L6250

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Cerebrovascular dilation via selective targeting of the cholane steroid-recognition site in the BK channel β1-subunit by a novel nonsteroidal agent.

Anna N Bukiya et al.

Molecular pharmacology, 83(5), 1030-1044 (2013-03-05)

The Ca(2+)/voltage-gated K(+) large conductance (BK) channel β1 subunit is particularly abundant in vascular smooth muscle. By determining their phenotype, BK β1 allows the BK channels to reduce myogenic tone, facilitating vasodilation. The endogenous steroid lithocholic acid (LCA) dilates cerebral

Hairless modulates ligand-dependent activation of the vitamin D receptor-retinoid X receptor heterodimer.

Masayuki Chuma et al.

Biological & pharmaceutical bulletin, 35(4), 582-587 (2012-04-03)

The active form of vitamin D, 1α,25-dihydroxyvitamin D(3) [1,25(OH)(2)D(3)], binds to the vitamin D receptor (VDR) and regulates various physiological and pharmacological processes. Secondary bile acids, such as lithocholic acid (LCA), also act as endogenous VDR ligands. The molecular basis

Specific bile acids inhibit hepatic fatty acid uptake in mice.

Biao Nie et al.

Hepatology (Baltimore, Md.), 56(4), 1300-1310 (2012-04-26)

Bile acids are known to play important roles as detergents in the absorption of hydrophobic nutrients and as signaling molecules in the regulation of metabolism. We tested the novel hypothesis that naturally occurring bile acids interfere with protein-mediated hepatic long

Ursodeoxycholic acid reduces antitumor immunosuppression by inducing CHIP-mediated TGF-β degradation.

Yingying Shen et al.

Nature communications, 13(1), 3419-3419 (2022-06-15)

TGF-β is essential for inducing systemic tumor immunosuppression; thus, blocking TGF-β can greatly enhance antitumor immunity. However, there are still no effective TGF-β inhibitors in clinical use. Here, we show that the clinically approved compound ursodeoxycholic acid (UDCA), by degrading

Comparative transcriptomic analysis of multiple cardiovascular fates from embryonic stem cells predicts novel regulators in human cardiogenesis.

Yang Li et al.

Scientific reports, 5, 9758-9758 (2015-05-23)

Dissecting the gene expression programs which control the early stage cardiovascular development is essential for understanding the molecular mechanisms of human heart development and heart disease. Here, we performed transcriptome sequencing (RNA-seq) of highly purified human Embryonic Stem Cells (hESCs)

Calcium- and voltage-gated potassium (BK) channel activators in the 5β-cholanic acid-3α-ol analogue series with modifications in the lateral chain.

Anna N Bukiya et al.

ChemMedChem, 7(10), 1784-1792 (2012-09-05)

Large conductance, calcium- and voltage-gated potassium (BK) channels regulate various physiological processes and represent an attractive target for drug discovery. Numerous BK channel activators are available. However, these agents usually interact with the ubiquitously distributed channel-forming subunit and thus cannot

Highly lipophilic 3-epi-betulinic acid derivatives as potent and selective TGR5 agonists with improved cellular efficacy.

Xiao-yin Wang et al.

Acta pharmacologica Sinica, 35(11), 1463-1472 (2014-10-07)

TGR5 is a G protein-coupled receptor that is expressed in intestinal L-cells and stimulates glucagon-like peptide 1 (GLP-1) secretion. TGR5 may represent a novel target for the treatment of metabolic disorder. Here, we sought to design and synthesize a series

Aspirated bile: a major host trigger modulating respiratory pathogen colonisation in cystic fibrosis patients.

F J Reen et al.

European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology, 33(10), 1763-1771 (2014-05-13)

Chronic respiratory infections are a leading global cause of morbidity and mortality. However, the molecular triggers that cause respiratory pathogens to adopt persistent and often untreatable lifestyles during infection remain largely uncharacterised. Recently, bile aspiration caused by gastro-oesophageal reflux (GOR)

Ultra high resolution SFC-MS as a high throughput platform for metabolic phenotyping: application to metabolic profiling of rat and dog bile.

Michael D Jones et al.

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 966, 200-207 (2014-05-13)

Ultra high resolution SFC-MS (on sub-2μm particles) coupled to mass spectrometry has been evaluated for the metabolic profiling of rat and dog bile. The selectivity of the SFC separation differed from that seen in previous reversed-phase UPLC-MS studies on bile

Lithocholic acid extends longevity of chronologically aging yeast only if added at certain critical periods of their lifespan.

Michelle T Burstein et al.

