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At least 19 recordsLinked to original sources
PubMed1978

Light-scattering studies on bile acid salts I: Pattern of self-association of sodium cholate, sodium glycocholate, and sodium taurocholate in aqueous electrolyte solutions.

The pattern of association of the trihydroxy bile salts in aqueous electrolyte solutions was investigated utilizing the light-scattering technique. The turbidity of the bile salts sodium cholate, sodium taurocholate, and sodium glycocholate was determined over the concentration range of 0-25 mg/ml at 25 degrees. For sodium cholate, the concentration of the supporting electrolyte was varied from 0.15 to 0.5 M. For all bile salts in 0.15 M electrolyte, the turbidity was determined in sodium fluoride, sodium chloride, sodium bromide, and sodium iodide. Comparison of the light-scattering data with amonomer-micellar model showed that qualitative agreement was obtained; however, quantitative agreement could not be achieved. Further examination of the data showed that the light-scattering results were in good agreement with a model that includes dimers, trimers, and a higher aggregate containing approximately eight monomeric units.

Chemical Phenomena↗
PubMed1978

Solubilization of napthalene by sodium cholate and pattern of self-association of sodium cholate in 0.15 M sodium chloride.

Naphthalene solubility was determined in aqueous 0.15 M NaCl containing sodium cholate in the 0-0.05 M concentration range at 25 +/- 0.1 degrees. Sodium cholate tends to self-associate in aqueous solutions. Most often, the association pattern has been described in terms of a monomer-micellar model in which it is assumed that no association occurs below the critical micelle concentration. By comparison of the experimental solubilization curve with curves calculated on the basis of the monomer-micellar model, it was shown that this model is inappropriate for the self-association pattern of sodium cholate. The solubility data were consistent with a model that assumes that sodium cholate associates to form dimers, trimers, and higher aggregates with an average aggregation number of 7.63. Model calculations suggest that naphthalene is solubilized by dimers and higher aggregates. Solubilization of naphthalene by trimers appears to be negligible.

Cholic Acids↗
PubMed1993

Spermicidal and antiviral properties of cholic acid: contraceptive efficacy of a new vaginal sponge (Protectaid) containing sodium cholate.

Cholic acid (sodium cholate) exhibits a strong spermicidal and antiviral [anti-human immunodeficiency virus (HIV)-1] activity. The same effects are observed for F-5 Gel, the active mixture of a new contraceptive sponge (Protectaid), which contains sodium cholate in association with low concentrations (0.5%) of nonoxynol-9 and benzalkonium chloride. Both cholic acid and the F-5 Gel exert a dose-dependent, in-vitro inhibitory effect (i) on the activity of HIV-1 associated reverse transcriptase in an acellular system and (ii) on the potential of HIV-1 efficiently to infect human lymphocytes. During 12 months use, the contraceptive efficacy of the 'Protectaid' sponge was 100% in 20 young women who had chosen this method for reasons of both contraception and anti-sexually transmitted disease. No side-effects were recorded throughout this period. Cervical cultures at 6-month intervals showed the presence of Mycoplasma hominis and Candida albicans in one or two cases. The combined spermicidal and anti-HIV properties of cholic acid reported in this paper and used in the 'Protectaid' sponge offer a new and modern protective method of contraception.

Adult↗
PubMed2003

Temperature effect on formation of sodium cholate micelles.

The micellization of sodium cholate (NaC) at 293.2, 298.2, 303.2, 308.2, and 313.2 K by cholate anion concentration was studied over the pH range from 6.0 to 7.2. Using a stepwise association model of cholate anions without bound sodium counterions, the aggregation number (nmacr;) of the cholate micelles was evaluated and found to increase with the total concentration, indicating that the stepwise association model is applicable. The nmacr; values go up and down with increasing temperature; 17 at 298.2 and 12 at 313.2 K and at 60 mM of the sodium cholate. The fluorescence of pyrene was measured in sodium cholate solution to determine the critical micelle concentration (CMC), indicating a narrow concentration range for CMC. A sodium-ion-specific electrode was used to determine a relatively low degree of counterion binding to micelles, supporting the validity of the present association model of cholate anions. The aggregation numbers evaluated at a constant ionic strength of 0.15 and at lower but variable ionic strengths were similar except for higher cholate concentrations.

Journal Article↗
PubMed2006

Sodium dodecyl sulfate promoting a cooperative association process of sodium cholate with bovine serum albumin.

