[HTML][HTML] Inhibition of cyclic adenosine monophosphate-specific phosphodiesterase by various food plant-derived phytotherapeutic agents

T Röhrig, O Pacjuk, S Hernández-Huguet, J Körner… - Medicines, 2017 - mdpi.com
T Röhrig, O Pacjuk, S Hernández-Huguet, J Körner, K Scherer, E Richling
Medicines, 2017mdpi.com
Background: Phosphodiesterases (PDEs) play a major role in the regulation of cyclic
adenosine monophosphate (cAMP)-and cyclic guanosine monophosphate (cGMP)-
mediated pathways. Their inhibitors exhibit anti-inflammatory, vasodilatory and
antithrombotic effects. Therefore, consumption of foods with PDE-inhibiting potential may
possess beneficial influence on the risk of cardiovascular diseases. Methods: Four plant
extracts (Arbutus unedo, Camellia sinensis, Cynara scolymus, Zingiber officinale) with …
Background
Phosphodiesterases (PDEs) play a major role in the regulation of cyclic adenosine monophosphate (cAMP)- and cyclic guanosine monophosphate (cGMP)-mediated pathways. Their inhibitors exhibit anti-inflammatory, vasodilatory and antithrombotic effects. Therefore, consumption of foods with PDE-inhibiting potential may possess beneficial influence on the risk of cardiovascular diseases.
Methods
Four plant extracts (Arbutus unedo, Camellia sinensis, Cynara scolymus, Zingiber officinale) with promising ingredient profiles and physiological effects were tested for their ability to inhibit cAMP-specific PDE in vitro in a radioactive assay.
Results
Strawberry tree fruit (Arbutus unedo) and tea (Camellia sinensis) extracts did not inhibit PDE markedly. Alternatively, artichoke (Cynara scolymus) extract had a significant inhibitory influence on PDE activity (IC50 = 0.9 ± 0.1 mg/mL) as well as its flavone luteolin (IC50 = 41 ± 10 μM) and 3,4-dicaffeoylquinic acid (IC50 > 1.0 mM). Additionally, the ginger (Zingiber officinale) extract and one of its constituents, [6]-gingerol, significantly inhibited PDE (IC50 = 1.7 ± 0.2 mg/mL and IC50 > 1.7 mM, respectively). Crude fractionation of ginger extract showed that substances responsible for PDE inhibition were in the lipoid fraction (IC50 = 455 ± 19 μg/mL).
Conclusions
A PDE-inhibitory effect was shown for artichoke and ginger extract. Whether PDE inhibition in vivo can be achieved through ingestion of artichoke or ginger extracts leading to physiological effects concerning cardiovascular health should be addressed in future research.
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