• Biomolecules & Therapeutics
• /
• v.8 no.4
• /
• pp.293-298
• /
• 2000

Bergenin is a C-glucoside of 4-O-methyl gallic acid that has been isolated from the cortex of Mallotus japonicus (Euphorbiaceae). Acetylbergenin was synthesized by acetylation from bergenin to increase lipophilic and physiological activities. The therapeutic effects of bergenin and acetylbergenin were evaluated against carbon tetrachloride ($CCl_4$)-induced hepatotoxicity in rats. Bergenin and acetylbergenin were administered orally once daily for successive 5 days, after the intraperitoneal injection of a mixture 0.5 m1/kg of $CCl_4$ in olive oil (1:1). The substantially elevated serum enzymatic activities of alanine/aspartate aminotransferase, sorbitol dehydrogenase and ${\gamma}$-glutamyltransferase induced by $CCl_4$ were restored towards normalization by posttreatment with bergenin and acetylbergenin. Bergenin and acetylbergenin also significantly prevented the elevation of hepatic malondialdehyde formation and depletion of glutathione content induced by $CCl_4$ in a dose dependent fashion. In addition, the decreased activities of glutathione S-transferase and glutathione reductase were restored towards normalization. These results suggest that therapeutic effects of bergenin and acetylbergenin may be related complex mechanisms that involve prevention of lipid peroxidation and preservation of hepatic GSH. The results of this study clearly indicate that bergenin and acetylbergenin have potent hepatothrapeutic action against $CCl_4$-induced hepatotoxicity in rats. In addition, acetylbergenin 50 mgHg showed almost the same levels of hepatoprotective activity as those of bergenin 100 mgAg, indicating the fact that lipophilic acetylbergenin is more effective in the hepatoprotective action against $CCl_4$ than bergenin.

• The Korean Journal of Physiology and Pharmacology
• /
• v.1 no.1
• /
• pp.13-17
• /
• 1997

Carbamazepine (CBZ), an anticonvulsant, has beeen reported to displace ligands at adenosine receptors. Several studies have demonstrated that as far as $A_2$adenosine receptors is concerned, CBZ acts as an antagonist. However, the situation with regard to Al receptors is less straightforward. In this study, we describe the effects of one-week CBZ treatment (25 mg/kg/day) on cerebrocortical $A_1$ adenosine receptors. $A_1$ adenosine receptor bindings as determined by using $[^3CH]DPCPX$ was not significantly altered in membranes prepared from CBZ-treated rats. However, there was a significant decrease in the $A_1$ adenosine receptor-mediated stimulation of $[^{35}S]GTP_{\gamma}S$ binding to cerebrocortical membranes prepared from CBZ-treated rats (20.0% decrease in basal activity; 17.8% decrease in maximal activity). The basal and $10^{-4}$ M forskolin-stimulated adenylyl cyclase activities were relatively unaffected by CBZ treatment, but 10 mM NaF-stimulated adenylyl cyclase activity was significantly reduced in CBZ-treated rats. It appears that one-week CBZ treatment caused an uncoupling of adenosine receptors from G proteins without alteration of $A_1$ adenosine receptor molecules, suggesting that CBZ acts as an agonist at $A_1$ adenosine receptors in rat brain.

