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Journal articles on the topic 'Novel Bile Acid Conjugates'

Author: Grafiati

Published: 4 June 2021

Last updated: 6 September 2023

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1

Mishra, Satyendra, and Sejal Patel. "Design, Synthesis, and Anti-bacterial Activity of Novel Deoxycholic Acid- Amino Alcohol Conjugates." Medicinal Chemistry 16, no. 3 (2020): 385–91. http://dx.doi.org/10.2174/1573406415666190206231002.

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Background: Numerous synthetic bile acid derivatives have been recognized for their various biological activities. Among these, bile acid amides have emerged as an attractive antibacterial agent. We herein illustrate the synthesis and antibacterial evaluation of deoxycholic acidamino alcohols conjugates. Objective: Design and Synthesis of novel deoxycholic acid-amino alcohol conjugates to investigate their antibacterial activity against E. coli and S. aureus. Methods: Novel deoxycholic acid-amino alcohol conjugates were synthesized, from conjugation of deoxycholic acid-NHS ester with amino alc

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2

Ahonen, Kari V., Manu K. Lahtinen, Miika S. Löfman, et al. "Structural studies of five novel bile acid-4-aminopyridine conjugates." Steroids 77, no. 11 (2012): 1141–51. http://dx.doi.org/10.1016/j.steroids.2012.06.003.

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3

Chong, Hyun-Soon, Yunwei Chen, Chi Soo Kang, Xiang Sun, and Ningjie Wu. "Novel 64Cu-radiolabeled bile acid conjugates for targeted PET imaging." Bioorganic & Medicinal Chemistry Letters 25, no. 5 (2015): 1082–85. http://dx.doi.org/10.1016/j.bmcl.2015.01.008.

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4

Li, Yan, Weijun Chu, and Yong Ju. "Novel bile acid derivedH-phosphonate conjugates: Synthesis and spectroscopic characterization." Heteroatom Chemistry 19, no. 4 (2008): 402–7. http://dx.doi.org/10.1002/hc.20447.

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5

Jin, Xue-Yuan, Chuan-Bao Zhu, Shi-Yong Fan, et al. "Novel hypolipidemic conjugates of fatty acid and bile acid with lysine for linkage." Drug Development and Industrial Pharmacy 45, no. 6 (2019): 995–98. http://dx.doi.org/10.1080/03639045.2019.1590393.

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6

Koivukorpi, Juha, and Erkki Kolehmainen. "Novel bile acid conjugates with aryl/alkenyl linker: Synthesis and characterization." Journal of Molecular Structure 889, no. 1-3 (2008): 211–16. http://dx.doi.org/10.1016/j.molstruc.2008.01.050.

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7

Noponen, Virpi, Shreedhar Bhat, Elina Sievänen, and Erkki Kolehmainen. "Novel two-step synthesis of gold nanoparticles capped with bile acid conjugates." Materials Science and Engineering: C 28, no. 7 (2008): 1144–48. http://dx.doi.org/10.1016/j.msec.2007.10.001.

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8

Blagbrough, I. S., A. J. Geall, and A. P. Neal. "Polyamines and novel polyamine conjugates interact with DNA in ways that can be exploited in non-viral gene therapy." Biochemical Society Transactions 31, no. 2 (2003): 397–406. http://dx.doi.org/10.1042/bst0310397.

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As a part of our continuing studies on ‘Polyamines and their role in human disease’ we are investigating how polyamines, and especially how novel polyamine conjugates, interact with DNA. We are studying how these conjugates interact with circular plasmids in order to produce nanometre-sized particles suitable for transfecting cells. Our considerations of structure--activity relationships (SAR) within naturally occurring and synthetic polyamines have shown the significance of the inter-atomic distances between the basic nitrogen atoms. As these atoms are typically fully protonated under physiol

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9

Yang, Min, Yu Gu, Lingfeng Li, et al. "Bile Acid–Gut Microbiota Axis in Inflammatory Bowel Disease: From Bench to Bedside." Nutrients 13, no. 9 (2021): 3143. http://dx.doi.org/10.3390/nu13093143.

