Structural modification and properties of cannabidiol
Alzheimer's disease(AD)is a neurodegenerative disease,and its treatment mechanism mainly involves inhibiting the activity of cholinesterase(ChE),increasing choline function and neuronal transmission.The natural product cannabidiol(CBD)has potential neuroprotective effects.CBD amino acid derivative(CB8)was synthesized in one step by esterification reaction with CBD as raw material,and its activity was tested in vitro.The results show that,CB8 has moderate antioxidant capacity,inhibiting tyrosinase activity(IC50=(1.02±0.13)μmol/L)and inhibiting cholinesterase activity(acetyl cholinesterase(AChE)IC50=(134.62±0.41)μmol/L,butyryl cholinesterase(BuChE)IC50=(1.02±0.13)μmol/L).Moreover,the inhibitory activity against butyryl cholinesterase was 4 times higher than that of the commercially available drug donepezil.At the same time,the toxicity of CB8 to PC12 cells was comparable to donepezil at(6.25～100 μmol/L)concentrations,demonstrating the potential of CB8 in the treatment of Alzheimer's disease.
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