Chemical constituents and pharmacological action of bile acids from animal:a review / 中国中药杂志

Bile of animal(mainly chicken, pig, snake, cow, and bear) has long been used as medicine. As the major active components of bile, bile acids mainly include cholic acid, deoxycholic acid, chenodeoxycholic acid, ursodeoxycholic acid, and taurochenodeoxycholic acid. They interact with intestinal microorganisms in enterohepatic circulation, thereby playing an important part in nutrient absorption and allocation, metabolism regulation, and dynamic balance. Bile acids have pharmacological effects such as protecting liver, kidney, heart, brain, and nerves, promoting bile secretion, dissolving gallstones, anti-cancer, relieving cough and dyspnea, dispelling phlegm, treating eye diseases, and regulating intestinal function and blood glucose, which are widely used in clinical practice. This study summarized and analyzed the research on the chemical constituents and pharmacological effects of bile acids from medicinal animals, in a bid to provide scientific basis and reference for the further development and utilization of bile acids.

Qualitative and quantitative analysis of major cholic acids in Suis Fellis Pulvis / 中国中药杂志

This study is to establish a qualitative method for rapid identification of bile acids in Suis Fellis Pulvis based on UHPLC-LTQ-Orbitrap-MS technology,and an HPLC-ELSD internal standard method for the quantitative determination of two glycine-conjugated BAs in Suis Fellis Pulvis.The chromatographic separation of the UHPLC-LTQ-Orbitrap-MS qualitative analysis was achieved on a Waters Acquity UPLC HSS T_3column(2.1 mm×100 mm,1.8μm),with 0.2%formic acid aqueous solution(A)-acetonitrile(B)as mobile phase ingradient elution.Electrospray ionization(ESI)source was applied and operated in negative ion mode.Quantitative analysis was performed at 30℃on a Diamonsil-C_(18)column(4.6 mm×250 mm,5μm).The mobile phase consisted of 0.2%formic acid solution and acetonitrile with gradient elution and the flow rate was 1.0 m L·min~(-1).An ELSD was used with a nitrogen flow-rate of1.4 L·min~(-1)at a drift tube temperature of 60℃and the gain was 1.A total of 14 bile acids in Suis Fellis Pulvis were characterized based on the accurate mass measurements,fragmentation patterns,chromatographic retention times,and reference materials.For the quantitative analysis method,the glycohyodeoxycholic acid and glycochenodeoxycholic acid had good linear relationship in the range of26.52-265.20 mg·L~(-1)(r=0.999 8)and 19.84-198.40 mg·L~(-1)(r=0.999 1),respectively.The average recoveries(n=6)were104.1%and 103.1%,and the RSD were 2.0%and 2.4%.The UHPLC-LTQ-Orbitrap-MS technology provides a fast and efficient qualitative analysis method for identification of bile acids in Suis Fellis Pulvis.The HPLC-ELSD internal standard method is accurate and reliable,which has reference value for the quality control of Suis Fellis Pulvis.

Safety, beneficial and technological properties of Enterococcus faecium isolated from Brazilian cheeses

This study aimed to characterize the safety and technological properties of Enterococcus faecium strains isolated from Brazilian Coalho cheeses. High levels of co-aggregation were observed between Enterococcus faecium strains EM485 and EM925 and both Escherichia coli and Clostridium perfringens. Both strains presented low levels of hydrophobicity. E. faecium EM485 and EM925 were both able to grow in the presence of 0.5% of the sodium salts of taurocholic acid (TC), taurodeoxycholic acid (TDC), glycocholic acid (GC), and glycodeoxycholic acid (GDC), although they showed the ability to deconjugate only GDC and TDC. Both strains showed good survival when exposed to conditions simulating the gastro intestinal tract (GIT). When tested for the presence of virulence genes, only tyrosine decarboxylase and vancomycin B generated positive PCR results.

A novel method for studying nuclear localization signal-mediated nuclear translocation / 南方医科大学学报

<p><b>OBJECTIVE</b>To establish a new method for studying the mechanism of nuclear localization signal (NLS)-mediated nuclear translocation in living cells.</p><p><b>METHODS</b>The cells were treated with 67 mg/L 3-[(3-Cholamidopropyl)dimethylammonio]propanesulfonate (CHAPS), followed by incubation with 1 g/L wheat germ agglutinin (WGA), and their effects on interferon- γ (IFN-γ)-induced nuclear translocation of signal transducer and activator of transcription 1 (STAT1) were observed.</p><p><b>RESULTS</b>Treatment with CHAPS alone had no effect on IFN-γ-induced nuclear translocation of STAT1, while this process was blocked by further WGA incubation.</p><p><b>CONCLUSION</b>We established a new, simple but effective method for studying the mechanism of NLS-mediated nuclear translocation in living cells by perforating the cell membrane with CHAPS treatment.</p>

