Natural products are essential sources of antitumor drugs.One such molecule,β-elemene,is a potent antitumor compound extracted from Curcuma wenyujin.In the present investigation,a series of novel 13,14-disubstituted ...Natural products are essential sources of antitumor drugs.One such molecule,β-elemene,is a potent antitumor compound extracted from Curcuma wenyujin.In the present investigation,a series of novel 13,14-disubstituted nitric oxide(NO)-donorβelemene derivatives were designed,withβ-elemene as the foundational compound,and subsequently synthesized to evaluate their therapeutic potential against leukemia.Notably,the derivative labeled as compound 13d demonstrated a potent anti-proliferative activity against the K562 cell line,with a high NO release.In vivo studies indicated that compound 13d could effectively inhibit tumor growth,exhibiting no discernible toxic manifestations.Specifically,a significant tumor growth inhibition rate of 62.9%was observed in the K562 xenograft tumor mouse model.The accumulated data propound the potential therapeutic application of compound 13d in the management of leukemia.展开更多
基金This project was supported by the Natural Science Foundation of Zhejiang province(No.LY20H300004)the National Natural Science Foundation of China(Nos.82073686,81730108,and 81973635)+1 种基金Scientific Research Foundation for Scholars of HZNU(Nos.2021QDL026 and 2019QDL003)the Ministry of Science and Technology of China(High-end foreign experts program,Nos.G20200217005 and G2021017004).
文摘Natural products are essential sources of antitumor drugs.One such molecule,β-elemene,is a potent antitumor compound extracted from Curcuma wenyujin.In the present investigation,a series of novel 13,14-disubstituted nitric oxide(NO)-donorβelemene derivatives were designed,withβ-elemene as the foundational compound,and subsequently synthesized to evaluate their therapeutic potential against leukemia.Notably,the derivative labeled as compound 13d demonstrated a potent anti-proliferative activity against the K562 cell line,with a high NO release.In vivo studies indicated that compound 13d could effectively inhibit tumor growth,exhibiting no discernible toxic manifestations.Specifically,a significant tumor growth inhibition rate of 62.9%was observed in the K562 xenograft tumor mouse model.The accumulated data propound the potential therapeutic application of compound 13d in the management of leukemia.
