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Journal articles on the topic 'Ursodeoxycholic Acid Conjugates'

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Published: 7 June 2025

Last updated: 2 August 2025

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1

Maeda, Yorinobu, and Teruo Murakami. "Diagnosis by Microbial Culture, Breath Tests and Urinary Excretion Tests, and Treatments of Small Intestinal Bacterial Overgrowth." Antibiotics 12, no. 2 (2023): 263. http://dx.doi.org/10.3390/antibiotics12020263.

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Small intestinal bacterial overgrowth (SIBO) is characterized as the increase in the number and/or alteration in the type of bacteria in the upper gastrointestinal tract and accompanies various bowel symptoms such as abdominal pain, bloating, gases, diarrhea, and so on. Clinically, SIBO is diagnosed by microbial culture in duodenum/jejunum fluid aspirates and/or the breath tests (BT) of hydrogen/methane gases after ingestion of carbohydrates such as glucose. The cultural analysis of aspirates is regarded as the golden standard for the diagnosis of SIBO; however, this is invasive and is not wit

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2

Wang, Rui, Jiaquan Wu, David Kin Jin та ін. "Structure of NADP+-bound 7β-hydroxysteroid dehydrogenase reveals two cofactor-binding modes". Acta Crystallographica Section F Structural Biology Communications 73, № 5 (2017): 246–52. http://dx.doi.org/10.1107/s2053230x17004460.

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In mammals, bile acids/salts and their glycine and taurine conjugates are effectively recycled through enterohepatic circulation. 7β-Hydroxysteroid dehydrogenases (7β-HSDHs; EC 1.1.1.201), including that from the intestinal microbeCollinsella aerofaciens, catalyse the NADPH-dependent reversible oxidation of secondary bile-acid products to avoid potential toxicity. Here, the first structure of NADP+bound to dimeric 7β-HSDH is presented. In one active site, NADP+adopts a conventional binding mode similar to that displayed in related enzyme structures. However, in the other active site a unique b

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3

Marchesi, Elena, Rita Cortesi, Lorenzo Preti, et al. "Antisense Oligonucleotides Conjugated with Lipophilic Compounds: Synthesis and In Vitro Evaluation of Exon Skipping in Duchenne Muscular Dystrophy." International Journal of Molecular Sciences 23, no. 8 (2022): 4270. http://dx.doi.org/10.3390/ijms23084270.

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Our groups previously reported that conjugation at 3′-end with ursodeoxycholic acid (UDCA) significantly enhanced in vitro exon skipping properties of ASO 51 oligonucleotide targeting the human DMD exon 51. In this study, we designed a series of lipophilic conjugates of ASO 51, to explore the influence of the lipophilic moiety on exon skipping efficiency. To this end, three bile acids and two fatty acids have been derivatized and/or modified and conjugated to ASO 51 by automatized solid phase synthesis. We measured the melting temperature (Tm) of lipophilic conjugates to evaluate their ability

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4

Bouscarel, B., S. Ceryak, T. W. Gettys, H. Fromm, and F. Noonan. "Alteration of cAMP-mediated hormonal responsiveness by bile acids in cells of nonhepatic origin." American Journal of Physiology-Gastrointestinal and Liver Physiology 268, no. 6 (1995): G908—G916. http://dx.doi.org/10.1152/ajpgi.1995.268.6.g908.

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The present study was undertaken to determine whether bile acids could inhibit hormone-induced adenosine 3',5'-cyclic monophosphate (cAMP) production in cells of nonhepatic origin, as previously reported in the liver [Bouscarel et al., Am. J. Physiol. 268 (Gastrointest. Liver Physiol. 31): G300-G310, 1995]. The bile acids, ursodeoxycholic acid (UDCA), chenodeoxycholic acid, and deoxycholic acid inhibited prostaglandin E1 (PGE1)- and isoproterenol-induced cAMP production by 40-60% in human skin fibroblasts and human umbilical vein endothelial cells, respectively, to a similar extent as that obs

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5

Maevskay, M. V. "Ursodeoxycholic acid: unique properties and clinical applications." Meditsinskiy sovet = Medical Council, no. 8 (May 25, 2023): 96–105. http://dx.doi.org/10.21518/ms2023-136.

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Ursodeoxycholic acid (UDCA) is a natural hydrophilic bile acid, which is present in humans as a small fraction of the total amount of bile acids (5%). Its unique properties underlie its use in a number of liver diseases as a first-line therapy. The ability of UDCA to reduce the secretion of cholesterol into bile, form mixed micelles (liquid crystals) with cholesterol molecules and interact with multifunctional nuclear receptors, are actively used in the treatment and prevention of cholelithiasis. UDCA has the ability to stimulate hepatobiliary secretion, promotes the secretion of bicarbonate b

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6

Odermatt, Alex, Thierry Da Cunha, Carlos A. Penno та ін. "Hepatic reduction of the secondary bile acid 7-oxolithocholic acid is mediated by 11β-hydroxysteroid dehydrogenase 1". Biochemical Journal 436, № 3 (2011): 621–29. http://dx.doi.org/10.1042/bj20110022.

