Yao xue xue bao = Acta pharmaceutica Sinica · 2006
[Resolution of racemic anti-hepatitis drug ( +/- ) -bicyclol].
Сравнительное исследованиеСтатьяНазвание и аннотация: Перевод в очереди
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Hu Wei, Zhang Chun-zhen, Li Yan
Аннотация
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.
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.