• Biomolecules & Therapeutics
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• v.18 no.1
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• pp.83-91
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• 2010

Bear bile has been used as a therapeutic for cerebral and coronary thrombosis, convulsion, hepatitis, jaundice, and abscess in traditional oriental medicine. In recent decades, the effects of bile acids on cancer, cholestasis, and liver injury have been investigated in many studies. In this study, we investigated the anti-inflammatory effects of whole bear bile (WBB) and its two major components, chenodeoxycholic acid (CDCA) and ursodeoxycholic acid (UDCA), on rectal inflammation in rats. Bile acids in WBB were quantitatively analyzed by HPLC. Rectal inflammation was induced in male Sprague-Dawley rats by insertion of croton oil-saturated cotton tips. WBB, UDCA or CDCA solution was orally administered to rats one hour after induction of rectal inflammation. Rats were sacrificed 4 or 24 hours after induction of rectal inflammation. The evaluation included measurement of weight and thickness of rectum and histopathologic examination of rectal tissue. Furthermore, we examined the inhibitory effect of WBB, UDCA or CDCA against NO production in LPS-stimulated RAW 264.7 cells. The contents of UDCA and CDCA in WBB were $39.26{\mu}g/mg$ and $47.11{\mu}g/mg$, respectively. WBB treatment significantly reduced the weight and thickness of rectum compared with UDCA or CDCA treatment. The inhibition of NO production by WBB, UDCA and CDCA in LPS-stimulated RAW 264.7 cells was much higher than that by the control. And, WBB treatment suppressed the induction of NO synthase in rectum homogenates. These results suggest that the anti-inflammatory effect of WBB is related to the suppression of NO synthase induction and the inhibition of NO production by UDCA, CDCA and other bile acids of WBB.

• Journal of the Korean Magnetic Resonance Society
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• v.20 no.2
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• pp.41-45
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• 2016

Chemical investigation of a marine-derived fungus, Penicillium sp. 108YD020, resulted in the discovery of six bile acid derivatives, glycocholic acid (1), glycocholic acid methyl ester (2), cholic acid (3), glycochenodeoxycholic acid (4), glycodeoxycholic acid methyl ester (5), and cholic acid methyl ester (6). The structures of six bile acid derivatives 1-6 were determined by the detailed analysis of 1D, 2D NMR and LC-MS data, along with chemical methods and literature data analysis.

• Journal of Microbiology and Biotechnology
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• v.17 no.4
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• pp.655-662
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• 2007

This study examined the effects of Lactobacillus acidophilus ATCC 43121 (LAB) on cholesterol metabolism in hypercholesterolemia-induced rats. Four treatment groups of rats (n=9) were fed experimental diets: normal diet, normal $diet+LAB(2{\times}10^6\;CFU/day)$, hypercholesterol diet (0.5% cholesterol, w/w), and hypercholesterol diet+LAB. Body weight, feed intake, and feed efficiency did not differ among the four groups. Supplementation with LAB reduced total serum cholesterol (25%) and VLDL+IDL+LDL cholesterol (42%) in hypercholesterol diet groups, although hepatic tissue cholesterol and lipid contents were not changed. In the normal diet group, cholesterol synthesis (HMG-CoA reductase expression), absorption (LDL receptor expression), and excretion via bile acids (cholesterol $7{\alpha}-hydroxylase$ expression) were increased by supplementation with LAB, and increased cholesterol absorption and decreased excretion were found in the hypercholesterol diet group. Total fecal acid sterols excretion was increased by supplementation with LAB. With proportional changes in both normal and hypercholesterol diet groups, primary bile acids (cholic and chenodeoxycholic acids) were reduced, and secondary bile acids (deoxycholic and lithocholic acids) were increased. Fecal neutral sterol excretion was not changed by LAB. In this experiment, the increase in insoluble bile acid (lithocholic acid) reduced blood cholesterol level in rats fed hypercholesterol diets supplemented with LAB. Thus, in the rat, L. acidophilus ATCC 43121 is more likely to affect deconjugation and dehydroxylation during cholesterol metabolism than the assimilation of cholesterol into cell membranes.

• YAKHAK HOEJI
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• v.42 no.6
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• pp.572-575
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• 1998

Chitosan has been known to have hypocholesterolemic and hypolipidemic effects in animal studies. Chitosan also absorbs bile acids in vitro and in vivo, which might result in the hypocholesterolemic action. Trialkyl chitosan derivatives were prepared and tested for bile acid absorption activity in vitro. The derivatives showed enhanced absorption capacities which were comparable to cholestyramine.

• Korean Journal of Pharmacognosy
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• v.27 no.3
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• pp.246-253
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• 1996

Coptis rhizoma was extracted with methanol or hot water. Methanol extracts had higher berberine content than water extracts, whereas the contents of Ca, Mg, Zn and K were higher in the water extracts. Rats were fed on the purified diets rich in 0.12% cholesterol only or supplemented with 0.5% of each extracts for four weeks. The concentration of total serum cholesterol was significantly lower in the rats given the extracts, irrespective of the extractants. Although the concentration of serum HDL-cholesterol was comparable among the groups, the ratio of HDL-/total-cholesterol was higher in rats given the extracts. The concentration of serum free fatty acids and ketone body were significantly elevated in rats given the extracts. On the other hand, the extracts supplements significantly decreased the contents of liver cholesterol and triacylglycerol. The amount of fecal bile acids was markedly higher in rats given the extracts, especially in those given water extracts. The results show an effective hypocholesterolemic action of Coptis rhizoma and it seems that the lower concentration of serum and liver cholesterol is resulted from the increased fecal bile acids in rats.

