| abstract |
The invention relates to the technical field of medicine, in particular to a prodrug of triptolide targeting inducible nitric oxide synthase (iNOS) and its preparation method and application. The R of the triptolide targeting prodrug is L-arginine, L-arginine methyl ester, L-N ω -NO-arginine, L-N ω -NO-arginine methyl ester , L-guanidine, L-thioguanine, L-lysine or L-ornithine. The present invention utilizes the characteristics of high expression of inducible nitric oxide synthase (iNOS) at the site of inflammation, uses iNOS specific substrate (group) to semi-synthesize triptolide to prepare prodrug, and reduces triptolide prodrug through its targeting properties. Toxicity and bioavailability of rattolide are improved, and its anti-inflammatory effect is significantly better than that of triptolide, which can realize the effective development and utilization of triptolide. |