Antidepressant-like profile and MAO-A inhibitory activity of 4-propyl-2H-benzo[h]-chromen-2-one

Vergel, Nadezdha E.; López, J. L.; Orallo, Francisco; Viña, Dolores; Buitrago, Diana Marcela; Olmo, Esther del; Micó, Juan Antonio; Guerrero, Mario

doi:10.1016/j.lfs.2010.04.001

Cited by 25 publications

(14 citation statements)

References 30 publications

(25 reference statements)

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“…Monoamine oxidase A (MAO-A) selectively targets the catalysts of the neurotransmitters of serotonin and norepinephrine and is a pharmacological target in seeking out bene cial agents for the treatment of depression (Vergel et al, 2010). The evidence shows that coumarin compounds inhibit TNF-α or PGE2 secretion by affecting NFkB nucleus transport and inhibiting the phosphorylation of P38, JNK1/2, PKC kinases in LPS-stimulated macrophages and mononuclear cell lines.…”

Section: Introductionmentioning

confidence: 99%

Possible Involvement Of L-Arginine-Nitric Oxide Pathway In The Antidepressant Activity Of Auraptene In Mice

Amini-Khoei

Boroujeni

Maghsoudi

et al. 2021

Preprint

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Background: Depression is one of the most common mental illnesses around the world. Nitric oxide (NO) is involved in the pathophysiology of depression. Auraptene (a coumarin derivative) has been shown to have pharmacological effects on neurological diseases. porpuse: The present study aimed to investigate the possible role of NO pathway in Auraptene antidepressant effects in male mice.Methods: Behavioral tests were used to assess depression-like behaviors. The mice received Auraptene at 10, 30 and 100 mg/kg, the combination of the sub-effective dose of Auraptene (10 mg/kg) and L-NAME, and the combination of the effective dose of Auraptene (30 mg/kg) and L-arginine. Finally, brain and serum MDA level and antioxidant capacity, as well as hippocampus and serum NO level was measured.Results: Auraptene (30 mg/kg) improved depression-like behaviors. Auraptene (30 mg/kg) also significantly reduced serum NO levels (P<0.05) and significantly increased serum MDA (10 mg/kg, P<0.05). Auraptene at 30 mg/kg also increased serum antioxidant capacity (P<0.01). Co-administration of L-NAME and the sub-effective dose of Auraptene enhanced the effects of Auraptene. However, co-administration of the effective dose of Auraptene and L-arginine reduced the effects of Auraptene.Conclusion: The results showed that Auraptene causes antidepressant effects in a dose-dependent manner and acts as a prooxidant at 100 mg/kg and exacerbates oxidative stress. The antidepressant effects of this active molecule are exerted by reducing the NO level in the hippocampus and serum, increasing the antioxidant capacity and reducing the MDA level in the serum.

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Section: Introductionmentioning

confidence: 99%

Possible Involvement Of L-Arginine-Nitric Oxide Pathway In The Antidepressant Activity Of Auraptene In Mice

Amini-Khoei

Boroujeni

Maghsoudi

et al. 2021

Preprint

View full text Add to dashboard Cite

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“…One study evaluated 1,2-Benzopyrone (obtained from Hygrophila tyttha Leonard species) and found that coumarin was responsible, at least in part, for the anxiolytic, anticonvulsant, and sedative effects described for this species (Ariza et al, 2007). Other coumarins, both natural and modified, have shown antidepressant (Vergel et al, 2010) and neuroprotective effects (Kang et al, 2005;Epifano et al, 2008). Some studies have shown that coumarinic compounds inhibit Page 2 / 10 MAO-B (Matos et al, 2004;Matos et al, 2009;Matos et al, 2010;Matos et al 2013).…”

Section: Introductionmentioning

confidence: 99%

8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects

Olaya

Vergel

López

et al. 2020

Braz. J. Pharm. Sci.

