• Journal of Pharmaceutical Investigation
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• v.27 no.1
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• pp.57-64
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• 1997

$Amino-{\beta}-lactam$ antibiotics are absorbed by the dipeptide transporter in the small intestine. These uptakes are coupled to a proton influx. The inward proton gradient is partly induced by the $Na^+/H^+$ exchanger and calcium ion is involved in control of this antiport. Interaction between ampicillin which is one of the $Amino-{\beta}-lactam$ antibiotics and nifedipine which is one of calcium channel blocking agents was studied in rats in vivo and with rabbit jejunum mounted on the Sweetana/Grass diffusion cells in vitro. Bioavailability of ampicillin was increased significantly when nifedipine was co-administered orally in rats. There were no differences in the distribution phase and the elimination phase when ampicillin was given either alone or with nifedipine intravenously. Conditions for in vitro experiments were determined. The lift rate of $O_2/CO_2$ gas was controlled to 3 bubbles/sec and ampicillin was stable in the Kreb's buffer at pH 6.0. Absorption of ampicillin was the greatest when the completely-stripped serosal membrane was used. Transport of ampicillin from mucosal to serosal side in the rabbit jejunum was enhanced by 32% in the presence of nifedipine (p=0.059). Above results suggest that nifedipine might increase the plasma level of ampicillin via the improved absorption in the intestine rather than the reduction in the elimination or/and alteration in the distribution.

• Analytical Science and Technology
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• v.11 no.4
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• pp.266-270
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• 1998

The Ag-treated activated carbon was prepared by the impregnation of Ag on the home made activated carbon. We investigated the nitrogen adsorption property, surface structure, and antibacterial activity of the carbon. The BET surface areas of Ag impregnated activated carbon are distributed to $740-1112.2m^2/g$ region. The results of nitrogen adsorption property show that BET surface areas move gradually to lower value with increasing $AgNO_3$ mole concentration. From the SEM results, we observed window blocking effect for micropores of external surface of adsorbent by Ag impregnation. Escherichia coli which is a kind of colon bacillus was used as bacteria for antibacterial test. From these results, we also observed that activity increase gradually to larger range with increasing $AgNO_3$ mole ratio.

• The Korean Journal of Pharmacology
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• v.8 no.2
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• pp.35-39
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• 1972

Previous studies on the effect of the visible lights on the organism have shown the possible influences on the nervous system. It was reported that the illumination of blue beam increased the sympathetic tone and that of red beam increased the parasympathetic tone. The pharmacological actions of the sympathomimetics were also known to be altered by various visible lights. But their modes and mechanisms of actions on the nervous system have not been clarified and is obscure. To elucidate the precise mechanism of action of the visible lights on the nervous system, present study was made to observe the survival time of the mole living in the dark environment, under the illumination of the various visible lights and influences of several drugs. The results are summerized as follows: 1. The illumination of the natural sun light caused the survival time of the mole to be shortened and visible monochromatic beams (red, blue and green) even more markedly shortened the survival time. No significant difference was noted depending on the wave length of the chromatic beam. 2. The shortened survival time caused by the visible monochromatic lights was prolonged by strychnine but not affected by morphine. 3. The survival time under the illumination of the visible monochromatic lights was prolonged by acetylcholine and physostigmine. 4. The shortened survival time under the illumination of the monochromatic visible lights was not affected by adrenaline but prolonged by priscoline. It is suggested that the shortened survival time of the mole by the illumination of the visible lights can be prolonged by the stimulation of central and parasympathetic nervous system and blocking of the sympathetic nervous system.

• The Korean Journal of Physiology and Pharmacology
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• v.13 no.4
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• pp.327-335
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• 2009

