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Journal articles on the topic 'Sequestrant'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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1

Daufin, Georges, Uzi Merin, François-Louis Kerherve, Jean-Pierre Labbe, Auguste Quemerais, and Charles Bousser. "Efficiency of cleaning agents for an inorganic membrane after milk ultrafiltration." Journal of Dairy Research 59, no. 1 (February 1992): 29–38. http://dx.doi.org/10.1017/s0022029900030211.

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SummaryCleaning of inorganic membranes after ultrafiltration (UF) of skim milk has been assessed using hydraulic, physicochemical and spectroscopic (i.r. and X-ray photoelectron spectroscopy) measurements. A cleaning sequence using hypochlorite alone or hypochlorite followed by HNO3 restored the membrane hydraulic resistance, in contrast to cleaning with HNO3 alone. When using NaOH, addition of Ca complexants (EDTA, gluconate, tripolyphosphate) and surfactants was required to obtain similar results. Three types of criteria (hydraulic, kinetic, chemical) are available to assess the effect of the sequestrant and surfactant types. In all the cases studied, traces of protein and Ca were detected on and within the membrane after cleaning. Nevertheless, it was concluded that it is possible to develop a single-step alkaline product to clean inorganic milk UF membranes if suitable surfactants and Ca sequestrants are included in its formula.

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Houlston, R., J. Quiney, G. F. Watts, and B. Lewis. "Gemfibrozil in the Treatment of Resistant Familial Hypercholesterolemia and Type III Hyperlipoproteinaemia." Journal of the Royal Society of Medicine 81, no. 5 (May 1988): 274–76. http://dx.doi.org/10.1177/014107688808100512.

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The efficacy of gemfibrozil in the treatment of resistant familial hypercholesterolaemia and type III hyperlipoproteinaemia was evaluated in 26 individuals over a mean period of 16 months. In the untreated state both disorders are associated with a high frequency of coronary heart disease. In the former, gemfibrozil with a bile acid sequestrant reduced plasma cholesterol by 32%, an incremental decrease of 17% compared with sequestrant therapy alone. In type III, plasma cholesterol was reduced by 40% and plasma triglyceride by 70%, while high-density lipoprotein cholesterol increased by 45%. In none of the patients studied did clinical or biochemical side effects occur.

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3

Tziomalos, Konstantinos, Asterios Karagiannis, Dimitri P. Mikhailidis, and Vasilios G. Athyros. "Colesevelam: A New and Improved Bile Acid Sequestrant?" Current Pharmaceutical Design 19, no. 17 (April 1, 2013): 3115–23. http://dx.doi.org/10.2174/1381612811319170019.

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Qian, Jian, Bradley P. Sullivan, and Cory Berkland. "pH-Responsive Micelle Sequestrant Polymers Inhibit Fat Absorption." Biomacromolecules 16, no. 8 (July 17, 2015): 2340–46. http://dx.doi.org/10.1021/acs.biomac.5b00560.

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Bays, H. E., K. C. Maki, and K. Schmitz. "The Bile Acid Sequestrant Acceptability Scale validation study." International Journal of Clinical Practice 64, no. 10 (July 5, 2010): 1393–97. http://dx.doi.org/10.1111/j.1742-1241.2010.02467.x.

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Manghat, Padmini, and Anthony S. Wierzbicki. "Colesevelam hydrochloride: a specifically engineered bile acid sequestrant." Future Lipidology 3, no. 3 (June 2008): 237–55. http://dx.doi.org/10.2217/17460875.3.3.237.

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7

Potthoff, Matthew J., Austin Potts, Tianteng He, João A. G. Duarte, Ronald Taussig, David J. Mangelsdorf, Steven A. Kliewer, and Shawn C. Burgess. "Colesevelam suppresses hepatic glycogenolysis by TGR5-mediated induction of GLP-1 action in DIO mice." American Journal of Physiology-Gastrointestinal and Liver Physiology 304, no. 4 (February 15, 2013): G371—G380. http://dx.doi.org/10.1152/ajpgi.00400.2012.