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Inflammatory bowel disease (IBD) is a chronic, relapsing inflammatory disorder of the gastrointestinal tract, with increasing prevalence, and its pathogenesis remains unclear. Accumulating evidence suggested that gut microbiota and bile acids play pivotal roles in intestinal homeostasis and inflammation. Patients with IBD exhibit decreased microbial diversity and abnormal microbial composition marked by the depletion of phylum Firmicutes (including bacteria involved in bile acid metabolism) and the enrichment of phylum Proteobacteria. Dysbiosis leads to blocked bile acid transformation. Thus,

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10

Thorpe, Cheleste M., Xi Qian, Karin Yanagi, et al. "2567. Effect of Broad vs. Narrow-Spectrum Clostridioides difficile Treatment on Human Stool Bile Acid Composition Over Time." Open Forum Infectious Diseases 6, Supplement_2 (2019): S891. http://dx.doi.org/10.1093/ofid/ofz360.2245.

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Abstract Background Secondary bile acid production by a diverse commensal flora may be a critical factor in preventing recurrence of Clostridioides difficile infection (CDI). Key enzymes involved are bacterial-encoded bile salt hydrolases (BSHs), felt to be “gatekeepers” to secondary bile acid synthesis. Ridinilazole, a novel narrow-spectrum drug for CDI, demonstrated superior sustained clinical response compared with vancomycin in Phase 2. Longitudinal sampling during this trial allowed for assessment of metabolites differentially present in stools during/after therapy with either broad or na

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11

Yu, Lei, Yan-Fang Jiang, Lei Sun, Bo-Hua Zhong, and Jun-Qi Niu. "EBHU18, a novel derivative of fatty acid bile acid conjugates, prevents cholesterol gallstone formation in experimental mice." Medicinal Chemistry Research 21, no. 11 (2011): 3382–89. http://dx.doi.org/10.1007/s00044-011-9828-5.

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12

Li, Yan, Yong Ju, and Yufen Zhao. "Synthesis and Characterization of Novel Bile Acids Derived H-Phosphonates Conjugates." Phosphorus, Sulfur, and Silicon and the Related Elements 183, no. 2-3 (2008): 706–11. http://dx.doi.org/10.1080/10426500701807533.

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13

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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14

Zhu, Quan-Fei, Yan-Zhen Wang, Na An, et al. "Alternating Dual-Collision Energy Scanning Mass Spectrometry Approach: Discovery of Novel Microbial Bile-Acid Conjugates." Analytical Chemistry 94, no. 5 (2022): 2655–64. http://dx.doi.org/10.1021/acs.analchem.1c05272.

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15

Koivukorpi, Juha, Arto Valkonen, Manu Lahtinen, and Erkki Kolehmainen. "Synthesis and characterization of novel bile-acid – heteroaryl conjugates with N-(2-aminoethyl)amido linker." Journal of Molecular Structure 892, no. 1-3 (2008): 53–57. http://dx.doi.org/10.1016/j.molstruc.2008.04.057.

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16

Koivukorpi, Juha, and Erkki Kolehmainen. "Design, synthesis and spectral studies of novel bile acid-arene conjugates: Trans to cis isomerization of azobenzene core controlled by bile acid hydrophobicity." Journal of Molecular Structure 875, no. 1-3 (2008): 63–67. http://dx.doi.org/10.1016/j.molstruc.2007.03.058.

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17

Déjean, Guillaume, Héloïse Tudela, Lisa Bruno, Déborah Kissi, Georges Rawadi, and Sandrine P. Claus. "Identifying a Novel Bile Salt Hydrolase from the Keystone Gut Bacterium Christensenella minuta." Microorganisms 9, no. 6 (2021): 1252. http://dx.doi.org/10.3390/microorganisms9061252.

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Christensenella minuta are human gut dwelling bacteria that have been proposed as key members of the gut microbiome, regulating energy balance and adiposity of their host. We formerly identified that a novel strain of C. minuta (strain DSM33407) boosted microbiota diversity and stimulated deconjugation of the primary bile acid taurocholic acid in human samples. However, there is no description of a bile salt hydrolase (BSH) protein carried in the genome of C. minuta. Here, we identified and cloned a protein from C. minuta’s genome that carries a potent BSH activity, which preferentially deconj

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18

Ray, Abhijit, Antara Banerjee, Cheng Chang, Chandra M. Khantwal, and Peter W. Swaan. "Design of novel synthetic MTS conjugates of bile acids for site-directed sulfhydryl labeling of cysteine residues in bile acid binding and transporting proteins." Bioorganic & Medicinal Chemistry Letters 16, no. 6 (2006): 1473–76. http://dx.doi.org/10.1016/j.bmcl.2005.12.050.

