The invention discloses a
rheum emodin double-chain biquaternary
ammonium salt with the anti-
cancer activity and a preparation method of the
rheum emodin double-chain biquaternary
ammonium salt. The
rheum emodin double-chain biquaternary
ammonium salt is a mixture of a rheum
emodin 1,3-site biquaternary ammonium salt and a rheum
emodin 3,8-site biquaternary ammonium salt. The preparation method comprises the following steps: performing Williamson etherification reaction on rheum
emodin and p-
benzyl bromide in the presence of K2CO3 so as to generate a mixture of 1,3-site dibromomethylbenzyl rheum emodin and 3,8-site dibromomethylbenzyl rheum emodin, and further reacting the dibromomethylbenzyl rheum emodin mixture with
tertiary amine so as to obtain the mixture of 1,3-site biquaternary ammonium salt and rheum emodin 3,8-site biquaternary ammonium salt, wherein the two biquaternary ammonium salts are isomerides which cannot be separated on a
chromatographic column. The anti-
cancer activity evaluation shows that the activity of the rheum emodin double-chain biquaternary ammonium salt disclosed by the invention is higher than that of monoquaternary ammonium salt, and the rheum emodin double-chain biquaternary ammonium salt can be used in a
medicine for treating malignant tumor, is particularly applicable to treatment on
liver cancer, has a relatively small inhibition effect on normal cells, and has relatively great application prospect.