Cell cycle (Georgetown, Tex.), 11(18), 3443-3462 (2012-08-17)

Our studies revealed that LCA (lithocholic bile acid) extends yeast chronological lifespan if added to growth medium at the time of cell inoculation. We also demonstrated that longevity in chronologically aging yeast is programmed by the level of metabolic capacity

[Effects of intestinal flora on the expression of cytochrome P450 3A in the liver].

Makoto Ishii et al.

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 132(3), 301-310 (2012-03-03)

Living organisms eliminate foreign low-antigenic substances, such as drugs and environmental pollutants, by detoxification mediated by metabolizing cytochrome P450 (CYP). We have examined the possible regulation of CYP expression by enteric bacteria. Cyp mRNA expression levels, Cyp3a protein expression level

Combination Therapy of Placenta-Derived Mesenchymal Stem Cells with WKYMVm Promotes Hepatic Function in a Rat Model with Hepatic Disease via Vascular Remodeling.

Ji Hye Jun et al.

Cells, 11(2) (2022-01-22)

Changes in the structure and function of blood vessels are important factors that play a primary role in regeneration of injured organs. WKYMVm has been reported as a therapeutic factor that promotes the migration and proliferation of angiogenic cells. Additionally

Detection and elimination of a novel non-toxigenic Clostridioides difficile strain from the microbiota of a mouse colony.

Jeffrey R Maslanka et al.

Gut microbes, 12(1), 1-15 (2020-12-12)

Clostridioides difficile is an enteric bacterial pathogen that can a cause nosocomial infection leading to debilitating colitis. The development of a murine model of C. difficile infection has led to fundamental discoveries in disease pathogenesis and the host immune response

Primary bile acid activates Egr‑1 expression through the MAPK signaling pathway in gastric cancer.

Su-Mi Lee et al.

Molecular medicine reports, 25(4) (2022-02-17)

Bile acids have been linked to pathomechanism and prognosis in various types of cancers. The present study aimed to investigate the effect of bile acids on the molecular change in gastric epithelial cancer cells and to evaluate gastric bile acid

TGR5 signaling mitigates parenteral nutrition-associated liver disease.

Kent A Willis et al.

American journal of physiology. Gastrointestinal and liver physiology, 318(2), G322-G335 (2020-01-07)

Bile acid receptors regulate the metabolic and immune functions of circulating enterohepatic bile acids. This process is disrupted by administration of parenteral nutrition (PN), which may induce progressive hepatic injury for unclear reasons, especially in the newborn, leading to PN-associated

Deciphering the role of charge, hydration, and hydrophobicity for cytotoxic activities and membrane interactions of bile acid based facial amphiphiles.

Manish Singh et al.

Biochimica et biophysica acta, 1828(8), 1926-1937 (2013-04-18)

We synthesized four cationic bile acid based facial amphiphiles featuring trimethyl ammonium head groups. We evaluated the role of these amphiphiles for cytotoxic activities against colon cancer cells and their membrane interactions by varying charge, hydration and hydrophobicity. The singly

Bile Acids Signal via TGR5 to Activate Intestinal Stem Cells and Epithelial Regeneration.

Giovanni Sorrentino et al.

Gastroenterology, 159(3), 956-968 (2020-06-03)

Renewal and patterning of the intestinal epithelium is coordinated by intestinal stem cells (ISCs); dietary and metabolic factors provide signals to the niche that control ISC activity. Bile acids (BAs), metabolites in the gut, signal nutrient availability by activating the

TGR5 signalling inhibits the production of pro-inflammatory cytokines by in vitro differentiated inflammatory and intestinal macrophages in Crohn's disease.

Kazuaki Yoneno et al.

Immunology, 139(1), 19-29 (2013-04-10)

Bile acids (BAs) play important roles not only in lipid metabolism, but also in signal transduction. TGR5, a transmembrane receptor of BAs, is an immunomodulative factor, but its detailed mechanism remains unclear. Here, we aimed to delineate how BAs operate

Dysbiosis-Induced Secondary Bile Acid Deficiency Promotes Intestinal Inflammation.

Sidhartha R Sinha et al.

Cell host & microbe, 27(4), 659-670 (2020-02-27)

Secondary bile acids (SBAs) are derived from primary bile acids (PBAs) in a process reliant on biosynthetic capabilities possessed by few microbes. To evaluate the role of BAs in intestinal inflammation, we performed metabolomic, microbiome, metagenomic, and transcriptomic profiling of

Lithocholic bile acid accumulated in yeast mitochondria orchestrates a development of an anti-aging cellular pattern by causing age-related changes in cellular proteome.

Adam Beach et al.