Sodium cholate (NaC) was used as a representative bile salt in the process of cooperative binding to bovine serum albumin (BSA) in a mixture with sodium dodecyl sulfate (SDS). The experiments were performed in 0.02 M Tris-HCl buffer solution (pH 7.50), in the presence of 0.1% BSA and at 25 degrees C. The aim of this study is to provide information on the performance of the BSA in the promotion of cooperative binding of sodium cholate promoted by the presence of SDS. The method used to monitor the binding was based on the analysis of the effect of SDS and NaC concentrations and their mixtures upon the fluorescence intensity of the BSA tryptophan residues. Plots of the fluorescence emission bands in terms of the A0/A ratio vs surfactant concentrations, where A0 and A represent the areas of emission bands in the presence and absence of the surfactants, respectively, were drawn in order to investigate the surfactant interaction with the protein. An alternative methodology, the specific conductivity vs surfactant concentration plots, was used, which involves mixtures of SDS and NaC to investigate the association processes, through the determination of the critical aggregation concentration (cac, when in the presence of protein) and the critical micellar concentration (cmc). The results led to a general conclusion that as the mixed micellar aggregates become richer in the bile salt monomer, the tendency to lose the reactivity with the protein increases. According to our results, a clear evidence of the predomination of BSA-SDS-NaC complexes is found only for the SDS molar fraction above approximately 0.6, and below this fraction a tendency toward free mixed micelles starts to predominate.

Animals↗
PubMed2003

Plastoquinones are effectively reduced by ferredoxin:NADP+ oxidoreductase in the presence of sodium cholate micelles. Significance for cyclic electron transport and chlororespiration.

The effect of sodium cholate and other detergents (Triton X-100, sodium dodecyl sulphate, octyl glucoside, myristyltrimethylammonium bromide) on the reduction of plastoquinones (PQ) with a different length of the side-chain by spinach ferredoxin:NADP(+) oxidoreductase (FNR) in the presence of NADPH has been studied. Both NADPH oxidation and oxygen uptake due to plastosemiquinone autoxidation were highly stimulated only in the presence of sodium cholate among the used detergents. Sodium cholate at the concentration of 20 mM was found to be the most effective on both PQ-4 and PQ-9-mediated oxygen uptake. The FNR-dependent reduction of plastoquinones incorporated into sodium cholate micelles was stimulated by spinach ferredoxin but inhibited by Mg(2+) ions. It was concluded that the structure of sodium cholate micelles facilitates contact of plastoquinone molecules with the enzyme and creates favourable conditions for the reaction similar to those found in thylakoid membranes for PQ-9 reduction. The obtained results were discussed in terms of the function of FNR as a ferredoxin:plastoquinone reductase both in cyclic electron transport and chlororespiration.

Anaerobiosis↗
PubMed2003

Simultaneous determination of 16 estrogens, dehydroepiandrosterone and their glucuronide and sulfate conjugates in serum using sodium cholate micelle capillary electrophoresis.

The simultaneous determination of 16 estrogens, dehydroepiandrosterone (DHEA) and their glucuronide and sulfate conjugates by micellar electrokinetic chromatography (MEKC) with sodium cholate micelle is reported. Sodium cholate, sodium dodecylsulfate (SDS) and alpha-, beta-, gamma-cyclodextrins were studied as micelle reagents in the pH range of 7.0-10.0. Estrogens, DHEA and their glucuronide and sulfate conjugates were separated using a 50 cm x 50 microm capillary with 10 mM borate-phosphate buffer (pH 8.0) containing 50 mM sodium cholate as carrier. The method could simultaneously determine 1.0-1000 microg/mL of steroids and metabolites in 100 microL of serum by photometric detection at 214 nm within 14 min and 80 ng/mL steroids could be determined by using 2.0 mL of serum. The relative standards deviations were 6.7-7.7% at 10 microg/mL in serum. The recoveries were 89.1-92.0% with 10 microg/mL serum samples.

Adult↗
PubMed1983

Effect of sodium cholate on the catalytic and structural properties of phosphorylase b.

Sodium cholate at millimolar concentration is able to induce activity in rabbit muscle phosphorylase b in the absence of AMP. The maximum activation of the enzyme in presence of 7 mM sodium cholate was 24% of that achieved by 1 mM AMP. Other bile salts tested showed a negligible activating effect. The Ka for AMP was lowered fivefold by 5 mM of the steroid detergent, while the cooperative binding of the nucleotide was abolished. Phosphorylase b', a modified form of phosphorylase in which the phosphorylation site has been removed by limited tryptic attack, presented an activation profile similar to that of phosphorylase b. In contrast, phosphorylase a was inhibited by the bile salt, while the activity of liver phosphorylase b was not significantly affected. Modification of the AMP site of the enzyme with 2,3-butanedione could not inhibit sodium-cholate-induced activity. tert-Butanol, an organic solvent activator of phosphorylase b, was found to enhance the activity induced by sodium cholate. The interaction of sodium cholate and phosphorylase b was also followed by difference spectroscopy using a fluorescein isothiocyanate--phosphorylase b conjugate. Furthermore, measurements of electron spin resonance demonstrated that the mobility of a spin-label bound at buried--NH2 groups of phosphorylase b decreases cooperatively with increasing bile salt concentration.

