Nuclear receptor agonist activity studies on some Plantago species and Scutellaria salviifolia Benth.: A particular focus on liver x receptor alpha and retinoid x receptor alpha connected with the inflammation process


KUTLUAY V. M. , GENÇ Y., DOĞAN Z. , Inoue M., SARAÇOĞLU İ.

Journal of Research in Pharmacy, vol.26, no.2, pp.272-278, 2022 (Refereed Journals of Other Institutions) identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 2
  • Publication Date: 2022
  • Doi Number: 10.29228/jrp.125
  • Title of Journal : Journal of Research in Pharmacy
  • Page Numbers: pp.272-278
  • Keywords: anti-inflammatory, liver x receptor, Plantago, retinoid x receptor, Scutellaria

Abstract

© 2022 Marmara University Press.Nuclear receptors are a superfamily of transcription factors that regulate gene transcription and intracellular function. They have a key role in various biological processes. Liver X receptors (LXR) mainly play role in lipid metabolism, cholesterol synthesis, glucose homeostasis, and inflammation whereas retinoid X receptor alpha (RXRα) plays important role in inflammation and immunity. In this study, Plantago holosteum, P. major subsp. major, P. lagopus, P. scabra, and Scutellaria salviifolia were selected for further investigation due to their anti-inflammatory activities. For this purpose, liver x receptor alpha (LXRα) and retinoid x receptor alpha (RXRα) agonist activity of the extracts was determined through luciferase reporter gene assay on HEK293 cells at a concentration of 100 µg/ml. P. holosteum, P. major subsp. major, P. lagopus, and P. scabra extracts showed weak LXRα agonist activity with the fold values in a range of 0.95-1.39. P. major showed the highest agonist activity among tested Plantago species. For LXRα agonist activity, S. salviifolia extract had a fold value of 2.37 which was comparable to the positive control T09011317 at 10 nM concentration. Results for RXRα agonist activity found to be similar to LXRα for all extracts. S. salviifolia showed the highest RXRα agonist activity with a fold value of 1.62. Results suggested that Scutellaria species, which are used as traditional medicine especially in eastern Asia due to its anti-inflammatory effects, might show this effect due to LXRα activation.