The invention discloses an
apigenin betaine compound and a preparation method thereof. According to the compound,
apigenin (Api) is taken as a parent
nucleus, hydroxyl groups at the 7 position, the 4'position and / or the 5 position of the
apigenin (Api) are substituted by-O-(CH2) n-N + (CH3) 2-CH2COO-fragments (n is equal to 2-12, and x is equal to 1-3), so that an inner salt type zwitterionic structure is formed. The preparation method comprises the following steps: firstly, carrying out
Mitsunobu reaction on apigenin and brominated
alcohol Br (CH2) nOH under the condition of
triphenylphosphine / dialkyl azodicarboxylate to obtain mono / polysubstituted
bromine-containing alkoxy apigenin; and then carrying out
nucleophilic substitution with N, N-
dimethylglycine under an alkaline condition to obtain a target product. The structure has an adjustable
alkyl chain and a
betaine cation / anion pair, the
solubility and hydration capacity of apigenin in a water /
alcohol medium are remarkably improved, and the affinity and stability of apigenin to a
biological membrane are enhanced, so that in-vivo absorption and distribution are improved, and the activities of
oxidation resistance,
inflammation resistance and the like of apigenin are expected to be maintained. The method is mild in condition, wide in
solvent and temperature range and suitable for amplification and preparation application.