Bile

Publication Title: 
Journal of Pharmaceutical and Biomedical Analysis

Spinosin, a major bioactive herbal ingredient isolated from Semen Ziziphi Spinosae, plays an important role in sedation and hypnosis. However, the pharmacokinetic behavior of spinosin in special sites has not been reported. Microdialysis (MD) technique, as a continuous, realtime monitoring sampling technique, is very suitable for the evaluation of the disposition of diverse drugs.

Author(s): 
Ma, Rong-Hua
Yang, Jie
Qi, Lian-Wen
Xin, Gui-Zhong
Wang, Chong-Zhi
Yuan, Chun-Su
Wen, Xiao-Dong
Li, Ping
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

[13-14C]Dihydroartemisinin was administered to male rats (35 micromol kg-1, iv). Within 0-1 hr and 0-5 hr of dosing, 34.8 +/- 5. 2% (mean +/- SD, N = 6) and 48.4 +/- 5.9% of the radiolabel, respectively, was recovered in bile. Only 1.1 +/- 1.2% was recovered in bladder urine after 5 hr. The biliary metabolites were identified by LC/MS. The principal metabolite (21.1 +/- 9.3% of dose) was the biologically inactive dihydroartemisinin (DHA) glucuronide.

Author(s): 
Maggs, J. L.
Madden, S.
Bishop, L. P.
O'Neill, P. M.
Park, B. K.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Ro 42-1611 (arteflene) is a synthetic endoperoxide antimalarial. The antimalarial activity of endoperoxides is attributed to iron(II)-mediated generation of carbon-centered radicals. An alpha, beta-unsaturated ketone (enone; 4-[2',4' bis(trifluoromethyl)phenyl]-3-buten-2-one), obtained from arteflene by reaction with iron(II), was identified previously as the stable product of a reaction that, by inference, also yields a cyclohexyl radical. The activation of arteflene in vivo has been characterized with particular reference to enone formation.

Author(s): 
Bishop, L. P.
Maggs, J. L.
O'Neill, P. M.
Park, B. K.
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

beta-Artemether (AM), the O-methyl ether prodrug of dihydroartemisinin (DHA), is an endoperoxide antimalarial. The biliary metabolites of AM in adult male Wistar rats were characterized with particular reference to potential antimalarial compounds and stable derivatives of free radical intermediates. [13-(14)C]-AM (35 micromol kg(-1), i.v.) was administered to anesthetized rats. Within 0 to 3 h, 38.6 +/- 4.8% (mean +/- S.D., n = 6) of the radiolabel was recovered in bile; the 0- to 5-h recovery was 42.3 +/- 4.3%.

Author(s): 
Maggs, J. L.
Bishop, L. P.
Edwards, G.
O'Neill, P. M.
Ward, S. A.
Winstanley, P. A.
Park, B. K.
Publication Title: 
The Journal of Nutrition

The purpose of this study was to determine whether bioflavonoid glucoside O-conjugates are absorbed from the intestine in the intact form or as their aglycones following hydrolysis by intestinal beta-glucosidases. In this study, the intestinal absorption of genistin, the beta-glucoside of the isoflavone genistein, was examined in anesthetized, adult female rats fitted with indwelling biliary cannulas. To first establish whether genistein, once absorbed, was converted into unique metabolites, genistin was infused into the femoral or portal veins and bile samples quantitatively collected.

Author(s): 
Prasain, Jeevan K.
Xu, Jun
Kirk, Marion
Smith Johnson, Michelle
Sfakianos, Jeff
Barnes, Stephen
Publication Title: 
Molecular Vision

PURPOSE: Bear bile has been used in Asia for over 3,000 years to treat visual disorders, yet its therapeutic potential remains unexplored in Western vision research. The purpose of this study was to test whether treatment of mice undergoing retinal degeneration with tauroursodeoxycholic acid (TUDCA), a primary constituent of bear bile, alters the course of degeneration. METHODS: Two retinal degeneration models were tested: the rd10 mouse, which has a point mutation in the gene encoding the beta subunit of rod phosphodiesterase, and light induced retinal damage (LIRD).

Author(s): 
Boatright, Jeffrey H.
Moring, Anisha G.
McElroy, Clinton
Phillips, Michael J.
Do, Vi T.
Chang, Bo
Hawes, Norm L.
Boyd, Amber P.
Sidney, Sheree S.
Stewart, Rachael E.
Minear, Steven C.
Chaudhury, Rajashree
Ciavatta, Vincent T.
Rodrigues, Cecilia M. P.
Steer, Clifford J.
Nickerson, John M.
Pardue, Machelle T.
Publication Title: 
Journal of Pharmaceutical and Biomedical Analysis

The purpose of this research was to develop a sensitive and reproducible UPLC-MS/MS method to analyze matrine, an anticancer compound, and to use it to investigate its biopharmaceutical and pharmacokinetic behaviors in rats. A sensitive and fast UPLC-MS/MS method was successfully applied to determine matrine in rat plasma, intestinal perfusate, bile, microsomes, and cell incubation media. The absolute oral bioavailability of matrine is 17.1+/-5.4% at a dose of 2mg/kg matrine.

Author(s): 
Yang, Zhen
Gao, Song
Yin, Taijun
Kulkarni, Kaustubh H.
Teng, Yang
You, Ming
Hu, Ming
Publication Title: 
Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences

A dynamic microdialysis sampling method with liquid chromatography-quadrupole time-of-flight mass spectrometry (Q-TOF-MS) was developed for rapid and sensitive analysis of the metabolite profile of Panax notoginseng extract (PNE) in rat bile. In vivo studies in male Sprague-Dawley rats were performed with microdialysis probes implanted into the bile duct before bile samples were collected from 0 to 12h. Metabolites of PNE were identified using dynamic adjustment of the fragmentor voltage to produce structure-relevant fragment ions.

Author(s): 
Wen, Xiao-Dong
Yang, Jie
Ma, Rong-Hua
Gao, Wen
Qi, Lian-Wen
Li, Ping
Bauer, Brent A.
Du, Guang-Jian
Zhang, Zhiyu
Somogyi, Jacqueline
Wang, Chong-Zhi
Yuan, Chun-Su
Publication Title: 
PloS One

BACKGROUND AND AIMS: Cholesterol gallstone disease is a complex process involving both genetic and environmental variables. No information exists regarding what role if any the indigenous gastrointestinal microbiota may play in cholesterol gallstone pathogenesis and whether variations in the microbiota can alter cholesterol gallstone prevalence rates. METHODS: Genetically related substrains (BALB/cJ and BALB/cJBomTac) and (BALB/AnNTac and BALB/cByJ) of mice obtained from different vendors were compared for cholesterol gallstone prevalence after being fed a lithogenic diet for 8 weeks.

Author(s): 
Fremont-Rahl, Jacqueline J.
Ge, Zhongming
Umana, Carlos
Whary, Mark T.
Taylor, Nancy S.
Muthupalani, Sureshkumar
Carey, Martin C.
Fox, James G.
Maurer, Kirk J.
Publication Title: 
Journal of Lipid Research

Hepatic outputs of biliary lipids can be measured by intestinal perfusion techniques, either during constant infusion of liquid formula into the duodenum or through-out a 24-hour period during which time three meals are given along with an overnight fast. The purpose of this study was to compare these two methods for estimating secretion of biliary lipids.

Author(s): 
Mok, H. Y.
von Bergmann, K.
Grundy, S. M.

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