Related Experiment Video
Updated: Jul 17, 2025
10:20
In vitro Measurements of Tracheal Constriction Using Mice
Published on: June 25, 2012
20.8K
Eriodictyol and thymonin act as GPR35 agonists
Fumie Nakashima1, Wei Qi Loh1, Mayuka Wakabayashi1
1Graduate School of Bioagricultural Sciences, Nagoya University, Nagoya, Japan.
Bioscience, Biotechnology, and Biochemistry
|September 5, 2023
Summary
Thyme contains compounds that activate G protein-coupled receptor 35 (GPR35), potentially explaining its traditional health benefits. Researchers identified eriodictyol and thymonin as key GPR35 agonists from thyme extracts.
Area of Science:
- Pharmacology
- Natural Products Chemistry
- Molecular Biology
Background:
- Herbs and spices have long been used in traditional medicine, but their mechanisms of action are often unclear.
- G protein-coupled receptor 35 (GPR35) is implicated in antioxidant and anti-inflammatory processes.
- Understanding GPR35's role could elucidate the health benefits of botanicals.
Purpose of the Study:
- To screen various herbs and spices for GPR35 agonists.
- To identify specific compounds within botanicals that modulate GPR35 activity.
- To investigate the GPR35-dependent functions of herbs and spices.
Main Methods:
- Screening of 19 different herb and spice extracts for GPR35 agonistic activity.
- Activity-guided fractionation of thyme extract.
- Identification and characterization of active phytochemicals using biochemical assays.
Main Results:
- The ethyl acetate extract of thyme demonstrated significant GPR35 agonistic activity.
- Two polyphenolic compounds, eriodictyol and thymonin, were identified as GPR35 agonists.
- Both compounds exhibited potent and specific agonist activity with low micromolar EC50 values.
Conclusions:
- Eriodictyol and thymonin from thyme are identified as novel GPR35 agonists.
- These phytochemicals may mediate the health benefits of thyme through GPR35 activation.
- Further research into GPR35 modulation by natural compounds is warranted.
Related Concept Videos
01:27Transducer Mechanism: Enzyme-Linked Receptors
2.5K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.5K
01:09GPCRs Regulate Adenylyl Cylase Activity
5.7K
Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
5.7K
01:30Transducer Mechanism: G Protein–Coupled Receptors
2.1K
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
GPCRs are also called heptahelical,...
2.1K
01:30Adrenergic Agonists: Direct-Acting Agents
1.6K
Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine.
These agents can be classified...
These agents can be classified...
1.6K
01:25Antiasthma Drugs: β2-Adrenoceptor Agonists
298
Bronchodilators are critical in managing asthma, a chronic respiratory condition characterized by airway constriction due to inflammation and hyper-reactivity. Specifically, bronchodilators ease this constriction by relaxing the bronchial muscles, facilitating easier breathing.
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce...
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce...
298
01:15G Protein-coupled Receptors
12.2K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
12.2K