Synthesis and in vitro evaluation of kidney-targeted prodrug triptolide-glucosamine conjugate
LIU Chang
HE Shan-shan
ZHANG Zhi-rong
Abstract：Objective: Synthesizing kidney-target triptolide-glucosamine conjugates through different bonds linked to C14-OH of triptolide, and evaluating their stability and in vitro activities. Methods: Designing and synthesizing triptolide-glucosamine conjugate via carbonate bond (TPG-2) and comparing it with triptolideglucosamine conjugate via ester bond (TPG-1) to find an appropriate compound to evaluate its cell toxicity and uptake ability. Results: In vitro stability test showed that TPG-1 was better. TPG-1 could obviously reduce the cytotoxicity and increase the cell uptake ability. Conclusion: It is feasible to build a small molecule kidneytargeted triptolide-glucosamine conjugates by C14-OH of triptolide.
Keywords：triptolideC14-OHkidney-targetedtoxicitybond
Publication Date：2018-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：6( 1787-1792 )