Abstract
Many Western drugs can give rise to serious side effects due to their ability to bind to acetylcholine receptors in the brain. This aggravates when they are combined, which is known as anticholinergic accumulation (AA). Some bioactives in Traditional Chinese Medicine (TCM) are known to block acetylcholine receptors and thus potentially cause AA. The AA of TCM was screened by quantifying the displacement of [3H] pirenzepine on acetylcholine receptors in a rat brain homogenate. We used a new unit to express AA, namely the Total Atropine Equivalents (TOAT). The TOAT of various herbs used in TCM was very diverse and even negative for some herbs. This is indicative for the broadness of the pallet of ingredients used in TCM. Three TCM formulas were screened for AA: Ma Huang Decotion (MHD), Antiasthma Simplified Herbal Medicine intervention (ASHMI), and Yu Ping Feng San (YPFS). The TOAT of ASHMI was indicative for an additive effect of herbs used in it. Nevertheless, it can be calculated that one dose of ASHMI is probably too low to cause AA. The TOAT of YPFS was practically zero. This points to a protective interaction of AA. Remarkably, MHD gave a negative TOAT, indicating that the binding to the acetylcholine receptors was increased, which also circumvents AA. In conclusion, our results indicate that TCM is not prone to give AA and support that there is an intricate interaction between the various bioactives in TCM to cure diseases with minimal side effects.
Highlights
Acetylcholine receptors (AChRs), or cholinergic receptors, are important targets in pharmacotherapy
We propose a new unit, Total Atropine Equivalents (TOAT), to estimate and express the binding of Traditional Chinese Medicine (TCM) toward muscarinic AChRs on the rat brain membrane
A radioligand binding assay interpreted using the TOAT seems a convenient way to screen for AA of TCM
Summary
Acetylcholine receptors (AChRs), or cholinergic receptors, are important targets in pharmacotherapy. They are located in parasympathetic and sympathetic ganglia and in the brain. AA may lead to dry mouth, blurred vison, falls, urinary disorders, impulsive behavior, and even cognitive impairment and delirium [6,7,8]. This is especially relevant for the elderly due to polypharmacy, changes in brain neurochemistry, and changes in pharmacokinetics and pharmacodynamics in this frail group [9,10,11]
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