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Bile acid sequestrants are nonabsorbable resins designed to treat hypercholesterolemia by preventing ileal uptake of bile acids, thus increasing catabolism of cholesterol into bile acids. However, sequestrants also improve hyperglycemia and hyperinsulinemia through less characterized metabolic and molecular mechanisms. Here, we demonstrate that the bile acid sequestrant, colesevelam, significantly reduced hepatic glucose production by suppressing hepatic glycogenolysis in diet-induced obese mice and that this was partially mediated by activation of the G protein-coupled bile acid receptor TGR5 and glucagon-like peptide-1 (GLP-1) release. A GLP-1 receptor antagonist blocked suppression of hepatic glycogenolysis and blunted but did not eliminate the effect of colesevelam on glycemia. The ability of colesevelam to induce GLP-1, lower glycemia, and spare hepatic glycogen content was compromised in mice lacking TGR5. In vitro assays revealed that bile acid activation of TGR5 initiates a prolonged cAMP signaling cascade and that this signaling was maintained even when the bile acid was complexed to colesevelam. Intestinal TGR5 was most abundantly expressed in the colon, and rectal administration of a colesevelam/bile acid complex was sufficient to induce portal GLP-1 concentration but did not activate the nuclear bile acid receptor farnesoid X receptor (FXR). The beneficial effects of colesevelam on cholesterol metabolism were mediated by FXR and were independent of TGR5/GLP-1. We conclude that colesevelam administration functions through a dual mechanism, which includes TGR5/GLP-1-dependent suppression of hepatic glycogenolysis and FXR-dependent cholesterol reduction.

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Walters, Julian R. F., Ramesh Arasaradnam, and H. Jervoise N. Andreyev. "Diagnosis and management of bile acid diarrhoea: a survey of UK expert opinion and practice." Frontline Gastroenterology 11, no. 5 (September 11, 2019): 358–63. http://dx.doi.org/10.1136/flgastro-2019-101301.

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ObjectiveBile acid diarrhoea (BAD), which includes bile acid malabsorption, causes a variety of digestive symptoms. Diagnostic rates and management vary considerably. We conducted a survey of current practice to review expert opinion and provide guidance on diagnosis and management.Design/methodAn online survey was conducted of clinical members of the UK Bile Acid Related Diarrhoea Network, who had all published research on BAD (n=21). Most were National Health Service consultants who had diagnosed over 50 patients with the condition.ResultsThe preferred terminology was to use BAD, with primary and secondary to classify causes. A wide range of presenting symptoms and associated conditions were recognised. SeHCAT (tauroselcholic acid) was the preferred diagnostic test, and 50% of respondents thought general practitioners should have access to this. Patients who met the Rome IV diagnostic criteria for functional diarrhoea, irritable bowel syndrome (IBS) with predominant diarrhoea or postcholecystectomy diarrhoea were usually investigated by SeHCAT, which was used sometimes in other types of IBS. Treatment with a bile acid sequestrant was offered to patients with low SeHCAT values, with expected response rates >70% in the most severe. Colestyramine was the usual sequestrant, starting between 2 g and 8 g daily; colesevelam was an alternative. In patients who had an incomplete response, increasing the dose, changing to an alternative sequestrant, use of loperamide and a low fat diet were suggested. Recommendations for follow-up and to improve the overall patient experience were made.ConclusionThis expert survey indicates current best practice in the diagnosis and management of BAD.

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9

Adio, Jitka, and Jennie Burch. "Chronic diarrhoea due to bile salt malabsorption: nurse-led assessment, medical treatment and dietary management." Gastrointestinal Nursing 18, no. 1 (February 2, 2020): 26–31. http://dx.doi.org/10.12968/gasn.2020.18.1.26.

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Bile salt malabsorption (BSM) occurs when bile salts, which are secreted in the small bowel to aid digestion of fats and vitamins, are not sufficiently re-absorbed in the terminal ileum. Consequently, an excess of bile salts enters the colon, causing chronic explosive diarrhoea, associated with abdominal cramps, flatulence and urgent, frequent and unpredictable bowel habits. BSM affects around 1% of the population, often occuring in ileal Crohn's disease or after ileal resection. Diagnosis begins with a nurse-led assessment, including blood and stool tests, to exclude other potential organic causes of chronic diarrhoea. BSM can then be confirmed and classified with a 75Se-homocholic acid taurine (SeHCAT) scan. BSM can be treated medically with bile salt sequestrants, including colestyramine sachets, which are approved but have an unpleasant taste, and colesevelam tablets, which are more tolerable but more expensive and not yet approved. However, long-term sequestrant use can impact absorption of vitamins and other medications. BSM can also be managed with a low-fat diet, which is cost-effective and can reduce the amount of bile secreted. Nurses should provide patient education to ensure adherence and safe use.

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10

Takahashi, Shogo, Yuhuan Luo, Suman Ranjit, Cen Xie, Andrew E. Libby, David J. Orlicky, Alexander Dvornikov, et al. "Bile acid sequestration reverses liver injury and prevents progression of nonalcoholic steatohepatitis in Western diet–fed mice." Journal of Biological Chemistry 295, no. 14 (February 19, 2020): 4733–47. http://dx.doi.org/10.1074/jbc.ra119.011913.