Cell cycle (Georgetown, Tex.), 14(11), 1643-1656 (2015-04-04)

We have previously revealed that exogenously added lithocholic bile acid (LCA) extends the chronological lifespan of the yeast Saccharomyces cerevisiae, accumulates in mitochondria and alters mitochondrial membrane lipidome. Here, we use quantitative mass spectrometry to show that LCA alters the

Effect of probiotics on serum bile acids in patients with ulcerative colitis.

Shinji Sato et al.

Hepato-gastroenterology, 59(118), 1804-1808 (2012-03-01)

Evaluation of bile acids (BA) is useful for assessing the changes of intestinal flora in patients with ulcerative colitis (UC). During enterohepatic circulation, the intestinal micro flora cause 7 alpha-dehydroxylation of cholic acid (CA) and chenodeoxycholic acid (CDCA), yielding deoxycholic

Potentiation of temozolomide cytotoxicity by inhibition of DNA polymerase beta is accentuated by BRCA2 mutation.

Gregory C Stachelek et al.

Cancer research, 70(1), 409-417 (2009-12-24)

Base excision repair (BER) plays a critical role in the repair of bases damaged by oxidative metabolism or alkylating agents, such as those commonly used in cancer therapy. Incomplete BER generates intermediates that require activation of homology-dependent DNA repair to

Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.

Hai-Bing He et al.

Bioorganic & medicinal chemistry letters, 22(23), 7237-7242 (2012-10-17)

Protein tyrosine phosphatase 1B (PTP1B) is a major negative regulator of both insulin and leptin signals. For years, inhibiting of PTP1B has been considered to be a potential therapeutics for treating Type 2 diabetes and obesity. Recently, we recognized lithocholic

Lithocholic acid, cholestasis, and liver disease.

J E King et al.

Mayo Clinic proceedings, 47(10), 725-730 (1972-10-01)

Lipidomics investigation of reversal effect of glycyrrhizin (GL) towards lithocholic acid (LCA)-induced alteration of phospholipid profiles.

Jing-Chun Han et al.

Pharmaceutical biology, 52(12), 1624-1628 (2014-10-08)

Glycyrrhizin (GL), the major ingredient isolated from licorice, exerts multiple pharmacological activities. To elucidate the protective mechanism of GL towards lithocholic acid (LCA)-induced liver toxicity using lipidomics. GL (200 mg/kg) dissolved in corn oil was treated intraperitoneally for 7 d. On the

Qingchang Huashi Formula attenuates DSS-induced colitis in mice by restoring gut microbiota-metabolism homeostasis and goblet cell function.

Jingyi Hu et al.

Journal of ethnopharmacology, 266, 113394-113394 (2020-09-18)

Inflammatory bowel disease (IBD) is a chronic and relapsing inflammatory disease of the gastrointestinal tract, consisting of ulcerative colitis (UC) and Crohn's disease (CD). Gut microbiota and their metabolites may play a role in the pathogen of IBD, especially of

Evaluation of cynomolgus monkeys for the identification of endogenous biomarkers for hepatic transporter inhibition and as a translatable model to predict pharmacokinetic interactions with statins in humans.

Xiaoyan Chu et al.

Drug metabolism and disposition: the biological fate of chemicals, 43(6), 851-863 (2015-03-31)

Inhibition of hepatic transporters such as organic anion transporting polypeptides (OATPs) 1B can cause drug-drug interactions (DDIs). Determining the impact of perpetrator drugs on the plasma exposure of endogenous substrates for OATP1B could be valuable to assess the risk for

Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs.

Charlotte Avet et al.

eLife, 11 (2022-03-19)

The recognition that individual GPCRs can activate multiple signaling pathways has raised the possibility of developing drugs selectively targeting therapeutically relevant ones. This requires tools to determine which G proteins and βarrestins are activated by a given receptor. Here, we

Novel surfactants with diglutamic acid polar head group: drug solubilization and toxicity studies.

Nathalie Ménard et al.

Pharmaceutical research, 29(7), 1882-1896 (2012-03-28)

Novel surfactants made of diglutamic acid (DG) polar head linked to lithocholic, arachidonic, linoleic or stearic acids were designed for drug solubilization. Surfactants 3-D conformer and packing parameter were determined by molecular modelling and self-assembling properties by pyrene fluorescence measurements.

Macromitophagy is a longevity assurance process that in chronologically aging yeast limited in calorie supply sustains functional mitochondria and maintains cellular lipid homeostasis.

Vincent R Richard et al.

Aging, 5(4), 234-269 (2013-04-05)

Macromitophagy controls mitochondrial quality and quantity. It involves the sequestration of dysfunctional or excessive mitochondria within double-membrane autophagosomes, which then fuse with the vacuole/lysosome to deliver these mitochondria for degradation. To investigate a physiological role of macromitophagy in yeast, we

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