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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

Call, Lee, Tiffany Molina, Barbara Stoll, et al. "Parenteral lipids shape gut bile acid pools and microbiota profiles in the prevention of cholestasis in preterm pigs." Journal of Lipid Research 61, no. 7 (2020): 1038–51. http://dx.doi.org/10.1194/jlr.ra120000652.

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Multi-component lipid emulsions, rather than soy-oil emulsions, prevent cholestasis by an unknown mechanism. Here, we quantified liver function, bile acid pools, and gut microbial and metabolite profiles in premature parenterally fed pigs given a soy-oil lipid emulsion, Intralipid (IL), a multi component lipid emulsion, SMOFlipid (SMOF), a novel emulsion with a modified fatty-acid composition [experimental emulsion (EXP)], or a control enteral diet (ENT) for 22 days. We assayed serum cholestasis markers, measured total bile acid levels in plasma, liver, and gut contents, and analyzed colonic b

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22

Parikh, Kalpesh, Dhaval Savaliya, and Deepkumar Joshi. "Antibacterial and Antifungal Screening of Novel α-amino Acid Conjugated Bile Acid Derivatives." Current Bioactive Compounds 10, no. 4 (2015): 260–70. http://dx.doi.org/10.2174/1573407210666140909201409.

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23

Domingue, Jada C., Mei Ao, Jayashree Sarathy, and Mrinalini C. Rao. "Chenodeoxycholic acid requires activation of EGFR, EPAC, and Ca2+ to stimulate CFTR-dependent Cl− secretion in human colonic T84 cells." American Journal of Physiology-Cell Physiology 311, no. 5 (2016): C777—C792. http://dx.doi.org/10.1152/ajpcell.00168.2016.

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Bile acids are known to initiate intricate signaling events in a variety of tissues, primarily in the liver and gastrointestinal tract. Of the known bile acids, only the 7α-dihydroxy species, deoxycholic acid and chenodeoxycholic acid (CDCA), and their conjugates, activate processes that stimulate epithelial Cl− secretion. We have previously published that CDCA acts in a rapid manner to stimulate colonic ion secretion via protein kinase A (PKA)-mediated activation of the dominant Cl− channel, the cystic fibrosis transmembrane conductance regulator (CFTR) (Ao M, Sarathy J, Domingue J, Alrefai W

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24

Richards, Steven J., Thomas W. von Geldern, Peer Jacobson, et al. "Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists." Bioorganic & Medicinal Chemistry Letters 16, no. 23 (2006): 6086–90. http://dx.doi.org/10.1016/j.bmcl.2006.08.133.

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25

Vicens, Marta, Manuel Medarde, Rocio I. R. Macias, et al. "Novel cationic and neutral glycocholic acid and polyamine conjugates able to inhibit transporters involved in hepatic and intestinal bile acid uptake." Bioorganic & Medicinal Chemistry 15, no. 6 (2007): 2359–67. http://dx.doi.org/10.1016/j.bmc.2007.01.027.

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26

GOTO, T., A. SHIBATA, D. SASAKI, et al. "Identification of a novel conjugate in human urine: bile acid acyl galactosides." Steroids 70, no. 3 (2005): 185–92. http://dx.doi.org/10.1016/j.steroids.2004.12.006.

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27

Mohammed, Ahmed Dawood, Ioulia Chatzistamou, Mary Roland, et al. "Does Dysbiosis Drive CVID Enteropathy by Enhancing Bile Acid Cytotoxicity?" Journal of Immunology 204, no. 1_Supplement (2020): 83.15. http://dx.doi.org/10.4049/jimmunol.204.supp.83.15.