The aim of this study was to determine whether losartan, an angiotensin II (Ang II) type 1 ($AT_1$) receptor could influence the CA release from the isolated perfused model of the rat adrenal medulla. Losartan (5${\sim}$50 ${\mu}$M) perfused into an adrenal vein for 90 min produced dose- and time-dependent inhibition of the CA secretory responses evoked by ACh (5.32 mM), high $K^+$ (56 mM, a direct membrane depolarizer), DMPP (100 ${\mu}$M) and McN-A-343 (100 ${\mu}$M). Losartan failed to affect basal CA output. Furthermore, in adrenal glands loaded with losartan (15 ${\mu}$M) for 90 min, the CA secretory responses evoked by Bay-K-8644 (10 ${\mu}$M, an activator of L-type $Ca^{2+}$ channels), cyclopiazonic acid (10 ${\mu}$M, an inhibitor of cytoplasmic $Ca^{2+}$ -ATPase), veratridine (100 ${\mu}$M, an activator of $Na^+$ channels), and Ang II (100 nM) were markedly inhibited. However, at high concentrations (150${\sim}$300 ${\mu}$M), losartan rather enhanced the CA secretion evoked by ACh. Collectively, these experimental results suggest that losartan at low concentrations inhibits the CA secretion evoked by cholinergic stimulation (both nicotininc and muscarinic receptors) as well as by membrane depolarization from the rat adrenal medulla, but at high concentration it rather inhibits ACh-evoked CA secretion. It seems that losartan has a dual action, acting as both agonist and antagonist to nicotinic receptors of the rat adrenal medulla, which might be dependent on the concentration. It is also thought that this inhibitory effect of losartan may be mediated by blocking the influx of both $Na^+$ and $Ca^{2+}$ into the rat adrenomedullary chromaffin cells as well as by inhibiting the $Ca^{2+}$ release from the cytoplasmic calcium store, which is thought to be relevant to the $AT_1$ receptor blockade, in addition to its enhancement of the CA release.

• The Journal of the Korea Contents Association
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• v.9 no.7
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• pp.37-44
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• 2009

Digital watermarking is a technology for preventing illegal copying, for protecting intellectual property rights and copyrights, and for suggesting grounds of the ownership by inserting watermarks into digital contents. Generally speaking, watermarking techniques cannot escape from data distortion and quality degradation due to the watermark insertion. In order to overcome the shortcoming, zero-watermarking techniques which do not change the original data have been proposed recently. This paper proposes CSMVQ(Chaotic SMVQ), a zero-watermarking system for SMVQ(Side Match Vector Quantization) which shows better compression ratio and quality and less blocking effect than VQ(Vector Quantization). In SMVQ, compression progresses from left top to right bottom in order to use the information of the two neighbor blocks, so it is impossible to insert watermarks chaotically. In the process of encoding, CSMVQ dynamically considers the information of the (1 to 4) neighbor blocks already encoded. Therefore, watermark can be inserted into digital contents in chaotic way. Experimental results show that the image quality compressed by CSMVQ is better than that of SMVQ and the inserted watermark is robust against some common attacks.

• The Korean Journal of Physiology and Pharmacology
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• v.14 no.6
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• pp.407-412
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• 2010

3-Deazaadenosine (DZA), a potent inhibitor of S-adenosylhomocysteine hydrolase, was previously proposed to induce intrinsic apoptosis in human leukemic cells. In the present study, we analyzed the mechanism underlying the DZA-induced intrinsic apoptotic pathway. DZA activated typical caspase-dependent apoptosis in HL-60 cells, as demonstrated by an accumulation of hypo-diploidic cells, the processing of multiple procaspases and an inhibitory effect of z-VAD-Fmk on this cell death. During DZA-induced apoptosis, cytochrome c (cyt c) was released into the cytosol. This was neither prevented by z-VAD-Fmk and nor was it associated with the dissipation of mitochondrial membrane potential (${\Delta}{\Psi}_m$). Prior to the release of cyt c, BAX was translocated from the cytosol to mitochondria and underwent oligomerization. Finally, the overexpression of BCL-XL protected HL-60 cells from apoptosis by blocking both the cyt c release and BAX oligomerization. Collectively, these findings suggest that DZA may activate intrinsic apoptosis by stimulating BAX activation and thereby the release of cyt c.

• The Korean Journal of Physiology and Pharmacology
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• v.22 no.6
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• pp.617-625
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• 2018

Neddylation is a post-translational protein modification process. MLN4924 is a newly discovered pharmaceutical neddylation inhibitor that suppresses cancer growth with several cancer types. In our study, we first investigated the effect of MLN4924 on colon cancer cells (HCT116 and HT29). MLN4924 significantly inhibited the neddylation of cullin-1 and colon cancer cell growth in a time and dose-dependent manner. MLN4924 induced G2/M cell cycle arrest and apoptosis in HCT116 and HT29 cells. Moreover, MLN4924 also triggered autophagy in HCT116 and HT29 cells via suppressing the PI3K/AKT/mTOR pathway. Inhibiting autophagy by autophagy inhibitor 3-MA or ATG5 knockdown reversed the function of MLN4924 in suppressing colon cancer cell growth and cell death. Interestingly, MLN4924 suppresses colon cell growth in a xenograft model. Together, our finding revealed that blocking neddylation is an attractive colon cancer therapy strategy, and autophagy might act as a novel anti-cancer mechanism for the treatment of colon cancer by MLN4924.

