• Molecular & Cellular Toxicology
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• v.4 no.1
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• pp.52-60
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• 2008

In order to investigate whether the particles reduced to almost nano grade might affect the chemical and physical properties of organic materials, whole Korean Black-Red Ginseng was pulverized into almost nano size and then ginsenosides, minerals, carbohydrates, lipids and proteins in the ultrafine particles were compared with those in the regular particles as control. The mean size of the ultrafine particles was in the 350 nm range, while that of the regular particles was $127{\mu}m$. More ginsenosides, minerals, carbohydrates, lipids and proteins were detected in the ultrafine particles than in the regular particles. Interestingly, more lipids from the ultrafine particles dissolved in the water than those from the regular particles in the ethanol. Absorption and transport of carbohydrate, lipid or antioxidant activity across the intestinal wall using everted intestine sacks of mice was also enhanced by particle size reduction at the almost nano scale. More cytotoxic effect against hepatoma cell growth by ultrafine particles was also found. These results could be used as the basic data for the understanding and evaluation of the effects of organic nanomaterials on the human health.

• Journal of Pharmaceutical Investigation
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• v.23 no.2
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• pp.61-69
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• 1993

Prodrug of cefazolin (CFZ) was prepared with the objective of improving its oral bioavailability. Cefazolin phthalidyl ester (CFZ-PT) was synthesized and evaluated as potential prodrug form. The successful synthesis of CFZ-PT was identified by spectroscopic analysis. Partition coefficient studies showed that CFZ-PT is more lipophilic than CFZ and the ester was hydrolyzed enzymatically into the parent drug in blood, liver and intestinal homogenates. The pharmacokinetic characteristics of CFZ-PT and CFZ were compared following oral administrations to rabbits. Serum CFZ concentration was determined by HPLC method and the ester compound (prodrug) was not detected in serum following oral administration of CFZ-PT. CFZ-PT did not have antimicrobial activity in vitro against Bacillus subtilis ATCC 6633, whereas CFZ-PT in serum after oral administration to rabbits had antimicrobial activity. From above observations, it was noted that CFZ-PT is rapidly hydrolyzed to CFZ in the body and the bioavailability of CFZ-PT was increased by 3.5-fold than that of CFZ. From these results of this study, it was concluded that CFZ-PT may be a novel prodrug of CFZ which can improve the oral absorption of CFZ.

• Journal of Pharmaceutical Investigation
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• v.38 no.5
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• pp.331-334
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• 2008

The objectives of this study were to formulate oral paclitaxel microemulsion and to compare the bioavailability of paclitaxel in the microemulsion formulation from the commercially available $Taxol^{(R)}$ formulation. Paclitaxel microemulsion was formulated with much less amount of Cremophor $EL^{TM}$ as compared with $Taxol^{(R)}$ to reduce severe adverse reactions produced by Cremophor $EL^{TM}$. The area under the plasma concentration-time curve from 0 hr to 24 hr ($AUC_{0-24}$), maximum plasma concentration ($C_{max}$), and relative bioavailability of palcitaxel microemulsion were increased as compared with $Taxol^{(R)}$ after oral administration. The time required to reach $C_{max}\;(T_{max})$ of palcitaxel microemulsion was significantly shorter than $Taxol^{(R)}$ following oral administration. These results suggest the faster intestinal absorption and the enhanced oral bioavailability of paclitaxel in the microemulsion formulation.

• Applied Microscopy
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• v.3 no.1
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• pp.17-22
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• 1973

The author studied ed the effect of ethionine upon the absorption epithelium of ileum with particular ettention to the endoplasmic reticulum. Five tenth per cent of DL-ethionine was added to the diet of the experimental group rats and they were sacrificed after 1, 2, 3, and 4 weeks. respectively. The ileum were observed by the electron microscope. The results obtained were summarized as follow: The changes were detachment of membrane bound ribosome, dilatation of endoplasmic reticulum, decrease of polysome with reciprocal increase of monosome, and dilatation of Golgi complex. These changes were occured at 2 nd to 3 rd week from start of ethionine feeding and more severe at fouth week. These observation suggested that ethionine induced degenerative changes of the organelles.