Adenosine Monophosphate↗
PubMed1995

Simultaneous dietary supplementation of sodium cholate and beta-carotene markedly enhances accumulation of beta-carotene in mice.

This study evaluated whether simultaneous supplementation of sodium cholate and beta-carotene to a diet enhanced the accumulation of beta-carotene in mice. For 2 wk, male ICR mice were fed either a basal diet or a diet containing Dunaliella-bardawil beta-carotene 50 mg/100g that was or was not supplemented with sodium cholate (0.25 g/100 g). The concentrations of beta-carotene in liver and plasma were approximately 5 and 10 times higher, respectively. In the mice fed the beta-carotene diet with sodium cholate than in those fed the beta-carotene diet without sodium cholate. Beta-carotene was not detectable in the liver or plasma of mice fed either basal diet. The concentrations of vitamin E in the plasma and liver of mice fed either beta-carotene diet or the basal diet with sodium cholate were significantly lower than in those fed the basal diet. In a second study, mice were fed a diet containing 50 mg/100 g synthetic beta-carotene supplemented with various concentrations of sodium cholate (0, 0.05, 0.1, 0.25, 0.5 g/100 g) for 2 wk. The concentrations of beta-carotene and vitamin E in plasma, liver and bone marrow cells were higher in mice fed the beta-carotene diet supplemented with 0.05 g/100 g of sodium cholate than in those fed the unsupplemented diet. These findings show that simultaneous supplementation of sodium cholate and beta-carotene to a diet markedly enhances the accumulation of beta-carotene. This dietary protocol may be useful to introduce a high amount of beta-carotene in the tissue of mice in a short period of time.

Animals↗
PubMed2003

Evaluation of efficiency of insulin suppository formulations containing sodium salicylate or sodium cholate in insulin dependent diabetic patients.

Two formulations of insulin suppositories were prepared to contain different amounts of sodium salicylate and sodium cholate as absorption promoters and also of insulin with the purpose of obtaining the most effective formulation in reducing plasma glucose levels after rectal administration to diabetic patients. The results show that insulin suppositories containing 100 mg sodium salicylate and 100 or 200 U of crystalline insulin showed no significant difference in AUC, Cmax and Tmax and both formulations showed significant reduction in plasma glucose level compared to initial values within 1.5-2 h. The results from experiments carried out in health volunteers showed that 100 mg sodium salicylate is the optimum amount to be included in insulin suppositories producing significantly higher Cmax and AUC compared to those produced after rectal administration of insulin suppositories containing 50 or 200 mg sodium salicylate. The results also show that using sodium cholate in 50 mg amount did not produce any significant reduction in plasma glucose levels of insulin dependent diabetic patients given suppositories containing 100 U of insulin, but this amount in suppositories containing 200 U of insulin was able to produce significant (p < 0.05) reduction in plasma glucose level within 1 h which lasted till end of experiment producing Cmax of 29.7 +/- 6.61% at Tmax of 1.5 +/- 0.61 h. On increasing the amount of sodium cholate to 100 mg in the suppositories, a marked (p < 0.01) reduction in plasma glucose level took place and the Cmax increased to 47.7 +/- 12.24% at Tmax of 1.5 +/- 0.63 h. This resulted in AUC of 86.7 +/- 22.4 mg%h which was non significantly higher from that produced after administration of suppositories containing 50 mg sodium cholate and 200 U insulin (62.5 +/- 17.6 mg%h). The results also show that insulin suppositories containing 100 mg sodium cholate and 200 U insulin resulted in a non significant differences in Cmax and AUC from those produced by S.C. injection of insulin (20 U) but significantly (p < 0.001) shorter Tmax. This formulation also shows non significant differences in Tmax and AUC and significantly (p < 0.05) higher Cmax than from those produced after rectal administration of suppositories containing 100 mg of sodium salicylate and same amount of insulin. Further more this formulation produced severe hypoglycemia in control healthy volunteers within 1 h of administration producing Cmax of 57.0 +/- 18.8% at Tmax of 0.75 +/- 0.35 h. The results of this study showed that the formulation containing 100 mg of sodium cholate and 200 U of insulin tested in fasted insulin dependent diabetic patients produced a maximum % reduction in plasma glucose levels (Cmax) of 47.7 +/- 12.24% at tmax of 1.5 +/- 0.63 h compared to Cmax of 50.56 +/- 6.8% at tmax of 2.93 +/- 0.19 h resulted after subcutaneous injection of 20 U insulin. These suppositories produced an area under the curve (AUC) of 87 +/- 22.4 mg%h compared to an AUC of 81 +/- 13.4 mg%h obtained after subcutaneous injection. This formulation of suppositories studied in 7 insulin dependent diabetic patients was found to abolish the 2-h post-prandial significant rise in plasma glucose levels after meal. These results show that these insulin suppositories containing 100 mg of sodium cholate and 200 U of insulin can serve as effective buffer against meal related hyperglycemia. The suppositories were safe, effective, accepted and well tolerated by the tested individuals.

