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Study on preparation and interferon inducing activity of tilorone dihydrochloride

[Objectives]The aim of this paper was to make preparation and quality investigation of tilorone dihydrochloride. On the other hand,drug effect on induction of interferon was also primarily proved. [Methods]Tilorone was synthesized by the substitution reaction of 2,7-dihydroxy-9H-fluoren-9-one with 2-diethylaminoethyl chloride hydrochloride,which was then acidified to give tilorone dihydrochloride. The structure of target compound was characterized by Infrared Spectroscopy（ IR）, 1 H Nuclear Magnetic Resonance（ 1 H MNR） and mass spectrum（ MS）. By the method of pharmacopeia,physiochemical properties and content determination were identified in sequence for primary specification establishment. Tilorone dihydrochloride was dissolved at suitable concentration permitting an inoculum of 250 mg·kg -1 （ mice） orally. After tilorone challenged,mice were bled for IFN-α1assay via ELISA method.[Results]Tilorone dihydrochloride was synthesized in good yield of 93% and stable for quality control. In addition,tilorone could characteristically induce an unusually delayed and prolonged interferon response with peak level of 2 000 pg·m L -1 observed from12 h to 24 h. [Conclusions]The compound was efficient to prepare,and was stable and effective to induce obvious interferon responses,which will have broader prospects of development.