• Journal of Nutrition and Health
• /
• v.34 no.1
• /
• pp.14-22
• /
• 2001

In this study, we examined the effects of dietary fatty acids and vitamin E supplementation on antioxidant systems in the rat brain regions. The Sprague Dawley rats were fed the experimental diets 3-4 wks prior to the conception. Experimental diet consisted of 10% fat(wt/wt) which were safflower oil(SO, poor in $\omega$3 fatty acids), mixed oil(MO, P/M/S ratio=1.03:1.45:1,$\omega$6/$\omega$3 ratio=6.3) and mixed oil supplemented with vitamin E(ME:MO+500mg vitamin E/kg diet). At 3 and 9 weeks of age of the newborn rats, frontal cortex(FC), corpus striatum(CS), hippocampus(H) cerebellum(CB) were dissected out from the whole brain. Activities of glutathione peroxidase(GSH-P(sub)x, superoxide dismutase(SOD) concentrations of malondialdehyde(MDA) were mesaured. Dietary fatty acids were not effective in antioxidative system for rat brain. However, when vitamin E was supplemented to the diet(ME), the activities of GSH-P(suh)x tended to increase in comparison to MO group. Therefore, the activites of GSH-P(suh)x of FC and H at the age of 3 weeks showed significant differences(p<0.05). The activities of Total-SOD tended to decrease in ME group compared to MO group. There were significant differences(p<0.05) in FC and CS at the age of 3 weeks. The activities of Mn-SOD tended to increase and Cu, Zn-SOD tended to decrease when vitamin E was supplemented. The activity levels of antioxidative enzymes at the age of 3 weeks and 9 weeks were similar. This suggested that the activity level of antioxidative enzymes reached to the adult level at the age of 3 weeks which is the end point of lactation period. The concentrations of MDA were not altered by experimental diets. When the activities of antioxidant enzymes were compared, the activities of antioxidant enzymes were the lowest in H and FC. In conclusion, the antioxidative system were not altered by dietary fatty acid at the age of 3 weeks and 9 weeks, but the supplementation of vitamin E altered the antioxidative systems. Therefore, these findings should be considered comprehensively in scope of the balance of various antioxidative systems and their interactions(Korean J Nutrition 34(1):14-22, 2001)

• Investigative Magnetic Resonance Imaging
• /
• v.16 no.2
• /
• pp.136-141
• /
• 2012

Purpose : To investigate the pharmacologic modulation of motor task-dependent physiologic responses by antiplatelet agent, clopidogrel, during hand motor tasks in healthy subjects. Materials and Methods: Ten healthy, right-handed subjects underwent three functional magnetic resonance (fMRI) sessions: one before drug administration, one after high dose drug administration and one after reaching drug steady state. For the motor task fMRI, finger flexion-extension movements were performed. Blood oxygenation level dependent (BOLD) contrast was collected for each subject using a 3.0 T VHi (GE Healthcare, Milwaukee, USA) scanner. $T2^*$-weighted echo planar imaging was used for fMRI acquisition. The fMRI data processing and statistical analyses were carried out using SPM2. Results: Second-level analysis revealed significant increases in the extent of activation in the contralateral motor cortex including primary motor area (M1) after drug administration. The number of activated voxels in motor cortex was 173 without drug administration and the number increased to 1049 for high dose condition and 673 for steady-state condition respectively. However, there was no significant difference in the magnitude of BOLD signal change in terms of peak T value. Conclusion: The current results suggest that cerebral motor activity can be modulated by clopidogrel in healthy subjects and that fMRI is highly senstive to evidence such changes.

• The Journal of Korean Medicine
• /
• v.31 no.1
• /
• pp.130-137
• /
• 2010

Objectives: So far it has been reported that acupuncture increases cerebral blood supply and stimulates the functional activity of brain nerve cells. Previous studies have demonstrated that frequently used electro-acupuncture (EA) therapies for stroke increased regional cerebral blood flow (rCBF) in normal volunteers. Though ST 36-ST 41 EA is another prevailing therapy for stroke, there had been no report about its effect on rCBF. This study was to evaluate the effect of ST 36-ST 41 EA on rCBF in normal volunteers using single photon emission computed tomography (SPECT) and statistical parametric mapping (SPM). Methods: In the resting state, $^{99m}Tc$-ECD brain SPECT scans were performed on 10 normal volunteers (5 males, 5 female, mean age $23.6{\pm}0.5$ years). On the other study day, 7 days after the resting examination, 15 minutesEA were applied at ST 36 and ST 41 on the right side of the subjects. Immediately after ST36-ST41 EA, the second SPECT images were obtained in the same manner as the resting state. Significant increases and decreases of rCBF after EA were estimated by comparing their SPECT images with those of the resting state using paired t statistics at every voxel, which were analyzed by SPM with a threshold of p = 0.01, uncorrected (extent threshold: k=100 voxels). Results: EA applied at the right ST36-ST41 significantly increased rCBF in the right inferior parietal lobule (Brodmann area [BA] 40), right retrosubicular area (BA 48), left inferior parietal lobule (BA 40), left middle temporal gyrus (BA 21), left fusiform gyrus (BA 37), left inferior parietal lobule (BA 39), left inferior temporal gyrus (BA 20), and left somatosensory association cortex (BA 7). However, right ST36-ST41 EA significantly decreased rCBF in the right parahippocampal gyrus (BA 35), right cerebellum, left frontopolar area (BA 10), left orbitofrontal area (BA 11), left dorsolateral prefrontal cortex (BA 9), and left dorsal anterior cingulate cortex (BA 32). Conclusions: These results demonstrate that rightST36-ST41 EA increased rCBF prominently in both inferior parietal lobule (BA 40) and right retrosubicular area (BA 48), which suggest that there be correlation between specific EA and corresponding rCBF.

