<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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2023-06-01T00:00:00Z.
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LEADER | 00000 am a22000003u 4500 | ||
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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. |