water loss (TEWL). Along with this, ARE increased hyaluronic acid levels by upregulating HA synthase genes. ARE markedly increased the density of collagen and the amounts of hydroxypoline via two pathways. First, ARE significantly downregulated the mRNA expression of matrix metalloproteinases responsible for collagen degradation by inactivating the mitogen-activated protein kinase/activator protein 1 pathway. Second, ARE stimulated the transforming growth factor beta/Smad signaling, consequently raising the mRNA levels of collagen-related genes. In addition, ARE not only increased the mRNA expression of anti-oxidant enzymes but also decreased inflammatory cytokines by blocking the protein expression of nuclear factor kappa B. Collectively, our findings suggest that A. rugosa may be a potential preventive and therapeutic agent for photoaging.

• Korean Journal of Metals and Materials
• /
• v.47 no.12
• /
• pp.797-810
• /
• 2009

A study was made of the effects of a Sn addition on the microstructure and microfracture mechanism of squeeze cast AZ51-xSn magnesium alloys. Microstructural observation, in situ fracture testing, and fractographic observations were conducted on these alloys to clarify the microfracture process. The microstructural analyses indicated that $Mg_2Sn$ particles as well as $Mg_{17}Al_{12}$ particles precipitated mainly along the solidification cell boundaries; the volume fraction of these hard particles increased as the amount of added Sn increased, with increased the strength. From in situ fracture observations of the AZ51-7Sn alloy, coarse precipitates located on the cell boundaries worked as easy crack propagation sites and caused abrupt intercellular fracturing. On the other hand, the overall fracture properties of the AZ51-3Sn alloy improved because crack propagation proceeded into the Mg matrix rather than into the cell boundaries as twins developed actively, as confirmed by an R-curve analysis. These findings suggest that the addition of 3~5 wt.% Sn is effective in improving both the tensile and fracture properties on the basis of well-developed twins, the blocking of crack propagation, and crack blunting.

• The Korea Journal of Herbology
• /
• v.28 no.3
• /
• pp.7-15
• /
• 2013

Objectives : Interruption and subsequent restoration of blood flow into the kidney result in renal injury. As an approach to preventing the renal injury, we determined the optimal conditions and the underlying mechanisms by which supernatant of hot water extract of ground Triticum aestivum L. (extract) attenuated ischemia/reperfusion (I/R) injury. Methods : One hour after administration of the extract (400 mg/kg) by intraperitoneal injection, renal I/R injury was generated by clamping the left renal artery in rats after surgical removal of the right kidney, followed by reperfusion. The maximal difference between the vehicle-treated and the extract-treated group under ketamine/xylazine or enflurane anesthetization was assessed at varying periods of ischemia (30-45 min) and reperfusion (3-48 hr), based on the renal function assessed with serum creatinine levels, tissue injury with hematoxylin/eosin staining, and apoptosis with terminal deoxynucleotidyltransferase-mediated dUTP nick-end labeling staining. Results : Enflurane anesthetization with 40 min of ischemia and 24 hr of reperfusion was identified to be the optimal condition, under which condition serum creatinine levels and tubular damage in the extract-treated group were significantly reduced compared with those in the vehicle-treated group ($1.3{\pm}0.2$ versus $2.7{\pm}0.3$ mg/dL, P < 0.01, and average score $1.8{\pm}0.1$ versus $3.5{\pm}0.3$, P < 0.01, respectively). These beneficial effects were mediated by inhibition of apoptotic cascades through attenuation of renal tissue malondialdehyde levels, Bax/Bcl-2 ratio and caspase-3 levels. Conclusions : The extract conferred renal protection against ischemia/reperfusion injury in rats by scavenging reactive oxygen species and consequently blocking apoptotic cascades, plausibly augmented by enflurane protection.