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A Competent Hepatocyte Model Examining Hepatitis B Virus Entry through Sodium Taurocholate Cotransporting Polypeptide as a Therapeutic Target
Published on: May 10, 2022
[Resolution of racemic anti-hepatitis drug ( +/- ) -bicyclol]
Wei Hu1, Chun-zhen Zhang, Yan Li
1Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing. hw@imm.ac.cn
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.
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