Possible anxiolytic effects of chrysin, a central benzodiazepine receptor ligand isolated from Passiflora Coerulea

Wolfman, Claudia; Viola, Haydeé; Paladini, Alejandro C.; Dajas, Federico; Medina, Jorge H.

doi:10.1016/0091-3057(94)90103-1

Cited by 306 publications

(195 citation statements)

References 14 publications

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“…When regards hesperetine, authors indicate on its antiallergic, antidepressant and memory improving effect [45,46]. In turn, scutellarin reveals antihypertensive and antivirus [47,48], while chrysin -antitumor, anxiolytic and anticonvulsant activities [49][50][51][52]. Since all listed flavonoids reveal a strong pharmacological activities, they finally may be engaged in the adaptogenic effect of Scutellariae radix.…”

Section: Resultsmentioning

confidence: 99%

Experimental Paper. Intrapopulation variability of flavonoid content in roots of Baikal skullcap (Scutellaria baicalensis Georgi)

Kosakowska

2017

Herba Polonica

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SummaryIntroduction: Baikal skullcap (Scutellaria baicalensis Georgi) is an important medicinal plant, indigenous to Asia. Due to a wide range of pharmacological activities, its roots has been used for ages in Traditional Chinese Medicine. Recently, the species has become an object of interest of Western medicine, as well. Objective: The aim of the study was to determine the variability of Baikal skullcap population originated from Mongolia and cultivated in Poland, in terms of content and composition of flavonoids in the roots. Methods: The objects of the study were 15 individual plants, selected within examined population and cloned in order to obtain a sufficient amount of raw material. The total content of flavonoids in roots was determined according to Polish Pharmacopeia 6th. The qualitative analysis of flavonoids was carried out using HPLC, Shimadzu chromatograph. Results: The dry mass of roots ranged from 25.88 to 56.14 g × plant-1. The total content of flavonoids (expressed as a quercetin equivalent) varied between 0.17 and 0.52% dry matter (DM). Nine compounds were detected within the group, with oroxylin A 7-Oglucuronide (346.90-1063.00 mg × 100 g-1DM) as a dominant, which differentiated investigated clones at the highest degree (CV=0.27). Baicalin (391.40-942.00 mg × 100 g-1DM), wogonoside (324.00-641.10 mg × 100 g-1DM) and hesperetine 7-O-glucoside (163.00-346.32 mg × 100 g-1DM) were also present in a considerable amounts. Clone 7 was distinguished by the highest content of all investigated compounds, except wogonin and oroxylin A 7-O-glucuronide. Conclusions: Results obtained in present study show a high variability within Baical skullcap investigated population in respect of flavonoid compounds detected in roots. Thus, the results may be used in future investigations concerning the selection and breeding of this species.

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Section: Resultsmentioning

confidence: 99%

Experimental Paper. Intrapopulation variability of flavonoid content in roots of Baikal skullcap (Scutellaria baicalensis Georgi)

Kosakowska

2017

Herba Polonica

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“…The animals were placed in the arena and the number of head dips on the holes was counted during 5 min. (Wolfman et al 1994).…”

Section: Test For Exploratory Behaviour In Micementioning

confidence: 99%

Behavioural Effects in Rodents of Methyl Angolensate: a Triterpenoid Isolated from *Entandrophragma angolense**

Amos

Orisadipe

Binda³

et al. 2002

Pharmacology & Toxicology

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Behavioral effects of methyl angolensate were investigated in mice and rats. Spontaneous motor activity, pentobarbital sleeping time, amphetamine-stereotyped behaviour, exploratory activity and apomorphine -induced climbing studies in mice were evaluated. The results revealed that methyl angolensate reduced spontaneous motor activity in mice, prolonged the duration of pentobarbital sleeping time in rats and attenuated amphetamine-induced stereotype behaviour in rats. Methyl angolensate also decreased exploratory activity in mice and reduced the rate of apomorphine-induced climbing in mice at the doses tested. It is suggested that methyl angolensate possesses some biologically active principles that are sedative in nature.