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Abstract Common variable immunodeficiency (CVID) is a primary immunodeficiency characterized by defects in the humoral immune response. CVID patients commonly present with a gastrointestinal enteropathy characterized by intestinal malabsorption. CVID is linked with abnormal gut microbiota composition (i.e. dysbiosis), which may be a contributing factor to CVID enteropathy. Recently, we demonstrated that CD19−/− mice represent a spontaneous animal model of CVID enteropathy that develop an associated dysbiosis. We now expand upon this work to identify how microbial dysbiosis may contribute to CV

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28

Danese, Elisa, Patricia M. J. Lievens, Andrea Padoan, et al. "Plasma Bile Acid Profiling and Modulation of Secreted Mucin 5AC in Cholangiocarcinoma." International Journal of Molecular Sciences 24, no. 16 (2023): 12794. http://dx.doi.org/10.3390/ijms241612794.

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Studies investigating the potential role of circulating bile acids (BAs) as diagnostic biomarkers for cholangiocarcinoma (CCA) are sparse and existing data do not adjust for confounding variables. Furthermore, the mechanism by which BAs affect the expression of the oncogenic mucin 5AC (MUC5AC) has never been investigated. We performed a case–control study to characterise the profile of circulating BAs in patients with CCA (n = 68) and benign biliary disease (BBD, n = 48) with a validated liquid chromatography–tandem mass spectrometry technique. Odd ratios (OR) for CCA associations were calcula

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29

Kim, Dongmyong, Jongseong Yoon, Seoju Kim, Hosoon Choi, and Insuk Han. "A Novel Transdermal Delivery System based on a Bile Acid- Conjugated Nanoparticle Model for Cosmetics." Asian Journal of Beauty and Cosmetology 17, no. 1 (2019): 81–91. http://dx.doi.org/10.20402/ajbc.2018.0265.

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30

Sundrud, Mark S., Wei Cao, Hisako Kayama, et al. "The xenobiotic transporter Mdr1 permits T cell adaptation to mucosa-associated bile acids in the ileum." Journal of Immunology 198, no. 1_Supplement (2017): 65.14. http://dx.doi.org/10.4049/jimmunol.198.supp.65.14.

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Abstract Intestinal CD4+ T helper (TH) cells are subject to extensive regulation by microbiota. By contrast, it is not known whether or how TH cells interface with other, host-derived intestinal metabolites. Here we show that bile acids directly regulate mucosal TH cell function in the distal small intestine (i.e., ileum) via the xenobiotic transporter, Mdr1. Using both Mdr1-dependent dye efflux and a novel CRISPR-generated Mdr1 reporter mouse, we show that wild type RORγt+IL-17A+ (Th17) and RORγt-IFNγ+ (Th1) cells upregulate Mdr1 expression upon migration into the ileum. By contrast, germline

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31

Huang, Yueh-Hsiang, Yi-Hong Wu, Hsiang-Yu Tang, et al. "Gut Microbiota and Bile Acids Mediate the Clinical Benefits of YH1 in Male Patients with Type 2 Diabetes Mellitus: A Pilot Observational Study." Pharmaceutics 14, no. 9 (2022): 1857. http://dx.doi.org/10.3390/pharmaceutics14091857.

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Our previous clinical trial showed that a novel concentrated herbal extract formula, YH1 (Rhizoma coptidis and Shen-Ling-Bai-Zhu-San), improved blood glucose and lipid control. This pilot observational study investigated whether YH1 affects microbiota, plasma, and fecal bile acid (BA) compositions in ten untreated male patients with type 2 diabetes (T2D), hyperlipidemia, and a body mass index ≥ 23 kg/m2. Stool and plasma samples were collected for microbiome, BA, and biochemical analyses before and after 4 weeks of YH1 therapy. As previous studies found, the glycated albumin, 2-h postprandial

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32

Thakare, Rhishikesh, Hongying Gao, Rachel E. Kosa, et al. "Leveraging of Rifampicin-Dosed Cynomolgus Monkeys to Identify Bile Acid 3-O-Sulfate Conjugates as Potential Novel Biomarkers for Organic Anion-Transporting Polypeptides." Drug Metabolism and Disposition 45, no. 7 (2017): 721–33. http://dx.doi.org/10.1124/dmd.117.075275.