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Nonalcoholic fatty liver disease is a rapidly rising problem in the 21st century and is a leading cause of chronic liver disease that can lead to end-stage liver diseases, including cirrhosis and hepatocellular cancer. Despite this rising epidemic, no pharmacological treatment has yet been established to treat this disease. The rapidly increasing prevalence of nonalcoholic fatty liver disease and its aggressive form, nonalcoholic steatohepatitis (NASH), requires novel therapeutic approaches to prevent disease progression. Alterations in microbiome dynamics and dysbiosis play an important role in liver disease and may represent targetable pathways to treat liver disorders. Improving microbiome properties or restoring normal bile acid metabolism may prevent or slow the progression of liver diseases such as NASH. Importantly, aberrant systemic circulation of bile acids can greatly disrupt metabolic homeostasis. Bile acid sequestrants are orally administered polymers that bind bile acids in the intestine, forming nonabsorbable complexes. Bile acid sequestrants interrupt intestinal reabsorption of bile acids, decreasing their circulating levels. We determined that treatment with the bile acid sequestrant sevelamer reversed the liver injury and prevented the progression of NASH, including steatosis, inflammation, and fibrosis in a Western diet–induced NASH mouse model. Metabolomics and microbiome analysis revealed that this beneficial effect is associated with changes in the microbiota population and bile acid composition, including reversing microbiota complexity in cecum by increasing Lactobacillus and decreased Desulfovibrio. The net effect of these changes was improvement in liver function and markers of liver injury and the positive effects of reversal of insulin resistance.

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11

Brønden, Andreas, and Filip K. Knop. "Gluco-Metabolic Effects of Pharmacotherapy-Induced Modulation of Bile Acid Physiology." Journal of Clinical Endocrinology & Metabolism 105, no. 1 (October 20, 2019): 362–73. http://dx.doi.org/10.1210/clinem/dgz025.

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Abstract Context The discovery and characterization of the bile acid specific receptors farnesoid X receptor (FXR) and Takeda G protein-coupled receptor 5 (TGR5) have facilitated a wealth of research focusing on the link between bile acid physiology and glucose metabolism. Modulation of FXR and TGR5 activation have been demonstrated to affect the secretion of glucagon-like peptide 1, insulin, and glucagon as well as energy expenditure and gut microbiota composition, with potential beneficial effects on glucose metabolism. Evidence Acquisition A search strategy based on literature searches in on PubMed with various combinations of the key words FXR, TGR5, agonist, apical sodium-dependent bile acid transporter (ASBT), bile acid sequestrant, metformin, and glucose metabolism has been applied to obtain material for the present review. Furthermore, manual searches including scanning of reference lists in relevant papers and conference proceedings have been performed. Evidence Synthesis This review provides an outline of the link between bile acid and glucose metabolism, with a special focus on the gluco-metabolic impact of treatment modalities with modulating effects on bile acid physiology; including FXR agonists, TGR5 agonists, ASBT inhibitors, bile acid sequestrants, and metformin. Conclusions Any potential beneficial gluco-metabolic effects of FXR agonists remain to be established, whereas the clinical relevance of TGR5-based treatment modalities seems limited because of substantial safety concerns of TGR5 agonists observed in animal models. The glucose-lowering effects of ASBT inhibitors, bile acid sequestrants, and metformin are at least partly mediated by modulation of bile acid circulation, which might allow an optimization of these bile acid–modulating treatment modalities. (J Clin Endocrinol Metab 106: 362–373, 2020)

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12

Randall, Debra J., and Ellen C. Robinson. "Acute Toxicologic Evaluation of DEQUEST® 2051 Deflocculant & Sequestrant." Journal of the American College of Toxicology 1, no. 2 (January 1990): 99–100. http://dx.doi.org/10.1177/109158189000100219.

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13

Randall, Debra J., and Ellen C. Robinson. "Acute Toxicologic Evaluation of DEQUEST® 2054 Deflocculant and Sequestrant." Journal of the American College of Toxicology 1, no. 2 (January 1990): 100–101. http://dx.doi.org/10.1177/109158189000100220.

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14

Randall, Debra J., and Ellen C. Robinson. "Acute Toxicologic Evaluation of DEQUEST® 2066 Deflocculant and Sequestrant." Journal of the American College of Toxicology 1, no. 2 (January 1990): 102. http://dx.doi.org/10.1177/109158189000100221.

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15

Lerke, Susan A., Gregory Nemeth, Ernest Schubert, and Paul K. Hovsepian. "NMR characterization of a novel bile acid sequestrant, DMP 504." Journal of Pharmaceutical and Biomedical Analysis 24, no. 4 (February 2001): 681–87. http://dx.doi.org/10.1016/s0731-7085(00)00470-2.

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16

Shrestha, Anurupa, Rongti Li, Diptesh Sil, Neha N. Pardeshi, Nancy Schwarting, Karl S. Schorno, Roger A. Rajewski, Apurba Datta, and Sunil A. David. "Pharmacokinetics of DS‐96, an Alkylpolyamine Lipopolysaccharide Sequestrant, in Rodents." Journal of Pharmaceutical Sciences 97, no. 12 (December 2008): 5376–85. http://dx.doi.org/10.1002/jps.21361.

