The invention discloses a high-water-
solubility paclitaxel compound chemically modified by diaconitic acid molecules as well as a synthesis method and application of the
paclitaxel compound chemically modified by the diaconitic acid molecules. The
paclitaxel compound comprises paclitaxel and two
aconitic acid molecules which are covalently bonded through ester bonds; the water-soluble paclitaxel compound is simple and convenient in preparation method and suitable for industrial production, paclitaxel
drug molecules have amphiphilic properties, namely hydrophilicity and
lipophilicity after being structurally modified by the method, the water
solubility and the permeability are improved, the possibility of developing various oral and
aerosol inhalation drug preparations is provided, and the compound is high in water
solubility at normal temperature, low in cost and suitable for industrial production. According to the present invention, the prepared paclitaxel compound has characteristics of no foam generation during
dissolution, more than 8 mg / ml, no need of any co-
solvent, compound
toxicity lower than the original
drug paclitaxel, and
ester bond accelerated
hydrolysis fracture under the weak acid condition of the
in vivo tumor tissue, such that the compound has advantages of certain
tumor tissue targeting, good
bioavailability and good anti-tumor effect.