Design, synthesis, and biological evaluation of novel nitric oxide releasing dehydroandrographolide derivatives.
10.1016/S1875-5364(18)30118-3
- Author:
Lin YAN
1
;
Yu-Xuan DAI
2
;
Guo-Long GU
3
;
Miao-Bo PAN
2
;
Shuai-Cong WU
2
;
Yu CAO
4
;
Wen-Long HUANG
5
,
6
Author Information
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. Electronic address: 2692327139@qq.com.
5. State Key Laboratory of Natural Medicines, Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China
6. Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, Nanjing 210009, China. Electronic address: ydhuangwenlong@126.com.
- Publication Type:Journal Article
- Keywords:
Anticancer;
Nitric oxide;
Tehydroandrographolide
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
Cell Proliferation;
drug effects;
Diterpenes;
chemistry;
pharmacology;
Drug Design;
Drug Screening Assays, Antitumor;
Humans;
K562 Cells;
MCF-7 Cells;
Nitric Oxide;
chemistry;
pharmacology;
Structure-Activity Relationship
- From:
Chinese Journal of Natural Medicines (English Ed.)
2018;16(10):782-790
- CountryChina
- Language:English
-
Abstract:
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 (IC 1.55 μmol·L) and MCF-7 (IC 2.91 μmol·L) 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.