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17

Orekoya, Oluwafikunayo, John McLaughlin, Eugenia Leitao, Wendy Johns, Simon Lal, and Peter Paine. "Quantifying bile acid malabsorption helps predict response and tailor sequestrant therapy." Clinical Medicine 15, no. 3 (June 2015): 252–57. http://dx.doi.org/10.7861/clinmedicine.15-3-252.

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18

Orekoya, Oluwafikunayo, John McLaughlin, Eugenia Leitao, Wendy Johns, Simon Lal, and Peter Paine. "Quantifying bile acid malabsorption helps predict response and tailor sequestrant therapy." Clinical Medicine 15, no. 4 (August 2015): 371.1–371. http://dx.doi.org/10.7861/clinmedicine.15-4-371.

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19

Haratake, Mamoru, Eisuke Hatanaka, Takeshi Fuchigami, Makoto Akashi, and Morio Nakayama. "A Strontium-90 Sequestrant for First-Aid Treatment of Radiation Emergency." Chemical and Pharmaceutical Bulletin 60, no. 10 (2012): 1258–63. http://dx.doi.org/10.1248/cpb.c12-00430.

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20

Kamar, Fareed B., and Rory F. McQuillan. "Hyperchloremic Metabolic Acidosis due to Cholestyramine: A Case Report and Literature Review." Case Reports in Nephrology 2015 (2015): 1–3. http://dx.doi.org/10.1155/2015/309791.

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Cholestyramine is a bile acid sequestrant that has been used in the treatment of hypercholesterolemia, pruritus due to elevated bile acid levels, and diarrhea due to bile acid malabsorption. This medication can rarely cause hyperchloremic nonanion gap metabolic acidosis, a complication featured in this report of an adult male with concomitant acute kidney injury. This case emphasizes the caution that must be taken in prescribing cholestyramine to patients who may also be volume depleted, in renal failure, or taking spironolactone.

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Hope, Janette H., and Bradley E. Hope. "A Review of the Diagnosis and Treatment of Ochratoxin A Inhalational Exposure Associated with Human Illness and Kidney Disease including Focal Segmental Glomerulosclerosis." Journal of Environmental and Public Health 2012 (2012): 1–10. http://dx.doi.org/10.1155/2012/835059.

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Ochratoxin A (OTA) exposure via ingestion and inhalation has been described in the literature to cause kidney disease in both animals and humans. This paper reviews Ochratoxin A and its relationship to human health and kidney disease with a focus on a possible association with focal segmental glomerulosclerosis (FSGS) in humans. Prevention and treatment strategies for OTA-induced illness are also discussed, including cholestyramine, a bile-acid-binding resin used as a sequestrant to reduce the enterohepatic recirculation of OTA.

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22

Edwards, J., Krystal Fontenot, Falk Liebner, and Brian Condon. "Peptide-Cellulose Conjugates on Cotton-Based Materials Have Protease Sensor/Sequestrant Activity." Sensors 18, no. 7 (July 18, 2018): 2334. http://dx.doi.org/10.3390/s18072334.

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The growing incidence of chronic wounds in the world population has prompted increased interest in chronic wound dressings with protease-modulating activity and protease point of care sensors to treat and enable monitoring of elevated protease-based wound pathology. However, the overall design features needed for the combination of a chronic wound dressing that lowers protease activity along with protease detection capability as a single platform for semi-occlusive dressings has scarcely been addressed. The interface of dressing and sensor specific properties (porosity, permeability, moisture uptake properties, specific surface area, surface charge, and detection) relative to sensor bioactivity and protease sequestrant performance is explored here. Measurement of the material’s zeta potential demonstrated a correlation between negative charge and the ability of materials to bind positively charged Human Neutrophil Elastase. Peptide-cellulose conjugates as protease substrates prepared on a nanocellulosic aerogel were assessed for their compatibility with chronic wound dressing design. The porosity, wettability and absorption capacity of the nanocellulosic aerogel were consistent with values observed for semi-occlusive chronic wound dressing designs. The relationship of properties that effect dressing functionality and performance as well as impact sensor sensitivity are discussed in the context of the enzyme kinetics. The sensor sensitivity of the aerogel-based sensor is contrasted with current clinical studies on elastase. Taken together, comparative analysis of the influence of molecular features on the physical properties of three forms of cellulosic transducer surfaces provides a meaningful assessment of the interface compatibility of cellulose-based sensors and corresponding protease sequestrant materials for potential use in chronic wound sensor/dressing design platforms.

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23

Viljoen, Adie, and Anthony S. Wierzbicki. "Colesevelam: an improved bile acid sequestrant for treating hypercholesterolemia and improving diabetes." Expert Review of Endocrinology & Metabolism 5, no. 6 (November 2010): 825–34. http://dx.doi.org/10.1586/eem.10.53.