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33

Stravitz, R. T., Y. P. Rao, Z. R. Vlahcevic, E. C. Gurley, W. D. Jarvis, and P. B. Hylemon. "Hepatocellular protein kinase C activation by bile acids: implications for regulation of cholesterol 7 alpha-hydroxylase." American Journal of Physiology-Gastrointestinal and Liver Physiology 271, no. 2 (1996): G293—G303. http://dx.doi.org/10.1152/ajpgi.1996.271.2.g293.

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We have recently shown that taurocholate (TCA) represses the transcriptional activity of cholesterol 7 alpha-hydroxylase, the rate-limiting enzyme of the bile acid biosynthetic pathway, through a protein kinase C (PKC)-dependent mechanism in primary cultures of rat hepatocytes. The present studies sought to determine the mechanisms by which bile acids activate hepatic PKC activity and the consequences of this activation on isoform distribution and cholesterol 7 alpha-hydroxylase mRNA levels. TCA (12.5-100 microM for 15 min) increased membrane-associated "classic" isoenzyme cPKC-alpha and "nove

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34

Sigurdsson, Valgardur, Hajime Takei, Svetlana Soboleva, Takashi Iida, Hiroshi Nittono, and Kenichi Miharada. "Taurine-Conjugated Bile Acids Protect Expanding Hematopoietic Stem/Progenitor Cells from Unfolded Protein Stress As Natural Chaperones." Blood 124, no. 21 (2014): 4318. http://dx.doi.org/10.1182/blood.v124.21.4318.4318.

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Abstract Hematopoietic stem cells (HSCs) give rise to all lineages of hematopoietic cells in the body for entire life span and are thus protected from risk factors by multiple defense systems. We have recently discovered that HSCs are highly susceptible to stress caused by accumulation of mis-/un-folded proteins, so called endoplasmic reticulum (ER) stress upon enhanced growth conditions, and addition of a specific type of bile acid (BA), Tauroursodeoxycholic acid (TUDCA), known as a chemical chaperone can maintain functional murine HSCs for 2 weeks in vitro, by reducing ER stress (Miharada et

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35

Pheiffer, Fazlin, Yannik K. H. Schneider, Espen Holst Hansen, et al. "Bioassay-Guided Fractionation Leads to the Detection of Cholic Acid Generated by the Rare Thalassomonas sp." Marine Drugs 21, no. 1 (2022): 2. http://dx.doi.org/10.3390/md21010002.

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Bacterial symbionts of marine invertebrates are rich sources of novel, pharmaceutically relevant natural products that could become leads in combatting multidrug-resistant pathogens and treating disease. In this study, the bioactive potential of the marine invertebrate symbiont Thalassomonas actiniarum was investigated. Bioactivity screening of the strain revealed Gram-positive specific antibacterial activity as well as cytotoxic activity against a human melanoma cell line (A2058). The dereplication of the active fraction using HPLC-MS led to the isolation and structural elucidation of cholic

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Pashankar, Dinesh, and Richard A. Schreiber. "Neonatal Cholestasis: A Red Alert for the Jaundiced Newborn." Canadian Journal of Gastroenterology 14, suppl d (2000): 67D—72D. http://dx.doi.org/10.1155/2000/657368.

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Neonatal jaundice may indicate cholestasis rather than a benign, physiological condition. Any four-week-old newborn with persistent jaundice should have a fractionated bilirubin screen to determine whether the hyperbilirubinemia is unconjugated. Conjugated hyperbilirubinemia, a hallmark of neonatal cholestasis, is pathological and requires further investigation. These infants need prompt diagnosis, early intervention and careful follow-up to ensure continued growth and development. Recent progress in the physiology of bile flow is reviewed, and the evaluation and management of neonatal cholest

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Keizman, D., N. Maimon, M. Ish-Shalom, et al. "An animal model for chemotherapy-associated steatohepatitis (CASH) and its prevention by the oral administration of fatty acid bile acid conjugate (FABAC)." Journal of Clinical Oncology 27, no. 15_suppl (2009): 4098. http://dx.doi.org/10.1200/jco.2009.27.15_suppl.4098.

