• Archives of Pharmacal Research
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• v.18 no.5
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• pp.320-324
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• 1995

Pretreatment of Glycyrrhizae Radix(GR) to male Sprague-Dawley rats was demonstrated to increase excretion of acetaminophen-glucuronide ocnjugate when bile nad urine were assayed after administration of acetaminophen. In order to study the effect of GR on the glucuronidation in rats, we examined enzymatic activities of hepatic UDP-glucuronosyl-transferases (UDP-GT1 and UDP-GT2) and intracellular concentrations of hepatic UDP-glucuronic acid (UDP-GA), upon the administration of GR (1 g/kg body weight, p.o.) or glycyrrhizin (23 mg/kg body weight, p.o.) a major component of GR, for 6 days. GR and glycyrrhizin caused increases in specific activities of UDP-GT2 111% and 96% respectively. Specific activity of UDP-GT1 was increased 25% by GR treatment whereas it was not significantly increased by glycyrrhizin. Concentrations of UDP-GA were increased 257% by GR and 484% by glycyrrhizin. These data indicate that GR activated glucuronidation and thus suggest the possibility that GR may influence detoxification of xenobiotics in rat liver.

• Bulletin of the Korean Chemical Society
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• v.35 no.1
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• pp.87-92
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• 2014

The work is directed toward the synthesis of a series of DO3A conjugates of tranexamates (1c-e) and their Gd complexes (2c-e) for use as a liver-specific MRI CA. All these complexes show thermodynamic and kinetic stabilities comparable to those of structurally related clinical agents such as Dotarem$^{(R)}$. Their $R_1$ relaxivities also compare well with those of commercial agent, ranging 3.68-4.84 $mM^{-1}s^{-1}$. In vivo MR images of mice with 2a-e reveal that only 2a exhibits liver-specificity. Although 2b and 2c show strong enhancement in liver, yet no bile-excretion is observed to be termed as a liver-specific agent. The rest behaves much like ordinary ECF CAs like Dotarem$^{(R)}$. The new series possess no toxicity to be employed in vivo.

• Advances in pediatric surgery
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• v.6 no.1
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• pp.19-26
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• 2000

This paper reports our 9-year experience treating 34 infants with biliary atresia utilizing a new non-invasive diagnostic method, ultrasonographic "triangular cord"(TC) sign. The TC sign is present when there is visualization of a triangular or a band-like echogenicity just cranial to the portal vein. The ultrasonographic TC sign appears to be a simple, non-invasive, time-saving and useful tool in the diagnosis of biliary atresia. Sensitivity is 84 %. Active bile excretion was restored in 90 % of the patients who were treated between 31-60days, 78 % of those between 61-90 days, and 33 % of those being 91days or older. The incidence of postoperative cholangitis was 36 %. Construction of an antireflux valve in the Roux-en-Y loop did not affect the incidence of postoperative cholangitis(p=0.18). Among 34 infants with biliary atresia, 23(68 %) are alive for 2-102 months after operation, and 12 are alive for more than 5 years. Five-year estimate survival by Kaplan-Meier method was 66 %.

• Archives of Pharmacal Research
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• v.9 no.2
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• pp.111-114
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• 1986

Bretylium tosylate is a quaternary ammonium compound used for the treatment of ventricular fibrilation in humans. It is advantageous to other cationic compound in the study of biliary excretion in that negligible amount is bound to plasma protein and metabolite is not likely is to be formed. Some researchers reported that the formation of ion-pair complex caused to increase the lipothilicity of cationic compound. The partition of bretylium between water and organic phase was increased with the addition of sodium taurodeoxycholate. Also sensitive gas chromatographical assay procedure using flame ionization detector was studied. This procedure can detect as low as 0.1 mg/ml using 0.1 ml biological sample, but contamination by previous injection is the major problem of this method.