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Umapathy, Chandraprakash, Claudia M. Ramos Rivers, Miguel Regueiro, Arthur Barrie, Jana G. Hashash, Marc Schwartz, Jason M. Swoger, Leonard Baidoo, Michael A. Dunn, and David G. Binion. "Su1398 Prospective Analysis of Bile Acid Sequestrant Therapy in Inflammatory Bowel Disease." Gastroenterology 146, no. 5 (May 2014): S—458—S—459. http://dx.doi.org/10.1016/s0016-5085(14)61641-3.

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Katti, Sanjeev, Vitaly Nivorozhkin, Florence Lutin, and Daniel Bar. "INNOVATIVE APPROACHES TO SYNTHESIS OF GT 267-004, A SEQUESTRANT FORC. DIFFICILETOXIN." Chemical Engineering Communications 194, no. 7 (April 2, 2007): 849–58. http://dx.doi.org/10.1080/00986440701193829.

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26

Linares, Carlos F., Elymar Valenzuela, Freddy Ocanto, Víctor Pérez, Oscar Valbuena, and Mireya R. Goldwasser. "K+ and Ca2+ modified Na-X zeolites as possible bile acids sequestrant." Journal of Materials Science: Materials in Medicine 19, no. 5 (October 24, 2007): 2023–28. http://dx.doi.org/10.1007/s10856-007-3295-z.

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27

Gledhill, William E., and Victor W. Saeger. "Degradation of sodium polyglyoxylate, a non-persistent metal sequestrant, in laboratory ecosystems." Journal of Industrial Microbiology 2, no. 2 (July 1987): 97–105. http://dx.doi.org/10.1007/bf01569508.

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28

Wang, Xin, Shiyao Jing, Xiumin Qiu, Shile Zhao, Yusheng Liu, and Yebang Tan. "Novel bile acid sequestrant: A biodegradable hydrogel based on amphiphilic allylamine copolymer." Chemical Engineering Journal 304 (November 2016): 493–502. http://dx.doi.org/10.1016/j.cej.2016.06.104.

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Raghavan, Krishnaswamy S., Rong-Kun Chang, Josephine Pang, Garret D. Figuly, and Munir A. Hussain. "Physical and Chemical Properties of DMP 504, a Polyalkylammonium-Based Bile Acid Sequestrant." Pharmaceutical Development and Technology 2, no. 3 (January 1997): 233–41. http://dx.doi.org/10.3109/10837459709031443.

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Seweryn, Artur, Tomasz Wasilewski, and Anita Bocho-Janiszewska. "Correlation between Sequestrant Type and Properties of Mild Soap-Based Hand Washing Products." Industrial & Engineering Chemistry Research 57, no. 38 (September 6, 2018): 12683–88. http://dx.doi.org/10.1021/acs.iecr.8b02910.

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Lindeblad, Matthew, Alexander Lyubimov, Richard van Breemen, Kamil Gierszal, Guy Weinberg, Israel Rubinstein, and Douglas L. Feinstein. "The Bile Sequestrant Cholestyramine Increases Survival in a Rabbit Model of Brodifacoum Poisoning." Toxicological Sciences 165, no. 2 (June 12, 2018): 389–95. http://dx.doi.org/10.1093/toxsci/kfy147.

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32

Schectman, Gordon, Janet Hiatt, and Arthur Hartz. "Telephone Contacts Do Not Improve Adherence to Niacin or Bile Acid Sequestrant Therapy." Annals of Pharmacotherapy 28, no. 1 (January 1994): 29–35. http://dx.doi.org/10.1177/106002809402800104.

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OBJECTIVE: Noxious adverse effects frequently limit patient acceptance of niacin and bile acid sequestrants (BAS), first-line agents in the management of hypercholesterolemia. The purpose of this study was to determine whether telephone contacts from a healthcare professional could improve drug adherence and tolerance in patients prescribed these medications. PATIENTS AND METHODS: This was a randomized, single-blind trial of telephone contacts vs. no intervention in patients with hyperlipidemia who were prescribed either niacin or BAS in a large, Veterans Affairs, lipid clinic. Patients randomized to telephone contact (n=81) received weekly calls from a trained healthcare professional during the first month of drug therapy. Counseling regarding adverse effects, and prescriptions to overcome minor adverse effects, were provided as needed to patients during the telephone contact. RESULTS: Significant differences were not observed between groups in the drug discontinuance rate, adherence assessed by two independent methods, or in the final dosage of medication ingested. CONCLUSIONS: Telephone contacts do not improve either adherence or tolerance to niacin or BAS. Alternative approaches to enhance acceptance of these medications requires further evaluation.

