Mode of Action

Finding out how it works

Mode of action studies are an important milestone in our product development process. The mode of action of an ingredient is a crucial rational to design a human study and to demonstrate overall evidence. Mode of action studies are mainly in vitro and ex vivo studies.

Vital Solutions carries out mode of action studies during the product development process. For ingredients, where the phytochemical standardization is not sufficient to demonstrate batch to batch activity, additional mode of action studies are selected and validated for standard quality control.

Studies are carried out in-house as well as with external partners.

Bioassay plates

Example. Bioassay-guided selection of raw material for Bluenesse®

History of Lemon balm for cognitive health

Research demonstrated effects of Lemon balm on cognitive performance. Surprisingly human studies reported that not all Lemon balm extracts show these beneficial cognitive effects, even if the extracts have similar phytochemical specifications (standardization on rosmarinic acid).

In order to clarify this several in vitro studies were carried out to understand the mode of action behind the beneficial effects on cognitive performance of Lemon balm and how they differ from extracts with the traditional calming effects. Studies showed that the traditional relaxing effects may be linked to elevated levels of the neurotransmitter GABA (γ-Aminobutyric acid) by inhibition of GABA-transaminase (GABA T), an enzyme which degrades GABA. Rosmarinic acid is described to be responsible for this effect. The antioxidant protection provided by Lemon balm shows promises in reducing oxidative-related brain cell death which contributes to the development of degenerative diseases.

It is known that CNS (central nervous system) cholinergic binding affinity to nicotinic and muscarinic receptors improves cognitive performance, e.g. attention, action selection, learning and memory improvement. Particularly the muscarinic receptors as part of the cholinergic system have been investigated for cognitive effects. Activation of muscarinic receptors helps to improve cognitive processing by synchronization of oscillatory activity (rhythmic activity of neurons) and the consequent transition of the brain from a deactivated to an activated status. Disruption of oscillatory activity leads to cognitive deficits. Muscarinic M1 receptor agonists are used as modulators for normal cognitive functions and reversal of cognitive deficits.

Melissa (Lemon balm) close up
Melissa officinalis cultivation for Bluenesse

Vital Solutions research

Vital Solutions screened Melissa officinalis special extract obtained from different lemon balm breeding lines on muscarinic M1 receptor properties. In vitro experiments were selected, which determined the competitive binding to muscarinic M1 receptor by measuring muscarinic displacement. A human recombinant muscarinic M1 receptor expressed in CHO (Chinese Hamster Ovary cells) was used.

The experiments clearly demonstrated significant muscarinic M1 receptor binding properties of Melissa officinalis special extract (Bluenesse®). Muscarinic receptors as part of the cholinergic system have been reported to be important for cognitive effects, like alertness and memory.

For more information click here:
Investigation of a Melissa officinalis special extract on Cognition I. In vitro study on muscarinic properties, Buchwald-Werner et al. Agro FOOD Industry Hi Tech – vol 26(1) – January/February 2015

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