CN: 32-1845/R
ISSN: 2095-6975
Cite this paper:
YAN Lin, DAI Yu-Xuan, GU Guo-Long, PAN Miao-Bo, WU Shuai-Cong, CAO Yu, HUANG Wen-Long. Design, synthesis, and biological evaluation of novel nitric oxide releasing dehydroandrographolide derivatives[J]. Chinese Journal of Natural Medicines, 2018, 16(10): 782-790

Design, synthesis, and biological evaluation of novel nitric oxide releasing dehydroandrographolide derivatives

YAN Lin1, DAI Yu-Xuan2, GU Guo-Long3, PAN Miao-Bo2, WU Shuai-Cong2, CAO Yu4, HUANG Wen-Long2,5
1 Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, Kaifeng 475004, China;
2 State Key Laboratory of Natural Medicines, Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China;
3 School of Pharmacy, Yancheng Teachers University, Yancheng 224007, China;
4 Department of Dermatology, First Affiliated Hospital of Guizhou Medical University, Guiyang 550025, China;
5 Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, Nanjing 210009, China
A series of new hybrids of dehydroandrographolide (TAD), a biologically active natural product, bearing nitric oxide (NO)-releasing moieties were synthesized and designated as NO-donor dehydroandrographolide. The biological activities of target compounds were studied in human erythroleukemia K562 cells and breast cancer MCF-7 cells. Biological evaluation indicated that the most active compound I-5 produced high levels of NO and inhibited the proliferation of K562 (IC50 1.55 μmol·L-1) and MCF-7 (IC50 2.91 μmol·L-1) cells, which were more potent than the lead compound TAD and attenuated by an NO scavenger. In conclusion, I-5 is a novel hybrid with potent antitumor activity and may become a promising candidate for future intensive study.
Key words:    Tehydroandrographolide    Nitric oxide    Anticancer   
Received: 2018-05-21   Revised:
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