Natural and synthetic flavonoid modulation of TRPC5 channels.

ABSTRACT:

Background and purpose

The TRPC5 proteins assemble to create calcium-permeable, non-selective, cationic channels. We sought novel modulators of these channels through studies of natural products.

Experimental approach

Intracellular calcium measurements and patch clamp recordings were made from cell lines. Compounds were generated by synthetic chemistry.

Key results

Through a screen of natural products used in traditional Chinese medicines, the flavonol galangin was identified as an inhibitor of lanthanide-evoked calcium entry in TRPC5 overexpressing HEK 293 cells (IC50 0.45 μM). Galangin also inhibited lanthanide-evoked TRPC5-mediated current in whole-cell and outside-out patch recordings. In differentiated 3T3-L1 cells, it inhibited constitutive and lanthanide-evoked

SUBMITTER: Naylor J 

PROVIDER: S-EPMC4728423 | biostudies-literature | 2016 Feb

REPOSITORIES: biostudies-literature