Adult↗
PubMed1998

Equilibrium Penetration of DMPC Monolayers by Sodium Cholate.

The interaction of dimyristoyl phosphatidylcholine (DMPC) with sodium cholate was studied by equilibrium penetration measurements. Surface pressure-area isotherms for DMPC on substrates containing various concentrations of sodium cholate are presented. From these isotherms, the saturation adsorptions of the bile salt for various surface concentrations of DMPC were calculated. It is shown that the equilibrium penetration of DMPC monolayers by sodium cholate can be satisfactorily described by the accessible-area theory of McGregor and Barnes. A plot of the surface excess concentration of cholate against the inverse of the area per DMPC molecule is linear. This plot yields a value for the adsorption into the accessible areas of the monolayer-covered surface that corresponds to the adsorption of cholate in a monolayer-free surface. The cholate molecules lie flat on the air-water interface. The effective cross-sectional area of the DMPC in the mixed monolayer is similar to the area occupied by a DMPC molecule in a close-packed liquid expanded monolayer. The composition of the penetrated monolayer at different areas per DMPC molecule was calculated. The penetration of cholate into DMPC monolayers is correlated with different results taken from the literature dealing with the incorporation of bile salts into lecithin bilayers. Copyright 1998 Academic Press.

Journal Article↗
PubMed1984

Sodium cholate interactions with rabbit's pulmonary surfactant.

In order to assay the possibility that sodium cholate interacts with pulmonary surfactant, we obtained bronchoalveolar lavage fluid from lungs of adult rabbits and measured the hysteresis area of surface tension-area loops of the bronchoalveolar lavage fluid in a Wilhelmy surface tension balance, before and after the addition of sodium cholate to reach different concentrations. We observed a biphasic behavior: at a low concentration of sodium cholate (1.5 x 10(5) mol/l; n = 6) the hysteresis area increased (p less than 0.05) as compared to its control (initial) area, meanwhile at a higher concentration (5 x 10(-5) mol/l; n = 6) the hysteresis area decreased (p less than 0.025), revealing a likely interaction of sodium cholate with pulmonary surfactant. We conclude that sodium cholate is able to interact in vitro with lung surfactant.

Animals↗
PubMed2006

Enantioseparation of palonosetron hydrochloride by micellar electrokinetic chromatography with sodium cholate as chiral selector.

The enantioseparation of four stereoisomers of palonosetron hydrochloride by micellar electrokinetic chromatography using sodium cholate as chiral surfactant was described. Sodium cholate was shown to be effective in separating palonosetron hydrochloride stereoisomers. For method optimization, several parameters such as sodium cholate concentration, buffer pH and concentration, the types and concentration of organic modifiers and applied voltage, on the enantioseparation were evaluated and the optimum conditions were obtained as follows: 30 mM borate buffer (pH 9.40) containing 70 mM sodium cholate and 20% (v/v) methanol with an applied voltage of 20 kV. Under these conditions, baseline separation of palonosetron hydrochloride stereoisomers was achieved within 18 min.

Chromatography, Micellar Electrokinetic Capillary↗
PubMed1998

Micelle formation of sodium cholate and solubilization into the micelle.

