Relationship Between Pharmacological Potency and Surface Activity of Cholic Acid Analogs

Zhang, T.H.; Lin, Jenn-Wei; Liu, C.G.; Ding, Ru; Ruan, Jin Xiu; Sun, Xiaohong; Huang, Chunqian; Zhang, X.C.

doi:10.3923/ijp.2008.407.409

Cited by 3 publications

(1 citation statement)

References 5 publications

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“…taurine and BAs, were multicomponent with large differences in polarity and molecular structure. 32 A suitable extraction solvent system was required to ensure successful establishment of methodology. Taurine and some BAs such as CA and DCA can be completely dissolved in water due to strong polarity, while other BAs with weaker polarity can be easily dissolved in methanol or acetonitrile.…”

Section: Optimization Of Extraction Conditionsmentioning

confidence: 99%

Development of a rapid and simple LC-MS/MS method for identification and quality control of natural Calculus bovis and Calculus bovis sativus

Feng

Zhang

et al. 2015

Anal. Methods

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Calculus bovis sativus (C. bovis sativus, CBS), with the same pharmacodynamics activities as those of natural C. bovis (CB), has been approved as an ideal substitute in China. However, in the latest edition of the Chinese Pharmacopoeia, only cholic acid and bilirubin are used as the markers for quality control. To overcome current limitations and to further improve its quality control method, a rapid and reliable method was herein developed for simultaneous qualitative and quantitative analyses of taurine and twelve bile acids (BAs) in natural CB and CBS by liquid chromatography coupled with tandem mass spectrometry. Taurine and BAs were separated using a Diamonsil C 18 column (150 mm Â 2.1 mm i.d., 5 mm) with acetonitrile:water containing 10 mM ammonium acetate (pH 3) as mobile phase in a gradient elution program. Mass spectra were obtained in the negative ion mode through multiple reaction monitoring of respective mass transitions. This method had satisfactory separation efficiency, high sensitivity, little potential interference, and short running time. The average recoveries ranged from 93.0% to 107.3%, with relative standard deviations of less than 9.0% for all thirteen analytes of interest. Taurine and characteristic BAs, especially conjugated BAs, may partially reflect the internal quality of CBS and natural CB. Combining the ratios of cholic acid/deoxycholic acid and unconjugated BAs/conjugated BAs with quantitative data of single BA and chromatographic profiles may be able to control the quality of CBS. In conclusion, this method can be used for explicit identification and quality control of CBS and natural CB.

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Section: Optimization Of Extraction Conditionsmentioning

confidence: 99%

Development of a rapid and simple LC-MS/MS method for identification and quality control of natural Calculus bovis and Calculus bovis sativus

Feng

Zhang

et al. 2015

Anal. Methods

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Plasma membrane as the target site of cholic acid analogs

et al. 2011

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Although the mechanism is unknown, Calculus Bovis and its active components, cholic acid analogs (CAAs), have been used in China to treat a wide range of diseases. Based on the previous finding that the potency of CAA is strongly dependent on the intrinsic surface activity, this paper aimed to investigate the role of the plasma membrane in the pharmacological activity of CAAs. First, CAAs (0.1 mM) caused a surface activity-dependent depression on ATPase activity in the cell membrane extract, but it had no effects on other cellular extracts, suggesting an indispensable role of the membrane environment for pharmacological activity. Second, CAAs lowered the membrane fluidity of cultured Caco-2 cells with the same rank-order of potency sequence. Third, the hypothesis that any functional protein located on the membrane is influenced by changes in cellular membrane fluidity was supported by: ileal contraction that was induced by acetylcholine and mediated by the muscarinic receptor (M-receptor) or the relaxation induced by adrenaline and mediated by the β-adrenergic receptor (β-receptor) was inhibited by CAAs. They also had similar rank-order of potency and the effects on the plasma membrane. Collectively, the plasma membrane may be a target for the CAAs to exert the multiple pharmacological effects which are mediated by the alteration of the membrane mobility and the function of integral membrane proteins.

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A novel “target constituent knock-out” strategy coupled with TLC, UPLC–ELSD and microcalorimetry for preliminary screening of antibacterial constituents in Calculus bovis

Kong

Wang

Zang

et al. 2011

Journal of Chromatography B

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Relationship Between Pharmacological Potency and Surface Activity of Cholic Acid Analogs

Cited by 3 publications

References 5 publications

Development of a rapid and simple LC-MS/MS method for identification and quality control of natural Calculus bovis and Calculus bovis sativus

Development of a rapid and simple LC-MS/MS method for identification and quality control of natural Calculus bovis and Calculus bovis sativus

Plasma membrane as the target site of cholic acid analogs

A novel “target constituent knock-out” strategy coupled with TLC, UPLC–ELSD and microcalorimetry for preliminary screening of antibacterial constituents in Calculus bovis

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