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The oxidized bile acid 7-oxoLCA (7-oxolithocholic acid), formed primarily by gut micro-organisms, is reduced in human liver to CDCA (chenodeoxycholic acid) and, to a lesser extent, UDCA (ursodeoxycholic acid). The enzyme(s) responsible remained unknown. Using human liver microsomes, we observed enhanced 7-oxoLCA reduction in the presence of detergent. The reaction was dependent on NADPH and stimulated by glucose 6-phosphate, suggesting localization of the enzyme in the ER (endoplasmic reticulum) and dependence on NADPH-generating H6PDH (hexose-6-phosphate dehydrogenase). Using recombinant huma

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7

Bouscarel, B., H. Fromm, S. Ceryak, and M. M. Cassidy. "Ursodeoxycholic acid increases low-density lipoprotein binding, uptake and degradation in isolated hamster hepatocytes." Biochemical Journal 280, no. 3 (1991): 589–98. http://dx.doi.org/10.1042/bj2800589.

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Ursodeoxycholic acid (UDCA), in contrast to both chenodeoxycholic acid (CDCA), its 7 alpha-epimer, and lithocholic acid, enhanced receptor-dependent low-density lipoprotein (LDL) uptake and degradation in isolated hamster hepatocytes. The increase in cell-associated LDL was time- and concentration-dependent, with a maximum effect observed at approx. 60 min with 1 mM-UDCA. This increase was not associated with a detergent effect of UDCA, as no significant modifications were observed either in the cellular release of lactate dehydrogenase or in Trypan Blue exclusion. The effect of UDCA was not d

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Iwaki, Tomomichi, Norio Miyazawa, Hiromi Hasegawa, Hirao Sakakuta, Norio Hirabayashi, and Hiroshi Kasai. "The choleretic effect of N-acetylglucosamine conjugates of Ursodeoxycholic acid (UDCA) in bile fistura rats." Japanese Journal of Pharmacology 73 (1997): 219. http://dx.doi.org/10.1016/s0021-5198(19)45378-x.

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9

Hata, Soichiro, Pijun Wang, Nicole Eftychiou, et al. "Substrate specificities of rat oatp1 and ntcp: implications for hepatic organic anion uptake." American Journal of Physiology-Gastrointestinal and Liver Physiology 285, no. 5 (2003): G829—G839. http://dx.doi.org/10.1152/ajpgi.00352.2002.

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Transport of a series of3H-radiolabeled C23, C24, and C27bile acid derivatives was compared and contrasted in HeLa cell lines stably transfected with rat Na+/taurocholate cotransporting polypeptide (ntcp) or organic anion transporting polypeptide 1 (oatp1) in which expression was under regulation of a zinc-inducible promoter. Similar uptake patterns were observed for both ntcp and oatp1, except that unconjugated hyodeoxycholate was a substrate of oatp1 but not ntcp. Conjugated bile acids were transported better than nonconjugated bile acids, and the configuration of the hydroxyl groups (α or β

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10

Bouscarel, B., H. Fromm, and R. Nussbaum. "Ursodeoxycholate mobilizes intracellular Ca2+ and activates phosphorylase a in isolated hepatocytes." American Journal of Physiology-Gastrointestinal and Liver Physiology 264, no. 2 (1993): G243—G251. http://dx.doi.org/10.1152/ajpgi.1993.264.2.g243.

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In isolated hamster hepatocytes, ursodeoxycholic acid (UDCA) mobilized intracellular free calcium ([Ca2+]i) and activated phosphorylase a with a half-maximally effective concentration of 188 and 9 microM, respectively. Addition of ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA) did not affect the maximum [Ca2+]i mobilized by UDCA; however, [Ca2+]i returned to basal levels in 4-5 min compared with > 10 min in the absence of EGTA. Both UDCA and vasopressin activated phosphorylase a to the same extent in the presence and absence of extracellular Ca2+, and the effec

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11

Yorinobu, Maeda*, Kyan Ryuji, Shigenaga Akira, Ohta Masaya, Goromaru Takeshi, and Murakami Teruo. "USE OF URSODEOXYCHOLIC ACID CONJUGATES AS A CARRIER OF 5-AMINOSALICYLIC ACID TO DELIVER TO THE COLONIC REGION: COMPARISON WITH SALAZOSULFAPYRIDINE IN FED RATS." World Journal of Pharmaceutical Science and Research 4, no. 1 (2025): 486–512. https://doi.org/10.5281/zenodo.14936826.