• The Journal of Korean Medicine
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• v.24 no.4
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• pp.54-63
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• 2003

Objectives : This study aimed to elucidate the effects of TBE on hyperlipidemia. Methods : We studied the effects of TBE on hyperlipidemia through gene expressions related with lipid metabolism and serum triglyceride as well as total and HDL-cholesterol levels, and perceived histological changes. Results : The present studies demonstrate that TBE can reduce the rise in plasma cholesterol and TG levels induced by a high-cholesterol diet and also reverse pre-established hypercholesterolemia and hypertriglycemia. In the TBE group total cholesterol levels decreased, TG levels decreased, but HDL-cholesterol levels also decreased. In the analysis of absolute and relative liver weight, TBE inhibited the weight gain induced by a high-cholesterol diet. In the histological observations, lipid droplet and apoptotic change in the TBE treated group were less compared with the control group. In the serum biochemical analysis, a difference of serum AST and ALT changes among groups was not shown, but TG and total cholesterol levels were less and HDL level decreased compared with the control group. In the gene expression related with TG and cholesterol metabolism, DGAT decreased slightly but ACAT decreased more as compared with control and Lipidil groups. Conclusion : From this study, we can infer that TBE possesses a hypolipidemic effect by inhibiting the intestinal absorption and storage of exogenous and endogenous cholesterol.

• Asian-Australasian Journal of Animal Sciences
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• v.30 no.1
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• pp.111-118
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• 2017

Objective: Adipose tissue plays a key role in the development of obesity and diabetes. We previously reported that lignosulfonic acid suppresses the rise in blood glucose levels through the inhibition of ${\alpha}$-glucosidase activity and intestinal glucose absorption. The purpose of this study is to examine further biological activities of lignosulfonic acid. Methods: In this study, we examined the effect of lignosulfonic acid on differentiation of 3T3-L1 cells. Results: While lignosulfonic acid inhibited proliferation (mitotic clonal expansion) after induction of differentiation, lignosulfonic acid significantly increased the size of accumulated lipid droplets in the cells. Semi-quantitative reverse transcription polymerase chain reaction analysis showed that lignosulfonic acid increased the expression of the adipogenic transcription factor, peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$), leading to increased glucose transporter 4 (Glut-4) expression and 2-deoxyglucose uptake in differentiated 3T3-L1 cells. Additionally, feeding lignosulfonic acid to diabetic KK-Ay mice suppressed increase of blood glucose level. Conclusion: Lignosulfonic acid may be useful as a functional anti-diabetic component of food.

• Journal of Pharmaceutical Investigation
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• v.36 no.3
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• pp.157-160
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• 2006

This study investigated the effect of clarithromycin on the pharmacokinetics of ambroxol in rats. The pharmacokinetic parameters of ambroxol in rats were determined after the oral administration of ambroxol (12 mg/kg) in the presence or absence of clarithromycin (5 or 10 mg/kg). Compared with the control (given ambroxol alone), coadministration of clarithromycin significantly (p<0.05 at 5 mg/kg; p<0.01 at 10 mg/kg) increased the area under the plasma concentration-time curve (AUC), peak plasma concentrations $(C_{max})$ and absorption rate constant $(K_a)$ of ambroxol. Clarithromycin increased the AUC of ambroxol in a dose dependent manner within the dose range of 5 to 10 mg/kg. The absolute bioavailability (AB%) of ambroxol in the presence of clarithromycin was significantly higher than that of the control (p<0.05 at 5 mg/kg; p<0.01 at 10 mg/kg), and the relative bioavailability (RB%) of ambroxol with clarithromycin was increased by 1.32-to 1.71-fold. However, there were no significant changes in time to reach peak concentration $(T_{max})$ and terminal half-life $(T_{1/2})$ of ambroxol in the presence of clarithromycin. Coadministration of clarithromycin enhanced the bioavailability of ambroxol, which may be due to the inhibition of intestinal and hepatic metabolism of ambroxol by CYP 3A4. Further studies for the potential drug interaction are necessary since ambroxol is often administrated concomitantly with clarithromycin in humans.