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Nguyen, Thuan B., Ashok Kumar Adisechan, E. V. K. Suresh Kumar, Rajalakshmi Balakrishna, Matthew R. Kimbrell, Kelly A. Miller, Apurba Datta, and Sunil A. David. "Protection from endotoxic shock by EVK-203, a novel alkylpolyamine sequestrant of lipopolysaccharide." Bioorganic & Medicinal Chemistry 15, no. 17 (September 1, 2007): 5694–709. http://dx.doi.org/10.1016/j.bmc.2007.06.015.

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Davidson, Michael H. "A systematic review of bile acid sequestrant therapy in children with familial hypercholesterolemia." Journal of Clinical Lipidology 5, no. 2 (March 2011): 76–81. http://dx.doi.org/10.1016/j.jacl.2011.01.005.

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35

Taggart, W. V., L. Mylecraine, and L. L. Rudel. "Effects of a water-soluble bile acid sequestrant, CK-3368, on bile composition." Atherosclerosis 109, no. 1-2 (September 1994): 8–9. http://dx.doi.org/10.1016/0021-9150(94)93043-0.

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36

van Doormaal, Jasper J., Nienke Smit, Berend J. Koopman, Jan C. van Der Molen, Bert G. Wolthers, and Hieronymus Doorenbos. "Hydroxycholesterols in serum from hypercholesterolaemic patients with and without bile acid sequestrant therapy." Clinica Chimica Acta 181, no. 3 (May 1989): 273–79. http://dx.doi.org/10.1016/0009-8981(89)90233-7.

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37

Lawrie, Kenneth W. M., Pravina Aggarawal, and David Saunders. "The synthesis of [14C]SK&F 97426A. A novel bile acid sequestrant." Journal of Labelled Compounds and Radiopharmaceuticals 34, no. 2 (February 1994): 165–72. http://dx.doi.org/10.1002/jlcr.2580340209.

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38

Fuchs, Claudia Daniela, Gustav Paumgartner, Veronika Mlitz, Victoria Kunczer, Emina Halilbasic, Nadja Leditznig, Annika Wahlström, et al. "Colesevelam attenuates cholestatic liver and bile duct injury in Mdr2−/− mice by modulating composition, signalling and excretion of faecal bile acids." Gut 67, no. 9 (April 10, 2018): 1683–91. http://dx.doi.org/10.1136/gutjnl-2017-314553.

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Background and aimsInterruption of the enterohepatic circulation of bile acids (BAs) may protect against BA-mediated cholestatic liver and bile duct injury. BA sequestrants are established to treat cholestatic pruritus, but their impact on the underlying cholestasis is still unclear. We aimed to explore the therapeutic effects and mechanisms of the BA sequestrant colesevelam in a mouse model of sclerosing cholangitis.MethodsMdr2−/− mice received colesevelam for 8 weeks. Gene expression profiles of BA homeostasis, inflammation and fibrosis were explored in liver, intestine and colon. Hepatic and faecal BA profiles and gut microbiome were analysed. Glucagon-like peptide 1 (GLP-1) levels in portal blood were measured by ELISA. Furthermore, Mdr2−/− mice as well as wild-type 3,5-diethoxy-carbonyl-1,4-dihydrocollidine-fed mice were treated with GLP-1-receptor agonist exendin-4 for 2 weeks prior to analysis.ResultsColesevelam reduced serum liver enzymes, BAs and expression of proinflammatory and profibrogenic markers. Faecal BA profiling revealed increased levels of secondary BAs after resin treatment, while hepatic and biliary BA composition showed a shift towards more hydrophilic BAs. Colonic GLP-1 secretion, portal venous GLP-1 levels and intestinal messenger RNA expression of gut hormone Proglucagon were increased, while ileal Fgf15 expression was abolished by colesevelam. Exendin-4 treatment increased bile duct mass without promoting a reactive cholangiocyte phenotype in mouse models of sclerosing cholangitis. Microbiota analysis showed an increase of the phylum δ-Proteobacteria after colesevelam treatment and a shift within the phyla Firmicutes from Clostridiales to Lactobacillus.ConclusionColesevelam increases faecal BA excretion and enhances BA conversion towards secondary BAs, thereby stimulating secretion of GLP-1 from enteroendocrine L-cells and attenuates liver and bile duct injury in Mdr2−/− mice.

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39

Synytsya, A., L. Fesslová, M. Marounek, and J. Čopíková. "Sodium cholate sorption on N-octadecylpectinamide in comparison with cholestyramine." Czech Journal of Food Sciences 25, No. 1 (January 7, 2008): 32–38. http://dx.doi.org/10.17221/739-cjfs.