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12

Goto, Michitaka, Yasuhiro Okamoto, Magobei Yamamoto, and Hatsumi Aki. "Anti-inflammatory effects of 5-aminosalicylic acid conjugates with chenodeoxycholic acid and ursodeoxycholic acid on carrageenan-induced colitis in guinea-pigs." Journal of Pharmacy and Pharmacology 53, no. 12 (2001): 1711–20. http://dx.doi.org/10.1211/0022357011778115.

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13

Bondarenko, L. B., N. O. Gorchakova, O. I. Golembiovska, and O. Y. Galkin. "Promising new fixed combination for the treatment of diseases of the hepatobiliar system: Substantiation of pharmacotherapeutic properties and pharmaceutical quality profile." Regulatory Mechanisms in Biosystems 9, no. 1 (2018): 23–40. http://dx.doi.org/10.15421/021804.

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In this review article an analysis of literature data on the pharmacological and clinical study of a fixed combination of medicinal substances (artichoke leaf extract, ursodeoxycholic acid, taurine, and Angelica sinensis roots extract), as well a scientific substantiation of the pharmaceutical quality profile of the corresponding finished solid dosage form has been conducted. Chronic diseases of the hepatobiliary system are some of the most common human diseases and inferior only to atherosclerosis . The fact that cholecystectomy is the most common surgical operation in the abdominal organs is

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14

Luu, Hung N., Chi Thi-Du Tran, Renwei Wang, et al. "Associations between Ileal Juice Bile Acids and Colorectal Advanced Adenoma." Nutrients 15, no. 13 (2023): 2930. http://dx.doi.org/10.3390/nu15132930.

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Background: There is an urgent need to identify biomarkers for advanced adenoma, an important precursor of colorectal cancer (CRC). We aimed to determine alterations in ileal juice bile acids associated with colorectal advanced adenoma. Methods: We quantified a comprehensive panel of primary and secondary bile acids and their conjugates using an ultraperformance liquid chromatography triple-quadrupole mass spectrometric assay in ileal juice collected at colonoscopy from 46 study subjects (i.e., 14 biopsy-confirmed advanced adenomas and 32 controls free of adenoma or cancer). Using analysis of

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15

Glantz, A., L. Benthin, F. Lammert, L. A. Mattsson, and H. U. Marschall. "697 Intrahepatic cholestasis of pregnancy: Effects of dexamethasone and ursodeoxycholic acid on serum bile acid profiles and urine progesterone conjugates." Journal of Hepatology 44 (April 2006): S257. http://dx.doi.org/10.1016/s0168-8278(06)80697-5.

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16

Chiang, Ping-I., Kuo-Hsuan Chang, Hsiang-Yu Tang, Yih-Ru Wu, Mei-Ling Cheng, and Chiung-Mei Chen. "Diagnostic Potential of Alternations of Bile Acid Profiles in the Plasma of Patients with Huntington’s Disease." Metabolites 14, no. 7 (2024): 394. http://dx.doi.org/10.3390/metabo14070394.

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Huntington’s disease (HD) is characterized by progressive involuntary chorea movements and cognitive decline. Recent research indicates that metabolic disturbance may play a role in its pathogenesis. Bile acids, produced during cholesterol metabolism in the liver, have been linked to neurodegenerative conditions. This study investigated variations in plasma bile acid profiles among individuals with HD. Plasma levels of 16 primary and secondary bile acids and their conjugates were analyzed in 20 healthy controls and 33 HD patients, including 24 with symptoms (symHD) and 9 carriers in the presym

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17

Caballero, Francisco Javier, Ivan Rivilla, Elisa Herraez, et al. "PS-011-New synthetic conjugates of ursodeoxycholic acid inhibit hepatorenal cystogenesis in experimental models of polycystic liver disease." Journal of Hepatology 70, no. 1 (2019): e10. http://dx.doi.org/10.1016/s0618-8278(19)30017-9.

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18

Chretien, Y., R. Poupon, M. F. Gherardt, et al. "Bile acid glycine and taurine conjugates in serum of patients with primary biliary cirrhosis: effect of ursodeoxycholic treatment." Gut 30, no. 8 (1989): 1110–15. http://dx.doi.org/10.1136/gut.30.8.1110.

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19

Peters, D., L. Norris, L. Tenora, et al. "P068 Discovery of IBD3540: A Novel Gut-Restricted Glutamate Carboxypeptidase II Inhibitor with Preclinical Anti-Colitis Activity." Journal of Crohn's and Colitis 16, Supplement_1 (2022): i174—i175. http://dx.doi.org/10.1093/ecco-jcc/jjab232.197.

