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Cell‐based screening for discovery of prostaglandin (PG) E1 agonist and PGE2 antagonist from dietary TMC herbs
Author(s) -
Chillar Annirudha J,
Mohite Anita J,
Ruan KeHe
Publication year - 2010
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.24.1_supplement.lb493
Subject(s) - prostaglandin e2 receptor , agonist , antagonist , pharmacology , inverse agonist , receptor , prostaglandin e2 , receptor antagonist , prostaglandin e , chemistry , medicine , biochemistry
Cell‐based screening for discovery of prostaglandin (PG) E1 agonist and PGE2 antagonist from dietary TMC herbs Annirudha J Chillar, Anita J Mohite, Ke‐He Ruan Centre for Experimental Therapeutics and Pharmacoinformatics, Department of Pharmacological and Pharmaceutical sciences, College of Pharmacy, University of Houston, and Houston, Texas 77004 The prostaglandin (PG) E1 (PGE1) and PGE2 acting through EP receptors (EP1, EP2, EP3 and EP4) are involved in a variety of biological functions. PGE1 is a potent anti‐inflammatory molecule whereas PGE2 is inflammatory and cancer mediators. Little information is available for the dietary herbs with PGE1 agonist or PGE2 antagonist properties. In this study, a HEK293 cell line expressing EP1 receptor stably was created by gene transferring and G418 screening. A highly sensitive fluorescence calcium signaling mediated by the EP1 receptor expressed in the cell line was created and used as indicator for identification of the dietary TMC herbs with PGE1 agonist and PGE2 antagonist activities. Six herbs that demonstrated PGE2 antagonist activity inhibited the PGE2 signal and seven herbs with PGE1 agonist activity, mimicked PGE1 signaling were identified by a wide range screening started from 96 TMC dietary herbs. In conclusion, the established cell line stably expressing EP1 receptor can be used as a cell‐based target screening for discovery of PGE1 agonist and PGE2 antagonist. Many anti‐inflammatory and anti cancer ingredients are present in the dietary TMC herbs, which have potential to be further developed into preventive and therapeutic interventions against inflammation and cancers. Funded by NIH grant‐ R01HL56712 (For KHR); RO1HLO79389 (For KHR).