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<i>N</i>-Octadecylpectinamide is hydrophobically modified HM citrus pectin. Previously, it had been prepared by heterogeneous amino-de-alkoxylation of initial pectin with <i>n</i>-octadecylamine in dimethylsulphoxide and characterised as potential hydrophobic sorbent and cholesterol lowering agent. The sorption properties of <i>N</i>-octadecylpectinamide were analysed in comparison with cholestyramine, an effective bile acid sequestrant. Sorption experiments were carried out using sodium cholate as a model bile acid. Cholate concentration was estimated by enzymatic spectroscopic method. Sorption kinetics curves and sorption isotherms of both sorbents were constructed and analysed.

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40

Scull, James R., Kurt L. Moyer, Jonathan S. Green, Robert W. Woodeshick, and Mark S. Alasandro. "Determination of a novel bile acid sequestrant in rodent diet by near-infrared spectroscopy." Journal of Pharmaceutical and Biomedical Analysis 19, no. 6 (May 1999): 903–10. http://dx.doi.org/10.1016/s0731-7085(98)00188-5.

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Corsini, Alberto, Eberhard Windier, and Michel Farnier. "Colesevelam hydrochloride: usefulness of a specifically engineered bile acid sequestrant for lowering LDL-cholesterol." European Journal of Cardiovascular Prevention & Rehabilitation 16, no. 1 (February 2009): 1–9. http://dx.doi.org/10.1097/hjr.0b013e32831215db.

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Taggart, W. V., L. Mylecraine, and L. L. Rudel. "Influence of a polycationic water-soluble bile acid sequestrant, CK-3368, on plasma lipids." Atherosclerosis 109, no. 1-2 (September 1994): 9. http://dx.doi.org/10.1016/0021-9150(94)93044-9.

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43

Shang, Quan, Matthew K. Liu, Monica Saumoy, Jens Juul Holst, Gerald Salen, and Guorong Xu. "The combination of colesevelam with sitagliptin enhances glycemic control in diabetic ZDF rat model." American Journal of Physiology-Gastrointestinal and Liver Physiology 302, no. 8 (April 15, 2012): G815—G823. http://dx.doi.org/10.1152/ajpgi.00295.2011.

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Bile acid sequestrants have been shown to reduce glucose levels in patients with type 2 diabetes. We previously reported that the bile acid sequestrant colesevelam HCl (Welchol) (COL) induced the release of glucagon-like peptide (GLP)-1 and improved glycemic control in insulin-resistant rats. In the present study, we tested whether adding sitagliptin (Januvia) (SIT), which prolongs bioactive GLP-1 half life, to COL would further enhance glycemic control. Male Zucker diabetic fatty (ZDF) rats were assigned to four groups: diabetic model without treatment (the model), the model treated with 2% COL or 0.4% (120 mg/day) SIT alone, or with the combination (COL+SIT). After 4 wk of treatment, the glucose area under the curve (AUC) was reduced more in the COL+SIT than the COL although both groups showed decreased glucose AUC with increased AUC of bioactive GLP-1 (GLP-1A) compared with the model group. The above changes were not observed after 8 wk. Increasing the SIT dose by 50% (180 mg SIT/day) in the diet reduced the glucose AUC in the COL+SIT group even after 8 wk but still not in the SIT alone group compared with the model. It was noteworthy that, after 8 wk, insulin levels in the SIT group declined to levels similar to the model. Histological examination of the pancreatic β-cell islets showed that islet sizes were larger, proliferation enhanced, and cell apoptosis reduced in the COL+SIT but not the SIT alone group compared with the model. We hypothesize that the combination of COL with SIT extends the half life of COL-induced GLP-1A and benefits preservation of the islets that delay the development of diabetes and improve glycemic control. This study suggests that the combined therapy (COL+SIT) is more effective than either drug alone for reducing glucose levels in diabetes.

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Sil, Diptesh, Anurupa Shrestha, Matthew R. Kimbrell, Thuan B. Nguyen, Ashok K. Adisechan, Rajalakshmi Balakrishna, Benjamin G. Abbo, et al. "Bound To Shock: Protection from Lethal Endotoxemic Shock by a Novel, Nontoxic, Alkylpolyamine Lipopolysaccharide Sequestrant." Antimicrobial Agents and Chemotherapy 51, no. 8 (June 4, 2007): 2811–19. http://dx.doi.org/10.1128/aac.00200-07.