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Abstract Background Glutamate carboxypeptidase II (GCPII) is robustly overexpressed in both Crohn’s disease and ulcerative colitis and is a promising therapeutic target for IBD. We have previously published that systemically or enema administered small molecule GCPII inhibitors have efficacy in multiple mouse colitis models. While this is a highly encouraging activity profile for a candidate IBD drug, an oral dose route would be strongly preferred. Thus, here we develop and characterize a new class of GCPII inhibitors designed to be gut-restricted for oral administration, with the intention of

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20

Peters, Diane, Lauren Norris, Lukas Tenora, et al. "DISCOVERY OF IBD3540: A NOVEL GUT-RESTRICTED GLUTAMATE CARBOXYPEPTIDASE II INHIBITOR WITH ORAL ACTIVITY IN MOUSE COLITIS MODELS." Inflammatory Bowel Diseases 28, Supplement_1 (2022): S4. http://dx.doi.org/10.1093/ibd/izac015.007.

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Abstract BACKGROUND & AIMS Glutamate carboxypeptidase II (GCPII) is robustly overexpressed in both Crohn’s disease and ulcerative colitis and is a promising therapeutic target for IBD. We have previously published that systemically or enema administered small molecule GCPII inhibitors have efficacy in multiple mouse colitis models. While this is a highly encouraging activity profile for a candidate IBD drug, an oral dose route would be strongly preferred. Thus, here we develop and characterize a new class of GCPII inhibitors designed to be gut-restricted for oral administration, with the i

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21

Hamilton, James P., Guofeng Xie, Jean-Pierre Raufman, et al. "Human cecal bile acids: concentration and spectrum." American Journal of Physiology-Gastrointestinal and Liver Physiology 293, no. 1 (2007): G256—G263. http://dx.doi.org/10.1152/ajpgi.00027.2007.

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To obtain information on the concentration and spectrum of bile acids in human cecal content, samples were obtained from 19 persons who had died an unnatural death from causes such as trauma, homicide, suicide, or drug overdose. Bile acid concentration was measured via an enzymatic assay for 3α-hydroxy bile acids; bile acid classes were determined by electrospray ionization mass spectrometry and individual bile acids by gas chromatography mass spectrometry and liquid chromatography mass spectrometry. The 3α-hydroxy bile acid concentration (μmol bile acid/ml cecal content) was 0.4 ± 0.2 mM (mea

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22

Sutherland, J. Derek, C. Noel Williams, Donna M. Hutchison та Lillian V. Holdeman. "Oxidation of primary bile acids by a 7α-hydroxysteroid dehydrogenase elaborating Clostridium bifermentans soil isolate". Canadian Journal of Microbiology 33, № 8 (1987): 663–69. http://dx.doi.org/10.1139/m87-116.

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A gram-positive, rod-shaped anaerobe (strain F-6) was isolated from soil. This organism was identified by cellular morphology as well as fermentative and biochemical data as Clostridium bifermentans. Strain F-6 formed 7-ketolithocholic acid from chenodeoxycholic acid and 7-ketodeoxycholic acid from cholic acid in whole cell cultures, but did not transform deoxycholic acid, ursodeoxycholic acid, or ursocholic acid. This reaction is reversible. The structures of 7-ketolithocholic acid and 7-ketodeoxycholic acid were verified by mass spectroscopy and by thin-layer chromatography using Komarowsky'

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23

Tessier, E., L. Neirinck, and Z. Zhu. "High-performance liquid chromatographic mass spectrometric method for the determination of ursodeoxycholic acid and its glycine and taurine conjugates in human plasma." Journal of Chromatography B 798, no. 2 (2003): 295–302. http://dx.doi.org/10.1016/j.jchromb.2003.09.054.

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24

LIN, Yuguang, Rick HAVINGA, Ingrid J. SCHIPPERS, Henkjan J. VERKADE, Roel J. VONK, and Folkert KUIPERS. "Characterization of the inhibitory effects of bile acids on very-low-density lipoprotein secretion by rat hepatocytes in primary culture." Biochemical Journal 316, no. 2 (1996): 531–38. http://dx.doi.org/10.1042/bj3160531.

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In this study the effects of bile acids and other organic anions on the secretion of very-low-density lipoproteins (VLDLs) were evaluated in rat hepatocytes in primary culture. Incubation of cells with portal blood concentrations (10–200 μM) of bile acids resulted in dose-dependent suppression of secretion of VLDL-associated [3H]triglyceride (TG) formed from [3H]glycerol, and also of TG mass. The degree of the inhibition was highly correlated with intracellular bile acid concentration. Prolonged incubation with 100 μM extracellular taurocholic acid (TC) decreased the secretion of [3H]TG and TG

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Chang, Jung-Chin, Ulrich Beuers, and Ronald P. J. Oude Elferink. "The Emerging Role of Soluble Adenylyl Cyclase in Primary Biliary Cholangitis." Digestive Diseases 35, no. 3 (2017): 217–23. http://dx.doi.org/10.1159/000450914.