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Parkinson's disease is a common neurodegenerative disorder. In this study, the monoamine oxidase inhibitory activity and potential anti-parkinsonian effects of 8-propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one (FCS303), a new synthetic coumarin, were evaluated. To do this, we used the reserpine model of Parkinson's disease, an assay of levodopa/carbidopa potentiation, the catalepsy model of haloperidol, and an in vitro assay against monoamine oxidase (MAO) activity. Additionally, lipid peroxidation and protein carbonyl group quantification was performed in mice brain homogenates previously treated with haloperidol. FCS303 inhibited monoamine oxidase B (MAO-B) with an IC 50 of 5.46 ± 0.36 µM; however, there was no effect on monoamine oxidase A (MAO-A). The oral administration of FCS303 led to a significant reversal of hypokinesia in the reserpine model (at 24 h, doses of 100 and 200 mg/kg) and in the levodopa/carbidopa potentiation assay (at 2 and 24 h, dose of 200 mg/kg). In addition, FCS303 (100 mg/kg) showed anti-cataleptic activity against haloperidol. FCS303 (50 mg/kg) significantly decreased lipid peroxidation and protein carbonyl quantification. These results suggest that FCS303 could present anti-parkinsonian activity related to MAO-B inhibitory activity.

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“…Previous work showed that the coumarin derivative, coded as FCS-304 (4-propyl-2Hbenzo[h]-chromen-2-one) displays MAO-A inhibition at the micromolar range, with no activity against MAO-B, as well as positive results in forced swimming and tail suspension test in mice (22). This work advances the antidepressant-like profile of this compound, assessing its activity in the 5-HTP test in mice to explore its pro-serotoninergic activity, as well as its response in rats; in reserpine induce ptosis and in the behavioral despair test.…”

Section: Introductionmentioning

confidence: 99%

Serotonergic-like profile of 4-propyl-2H-benzo[h]-chromen-2-one (FCS-304) in mice and rats

Moreno

Suárez

Guerrero

2019

Vitae

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ANTECEDENTES: 4-propil-2H-benzo [h] -cromen-2-ona (FCS-304) es una cumarina semisintética con actividad inhibidora de MAO-A y resultados positivos en natación forzada y prueba de suspensión de cola en ratones, pero hasta ahora, no se ha estudiado en otros modelos de antidepresivos de detección en ratones y ratas.OBJETIVOS: El objetivo de este trabajo fue evaluar el efecto similar a la serotonina de FCS-304 en la prueba de 5-hidroxitriptófano (5-HTP) en ratones, en la prueba de desesperación del comportamiento en ratas y en la prueba de reserpina en ratas.MÉTODOS: Se evaluó la potenciación de 5-HTP (100 mg / kg, ip), sacudidas de cabeza inducidas en ratones, previamente tratados con FCS-304 (50-75-150 mg / Kg, po). La prueba de desesperación del comportamiento se realizó en ratas tratadas con FCS-304, registrando el tiempo de inmovilidad alcanzado por los animales sometidos a natación forzada. Se examinó el antagonismo de la ptosis inducida por reserpina en ratas, evaluando el nivel de cierre palpebral. La imipramina (30 mg / kg, po) y el vehículo (aceite de canola) sirvieron como controles positivos y negativos, respectivamente.RESULTADOS: FCS-304 potenció significativamente las contracciones en la cabeza inducidas por 5-HTP en ratones, de una manera dependiente de la dosis. En ratas, FCS-304 redujo significativamente el tiempo de inmovilidad en la prueba de desesperación conductual y antagonizó la ptosis inducida por reserpina.CONCLUSIÓN: Estos resultados agregan apoyo para proponer que el FCS-304 podría provocar efectos antidepresivos relacionados con la actividad inhibidora de MAO-A.

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Antidepressant-like profile and MAO-A inhibitory activity of 4-propyl-2H-benzo[h]-chromen-2-one

Cited by 25 publications

References 30 publications

Possible Involvement Of L-Arginine-Nitric Oxide Pathway In The Antidepressant Activity Of Auraptene In Mice

Possible Involvement Of L-Arginine-Nitric Oxide Pathway In The Antidepressant Activity Of Auraptene In Mice

8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects

Serotonergic-like profile of 4-propyl-2H-benzo[h]-chromen-2-one (FCS-304) in mice and rats

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