• Biomolecules & Therapeutics
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• v.2 no.2
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• pp.173-184
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• 1994

The general and some pharmacological actions of DWP 305 were investigated in animals and the following results were obtained. In central nervous system, DWP 305 had no effects on the pentobarbital induced anaesthesia, locomotor activity, rotarod test, traction test, analgesic action in mice and body temperature in rat. DWP 305 showed no depressive action on convulsion induced by strychnine, electronic shock and pentylenetetrazole. From these results, DWP 305 was considered to have no pharmacological effect on the central nervous system. Furthermore, DWP 305 had no influences on the normal blood pressure and heart rate. In the isolated ileum of guinea pig, DWP 305 inhibited contractive effects against the acetylcholine (10$^{-6}$ g/mι), histamine (10$^{-6}$ g/mι), 5-hydroxytryptamine (10$^{-6}$ g/mι) and BaCl$_2$(10$^{-4}$ g/mι) at a concentration of 2.15$\times$10$^{-4}$ g/ml in bath. In the isolated trachea and vats deference, DWP 305 showed no effect on the contractions produced by histamine and norepinephrine, respectively. DWP 305 showed inhibitory effect on the contractions produced by acetylcholine and oxytocin at a concentration of 2.15$\times$10$^{-4}$ g/ml on the isolated nonpregnant rat uterus. DWP 305 had no effect on the isolated right atrium of guinea pig, bile excretion, urine volume, pH, gastrointestinal motility, gastric secretion and blood aggregation.

• Pediatric Gastroenterology, Hepatology & Nutrition
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• v.5 no.1
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• pp.101-107
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• 2002

We experienced two cases of Rotor syndrome in brothers who were a 13 year-old boy and an 11 year-old boy, respectively. They presented with icteric scleras for a few months. Their common laboratory characteristics were as follows: Direct bilirubin was more increased than indirect bilirubin, but aminotransferases were normal. Plasma indocyanine green (ICG) test revealed hepatic excretory defect: plasma ICG concentrations 15 minutes after intravenous injection were 80.45% and 78.28%, respectively. 99mTc-DISIDA Hepatobiliary scan showed that severely decreased hepatic extraction with mild cardiac blood pool, markedly delayed biliary excretion in both intra- & extra- hepatic bile ducts, delayed visualization of gall bladder, and markedly delayed intestinal biliary passage. Needle liver biopsy showed normal hepatic histology without pigmentation.

• Journal of the Korean Society of Food Science and Nutrition
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• v.37 no.10
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• pp.1258-1263
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• 2008

The current study examined the effects of radish leaves powder on the excretion of fecal triglyceride, and sterol and hepatic UDP-glucuronyl transferase (UDPGT) activity in rats fed hypercholesterolemic diet. Male Sprague-Dawley rats weighing 100$\pm$10 g were randomly assigned to normal control group (N group), normal diet with 5% radish leaves powder supplemented group (NR) and hypercholesterolemic groups, which were sub-divided into radish leaves powder free diet group (HC) and 2.5% (HRL), 5% (HRM), and 10% (HRH) radish leaves powder supplemented groups. The experimental diets were fed ad libitum for 4 weeks. Fecal weights and water contents were significantly increased in all radish leaves powder supplemented groups (NR, HRL, HRM, and HRH) than that of N and HC groups. Fecal total lipid contents including fecal neutral and acidic sterols in radish leaves powder supplemented groups were higher than those of the HC group, and especially that of HRH group was the highest among all experimental groups. Hepatic UDPGT activity of HRH group was 38% higher than that of HC group. Excretions of fecal bile acid were increased 2.3 and 2.7 folds in HRM and HRH groups compared with that of HC group. And neutral sterol, coprostanol, and coprostanone contents of them were higher in radish leaves supplemented groups than in HC group. These results suggest that radish leaves may act as potential substitute for a dietary fiber capable of improving a gastrointestinal function and lipid metabolism.

• Food Science of Animal Resources
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• v.31 no.2
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• pp.250-256
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• 2011

This study was conducted to evaluate the effect of whole egg supplementation on the blood lipid profiles and cholesterol levels of C57BL/6 mice. Sixty-six mice were divided into two groups: normal-diet supplemented and high-cholesterol diet supplemented. Lyophilized whole egg powder was mixed with the two diets at 2 and 10%: normal diet only, normal diet with 2 and 10% whole egg powder, high cholesterol diet only, high cholesterol diet with 2 and 10% whole egg powder. The mixed diets were fed for 5 wk and feeding condition (body weight change, feed intake, and feed efficiency ratio (FER)), blood lipid profiles (total cholesterol (TC), triglyceride (TG), high density lipoprotein-cholesterol (HDL-C), low density lipoprotein cholesterol, hepatic and fecal lipids (TG, TC)), and fecal bile acids were determined. No significant differences were found in body weight gain or FER after whole egg supplementation in both the normal and high-cholesterol diet fed groups. In the normal-diet fed mice, HDL-C increased significantly in the 2 and 10% whole-egg powder groups. In the high-cholesterol diet fed mice, administering 10% egg powder increased the atherogenic index compared to the control. Furthermore, administration of whole egg powder increased fecal bile acids dose dependently (p<0.05). These results indicate that administering 2% hen whole egg powder did not affect blood lipid profiles and was more beneficial for health by increasing HDL-C and aiding in the excretion of cholesterol by fecal bile acids than those in the control.