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Background: Primary biliary cholangitis (PBC; previously referred to as primary biliary cirrhosis) is a chronic fibrosing cholangiopathy with the signature of an autoimmune disease and features of intrahepatic cholestasis. Immunosuppressing treatments are largely unsuccessful. Responsiveness to ursodeoxycholic acid and reduced expression of anion exchanger 2 (AE2) on canalicular membranes and small bile ducts underline the importance of bicarbonate transportation in its disease mechanism. Soluble adenylyl cyclase (sAC; ADCY10) is an evolutionarily conserved bicarbonate sensor that regulates ap

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Amuro, Y., W. Yamade, K. Kudo, T. Yamamoto, T. Hada, and K. Higashino. "Reduction of 7-ketolithocholic acid by human liver enzyme preparations in vitro." American Journal of Physiology-Gastrointestinal and Liver Physiology 256, no. 1 (1989): G67—G71. http://dx.doi.org/10.1152/ajpgi.1989.256.1.g67.

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The formation of chenodeoxycholic and ursodeoxycholic acids from 7-ketolithocholic acid by human liver preparations was examined in vitro. Liver preparations were incubated with 7-ketolithocholic acid at pH 5.5 in a sodium-potassium-phosphate buffer containing NADPH or NADH. The products formed were analyzed by gas chromatography and gas chromatography-mass spectrometry. Results showed that chenodeoxycholic and ursodeoxycholic acids could be formed from 7-ketolithocholic acid by human liver enzyme(s). The enzyme(s) required NADPH but not NADH as coenzyme and was localized largely in the micros

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27

Malavolti, M., H. Fromm, E. Nsien, et al. "Formation, absorption, and biotransformation of delta 6-lithocholenic acid in humans." American Journal of Physiology-Gastrointestinal and Liver Physiology 264, no. 1 (1993): G163—G171. http://dx.doi.org/10.1152/ajpgi.1993.264.1.g163.

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delta 6-Lithocholenic acid was identified in small amounts in fecal samples in vitro after incubation with ursodeoxycholic acid and in vivo in controls and after chenodeoxycholic and ursodeoxycholic acid ingestion. Fourteen to 45.0% of delta 6-[24-14C]lithocholenic acid was biotransformed in vitro in feces within 30 s. After colonic instillation of delta 6-[24-14C]lithocholenic acid, 50% of the radioactivity appeared in bile acids, most of it in lithocholic acid, within 3 h. Jejunal perfusions with delta 6-[24-14C]lithocholenic acid showed 33-92% absorption. One hour after jejunal instillation

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28

Varanasi, Siva Karthik, Dan Chen, Yingluo Liu, et al. "Bile acid synthesis impedes tumor-specific T cell responses during liver cancer." Science 387, no. 6730 (2025): 192–201. https://doi.org/10.1126/science.adl4100.

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The metabolic landscape of cancer greatly influences antitumor immunity, yet it remains unclear how organ-specific metabolites in the tumor microenvironment influence immunosurveillance. We found that accumulation of primary conjugated and secondary bile acids (BAs) are metabolic features of human hepatocellular carcinoma and experimental liver cancer models. Inhibiting conjugated BA synthesis in hepatocytes through deletion of the BA-conjugating enzyme bile acid–CoA:amino acid N -acyltransferase (BAAT) enhanced tumor-specific T cell responses, reduced tumor growth, and sensitized tumors to an

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Lee, Seung Yun, Sung Yeoul Yoon, Da Young Lee, et al. "Development of batch processing to obtain bioactive materials from pork byproducts." Animal Production Science 60, no. 2 (2020): 316. http://dx.doi.org/10.1071/an18600.

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The purpose of this study was to develop batch-processing methods for the extraction of collagen, peptides and heparin, and synthesis of conjugated linoleic acid and ursodeoxycholic acid from pork byproducts. The first steps in utilisation of byproducts involved washing, followed by grinding and mixing, then separation into protein and lipids. The 6% yield of collagen and 4% yield of peptides were extracted from the protein. The lipids were separated into saturated fatty acids and unsaturated fatty acids, and then the 20% yield by synthesis of conjugated linoleic acid from crude lipids and the

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Vakhrushev, Ya M., A. P. Lukashevich, and E. V. Suchkova. "Evaluation of enterohepatic circulation of the bile acids in patients with non-alcoholic fatty liver disease." Experimental and Clinical Gastroenterology, no. 8 (October 9, 2023): 73–78. http://dx.doi.org/10.31146/1682-8658-ecg-216-8-73-78.

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The aim. To study the clinical manifestations and features of changes in the spectrum of the bile acids in bile and blood in patients with non-alcoholic fatty liver disease. Materials and methods. 54 patients with non-alcoholic fatty liver disease at the stage of steatosis were examined. The median age was 50 years (45; 55). Complaints, objective symptoms and the results of laboratory and instrumental studies of the liver were used to verify non-alcoholic fatty liver disease. The content of the bile acids in bile and blood was determined using an AmazonX mass spectrometer (Bruker Daltonik GmbH

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Li, Wei, Wei Chen, Xiaoya Niu, et al. "Characterization of Metabolic Correlations of Ursodeoxycholic Acid with Other Bile Acid Species through In Vitro Sequential Metabolism and Isomer-Focused Identification." Molecules 28, no. 12 (2023): 4801. http://dx.doi.org/10.3390/molecules28124801.

