<i>Pistacia vera</i> Extract Potentiates the Effect of Melatonin on Human Melatonin MT<sub>1</sub> and MT<sub>2</sub> Receptors with Functional Selectivity

Melatonin is a tryptophan derivative synthesized in plants and animals. In humans, melatonin acts on melatonin MT<sub>1</sub> and MT<sub>2</sub> receptors belonging to the G protein-coupled receptor (GPCR) family. Synthetic melatonin receptor agonists are prescribed for insom...

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Main Authors: Nedjma Labani (Author), Florence Gbahou (Author), Marc Noblet (Author), Bernard Masri (Author), Olivier Broussaud (Author), Jianfeng Liu (Author), Ralf Jockers (Author)
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Published: MDPI AG, 2023-06-01T00:00:00Z.
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LEADER 00000 am a22000003u 4500
001 doaj_79a981ecc07d4f81b4efc193ea0f6ac0
042 |a dc 
100 1 0 |a Nedjma Labani  |e author 
700 1 0 |a Florence Gbahou  |e author 
700 1 0 |a Marc Noblet  |e author 
700 1 0 |a Bernard Masri  |e author 
700 1 0 |a Olivier Broussaud  |e author 
700 1 0 |a Jianfeng Liu  |e author 
700 1 0 |a Ralf Jockers  |e author 
245 0 0 |a <i>Pistacia vera</i> Extract Potentiates the Effect of Melatonin on Human Melatonin MT<sub>1</sub> and MT<sub>2</sub> Receptors with Functional Selectivity 
260 |b MDPI AG,   |c 2023-06-01T00:00:00Z. 
500 |a 10.3390/pharmaceutics15071845 
500 |a 1999-4923 
520 |a Melatonin is a tryptophan derivative synthesized in plants and animals. In humans, melatonin acts on melatonin MT<sub>1</sub> and MT<sub>2</sub> receptors belonging to the G protein-coupled receptor (GPCR) family. Synthetic melatonin receptor agonists are prescribed for insomnia and depressive and circadian-related disorders. Here, we tested 25 commercial plant extracts, reported to have beneficial properties in sleep disorders and anxiety, using cellular assays (2─[<sup>125</sup>I]iodomelatonin binding, cAMP inhibition, ERK1/2 activation and β-arrestin2 recruitment) in mock-transfected and HEK293 cells expressing MT<sub>1</sub> or MT<sub>2</sub>. Various melatonin receptor-dependent and -independent effects were observed. Extract 18 (<b>Ex18</b>) from <i>Pistacia vera</i> dried fruits stood out with very potent effects in melatonin receptor expressing cells. The high content of endogenous melatonin in <b>Ex18</b> (5.28 ± 0.46 mg/g extract) is consistent with this observation. <b>Ex18</b> contains an additional active principle that potentiates the effect of melatonin on G<sub>i</sub> protein-dependent pathways but not on β-arrestin2 recruitment. Further active principles potentiating exogenous melatonin were detected in several extracts. In conclusion, we identified plant extracts with various effects in GPCR-based binding and signalling assays and identified high melatonin levels and a melatonin-potentiating activity in <i>Pistacia vera</i> dried fruit extracts that might be of therapeutic potential. 
546 |a EN 
690 |a plant extracts 
690 |a GPCR 
690 |a signalling 
690 |a melatonin 
690 |a insomnia 
690 |a depression 
690 |a Pharmacy and materia medica 
690 |a RS1-441 
655 7 |a article  |2 local 
786 0 |n Pharmaceutics, Vol 15, Iss 7, p 1845 (2023) 
787 0 |n https://www.mdpi.com/1999-4923/15/7/1845 
787 0 |n https://doaj.org/toc/1999-4923 
856 4 1 |u https://doaj.org/article/79a981ecc07d4f81b4efc193ea0f6ac0  |z Connect to this object online.