• Journal of the Korean Society of Food Science and Nutrition
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• v.34 no.5
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• pp.573-580
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• 2005

Cholesterol $7\alpha-hydroxylase$ (CYP7A1) is the rate-limiting enzyme in the conversion of cholesterol to bile acids and plays a central role in regulating cholesterol homeostasis. We previously showed that a fermentable $\beta-glucan$ ingestion decreased plasma cholesterol levels due to fecal bile acid excretion elevation involved inincrease of cholesterol $7\alpha-hydroxylase$ mRNA expression and activity. It is proposed that short chain fatty acids (SCFA) produced by cecal and colonic fermentation of soluble fiber are associated with cholesterol-lowering effect of fiber. In the present study, we investigated whether CYP7A1 expression is up-regulated by short chain fatty acids or by hormones in cultured human hepatoma (HepG2) cells. Confluent HepG2 cell were incubated with acetate, propionate, or butyrate at 1 mM concentration for 24 hrs. Acetate as well as propionate increased to 1.8-fold expression of CYP7A1 mRNA than the control. Butyrate also increased 1.5-fold expression of CYP7A1 mRNA. Our data show for the first time that SCFA increase expression of CYP7A1 mRNA. Adding insulin, dexamethasone and triiodothyronine $(1\;{\mu}M)$ to HepG2 cell increased the expression of CYP7A1 mRNA to $150\%,\;173\%,\;141\%$, respectively. These results suggest that SCFA produced by cecal fermentation stimulate enteric nervous system, in which secreted some neuropeptides may be responsible for change in cholesterol and bile acid metabolism. These findings suggest that SCFA are involved in lowering plasma cholesterol levels due to the up-regulation of CYP7A1 and bile acid synthesis.

• Journal of Pharmaceutical Investigation
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• v.36 no.6
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• pp.377-383
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• 2006

The purpose of the present study was to examine the pharmacokinetic characteristics of arsenic hexaoxide($As_4O_6$), a novel anticancer compound, after i.v. bolus and oral administration in rats. We developed an ICP-Mass based method to analyze arsenic hexaoxide levels in plasma, bile, urine, feces, and tissue and validated the method. Arsenic hexaoxide rapidly disappeared from the plasma by 10 min($\alpha$ phase) after i.v. administration, which was followed by the late disappearance in the $\beta$ phase. The mean plasma half-lives($t_{1/2}$) of arsenic hexaoxide at the a and $\beta$ phase when administered at a dose of 5 mg/kg were 1.57 and 29.8 min, respectively. The maximum plasma concentration($C_{max}$) was 230 ng/mL, after oral administration of arsenic hexaoxide at a dose of 50 mg/kg. The bioavailability, which was calculated from the dose-adjusted ratio, of the oral administered arsenic hexaoxide was 1.61%. Of the various tissues tested, arsenic hexaoxide was mainly distributed in the spleen, lung, liver and kidney after oral administration. Arsenic hexaoxide levels in the spleen or lung at 24 hr after oral administration were higher than those of maximum plasma concentration($C_{max}$). The cumulative amounts of arsenic hexaoxide found in the urine by 48 hr after the administration of 50 mg/kg were 5-fold higher than those in the bile. However, the cumulative amounts in the feces were 10-fold higher compared with those of urine, suggesting that arsenic hexaoxide is mostly excreted in the feces. In conclusion, our observations indicated that arsenic hexaoxide was poorly absorbed from the gastro-intestinal tract to the blood circulation and transferred to tissues such as the spleen and lung at 24 hr after oral administration. Moreover, the majority of arsenic hexaoxide appears to be excreted in the feces by 48 hr after oral administration.