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As a first-line agent for cholestasis treatment in a clinic, ursodeoxycholic acid rectifies the perturbed bile acids (BAs) submetabolome in a holistic manner. Considering the endogenous distribution of ursodeoxycholic acid and extensive occurrences of isomeric metabolites, it is challenging to point out whether a given bile acid species is impacted by ursodeoxycholic acid in a direct or indirect manner, thus hindering the therapeutic mechanism clarification. Here, an in-depth exploration of the metabolism pattern of ursodeoxycholic acid was attempted. Sequential metabolism in vitro with enzyme

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Farges, O., M. Corbic, M. Dumont, M. Maurice, and S. Erlinger. "Permeability of the rat biliary tree to ursodeoxycholic acid." American Journal of Physiology-Gastrointestinal and Liver Physiology 256, no. 4 (1989): G653—G660. http://dx.doi.org/10.1152/ajpgi.1989.256.4.g653.

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The permeability of the biliary epithelium to [14C]ursodeoxycholic acid (UDCA), a hypercholeretic bile acid, was compared to that of the 14C-labeled nonhypercholeretic bile acids cholic acid (CA), taurocholic acid (TCA), and tauroursodeoxycholic acid (TUDCA) by means of anterograde intrabiliary infusions and retrograde intrabiliary injections in the anesthetized rat. Anterograde intrabiliary infusions were performed by perfusing an isolated segment of common bile duct in vivo. After anterograde intrabiliary infusions, the fraction of unrecovered UDCA (that had presumably been absorbed from the

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Dinler, Gönül, Nurten Koçak, Aysel Yüce, Figen Gürakan, and Hasan Özen. "Ursodeoxycholic acid therapy in children with cholestatic liver disease." Turkish Journal of Pediatrics 41, no. 1 (1999): 91–98. http://dx.doi.org/10.24953/turkjpediatr.1999.3203.

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The beneficial effect of ursodeoxycholic acid have been documented in adults but experience with this agent is limited in the pediatric population. The objective of this study was to evaluate ursodeoxycholic acid treatment in children with cholestatic liver disease. Twenty-four patients with intrahepatic cholestasis (neonatal hepatitis 7, Byler disease 7, idiopathic intrahepatic cholestasis 10) whose ages ranged from 1.5 months to 15 years were treated with ursodeoxycholic acid (15-20 mg/kg/day) for 12 months. Liver biopsy was performed initially on all patients and on 17 at the end of the twe

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Garcia-Marin, J. J., P. Regueiro, J. C. Perez-Antona, G. R. Villanueva, and F. Perez-Barriocanal. "Pre-replicative phase-related changes in bile acid-induced choleresis in the regenerating rat liver." Clinical Science 78, no. 1 (1990): 55–62. http://dx.doi.org/10.1042/cs0780055.

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1. During the pre-replicative phase of the regenerating rat liver some interesting changes occur, which might selectively modify some mechanisms involved in bile formation, such as those responsible for the hypercholeretic effect of ursodeoxycholic acid. The aim of the present work was to gain information on this point. 2. Anaesthetized male Wistar rats (∼ 250 g) were used. The animals underwent two-thirds hepatectomy 1, 6 or 12 h before collection of bile samples was begun. Very early after hepatectomy (1 h) spontaneous bile flow and bile acid output were increased. Both returned to values no

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Melloni, Elisabetta, Elena Marchesi, Lorenzo Preti, et al. "Synthesis and Biological Investigation of Bile Acid-Paclitaxel Hybrids." Molecules 27, no. 2 (2022): 471. http://dx.doi.org/10.3390/molecules27020471.

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Chenodeoxycholic acid and ursodeoxycholic acid (CDCA and UDCA, respectively) have been conjugated with paclitaxel (PTX) anticancer drugs through a high-yield condensation reaction. Bile acid-PTX hybrids (BA-PTX) have been investigated for their pro-apoptotic activity towards a selection of cancer cell lines as well as healthy fibroblast cells. Chenodeoxycholic-PTX hybrid (CDC-PTX) displayed cytotoxicity and cytoselectivity similar to PTX, whereas ursodeoxycholic-PTX hybrid (UDC-PTX) displayed some anticancer activity only towards HCT116 colon carcinoma cells. Pacific Blue (PB) conjugated deriv

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Trauner, Michael, Emina Halilbasic, Thierry Claudel, et al. "Potential of nor-Ursodeoxycholic Acid in Cholestatic and Metabolic Disorders." Digestive Diseases 33, no. 3 (2015): 433–39. http://dx.doi.org/10.1159/000371904.

