Involvement of GABAergic pathway in the sedative activity of apigenin, the main flavonoid from Passiflora quadrangularis pericarp

Gazola, Andressa Córneo; Costa, Geison Modesti; Castellanos, Leonardo; Ramos, Freddy A.; Reginatto, Flávio Henrique; Lima, Thereza Christina Monteiro de; Schenkel, Eloir Paulo

doi:10.1016/j.bjp.2015.03.009

Cited by 36 publications

(22 citation statements)

References 23 publications

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“…Another study conducted by Gazola et al, showed that apigenin as the main constituent of Passiflora quadrangularis pericarp induced sedative effects. They showed that apigenin sedative effect was blocked by flumazenil as benzodiazepine antagonist and therefore suggested that apigenin was doing its effect through binding to inhibitory gama amino-butyric acid (GABA) receptor or due to an enhancement of the GABAergic system (16). There is more evidence on flavonoids to act as GABAA modulators in the brain.…”

Section: Discussionmentioning

confidence: 99%

Bioactivity guided isolation of apigenin from Stachys lavandulifolia Vahl. in mice with anxiolytic effects

Rabbani¹,

Sajjadi²,

Karimi-Firozjai³

et al. 2018

J Herbmed Pharmacol

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Section: Discussionmentioning

confidence: 99%

Bioactivity guided isolation of apigenin from Stachys lavandulifolia Vahl. in mice with anxiolytic effects

Rabbani¹,

Sajjadi²,

Karimi-Firozjai³

et al. 2018

J Herbmed Pharmacol

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“…Hence, apigenin could play a pivotal role in the cardiovascular properties showed by P. quadrangularis L., but other active metabolites could be implicated, as some of them have flavonoid nature, given the high phenolic content described in this species (58). Anxiolytic like properties from leaves extract of P. quadrangularis L. have also been studied in experimental models (59) and apigenin could be involved in the sedative properties showed by this species in mice, maybe be due to an enhancement of the GABAergic system (60).…”

Section: Discussionmentioning

confidence: 99%

Passiflora quadrangularis L. PREVENTS EXPERIMENTAL HYPERTENSION AND VASCULAR REMODELLING IN RATS EXPOSED TO NITRIC OXIDE DEFICIT

Bareño

Puebla

Guerra

et al. 2017

Vitae

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Background: Passiflora quadrangularis L. is among the species used in Colombian folk medicine for hypertension, but until now it has not been studied in experimental models. Objectives: To assess the capacity of P. quadrangularis L. EtOH extract to prevent the hypertension and vascular remodelling induced by nitric oxide (NO) deficit in Wistar rats. Methods: The nitric oxide (NO) synthase inhibitor L-NAME (10 mg/kg, i.p (intraperitoneal), every 48h) was administered for seven weeks to the following groups of rats: P. quadrangularis L.75, 150 and 300 mg/kg/d, p.o. (oral route); enalapril as reference agent, 10 mg/kg/d, p.o. and vehicle as control (mixture of propylene glycol 10%, glycerine 10% and polysorbate 2%). Arterial blood pressure (BP) and heart rate (HR) were measured twice a week. After sacrifice, the aortic rings were isolated, contraction was triggered with phenylephrine (PE 10 -6 M) and then the relaxant response achieved with cumulative concentrations of acetylcholine (ACh, 10 -10 -10 -5 M) or sodium nitroprusside (SNP, 10 -10 -10 -5 M) was assessed. Histopathologic measures of thickness/lumen ratio from both the left ventricle and aorta walls, as well as phytochemical screening, were also performed. Results: As for enalapril, all doses of P. quadrangularis L. prevented the hypertension induced by L-NAME (122±1.2 versus 155±1.3 mmHg at seventh week). P. quadrangularis L. significantly increased the relaxant effect induced by ACh in isolated aorta and decreased the thickness/lumen ratio of aorta wall specimens. Conclusions: P. quadrangularis L. prevents experimental hypertension induced in rats with nitric oxide deficits improving the endothelium vasodilatation response and protecting against vascular remodelling.

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“…Because aqueous extracts (100–300 mg/kg, p.o.) from the pericarp of Passiflora quadrangularis (Passifloraceae) prolonged the sleep duration of mice in an ethyl ether-induced hypnosis test, Gazola et al, [ 120 ] evaluated the neurological effects of their main component apigenin. Apigenin (0.6 mg/kg, p.o.)…”

Section: Phytochemicals With the General Anesthetic Activitymentioning

confidence: 99%

Anesthetic Agents of Plant Origin: A Review of Phytochemicals with Anesthetic Activity

Tsuchiya

2017

Molecules

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The majority of currently used anesthetic agents are derived from or associated with natural products, especially plants, as evidenced by cocaine that was isolated from coca (Erythroxylum coca, Erythroxylaceae) and became a prototype of modern local anesthetics and by thymol and eugenol contained in thyme (Thymus vulgaris, Lamiaceae) and clove (Syzygium aromaticum, Myrtaceae), respectively, both of which are structurally and mechanistically similar to intravenous phenolic anesthetics. This paper reviews different classes of phytochemicals with the anesthetic activity and their characteristic molecular structures that could be lead compounds for anesthetics and anesthesia-related drugs. Phytochemicals in research papers published between 1996 and 2016 were retrieved from the point of view of well-known modes of anesthetic action, that is, the mechanistic interactions with Na+ channels, γ-aminobutyric acid type A receptors, N-methyl-d-aspartate receptors and lipid membranes. The searched phytochemicals include terpenoids, alkaloids and flavonoids because they have been frequently reported to possess local anesthetic, general anesthetic, antinociceptive, analgesic or sedative property. Clinical applicability of phytochemicals to local and general anesthesia is discussed by referring to animal in vivo experiments and human pre-clinical trials. This review will give structural suggestions for novel anesthetic agents of plant origin.

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Involvement of GABAergic pathway in the sedative activity of apigenin, the main flavonoid from Passiflora quadrangularis pericarp

Cited by 36 publications

References 23 publications

Bioactivity guided isolation of apigenin from Stachys lavandulifolia Vahl. in mice with anxiolytic effects

Bioactivity guided isolation of apigenin from Stachys lavandulifolia Vahl. in mice with anxiolytic effects

Passiflora quadrangularis L. PREVENTS EXPERIMENTAL HYPERTENSION AND VASCULAR REMODELLING IN RATS EXPOSED TO NITRIC OXIDE DEFICIT

Anesthetic Agents of Plant Origin: A Review of Phytochemicals with Anesthetic Activity

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