Primary Biliary Cirrhosis / 대한간학회지

Primary biliary cirrhosis (PBC) is a chronic cholestatic autoimmune liver disease that predominantly affects middle-aged women. It is characterized by slowly progressive destruction of the small intrahepatic bile ducts together with portal inflammation, and this initially leads to fibrosis and later to cirrhosis. It is currently accepted that the pathogenesis of PBC is multifactorial with genetic and environmental factors interplaying to determine the disease onset and progression. In addition to antimitochondrial antibody (AMA), which is the hallmark of PBC and is detected in at least 90% of the patients, other autoantibodies (antinuclear antibody, anti-smooth muscle antibody and rheumatoid factor, etc.) may also be found in the patients. There is no correlation between the titer of AMAs and the disease severity. Most patients are diagnosed either during the asymptomatic phase of PBC or after presenting with non-specific symptoms. Pruritus and fatigue are the most common symptoms of PBC. The prognosis of PBC has improved significantly during the last few decades. Patients are now diagnosed earlier in its clinical course, they are more likely to be asymptomatic at diagnosis and they are more likely to receive medical treatment. A wide variety of drugs have been assessed for the treatment of this condition: such immunosuppressive agents as corticosteroids, cyclosporine and azathioprine have a weak effect on the disease's natural history. Ursodeoxycholic acid (UDCA) is the only currently approved medical treatment. For PBC patients with end-stage liver disease or an unacceptable quality of life, liver transplantation is the only accepted therapeutic option. Early diagnosis and treatment of PBC are important because effective treatment with UDCA has been shown to delay disease progression and improve rate survival in the early stage.

Bile Acid Analysis in Biliary Tract Canacer

The etiology of biliary tract cancer is obscure, but there are evidences that bile acid plays a role in carcinogenesis. To find the association between biliary tract cancer and bile acid, this study compared the bile acid concentration and composition among patients with biliary cancer, biliary tract stones, and no biliary disease. Bile was compared among patients with biliary tract cancer (n = 26), biliary tract stones (n = 29), and disease free controls (n = 9). Samples were obtained by percutaneous transhepatic biliary drainage, endoscopic nasobiliary drainage, or gallbladder puncture, and analyzed for cholic, deoxycholic, chenodeoxycholic, lithocholic, and ursodeoxycholic acid composition. Total bile acid concentration was lower in the cancer group than the biliary stone and control groups; the proportions of deoxycholic (2.2% vs. 10.2% and 23.6%, p < 0.001 and p < 0.001, respectively) and lithocholic acid (0.3% vs. 0.6% and 1.0%, p = 0.065 and p < 0.001, respectively) were also lower. This result was similar when disease site was limited to bile duct or gallbladder. Analysis of cases with bilirubin < or = 2.0 mg/dL also showed lower total bile acid concentration and deoxycholic acid composition in the cancer group compared to controls (5.7% vs. 23.6%, p = 0.003). Although the presence of bile duct obstruction explains some of the difference in total concentration and composition of bile acid, there are other contributing mechanisms. We suspect the alteration of bile acid transport might decrease bile acid excretion and cause the accumulation of carcinogenic bile acid in bile duct epithelium.

Bile Acid Analysis in Biliary Tract Canacer

The etiology of biliary tract cancer is obscure, but there are evidences that bile acid plays a role in carcinogenesis. To find the association between biliary tract cancer and bile acid, this study compared the bile acid concentration and composition among patients with biliary cancer, biliary tract stones, and no biliary disease. Bile was compared among patients with biliary tract cancer (n = 26), biliary tract stones (n = 29), and disease free controls (n = 9). Samples were obtained by percutaneous transhepatic biliary drainage, endoscopic nasobiliary drainage, or gallbladder puncture, and analyzed for cholic, deoxycholic, chenodeoxycholic, lithocholic, and ursodeoxycholic acid composition. Total bile acid concentration was lower in the cancer group than the biliary stone and control groups; the proportions of deoxycholic (2.2% vs. 10.2% and 23.6%, p < 0.001 and p < 0.001, respectively) and lithocholic acid (0.3% vs. 0.6% and 1.0%, p = 0.065 and p < 0.001, respectively) were also lower. This result was similar when disease site was limited to bile duct or gallbladder. Analysis of cases with bilirubin < or = 2.0 mg/dL also showed lower total bile acid concentration and deoxycholic acid composition in the cancer group compared to controls (5.7% vs. 23.6%, p = 0.003). Although the presence of bile duct obstruction explains some of the difference in total concentration and composition of bile acid, there are other contributing mechanisms. We suspect the alteration of bile acid transport might decrease bile acid excretion and cause the accumulation of carcinogenic bile acid in bile duct epithelium.

