Related Experiment Video
Updated: Jun 13, 2025

Network Pharmacology Prediction and Experimental Validation of Trichosanthes-Fritillaria thunbergii Action Mechanism Against Lung Adenocarcinoma
Published on: March 3, 2023
Tripterygium-derived celastrol inhibits 5-HT3A receptors via key residue interactions: A comparative
Hye Duck Yeom1, Jihwon Yun2, Chaewon Seo3
1Department of Biotechnology and Department of Integrative Food, Bioscience and Biotechnology (BK21 FOUR), Chonnam National University, Gwangju 61186, Korea; GoPath Laboratories, Buffalo Grove, IL 60089, USA.
Abstract:
This study examines the effects of three Tripterygium wilfordii compounds-celastrol, triptolide, and triptonide-on 5-HT3A receptors. Using two-electrode voltage-clamp recordings, we found all three compounds reversibly and concentration-dependently inhibited 5-HT-induced inward currents (I5-HT), with celastrol showing the strongest inhibition (∼83 % at 100 µM) compared to triptolide (∼40 %) and triptonide (∼30 %) at 300 µM. Their voltage- and use-independent inhibition suggests they are not open-channel blockers. Further molecular docking and mutational analysis revealed celastrol binds to K127 and Y114, with mutations at these sites significantly reducing its inhibitory effect. Overall, celastrol, triptolide, and triptonide may suppress hyperactive gut signaling via 5-HT3A inhibition, with celastrol emerging as a promising therapeutic candidate.
More Related Videos
11:44Cellular Membrane Affinity Chromatography Columns to Identify Specialized Plant Metabolites Interacting with Immobilized Tropomyosin Kinase Receptor B
Published on: January 19, 2022
10:20Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
Published on: November 11, 2016
Related Concept Videos
Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists
Drugs that Stabilize Microtubules
Drugs Affecting Neurotransmitter Release or Uptake
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...