• The Journal of the Korea Contents Association
• /
• v.11 no.4
• /
• pp.273-282
• /
• 2011

This study was to investigate the effect of improve forelimb sensorimotor function and neurotrophic factor(GAP-43) expression when differing an application time of tDCS in ischemic brain injury rat model(pre, $1^{st}$, $7^{th}$, $14^{th}$). Focal ischemic brain injury was induced in 80 Sprague-Dawley rats through middle cerebral artery occlusion(MCAO) by 'Longa' method. And then experimental groups were randomly divided into four groups; GroupI: MCAO induction, GroupII: application of tDCS(10 min) after MCAO induction, GroupIII: application of tDCS(20 min) after MCAO induction, GroupIV: application of tDCS(30 min) after MCAO induction. Modified limb placing test and single pellet reaching test were performed to test forelimb sensorimotor function. And the histological examination was also observed through the immunohistochemistric response of GAP-43(growth-associated protein-43) in the cerebral cortex. In modified limb placing test, groupIII(p<0.05) showed significantly improve than the other groups on $14^{th}$). day. In single pellet reaching test, groupIII(p<0.01) and groupIV(p<0.05) significantly improved on $14^{th}$) day. And in immunohistochemistric response of GAP-43, group III showed significantly positive response than the other groups on $14^{th}$ day. These results suggest that the intensity(0.1 mA)/time(20 min) condition of tDCS application has a significant impact on the sensorimotor functional recovery in focal ischemic brain injury rat models.

• The Korean Journal of Nuclear Medicine
• /
• v.23 no.2
• /
• pp.155-163
• /
• 1989

Regional cerebral perfusion was evaluated in 15 normal controls by single photon emission computed tomography using $^{99m}Tc$ HM-PAO. For quantitative analysis, 13 pairs of homologous region of interest (ROI) were drawn on three transverse slices matching the vascular territories and cerebral cortices, and normal values of 3 semiqunatitative indices including 'Right to left ratio'(R/L ratio), 'Regional index'(RI), and 'Region to cerebellum ratio'(R/cbll ratio) were calculated. Mean values of R/L ratios of homotogous regions were ranged from 0.985 to 1.023, and mean ${\pm}2$ s.d. of all regions did not exceed 11% of mean. Significant difference of RIs (mean count per voxel of a ROI/mean count per voxel of total ROIs) between regions were found (p<0.001) with highest values in occipital cortex and cerebellum. After attenuation correction, RIs in deep gray, cranial portion of anterior cerebral artery and vascular territories in the 2nd slice increased significantly (p < 0.05-0.001), but vise versa in other ROIs. Region to cerebellum ratios also showed regional difference similar to RIs.

