0

Identification of Three Antimicrobials Activating Serotonin Receptor 4 in Colon Cells

Emily A Yasi, Aurelia A Allen, Widianti Sugianto, Pamela Peralta-Yahya

ACS Synth Biol. 2019 Dec 20;8(12):2710-2717.

PMID: 31714751

Abstract:

The serotonin receptor 4b (5-HTR4b) is expressed throughout the gastrointestinal tract, and its agonists are used in the treatment of irritable bowel syndrome with constipation (IBS-C). Today, there are no rapid assays for the identification of 5-HTR4b agonists. Here, we developed a luciferase-based 5-HTR4b assay capable of assessing one compound per second with a 38-fold dynamic range and nM limit of detection for serotonin. We used the assay to screen more than 1000 natural products and anti-infection agents and identified five new 5-HTR4b ligands: hordenine, halofuginone, proflavine, ethacridine, and revaprazan. We demonstrate that hordenine (antibiofilm), halofuginone (antiparasitic), and revaprazan (gastric acid reducer) activate 5-HTR4b in human colon epithelial cells, leading to increased cell motility or wound healing. The 5-HTR4b assay can be used to screen larger pharmaceutical libraries to identify novel treatments for IBS-C. This work shows that antimicrobials interact not only with the gut microbiota, but also with the human host.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
LPLC81201 4-Aminophenyl-β-D-thiogalactopyranoside-Agarose 4B 4-Aminophenyl-β-D-thiogalactopyranoside-Agarose 4B Price
qrcode

We use cookies to understand how you use our site and to improve the overall user experience. This includes personalizing content and advertising. Read our Privacy Policy

Accept Cookies
x