Screening of active compounds as neuromedin U2 receptor agonist from natural products.
Reporter cell lines are often used for high-throughput screening of natural product libraries or chemical libraries to identify new receptor ligands. Screening of neuromedin U2 receptor (NMU2R) ligands may be very useful to treat obesity for the reason that centrally administered neuromedin U affects feeding behavior, energy expenditure, and pituitary. Here, we have developed a stable cell line of neuromedin U2 receptor (NMU2R) to screen for its agonist. The experimental results demonstrate that icariin, isolated from Herba epimedii, was a strong agonist for NMU2R, which could selectively activate NMU2R, but not M1R, MC4R, and negative cell lines.
Zheng
Xuxu
X
Research Center of Medicinal Chemistry and Chemical Biology, Chongqing Technology and Business University, Chongqing 400067, China. xuxuzheng@ctbu.edu.cn
Hu
Yinghe
Y
Liu
Jianhui
J
Ouyang
Keqing
K
D001483:Base Sequence; D001688:Biological Products / Q000737:chemistry*; D002460:Cell Line; D017931:DNA Primers; D004305:Dose-Response Relationship, Drug; D004734:Energy Metabolism; D005247:Feeding Behavior / Q000187:drug effects; D005419:Flavonoids / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008156:Luciferases / Q000235:genetics; D008565:Membrane Proteins / Q000819:agonists*; D010902:Pituitary Gland / Q000187:drug effects; D017981:Receptors, Neurotransmitter / Q000819:agonists*
D001688:Biological Products; D017931:DNA Primers; D005419:Flavonoids; D008565:Membrane Proteins; D017981:Receptors, Neurotransmitter; C082444:neuromedin U receptor; D008156:Luciferases; C056599:icariin