• Geomechanics and Engineering
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• v.14 no.5
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• pp.467-477
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• 2018

Estimation of hydraulic parameters is a critical step during design of foundation dewatering works. When many piles are installed in an aquifer, estimation of the hydraulic conductivity should consider the blocking of groundwater seepage by the piles. Based on field observations during a dewatering project in Shanghai, hydraulic conductivities are back-calculated using a numerical model considering the actual position of each pile. However, it is difficult to apply the aforementioned model directly in field due to requirement to input each pile geometry into the model. To develop a simple numerical model and find the optimal hydraulic conductivity, three scenarios are examined, in which the soil mass containing the piles is considered to be a uniform porous media. In these three scenarios, different sub-regions with different hydraulic conductivities, based on either automatic inverted calculation, or on effective medium theory (EMT), are established. The results indicate that the error, in the case which determines the hydraulic conductivity based on EMT, is less than that determined in the automatic inversion case. With the application of EMT, only the hydraulic conductivity of the soil outside the pit should be inverted. The soil inside the pit with its piles is divided into sub-regions with different hydraulic conductivities, and the hydraulic conductivity is calculated according to the volume ratio of the piles. Thus, the use of EMT in numerical modelling makes it easier to consider the effect of piles installed in an aquifer.

• Journal of Yeungnam Medical Science
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• v.6 no.2
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• pp.57-62
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• 1989

Clonidine, ${\alpha}2$-adrenergic agonist, applied spinally or epidurally has been shown to be effective in blocking noxious stimuli in human applications. The purpose of this study is to evaluate the analgesic effect of epidurally administered clonidine. In 40 patients undergoing hemorrhoidectomy or anal fistulectomy, 1.33% lidocaine 15ml (Group I) or 1.33% lidocaine mixed with $75{\mu}g$ clonidine(Group II) administered epidurally through sacral hiatus. Intraoperative changes of vital signs and duration of postoperative analgesic effects were observed. The results were as follows : 1) In the group I, average analgesic duration was 2.42 hours. 2) In the group II, average analgesic duration was 7.32 hours. 3) After epidural clonidine injection, the decrease in heart rate and blood pressure was not significant without sedation. 4) Postoperatively, any complaints related clonidine were not reported. In conclusion, postoperative pain control with epidural clonidine was effective.

• Clinical and Experimental Pediatrics
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• v.59 no.1
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• pp.8-15
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• 2016

Purpose: Nephrogenesis is normally accompanied by a tightly regulated and efficient vascularization. We investigated the effect of angiotensin II inhibition on angiogenesis in the developing rat kidney. Methods: Newborn rat pups were treated with enalapril (30 mg/kg/day) or vehicle (control) for 7 days after birth. Renal histological changes were checked using Hematoxylin & Eosin staining. We also investigated the intrarenal expression of vascular endothelial growth factor (VEGF)-A, VEGF receptor 1 (VEGFR1), VEGFR2, platelet-derived growth factor (PDGF)-B, and PDGF receptor-${\beta}$ with Western blotting and immunohistochemical staining at postnatal day 8. Expression of the endothelial cell marker CD31 was examined to determine glomerular and peritubular capillary density. Results: Enalapril-treated rat kidneys showed disrupted tubules and vessels when compared with the control rat kidneys. In the enalapril-treated group, intrarenal VEGF-A protein expression was significantly higher, whereas VEGFR1 protein expression was lower than that in the control group (P<0.05). The expression of VEGFR2, PDGF-B, and PDGF receptor-${\beta}$ was not different between the 2 groups. The increased capillary CD31 expression on the western blots of enalapril-treated rat kidneys indicated that the total endothelial cell protein level was increased, while the cortical capillary density, assessed using CD31 immunohistochemical staining, was decreased. Conclusion: Impaired VEGF-VEGFR signaling and altered capillary repair may play a role in the deterioration of the kidney vasculature after blocking of angiotensin II during renal development.