Abstract
Biphenyl neolignans such as honokiol and magnolol, which are the major active constituents of the Asian medicinal plant Magnolia officinalis, are known to exert a multitude of pharmacological and biological activities. Among these, cytotoxic and tumor growth inhibitory activity against various tumour cell lines are well-documented. To further elucidate the cytotoxic effects of honokiol derivatives, derivatizations were performed using tetrahydrohonokiol as a scaffold. The derivatizations comprised the introduction of functional groups, e.g., nitro and amino groups, as well as alkylation. This way, 18 derivatives, of which 13 were previously undescribed compounds, were evaluated against CCRF-CEM leukemia cells, U251 glioblastoma and HCT-116 colon cancer cells. The results revealed no significant cytotoxic effects in any of the three tested cell lines at a test concentration of 10 µM.
Highlights
Occurring biphenyl neolignans such as honokiol (1) and the isomeric magnolol from the bark of Asian species of Magnolia (e.g., M. officinalis Rehd. et Wils. and M. obovata Thunb.) are considered the active principle in various multi-herb compositions of Chinese materia medica.Cortex Magnoliae officinalis (Hou Po) is listed in the Chinese Pharmacopoeia as a stomachic, an antihistamine, a sedative and used to treat cough and asthma, diarrhea and gastric ulcers [1,2].Especially honokiol, 4'-O-methylhonokiol and further derivatives of honokiol are known for a great variety of biological and pharmacological activities [3]
The biphenyl neolignan scaffold shows structural characteristics such as flexibility combined with partial rigidity and the presence of certain functional groups [9,10]
The results indicated that neither honokiol nor any of the derivatives showed a significant cytotoxic effect at this concentration (Figure 1)
Summary
Occurring biphenyl neolignans such as honokiol (1) and the isomeric magnolol from the bark of Asian species of Magnolia (e.g., M. officinalis Rehd. et Wils. and M. obovata Thunb.) are considered the active principle in various multi-herb compositions of Chinese materia medica.Cortex Magnoliae officinalis (Hou Po) is listed in the Chinese Pharmacopoeia as a stomachic, an antihistamine, a sedative and used to treat cough and asthma, diarrhea and gastric ulcers [1,2].Especially honokiol, 4'-O-methylhonokiol and further derivatives of honokiol are known for a great variety of biological and pharmacological activities [3]. Occurring biphenyl neolignans such as honokiol (1) and the isomeric magnolol from the bark of Asian species of Magnolia M. obovata Thunb.) are considered the active principle in various multi-herb compositions of Chinese materia medica. Biphenyl-type compounds are considered to be privileged structures, i.e., molecules that provide extraordinary binding properties toward proteinous targets. The biphenyl neolignan scaffold shows structural characteristics such as flexibility combined with partial rigidity and the presence of certain functional groups [9,10]. It provides an ideal scaffold for derivatizations that may be employed in structure activity relationship studies
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