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4098 Background: Preoperative chemotherapy (irinotecan and oxaliplatin), used in patients undergoing hepatic resection of colorectal liver metastases, is associated with the development of CASH. This hepatic injury increases the risk of perioperative morbidity and mortality. An animal model for CASH has not yet been described. Fatty acid bile acid conjugates (FABACs) are novel synthetic lipid molecules that were shown to prevent the formation of diet induced fatty liver. The present study was designed to establish an animal model of CASH and to use it to study the effect of FABAC on its occurr

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Fu, Zhenzhen, Qinyi Wu, Wen Guo, et al. "Impaired Insulin Clearance as the Initial Regulator of Obesity-Associated Hyperinsulinemia: Novel Insight Into the Underlying Mechanism Based on Serum Bile Acid Profiles." Diabetes Care 45, no. 2 (2021): 425–35. http://dx.doi.org/10.2337/dc21-1023.

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OBJECTIVE To investigate the roles of insulin clearance and insulin secretion in the development of hyperinsulinemia in obese subjects and to reveal the association between insulin clearance and bile acids (BAs). RESEARCH DESIGN AND METHODS In cohort 1, insulin secretion, sensitivity, and endogenous insulin clearance were evaluated with an oral glucose tolerance test in 460 recruited participants. In cohort 2, 81 participants underwent an intravenous glucose tolerance test and a hyperinsulinemic-euglycemic clamp to assess insulin secretion, endogenous and exogenous insulin clearance, and insul

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Park, So-Hyeon, Jun-Hyuck Lee, Seong-Bin Yang, Dong-Nyeong Lee, Tae-Bong Kang, and Jooho Park. "Development of a Peptide-Based Nano-Sized Cathepsin B Inhibitor for Anticancer Therapy." Pharmaceutics 15, no. 4 (2023): 1131. http://dx.doi.org/10.3390/pharmaceutics15041131.

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Numerous cathepsin B inhibitors have been developed and are under investigation as potential cancer treatments. They have been evaluated for their ability to inhibit cathepsin B activity and reduce tumor growth. However, they have shown critical limitations, including low anticancer efficacy and high toxicity, due to their low selectivity and delivery problems. In this study, we developed a novel peptide and drug conjugate (PDC)-based cathepsin B inhibitor using cathepsin-B-specific peptide (RR) and bile acid (BA). Interestingly, this RR and BA conjugate (RR–BA) was able to self-assemble in an

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Barbara, Cecilia, Paola Orlandi, Guido Bocci, et al. "In vitro and in vivo antitumour effects of novel, orally active bile acid-conjugated platinum complexes on rat hepatoma." European Journal of Pharmacology 549, no. 1-3 (2006): 27–34. http://dx.doi.org/10.1016/j.ejphar.2006.08.015.

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41

Suarez, Gabriel, Bo Liu, Jeremy Herzog, and Ryan Sartor. "PRO-INFLAMMATORY MOLECULAR AND INFLAMMATORY MECHANISMS OF SULFUR METABOLISM IN IBD-RELEVANT CLOSTRIDIA SPECIES." Inflammatory Bowel Diseases 27, Supplement_1 (2021): S30—S31. http://dx.doi.org/10.1093/ibd/izaa347.072.

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Abstract Sulfur metabolism is emerging as a signature of IBD gut microbiota. Overrepresentation of sulfur-reducing bacteria (SRB) in IBD results in SRB-derived epithelial toxic H2S production that can overwhelm the body’s detoxification capacity, leading to impaired cellular respiration by inhibiting oxygen binding to mitochondrial cytochrome-c-oxidase. Butyrate potently inhibits SRBs and H2S, yet IBD patients have reduced short chain fatty acid (SCFA) production. More critically, H2S blocks butyrate oxidation, the primary energy source of colonocytes; butyrate oxidation deficiency is a defini

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Sigurdsson, Valgardur, Hajime Takei, Svetlana Soboleva, et al. "Bile Acids Protect Expanding Hematopoietic Stem Cells from Unfolded Protein Stress in Fetal Liver." Blood 126, no. 23 (2015): 897. http://dx.doi.org/10.1182/blood.v126.23.897.897.