Application of magnetic resonance DW imaging technique in studying treatment of cerebral ischemia in rats by single or combined use of jasminoidin and cholalic acid / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To estimate the therapeutic effect of single or combined use of jasminoidin and cholalic acid on focal cerebral ischemia rat with magnetic resonance-diffusion-weighted imaging (MR-DWI) technique, ultra-microscopy, and neuro-behavior scoring.</p><p><b>METHODS</b>The model of cerebral ischemia-reperfusion injury was induced by string method. Three hours after reperfusion, MR-DWI was applied with ultra-microscopy and neuro-behavior test to give evaluation on cerebral ischemic rats, and pathologic, ultramicroscopic observation of tissue were taken as adjuvant measures to comprehensively evaluate the pharmacological effect on ischemia-reperfusion rats and delimit the efficacy of the two different components and their combination.</p><p><b>RESULTS</b>Compared with the model group, ADC and DCavg values of the foci in all the treated groups had the incrensing trend. There was significant difference arund the foci in the group of combined use of jasminoidin and cholalic acid (P < 0.05).</p><p><b>CONCLUSION</b>Combined use of jasminoidin and cholalic acid had protective effects on nerve and brain. MR-DWI technique accompanied with ultramicroscopic observation of tissues and neuro-behavior test is an effective method for evaluating the effect of neuro-protective agent.</p>

Interaction of sodium dehydrocholate and sodium cholate with polyvinyl pyrrolidone in aqueous medium.

The results of interaction of the bile salts sodium dehydrocholate (NaDHC) and sodium cholate (NaC) with the water soluble polymer polyvinyl pyrrolidone (PVP) studied by the methods of conductance, surface tension, viscosity and calorimetry are reported. Both of the bile salts exhibited PVP influenced self-aggregation. While NaC showed expected surface tension behaviour, NaDHC exhibited anomalous behaviour. The minimum interfacial area per molecule of the bile salt, the maximum interfacial adsorption, the free energy of micellization and the free energy of interfacial adsorption are presented for NaC. This information was not obtained for NaDHC because of its anomalous surface tension behaviour. The bile-salt-adhered PVP exhibited polyelectrolyte behaviour at PVP concentrations < 0.25 g dl-1. The enthalpy of interaction of NaC with PVP had a maximum at 0.25 mole dm-3 (delta Hi = +180 cal/mole); NaDHC produced too little heat to be detected by the calorimeter.

Hypolipidemic action of taurine in rats.

The effect of taurine on the serum and liver cholesterol and triglyceride levels was studied in rats fed cholesterol plus cholic acid. Four groups of 4 weeks old rats were fed control diet, hypercholesterolemic diet (HCD), HCD + 1% taurine or HCD + 2% taurine for 8 weeks. Addition of taurine in HCD diet showed a significant reduction not only in serum total cholesterol and triglyceride levels but also in liver total cholesterol, lipid and triglyceride contents compared to the animals fed HCD alone. Histological examination of organs of these animals showed severe fatty vacuolation in livers and signet ring type vacuolation in kidneys of rats fed HCD. Taurine showed ameliorating effect on these abnormalities. The animals fed taurine in HCD also showed increased bile and sterol excretion in faeces compared to rats fed HCD alone. Taurine showed significant hypocholesterolemia in rats probably by enhancing the catabolism of cholesterol and reducing the absorption of dietary cholesterol.

Efecto de los ácidos biliares sobre la contractibilidad miometral en útero gestante aislado / Effect of bile acids on myometral contractility of isolated pregnant uterus

Usando un bioensayo tipo cascada nosotros estudiamos el efecto de los ácidos biliares sobre la contracción del útero aislado de ratas preñadas (día 19). Tanto el ácido cólico como deoxicólico a concentraciones entre 2 y 20 *M, causaron una estimulación significativa y dosis-dependiente de la contracción uterina (p<0,0001). El efecto máximo se alcanzó con una concentración de 15 *M. Ambos ácidos biliares fueron también estudiados en un medio libre de calcio y en presencia de calcio más indometacina. La oxitocina fue también administrada bajo las mismas condiciones. La ausencia de calcio en el medio de perfusión, inhibió la actividad uterina inducida por ambos ácidos biliares, en cambio la indometacina sólo logró reducir la contractibilidad levemente y en forma no significativa. El efecto de la oxitocina no fué modificado ni por la ausencia de calcio, ni por la presencia de indometacina. Nosotros concluímos que tanto el ácido cólico como el deoxicólico estimulan la actividad uterina in vitro y sugerimos que dichos agentes aumentan la entrada de calcio a la miocélula, ya sea alterando la arquitectura de la membrana plasmática o penetrando a la célula como complejos calcio-ácidos biliares