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ABSTRACT Lipopolysaccharide (LPS), or endotoxin, a structural component of gram-negative bacterial outer membranes, plays a key role in the pathogenesis of septic shock, a syndrome of severe systemic inflammation which leads to multiple-system organ failure. Despite advances in antimicrobial chemotherapy, sepsis continues to be the commonest cause of death in the critically ill patient. This is attributable to the lack of therapeutic options that aim at limiting the exposure to the toxin and the prevention of subsequent downstream inflammatory processes. Polymyxin B (PMB), a peptide antibiotic, is a prototype small molecule that binds and neutralizes LPS toxicity. However, the antibiotic is too toxic for systemic use as an LPS sequestrant. Based on a nuclear magnetic resonance-derived model of polymyxin B-LPS complex, we had earlier identified the pharmacophore necessary for optimal recognition and neutralization of the toxin. Iterative cycles of pharmacophore-based ligand design and evaluation have yielded a synthetically easily accessible N 1,mono-alkyl-mono-homologated spermine derivative, DS-96. We have found that DS-96 binds LPS and neutralizes its toxicity with a potency indistinguishable from that of PMB in a wide range of in vitro assays, affords complete protection in a murine model of LPS-induced lethality, and is apparently nontoxic in vertebrate animal models.

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Gillies, Peter J., Jeffrey T. Billheimer, Verdell A. Blackston, Debra A. Cromley, Garret D. Figuly, Robert T. Fischer, Sandra J. Germain, et al. "DMP 504, a novel hydrogel bile acid sequestrant: II. Lipid-lowering pharmacology in the hamster." Drug Development Research 41, no. 2 (June 1997): 65–75. http://dx.doi.org/10.1002/(sici)1098-2299(199706)41:2<65::aid-ddr3>3.0.co;2-p.

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Odunsi–Shiyanbade, Suwebatu T., Michael Camilleri, Sanna McKinzie, Duane Burton, Paula Carlson, Irene A. Busciglio, Jesse Lamsam, Ravinder Singh, and Alan R. Zinsmeister. "Effects of Chenodeoxycholate and a Bile Acid Sequestrant, Colesevelam, on Intestinal Transit and Bowel Function." Clinical Gastroenterology and Hepatology 8, no. 2 (February 2010): 159–65. http://dx.doi.org/10.1016/j.cgh.2009.10.020.

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Chakraborty, Soma, Patricia Teresa F. Agbayani, and Modesto T. Chua. "Novel Chitosan Microparticles for Sequestration of Overdosed Drug." KIMIKA 28, no. 1 (July 7, 2017): 26–31. http://dx.doi.org/10.26534/kimika.v28i1.26-31.

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Chitosan microparticles were synthesized by crosslinking chitosan and glycidyl trimethylammonium chloride modified chitosan inside the reverse micelles of Span and Tween 80. The particles were of uniform size with the average diameter of 10 μm. The particles swelled almost twice the original size in 20 min when dispersed in a buffer solution of pH 7.4. The feasibility of chitosan microparticles as drug sequestrant was tested using propafenone as the model drug. The particles sequestered free propafenone from a buffer solution of pH 7.4. In 20 min unmodified chitosan and modified chitosan microparticles sequestered 53% and 51.5% of the free drug respectively. The amount of drug sequestered increased with increase in the initial free drug concentration. The presence of normal saline also improved propafenone sequestration.

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Chouikhi, Dalila, Ihor Kulai, David Bergbreiter, Mohammed Al-Hashimi, and Hassan Bazzi. "Functionalized Polyisobutylene and Liquid/Liquid Separations as a Method for Scavenging Transition Metals from Homogeneously Catalyzed Reactions." Applied Sciences 9, no. 1 (December 31, 2018): 120. http://dx.doi.org/10.3390/app9010120.

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Ethanedithiol-functionalized polyisobutylene was prepared in one step by a photoinitiated thiol-ene “click” reaction starting from ethanedithiol and polyisobutylene (PIB). The functionalized oligomer product was then used as a soluble sequestrant for transition metals. This PIB-bound thioether-thiol ligand is phase selectively soluble in alkanes and it quantitatively sequesters common transition metals like Cu2+ and Pd2+ into an alkane phase, separating them from polar solvents in a biphasic liquid/liquid separation. The chelating thioether-thiol ligand was also successfully used to remove Cu and Pd transition metal catalyst residues from products in crude reaction mixtures in both azide/alkyne click reactions and cross-coupling reactions using a liquid/liquid extraction. Separation efficiencies exceeding 95% and in many cases 99% were achieved.

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Smushkin, G., M. Sathananthan, F. Piccinini, C. Dalla Man, J. H. Law, C. Cobelli, A. R. Zinsmeister, R. A. Rizza, and A. Vella. "The Effect of a Bile Acid Sequestrant on Glucose Metabolism in Subjects With Type 2 Diabetes." Diabetes 62, no. 4 (December 18, 2012): 1094–101. http://dx.doi.org/10.2337/db12-0923.

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Katti, Sanjeev. "APPLICATION OF UF TECHNOLOGY TO LARGE-SCALE SYNTHESIS OF GT 267-004, A SEQUESTRANT FORC. DIFFICILETOXIN." Chemical Engineering Communications 194, no. 2 (February 2007): 194–204. http://dx.doi.org/10.1080/00986440600724336.

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