• Journal of Nutrition and Health
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• v.32 no.6
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• pp.637-643
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• 1999

The effects of yam(Dioscorea) on lowering cholesterol level and its mechanism were investigated. The concentrations of plasma and liver lipids, and the excretions of fecal neutral sterol and bile acid were measured in male Sprague-Dawley rats. Five Groups of 8 rats were fed hypercholesterolemic diet(1% cholesterol, 10% lard ; control), hypercholesterolemic diet plus 15% or 30% dried yam powder prepared by either hot-air(15HY, 30HY) or freeze dry(15FY, 30FY) for 4wk. Plasma total lipid, total cholesterol and cholesterol level was also significantly lower(28%, p<0.05), buy HMG-CoA reductase activity was higher in 30FY(230%, p<0.05) than in control. Although no significant differences in fecal neutral sterols were observed among groups, the yam-fed rats apparently had less bacterial degradation of cholesterol as indicated by a significantly greater of fecal cholesterol to coprostanol than in controls. Total fecal bile acids were significantly greater in rats fed yam(15HY : 5 folds, 15FY ; 12,30HY ; 12, 20FY ; 22) than in controls. The ratio of secondary to primary bile acids was almost 8 times lower in 30FY than in control. These data indicate that yam lowers cholesterol both in plasma and in liver through increasing fecal bile acid excretion as well as HMG-CoA reductase activity. Freeze-dried yam, which possesses viscosity, was more effective in cholesterol-lowering action than hot-air dried one.

• Journal of the Korean Society of Food Science and Nutrition
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• v.24 no.6
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• pp.978-983
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• 1995

The effect of sulfur-containing amino acids on lipid metabolism was studied in rats fed casein as a protein source. Plasma cholesterol, HDL-cholesterol and atherosclerotic index decreased in the cysteine group compared to the methionine group. Plasma triglyceride and phospholipid level were not affected by the supplementation of the sulfur-containing amino acids. The levels of cholesterol and triglyceride in liver decreased by both methionine and cysteine. Cysteine increased the fecal excretion of coprostanol, total neutral steroid and bile acid. The results suggest that plasma cholesterol level is affected by dietary ratio of cysteine/methionine and that the hypocholesterolemic effects of cysteine is, at least in part, through reducing cholesterol absorption from small intestine and through enhancing fecal excretion of bile acids.

• YAKHAK HOEJI
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• v.42 no.1
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• pp.82-88
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• 1998

The effect of hepatoprotective agents and bile acids on tumor necrosis factor-alpha, (TNF-${\alpha}$) production in murine and human macrophage cell line (RAW264.7 and U937) was inve stigated. The hepatoprotective agents including silymarin and its major component, silybin, significantly inhibited TNF-alpha production in a concentration dependent manner ($IC_50$ of silybin=67.7${\mu}g$/ml (140.3${\mu}g$M)). In differentiated U937 cells, especially, silybin showed more effective inbitory activity ($IC_50$=35.1${\mu}g$g/ml (72.7${\mu}g$M)). These results suggest that silymarin and silybin may inhibit TNF-alpha production in the process of hepatic diseases in human. However, biphenyldimethyl dicarboxylate (DDB) was not effective. In the case of bile acids, chenodeoxycholic acid (CDCA) showed a concentration dependent inhibitory effect on TNF-alpha production ($IC_50$ of CDCA= 71.5${\mu}g$g/ml (182.1${\mu}g$M)). In contrast, glycine or taurine conjugated form (G-CDCA or T-CDCA) restored to the control level or significantly increased TNF-${\alpha}$ production. And also ursodeoxycholic acid (UDCA) and its conjugated forms (G-UDCA and T-UDCA) showed a variety of patterns on TNF-${\alpha}$ production by changes of functional groups and concentration. These results also indicate that bile acids may regulate TNF-${\alpha}$ production in normal hepatic function or disease conditions.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.245.2-246
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• 2002

We studied on the antiproliferative effects of bile acids and their derivatives on HepG2 human hepatocellular carcinoma cells. Ursodeoxycholic acid (UDCA) and its synthetic derivative HS-1030. and chenodeoxycholic acid (CDCA) and its synthetic derivatives. HS-1199 and HS\ulcorner200, were used. We focused on the regulation of cell cycle and induction of apoptosis by these bile acid derivatives. (omitted)

• Archives of Pharmacal Research
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• v.9 no.1
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• pp.49-54
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• 1986

Effect of sodium taurodeoxycholate (TDC) infused intravenously on the pharmacokinetics of methylene blue (MB) was studied in the rat to investigate the role of ion-pair complexation in the body on drug elimination and disposition. Distribution volume (Vd) of MB was increased significantly (p< 0.05) by TDC infusion. Considering together with the fact that apparent partition coefficient (APC) of MB between phosphate buffer (pH 7.4) and n-octanol was increased markedly by TDC, the increase in Vd seemed to be the result of decreased polarity of MB by ion-pair formation with TDC. But total body clearance (CLt) and biliary excretion clearance (CLbil) of MB were not increased significantly by TDC.