Syntheses and bioactivities of songorine derivatives as novel G protein-coupled receptor antagonists |
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| Authors: | Jiangming Wang Changhao Bian Yinan Wang Quan Shen Bin Bao Junting Fan Aixue Zuo Wenhui Wu Ruihua Guo |
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| Institution: | 1. College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China;2. College of Traditional Chinese Medicine, Yunnan University of Chinese Medicine, Kunming 650500, China;3. Shanghai Engineering Research Center of Aquatic-Product Processing & Preservation, Shanghai 201306, China;4. Laboratory of Quality and Safety Risk Assessment for Aquatic Products on Storage and Preservation (Shanghai), Ministry of Agriculture, Shanghai 201306, China;5. School of Pharmacy, Nanjing Medical University, Nanjing 211166, China |
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| Abstract: | Songorine isolated from Aconitum brachypodum Diels possesses prominent activity of inhibiting G protein-coupled receptors (GPCRs) in the early screening process. In this paper, a series of Songorine derivatives were synthesized and their inhibitory activities on GPCRs were also evaluated by using the Double Antibody Sandwich ELISA (DAS-ELISA) in vitro. Among them, three derivatives (3a, 4, 7) exhibited significant inhibitory activity against GPCRs with IC50 values of 0.08–0.29?nM. Moreover, the structure-activity relationships (SARs) of songorine derivatives were discussed in detail. They have great potentials as novel GPCRs antagonists in the future. |
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| Keywords: | Songorine Derivatives G protein-coupled receptors Inhibition Synthesis |
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