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Abstract Hematopoietic stem cells (HSCs) are effectively expanded in fetal liver (FL), while they are maintained in a dormant state in adult bone marrow (BM). However, developmental mechanisms allowing this have not been fully explained. BM-HSCs have the lowest protein synthesis rate within the blood hierarchy, even under forced self-renewal divisions. In addition, HSCs are vulnerable to and quickly activate endoplasmic reticulum (ER) stress responses fueled by accumulation of unfolded / misfolded proteins (Miharada et al., Cell Rep. 2014). Of note, we have seen that FL-HSCs have low levels of

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43

Petzinger, Ernst, Annette Wickboldt, Peter Pagels, Dieter Starke, and Werner Kramer. "Hepatobiliary transport of bile acid amino acid, bile acid peptide, and bile acid oligonucleotide conjugates in rats." Hepatology 30, no. 5 (1999): 1257–68. http://dx.doi.org/10.1002/hep.510300529.

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Salunke, Deepak B., Braja G. Hazra, and Vandana S. Pore. "Bile acid-polyamine conjugates as synthetic ionophores." Arkivoc 2003, no. 9 (2004): 115–25. http://dx.doi.org/10.3998/ark.5550190.0004.914.

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Gilat, Tuvia, Giora Somjen, Yehuda Mazur, et al. "The prevention of cholesterol crystallization in bile using fatty acid bile acid conjugates." Gastroenterology 118, no. 4 (2000): A714. http://dx.doi.org/10.1016/s0016-5085(00)84985-9.

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Lillienau, J., and B. Borgstrom. "Bacterial deconjugation and enterohepatic circulation of norursocholic acid conjugates in rats." American Journal of Physiology-Gastrointestinal and Liver Physiology 261, no. 6 (1991): G1065—G1071. http://dx.doi.org/10.1152/ajpgi.1991.261.6.g1065.

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Experiments were performed to define the metabolism of norusocholic acid (nUC) conjugates and to quantify to what extent the bile acid pool can be enriched in these bile acids. In vitro incubations of norusocholylglycine (nUCG) and -taurine (nUCT) with small intestinal or cecal content showed deconjugation with only cecal content. Cholylglycine (CG) was deconjugated by small intestinal and cecal content. Infusion of nUCG and CG showed that only a small proportion of nUCG was deconjugated after 24 h of enterohepatic circulation, whereas all CG was deconjugated. When nUCT was administered orally

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Dayal, B., K. R. Rapole, G. Salen, S. Shefer, G. S. Tint, and S. R. Wilson. "Microwave-induced Rapid Synthesis of Bile acid Conjugates." Synlett 1995, no. 08 (1995): 861–62. http://dx.doi.org/10.1055/s-1995-5101.

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Jin, Xue-Yuan, and Hui-Fen Wang. "Research progress in liver targeted fatty acid bile acid conjugates." World Chinese Journal of Digestology 16, no. 33 (2008): 3769. http://dx.doi.org/10.11569/wcjd.v16.i33.3769.

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Konikoff, Fred M., Alicia Leikin-Frenkel, Ilana Goldiner, et al. "Biliary and systemic effects of fatty acid bile acid conjugates." European Journal of Gastroenterology & Hepatology 15, no. 6 (2003): 649–55. http://dx.doi.org/10.1097/00042737-200306000-00012.

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Mireault, Myriam, Vivaldy Prinville, Leanne Ohlund, and Lekha Sleno. "Semi-Targeted Profiling of Bile Acids by High-Resolution Mass Spectrometry in a Rat Model of Drug-Induced Liver Injury." International Journal of Molecular Sciences 24, no. 3 (2023): 2489. http://dx.doi.org/10.3390/ijms24032489.

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Using a semi-targeted approach, we have investigated the effect of acetaminophen on circulating bile acid profiles in rats, including many known bile acids and potential isomeric structures, as well as glucuronide and sulfate conjugates. The chromatographic separation was based on an optimized reverse-phase method exhibiting excellent resolution for a complex mix of bile acids using a solid-core C18 column, coupled to a high-resolution quadrupole time-of-flight system. The semi-targeted workflow consisted of first assigning all peaks detectable in samples from 46 known bile acids contained in

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