The micellization of sodium cholate (NaC) was studied at 298.2 K by aqueous solubility at different pH values. Using a stepwise association model of cholate anions without the sodium counterion, the aggregation number (n) of the cholate micelle was evaluated and found to increase with the total concentration, indicating that the mass action model worked quite well. The n value at 60 mM was found equal to 16. The membrane potential measurement of sodium ion with a cation exchange membrane was made in order to confirm the low counterion binding to micelle. The solubilization of alkylbenzenes (benzene, toluene, ethylbenzene, n-propylbenzene, n-butylbenzene, n-pentylbenzene, n-hexylbenzene) and polycyclic aromatic compounds (naphthalene, anthracene, pyrene) into the aqueous micellar solution of sodium cholate was carried out. Solubilizate concentrations at equilibrium were determined spectrophotometrically at 298.2 K. The first stepwise association constants (K1) between solubilizate monomer and vacant micelle were evaluated from the equilibrium concentrations and found to increase with increasing hydrophobicity of the solubilizate molecules. From the Gibbs energy change for solubilization at the different mean aggregation numbers and from molecular structure of the solubilizates, the function of sodium cholate micelle for solubilization was discussed and was compared with data from conventional aliphatic micelles.

Micelles↗
PubMed1997

In situ aggregational state of M13 bacteriophage major coat protein in sodium cholate and lipid bilayers.

The in situ aggregational behavior of the bacteriophage M13 major coat protein was determined for the protein isolated in sodium cholate and reconstituted into DOPC lipid bilayers. For this purpose, the cysteine mutants A49C and T36C of the major coat protein were labeled with either a maleimido spin-label or a fluorescence label (IAEDANS). The steric restrictions sensed by the spin-label were used to evaluate the local protein conformation and the extent of protein-protein interactions at the position of the labeled residue. In addition, fluorescent labels covalently attached to the protein were used to determine the polarity of the local environment. The labeled coat protein mutants were examined under different conditions of protein association (amphiphile environment, ionic strength, temperature, and pH). The aggregational state of the major coat protein solubilized from the phage particle in sodium cholate was not dependent on the ionic strength, but was strongly dependent on cholate concentration and pH during sample preparation. At pH 7.0 and high sodium cholate concentration, the protein was in a dimeric form. The unusually strong association properties of the protein dimer in sodium cholate at pH 7.0 were attributed to the inability of sodium cholate to disrupt the strong hydrophobic forces between neighboring protein subunits in the phage particle. Such a "structural protein dimer" was, however, completely and irreversibly disrupted at pH 10.0. Qualitatively the same aggregational tendency was found upon changing the pH for the coat protein reconstituted in DOPC lipid bilayers. This reveals that the dimer disruption process is primarily a protein property, because there are no titratable groups on DOPC in the experimental pH range. The results are interpreted in terms of a model relating the protein aggregational state in the assembled phage to the protein aggregational behavior in sodium cholate and lipid bilayers.

Bacteriophage M13↗
PubMed1980

An analysis of the choleretic effects of infusions of sodium cholate in the guinea-pig.

The choleretic effects of infusions of sodium cholate, with and without the simultaneous infusion of taurine was compared with the choleretic effect of infusions of sodium taurocholate at rates ranging from 20--70 nmole/min. g. liver in anaesthetized guinea-pigs. Sodium cholate was secreted in bile mainly conjugated with taurine and with glycine. 10% was secreted unconjugated. Not more than 10% of the total bile salts secreted may have undergone reduction at C-3. The increase in bile flow with sodium cholate was generally greater than that with sodium taurocholate. The additional flow could not be correlated with the presence of glycocholate or free cholate in bile, and may be due to an action of cholate on biliary secretory mechanisms before the bile salt is secreted into the canaliculi.

Animals↗
PubMed1997

Promotion of oral insulin absorption in diabetic rabbits using pH-dependent coated capsules containing sodium cholate.

The hypoglycemic effect of oral insulin (40 U) capsules coated with a pH-dependent soluble polymer (Eudragit S100) and containing various doses of sodium cholate (20, 50, 100 mg) was studied in alloxan-hyperglycemic rabbits and compared with that of s.c. insulin injection (20 U). Sodium cholate (20 and 50 mg/capsule) produced a dose-related enhancement of an insulin-induced decrease in the blood glucose level. Insulin capsules containing sodium cholate (50 mg/capsule) produced a steady reduction of the blood glucose level reaching 69% of the initial values (P < 0.01) by 3 h and 48% (P < 0.001) by 5 h after administration. This capsule produced an AUC0-5 h of 125 +/- 14.8 mg.h/dl with relative hypoglycemia (R.H.) of 25.8% compared with insulin s.c. The capsules containing sodium cholate (100 mg), however, did not significantly (P > 0.05) improve the hypoglycemic effect of insulin more than the smaller dose (50 mg/capsule) producing an AUC and R.H. of 135 +/- 12.3 mg.h/dl and 27.9%, respectively. The capsule coated with Eudragit S100 and containing insulin mixed with sodium cholate seems to be a promising formulation to overcome the unavailability of oral insulin.

Administration, Oral↗