• Clinical and Experimental Pediatrics
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• v.46 no.3
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• pp.308-311
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• 2003

Congenital chloride diarrhea is a serious autosomal recessive disease, and defect of intestinal electrolyte absorption that involves, specifically, $Cl^-/{HCO_3}^-$ exchange in the distal part of the ileum and colon. The clinical feature is dominated by profuse, watery diarrhea containing high concentrations of chloride(>90 mmol/L) and sodium. The chloride loss results in severe dehydration with a hypochloremic alkalosis. The molecular pathology involves an epithelial $Cl^-/{HCO_3}^-$ exchanger protein. Mucosal ion transport is affected to differing degrees and the severity of the disease may thus vary. Recently, a gene defect on chromosome 7 has been identified. However, there was a deficit in replacement of fluid and electrolyte, abdominal distension remained and the character of stools was watery. We report a case of congenital chloride diarrhea in a premature female who presented with watery diarrhea containing high concentrations of chloride and abdominal distension.

• Journal of Nutrition and Health
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• v.28 no.2
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• pp.107-114
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• 1995

These works were designed to examine the effects of dietary fiber sources and levels on lipid metabolism in rats fed high lard diet. Rats were divided into three($\alpha$-cellulose, polydextrose, carrageenan) groups and were fed with containing 6% fiber diet. Serum, liver and fecal lipid contents were examined after four weeks of dieting. Also, in order to investigate whether hypocholesterolemic effect of dietary fiber at 4 weeks is continued at 8 weeks, rats were fed with diets containing same sources with different levels of each dietary fiber and were sacrificed after eight weeks of dieting. Serum cholesterol in rats fed carrageenan diet and polydextrose diet were reduced compared with $\alpha$-cellulose-fed group at both four and eight weeks dieting. Liver cholesterol in both polydextrose-fed and carrageenan-fed group were lower than $\alpha$-cellulose-fed group. Fecal total group were increased compared with $\alpha$-cellulose-fed group. On the other hand, there was no significant difference between polydextrose-fed and carrageenan-fed group. On the basis of the results, it was suggested that the hypocholesterolemic effect of soluble fiber used in this study (polydextrose, carageenan) on rats was due to the inhibition of cholesterol absorption on the intestinal lumen and acceleration of cholesterol catabolism in the liver and enhancement of bile acids excretion. On the other hand, insoluble fiber($\alpha$-cellulose) showed no hypo-cholesterolemic effect.

• Mass Spectrometry Letters
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• v.9 no.2
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• pp.61-65
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• 2018

KPLA-012, a benzopyranyl 1,2,3-triazole compound, is considered a potent $HIF-1{\alpha}$ inhibitor based on the chemical library screening, and is known to exhibit anti-angiogenetic and anti-tumor progressive effects. The aim of this study was to investigate the pharmacokinetic properties of KPLA-012 in ICR mice and to investigate in vitro characteristics including the intestinal absorption, distribution, metabolism, and excretion of KPLA-012. The oral bioavailability of KPLA-012 was 33.3% in mice. The pharmacokinetics of KPLA-012 changed in a metabolism-dependent manner, which was evident by the low recovery of parent KPLA-012 from urine and feces and metabolic instability in the liver microsomes. However, KPLA-012 exhibited moderate permeability in Caco-2 cells ($3.1{\times}10^{-6}cm/s$) and the metabolic stability increased in humans compared to that in mice (% remaining after 1 h; 47.4% in humans vs 14.8% in mice). Overall, the results suggest that KPLA-012 might have more effective pharmacokinetic properties in humans than in mice although further studies on its metabolism are necessary.