• 생약학회지
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• 제15권3호
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• pp.139-146
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• 1984

High performance liquid chromatographic separation is described for the analysis of bile acids after hydrolysis in seven commercial crude bile drugs and ox and pig galls. They are simultaneously separated with HPLC mobile phase of acetonitrile/0.5% ammonium carbonate (pH 6.7) (25.5 : 74.5) at a flow rate $(1.0{\rightarrow}1.5ml/min.)$ and differential refractometer. The linearity of calibration curve and recovery test are good by using the method. The analysis of major bile acids in seven commercial crude bile drugs using the described method is presented. Sample no. 1 of them is similar to separation pattern of ox gall. Sample no. 6 of them is supposed to be genuine bear gall on the basis of identification of ursodeoxycholic acid. Sample $no.\;2{\sim}5$ and 7 of them are supposed to be pig gall on the basis of identification of hyodeoxycholic acid which is a characteristic component of pig gall.

• Biomolecules & Therapeutics
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• 제4권2호
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• pp.162-166
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• 1996

This study was done to investigate whether cholic acid derivatives have anti-stress activity and what is a cause of this anti-stress effect. Seven cholic acid derivatives (cholic acid, taurocholic acid, ursodeoxycholic acid, tauroursodeoxychoic acid, chenodeoxy cholic acid, dehydrocholic acid, hyodeoxycholic acid) were used, silymarin and valproic acid were used as positive controls. Stress was induced by restraint immobilization technique plus water immersion (24hrs) and adrenal weight, spleen weight, adrenal ascorbic acid, serum cholesterol, lactate dehydrogenase (LDH), alkaline phosphatase (ALP), adrenal cholesterol, glucose and corticosterone levels were measured as stress indicators. Most cholic acid derivatives markedly decreased the adrenal weight, and TUDCA and DHCA increased the spleen weight. The restraint stress induced increments in serum LDH, ALP and cholesterol were attenuated by most cholic acid derivatives. Cholic acid, taurocholic acid and tauroursodeoxycholic acid only increased the content of adrenal ascorbate. While valproic acid showed an inhibitory effect against stress, silymarin did not. Our findings suggest that most cholic acid derivatives have anti-stress effect and that their anti-stress effect is, in part, related to choleretic activity.

• Archives of Pharmacal Research
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• 제20권5호
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• pp.454-458
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• 1997

Two human liver UDP-glucuronosyltransferase cDNA clones, HLUG25 and UDPGTh2 were previously shown to encode isozymes active in the glucuronidation of hyodeoxycholic acid (HDCA) and certain estrogen derivatives (e.g., estriol and 3,4-catechol estrogens), respectively. in this study we have found that the UDPGTh2-encoded isoform (UDPGTh2) and HLUG25-encoded isoform (UDPGThl) have parallel aglycone specificities. When expressed in COS 1 cells, each isoform metabolized three types of dihydroxy- or trihydroxy-substituted ring structures, including the 3,4-catechol estrogen (4-hydroxyestrone), estriol, 17-epiestriol, and HDCA, but the UDPGTh2 isozyme was 100-fold more efficient than UDPGTh1. UDPGTh1 and UDPGTh2 were 86% identical overall (76 differences out of 528 amino acids), including 55 differences in the first 300 amino acids of the amino terminus, a domain which conferred the substrate specificity. The data indicated that a high level of conservation in the amino terminus was not required for the preservation of substrate selectivity. Analysis of glucuronidation activity encoded by UDPGTh1/UDPGTh2 chimeric cDNA constructed at their common restriction sites, Sac I (codon 297), Nco I (codon 385), and Hha I (codon 469), showed that nine amino acids between residues 385 and 469 were important for catalytic efficiency, suggesting that this region represented a domain which was critical for the catalysis but distinct from that responsible for aglycone-selection. These data indicate that UDPGTh2 is a primary isoform responsible for the detoxification of the bile salt intermediate as well as the active estrogen intermediates.