• IEMEK Journal of Embedded Systems and Applications
• /
• v.11 no.2
• /
• pp.97-105
• /
• 2016

Microcontrollers (MCUs) for endpoint smart sensor devices of internet-of-thing (IoT) are being implemented as system-on-chip (SoC) with on-chip instruction flash memory, in which user firmware is embedded. MCUs directly fetch binary code-based instructions through bit-line sense amplifier (S/A) integrated with on-chip flash memory. The S/A compares bit cell current with reference current to identify which data are programmed. The S/A in reading '0' (erased) cell data consumes a large sink current, which is greater than off-current for '1' (programmed) cell data. The main motivation of our approach is to reduce the number of accesses of erased cells by binary code level transformation. This paper proposes a built-in write/read path architecture using binary code inversion method based on hot-spot region detection of instruction code access to reduce sensing current in S/A. From the profiling result of instruction access patterns, hot-spot region of an original compiled binary code is conditionally inverted with the proposed bit-inversion techniques. The de-inversion hardware only consumes small logic current instead of analog sink current in S/A and it is integrated with the conventional S/A to restore original binary instructions. The proposed techniques are applied to the fully-custom designed MCU with ARM Cortex-M0$^{TM}$ using 0.18um Magnachip Flash-embedded CMOS process and the benefits in terms of power consumption reduction are evaluated for Dhrystone$^{TM}$ benchmark. The profiling environment of instruction code executions is implemented by extending commercial ARM KEIL$^{TM}$ MDK (MCU Development Kit) with our custom-designed access analyzer.

• The Korean Journal of Physiology
• /
• v.22 no.2
• /
• pp.307-318
• /
• 1988

Properties of succinate transport were examined in basolaterat membrane vesicles (BLMV) isolated from rabbit renal cortex. An inwardly directed $Na^+$ gradient stimulated succinate uptake and led to a transient overshoot. $K^+,{\;}Li^+,{\;}Rb^+$ and choline could not substitute for $Na^+$ in the uptake process. The dependence of the initial uptake rate of succinate on $Na^+$ concentration exhibited sigmoidal kinetics, indicating interaction of more than one $Na^+$ with transporter Hill coefficient for $Na^+$ was calculated to be 2.0. The $Na^+-dependent$ succinate uptake was electrogenic, resulting in the transfer of positive charge across the membrane. The succinate uptake into BLMV showed a pH optimum at external pH $7.5{\sim}8.0$, whereas succinate uptake into brush border membrane vesicles (BBMV) did not depend on external pH. Kinetic analysis showed that a Na-dependent succinate uptake in BLMV occurred via a single transport system, with an apparent Km of $15.5{\pm}0.94{\;}{\mu}M$ and Vmax of $16.22{\pm}0.25{\;}nmole/mg{\;}protein/min$. Succinate uptake was strongly inhibited by $4{\sim}5$ carbon dicarboxylates, whereas monocarboxylates and other organic anions showed a little or no effect. The succinate transport system preferred dicarboxylates in trans-configuration (furmarate) over cis-dicarboxylates (maleate). Succinate uptake was inhibited by the anion transport inhibitors DIDS, SITS and furosemide, and $Na^+-coupled$ transport inhibitor harmaline. These results indicate the existence of a $Na^+-dependent$ succinate transport system in BLMV that may be shared by the other Krebs cycle intemediates. This transport system seems to be very similar to the luminal transport system for dicarboxylates.

• The Korean Journal of Physiology and Pharmacology
• /
• v.17 no.4
• /
• pp.253-257
• /
• 2013

This study examined the mechanism of action of a local anesthetic, lidocaine HCl. Energy transfer between the surface fluorescent probe, 1-anilinonaphthalene-8-sulfonic acid, and the hydrophobic fluorescent probe, 1,3-di(1-pyrenyl) propane, was used to determine the effect of lidocaine HCl on the thickness (D) of the synaptosomal plasma membrane vesicles (SPMV) isolated from the bovine cerebral cortex, and liposomes of the total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. The thickness (D) of the intact SPMV, SPMVTL and SPMVPL were $1.044{\pm}0.008$, $0.914{\pm}0.005$ and $0.890{\pm}0.003$ (arbitrary units, n=5) at $37^{\circ}C$ (pH 7.4), respectively. Lidocaine HCl decreased the thickness of the neuronal and model membrane lipid bilayers in a dose-dependent manner with a significant decrease in the thickness, even at 0.1 mM. The decreasing effect of lidocaine HCl on the membrane thickness might be responsible for some, but not all of its anesthetic action.