[Resolution of racemic anti-hepatitis drug ( +/- ) -bicyclol]

Yao Xue Xue Bao. 2006 Mar;41(3):221-4.
[Article in Chinese]

Abstract

Aim: To study the different biological activities of the enantiomers of the anti-hepatitis drug (+/-)-bicyclol, the (+/-)-bicyclol was resolved.

Methods: By being treated with optically active alkaloid, the two diastereoisomers alkaloid salts of the compound could be obtained, separately. After decomposing and methylating, they were transformed separately into (-)-bicyclol and (+)-bicyclol.

Results: The two enantiomers of bicyclol were determined by melting point, [alpha]D, 1H NMR, MS and chiral column HPLC.

Conclusion: Comparison of hepatoprotective action of racemic bicyclol and (-)-, (+)-bicyclol on experimental liver injury, the effect of (-)-bicyclol was two times more potent than that of racemic bicyclol and the potency of (+)-bicyclol was much less than that of the racemate.

Publication types

  • Comparative Study

MeSH terms

  • Alanine Transaminase / blood
  • Animals
  • Aspartate Aminotransferases / blood
  • Biphenyl Compounds / chemical synthesis
  • Biphenyl Compounds / chemistry*
  • Biphenyl Compounds / pharmacology
  • Carbon Tetrachloride Poisoning
  • Chemical and Drug Induced Liver Injury / blood*
  • Chemical and Drug Induced Liver Injury / etiology
  • Mice
  • Molecular Structure
  • Optical Rotation
  • Stereoisomerism

Substances

  • Biphenyl Compounds
  • bicyclol
  • Aspartate Aminotransferases
  • Alanine Transaminase