J Neurogastroenterol Motil.  2014 Oct;20(4):469-474. 10.5056/jnm14010.

Effects of GC7101, a Novel Prokinetic Agent on Gastric Motor Function: Ex Vivo Study

• Jung DH
• Choi EJ
• Jeon HH
• Lee YH
• Park H

• KMID: 2381210
• DOI: http://doi.org/10.5056/jnm14010

Abstract

BACKGROUND/AIMS
GC7101, an extract of Lonicera Flos, is a novel developing drug for reflux esophagitis and functional dyspepsia. However, the drug's exact pharmacological mechanism of action remains unclear. This study assessed the effects of GC7101 on gastrointestinal (GI) motor function.
METHODS
We used male guinea pigs to evaluate the effects of GC7101 on GI motility. The contraction of antral circular muscle in the presence of different doses of GC7101 was measured in a tissue bath. The prokinetic effects of GC7101 were tested using the charcoal transit assay from the pylorus to the most distal point of migration of charcoal mixture. To clarify the mechanism of action of GC7101, atropine, dopamine and the selective 5-hydroxytryptamine 4 receptor antagonist, GR113808 were used.
RESULTS
The maximal amplitude of circular muscle contraction was induced by 5 mg mL(-1) GC7101. The area under the curve of contraction was significantly increased at 5 mg mL(-1) GC7101. Addition of 10(-6) M atropine, 10(-8) M dopamine or 10(-7) M GR 113808 to GC7101 5 mg mL(-1) decreased the amplitude and area under curve compared to GC7101 5 mg mL(-1) alone. GC7101 accelerated GI transit in a dose dependent manner except 100 mg kg(-1). Delayed GI transit caused by atropine, dopamine and GR 113808 was restored by GC7101 50 mg kg(-1).
CONCLUSIONS
GC7101, an extract of Lonicera Flos, exerts a gastric prokinetic effect in guinea pig through cholinergic, antidopaminergic and serotonergic mechanisms. Therefore, GC7101 might be a novel drug for the treatment of functional dyspepsia.

Keyword

Functional dyspepsia; Gastrointestinal motility; Lonicera Flos; Prokinetic

MeSH Terms

Animals
Area Under Curve
Atropine
Baths
Charcoal
Dopamine
Dyspepsia
Esophagitis, Peptic
Gastrointestinal Motility
Guinea Pigs
Humans
Lonicera
Male
Muscle Contraction
Pylorus
Serotonin
Atropine
Charcoal
Dopamine
Serotonin