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24-nor-ursodeoxycholic acid (norUDCA) is a side-chain shortened derivate of ursodeoxycholic acid (UDCA). Since norUDCA is only ineffectively conjugated with glycine or taurine, it has specific physicochemical and therapeutic properties distinct from UDCA. Nonamidated norUDCA undergoes cholehepatic shunting enabling ‘ductular targeting' and inducing a bicarbonate-rich hypercholeresis, with cholangioprotective effects. At the same time it has direct anti-inflammatory, antilipotoxic, anti fibrotic, and antiproliferative properties targeting various liver cell populations. norUDCA appears to be on

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MAEDA, Yorinobu, and Makoto TAKAHASHI. "Hydrolysis and absorption of a conjugate of ursodeoxycholic acid with para-aminobenzoic acid." Journal of Pharmacobio-Dynamics 12, no. 12 (1989): 744–53. http://dx.doi.org/10.1248/bpb1978.12.744.

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Mathavan, Sangeetha, Corina M. Ionescu, Bozica Kovacevic, et al. "Formulation buoyancy of nanoencapsulated gliclazide using primary, conjugated and deconjugated bile acids." Therapeutic Delivery 10, no. 9 (2019): 573–83. http://dx.doi.org/10.4155/tde-2019-0058.

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Aim: Recent studies suggest potential applications of endogenously produced human bile acids as formulation-excipient and drug tissue permeation enhancers in Type 1 diabetes. We aimed to examine the stability, tissue permeation and ex vivo muscle-cell effects of microencapsulated gliclazide (G) incorporated with a primary (chenodeoxycholic acid [CDCA]), a secondary (ursodeoxycholic acid [UDCA]) or a tertiary (taurocholic acid [TCA]) bile acid. Materials & methods: Four formulations made of sodium alginate, CDCA, UDCA and TCA were examined for buoyancy, tissue-enhancing effects ( in vivo) a

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Thibault, Maxime, Jessica McMahon, Guillaume Faubert, et al. "Parenteral Nutrition-Associated Liver Disease: a Retrospective Study of Ursodeoxycholic Acid Use in Neonates." Journal of Pediatric Pharmacology and Therapeutics 19, no. 1 (2014): 42–48. http://dx.doi.org/10.5863/1551-6776-19.1.42.

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OBJECTIVES To verify the effect of ursodeoxycholic acid (UDCA) on the duration of neonatal parenteral nutrition-associated liver disease. METHODS Retrospective cohort study of neonates in intensive care between 2004 and 2007 presenting with parenteral nutrition-associated liver disease. RESULTS Of 118 eligible infants, 64 received UDCA. Cholestasis lasted longer in the UDCA group (79 vs. 50 days, p=0.001). However, treatment was delayed for a median of 24 days after cholestasis onset. Multivariate Cox regression analysis showed no association between UDCA and cholestasis duration. The rate of

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Rudolph, G., P. Kloeters-Plachky, P. Sauer, and A. Stiehl. "Intestinal absorption and biliary secretion of ursodeoxycholic acid and its taurine conjugate." European Journal of Clinical Investigation 32, no. 8 (2002): 575–80. http://dx.doi.org/10.1046/j.1365-2362.2002.01030.x.

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Batta, Ashok K., G. Stephen Tint, Guorong Xu, Sarah Shefer, and Gerald Salen. "Synthesis and intestinal metabolism of ursodeoxycholic acid conjugate with an antiinflammatory agent, 5-aminosalicylic acid." Journal of Lipid Research 39, no. 8 (1998): 1641–46. http://dx.doi.org/10.1016/s0022-2275(20)32193-3.

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Yamaguchi, Yuji, Satoshi Itami, Kenju Nishida, and Yumi Ando. "Taurin-conjugated ursodeoxycholic acid has a reversible inhibitory effect on human keratinocyte growth." Journal of Dermatological Science 18, no. 1 (1998): 35–42. http://dx.doi.org/10.1016/s0923-1811(98)00023-1.

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Lee, Hye Myeong, Young-Il Jeong, Do Hyung Kim, et al. "Ursodeoxycholic acid-conjugated chitosan for photodynamic treatment of HuCC-T1 human cholangiocarcinoma cells." International Journal of Pharmaceutics 454, no. 1 (2013): 74–81. http://dx.doi.org/10.1016/j.ijpharm.2013.06.035.

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Marschall, Hanns-Ulrich, William James Griffiths, Ulrich Götze, et al. "The major metabolites of ursodeoxycholic acid in human urine are conjugated withN-acetylglucosamine." Hepatology 20, no. 4 (1994): 845–53. http://dx.doi.org/10.1002/hep.1840200412.

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Yu, Jingfeng, Sihan Sheng, Xiaosu Zou, and Zhengwu Shen. "Dihydroartemisinin-ursodeoxycholic acid conjugate is a potential treatment agent for inflammatory bowel disease." International Immunopharmacology 117 (April 2023): 109918. http://dx.doi.org/10.1016/j.intimp.2023.109918.

