Possible Interaction: Acetylcholine and Berberine

“Both CCF and berberine suppressed the cellular calcium influx and ROCK-1 expression upon ACh stimulation, demonstrating that berberine was one of the active compounds that contributed to CCF-improved micturition symptoms and function.”

“Extracts of ZJW and RC and berberine , palmatine and jatrorrhizine, components of RC, all inhibited CA secretion and rise in [Ca(2+)](i) induced by acetylcholine ( ACh ), veratridine (Ver) and/or 56 mM K(+).”

“On the other hand, berberine as well as PAP exhibited a noncompetitive inhibition of the contractile response induced by ACh , whereas ATR showed a competitive inhibition.”

“The results suggest that berberine increases ileal contractility by: 1) increasing acetylcholine release from the postganglionic parasympathetic nerve terminal, 2) increasing acetylcholine retention through an inhibition of cholinesterase activity, and 3) blocking alpha 2-adrenoceptors, possibly in the postganglionic parasympathetic nerve.”

“At higher concentration, berberine (1 x 10(-4) M) facilitated a rightward shift of the dose-response curve of acetylcholine with a reduction of maximum response, indicating that the interactions of the two agents changed from competitive to noncompetitive antagonism.”

“Lower concentrations of berberine (less than or equal to 5 x 10(-5) M) induced a parallel rightward shift of the dose-response curve of acetylcholine , suggesting that berberine is antagonizing the actions of acetylcholine at the receptors competitively.”

“The contraction induced by acetylcholine was competitively inhibited by atropine (PA2 = 8.7), whereas berberine , which differs basically from atropine, shifted the dose-response curve for acetylcholine non-parallelly to the right with its maximal response reduced concomitantly.”

“The effects of phenylephrine and acetylcholine were blocked by berberine as well as by atropine.”

“The contraction induced by acetylcholine was competitively inhibited by atropine (PA2 = 8.7), whereas berberine , which differs basically from atropine, shifted the dose-response curve for acetylcholine non-parallelly to the right with its maximal response reduced concomitantly.”

“The effects of phenylephrine and acetylcholine were blocked by berberine as well as by atropine.”

“Treatment with berberine inhibited acetylcholinesterase activity, and upregulated acetylcholine levels in the serum and alpha7 nicotinic acetylcholine receptor gene expression in the liver tissue.”

“Additionally, acetylcholine levels were enhanced after berberine treatment in diabetic rats.”

“Application of Ber reversed the APD shortening induced by ACh (APD50: 81 ± 10 vs. 134 ± 15 msec; APD90: 132 ± 13 vs: 213 ± 17 msec, both P<0.01).”

“The induced rate of sustained 1 min AF was lower during ACh infusion with Ber than during ACh infusion alone (4/10 vs. 30/35, P<0.01).”