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Zhang, Wei, Clifford J. Steer, Kenneth T. Douglas, and Cecilia M. P. Rodrigues. "Binding Studies of Bile Acids using the Native Fluorescence of the Tryptophan Residue Of Bax Protein." Bioscience Reports 26, no. 3 (2006): 245–50. http://dx.doi.org/10.1007/s10540-006-9019-7.

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Ursodeoxycholic acid (UDCA) and its taurine-conjugate, tauroursodeoxycholic acid (TUDCA), play a unique role in modulating the apoptotic threshold in cells. The mechanism is thought to involve, in part, inhibition of translocation for Bax from the cytosol to mitochondria. Here, we attempted to use the native fluorescence of the tryptophan residues of Bax to determine whether bile acids bind directly to recombinant Bax protein. The results showed that UDCA had no effect on the tryptophan fluorescence of Bax. Similarly, there was no evidence of direct binding between Bax protein and the more hyd

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Xing, Luwen, Yiwen Zhang, Saiyu Li, et al. "A Dual Coverage Monitoring of the Bile Acids Profile in the Liver–Gut Axis throughout the Whole Inflammation-Cancer Transformation Progressive: Reveal Hepatocellular Carcinoma Pathogenesis." International Journal of Molecular Sciences 24, no. 5 (2023): 4258. http://dx.doi.org/10.3390/ijms24054258.

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Hepatocellular carcinoma (HCC) is the terminal phase of multiple chronic liver diseases, and evidence supports chronic uncontrollable inflammation being one of the potential mechanisms leading to HCC formation. The dysregulation of bile acid homeostasis in the enterohepatic circulation has become a hot research issue concerning revealing the pathogenesis of the inflammatory-cancerous transformation process. We reproduced the development of HCC through an N-nitrosodiethylamine (DEN)-induced rat model in 20 weeks. We achieved the monitoring of the bile acid profile in the plasma, liver, and inte

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Thounaojam, Menaka C., Ravirajsinh N. Jadeja, Shubhra Rajpurohit, et al. "Ursodeoxycholic Acid Halts Pathological Neovascularization in a Mouse Model of Oxygen-Induced Retinopathy." Journal of Clinical Medicine 9, no. 6 (2020): 1921. http://dx.doi.org/10.3390/jcm9061921.

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Retinopathy of prematurity (ROP) is the leading cause of blindness in infants. We have investigated the efficacy of the secondary bile acid ursodeoxycholic acid (UDCA) and its taurine and glycine conjugated derivatives tauroursodeoxycholic acid (TUDCA) and glycoursodeoxycholic acid (GUDCA) in preventing retinal neovascularization (RNV) in an experimental model of ROP. Seven-day-old mice pups (P7) were subjected to oxygen-induced retinopathy (OIR) and were treated with bile acids for various durations. Analysis of retinal vascular growth and distribution revealed that UDCA treatment (50 mg/kg,

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Ringoringo, Harapan Parlindungan. "The Role of Ursodeoxycholic Acid and Phenobarbital in a Child with Cholestasis: A Longitudinal Study." Open Access Macedonian Journal of Medical Sciences 9, no. C (2021): 254–57. http://dx.doi.org/10.3889/oamjms.2021.7735.

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BACKGROUND: Cholestasis is a condition that starts in the 1st months of life and progresses with direct (conjugated) bilirubin increase and jaundice as a result of impaired bile production or excretion. Its incidence is known as 1 in 2500 live births. This study shows the effectiveness of ursodeoxycholic acid (UDCA) and phenobarbital in infant cholestasis treatment. CASE REPORT: A 28-days-old boy came with a complaint of yellow eyes. At the age of 3 days, the patient looked yellow, had a fever and difficulty drinking, received phototherapy. After 2 weeks of treatment with neonatal sepsis, the

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Marchesi, Elena, Matteo Bovolenta, Lorenzo Preti, et al. "Synthesis and Exon-Skipping Properties of a 3′-Ursodeoxycholic Acid-Conjugated Oligonucleotide Targeting DMD Pre-mRNA: Pre-Synthetic versus Post-Synthetic Approach." Molecules 26, no. 24 (2021): 7662. http://dx.doi.org/10.3390/molecules26247662.

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Steric blocking antisense oligonucleotides (ASO) are promising tools for splice modulation such as exon-skipping, although their therapeutic effect may be compromised by insufficient delivery. To address this issue, we investigated the synthesis of a 20-mer 2′-OMe PS oligonucleotide conjugated at 3′-end with ursodeoxycholic acid (UDCA) involved in the targeting of human DMD exon 51, by exploiting both a pre-synthetic and a solution phase approach. The two approaches have been compared. Both strategies successfully provided the desired ASO 51 3′-UDC in good yield and purity. It should be pointe

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