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“…The first suggests that different benzodiazepine receptor subtypes may be responsible for the behavioral effects of benzodiazepine compounds. According to this hypothesis, two receptor subtypes, benzodiazepine (omega) 1 and benzodiazepine (omega) 2 receptors, exist in different brain areas responsible for different physiological functions (2). The alternative hypothesis proposes the development of benzodiazepine receptor partial agonists which present lower intrinsic efficacy sufficient to maintain the anxiolytic and anticonvulsant responses, but insufficient to induce the side effects seen with full agonists (2,4).…”

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confidence: 99%

“…search laboratories in the past 6 years (14-16) and has been extensively validated for use with both rats (2,15) and mice (1,11,13,17). The conventional indices of anxiety in this test, percent of open arm entries and percent time spent in the open arm, are exquisitely sensitive to agents thought to act via the GABA A receptor complex (i.e., benzodiazepines, barbiturates, ethanol, and neurosteroids) (14,17).…”

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confidence: 99%

“…However, undesirable side effects like muscle relaxation, sedation, physical dependence, tolerance, ataxia and memory impairment have been associated with the use of benzodiazepines. A variety of novel agents capable of interacting with benzodiazepine receptors have been investigated in order to develop non-sedative anxioselective agents (1)(2)(3). Two main hypotheses for the development of such anxioselective drugs have been proposed.…”

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confidence: 99%

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Anxiolytic-like effects of 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate in mice

Rubin

Albach

Berlese

et al. 2000

Braz J Med Biol Res

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The pharmacological effects of 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate (PTMB), a novel synthetic benzodiazepine, were examined in mice. In the elevated plus-maze test of anxiety, 0.3-1 mg/kg diazepam ip (F(3,53) = 3.78; P<0.05) and 1-10 mg/kg PTMB ip increased (F(5,98) = 3.26; P<0.01), whereas 2 mg/kg picrotoxin ip decreased (F(3,59) = 8.32; P<0.001) the proportion of time spent in the open arms, consistent with an anxiolytic action of both benzodiazepines, and an anxiogenic role for picrotoxin. In the holeboard, 1.0 mg/kg diazepam ip increased (F(3,54) = 2.78; P<0.05) and 2 mg/kg picrotoxin ip decreased (F(3,59) = 4.69; P<0.01) locomotor activity. Rotarod assessment revealed that 1 mg/kg diazepam ip and 3, 10 and 30 mg/kg PTMB ip produced significant motor incoordination compared to vehicle control (F(4,70) = 7.6; P<0.001). These data suggest that the recently synthesized PTMB compound possesses anxiolytic activity and produces motor incoordination similar to those observed with diazepam. PicrotoxinBenzodiazepine compounds have been reported to be the most extensively consumed psychoactive drugs worldwide due to their anxiolytic and anticonvulsant activity. However, undesirable side effects like muscle relaxation, sedation, physical dependence, tolerance, ataxia and memory impairment have been associated with the use of benzodiazepines. A variety of novel agents capable of interacting with benzodiazepine receptors have been investigated in order to develop non-sedative anxioselective agents (1-3). Two main hypotheses for the development of such anxioselective drugs have been proposed. The first suggests that different benzodiazepine receptor subtypes may be responsible for the behavioral effects of benzodiazepine compounds. According to this hypothesis, two receptor subtypes, benzodiazepine (omega) 1 and benzodiazepine (omega) 2 receptors, exist in different brain areas responsible for different physiological functions (2). The alternative hypothesis proposes the development of benzodiazepine receptor partial agonists which present lower intrinsic efficacy sufficient to maintain the anxiolytic and anticonvulsant responses, but insufficient to induce the side effects seen with full agonists (2,4). Most of the benzodiazepines used in clinical therapeutics are 1,4-benzodiazepines (5-7), since several products were generated by introducing substituents at different positions of the benzodiazepine ring of diazepam. Modifications in the structure of the ring have also been made, and the anxiolytic effect of 1,5-benzodiazepines (clobazam) has been described (8,9). However, considerably less is known about the effects of substituents on 1,5-benzodiazepines compared to the 1,4 group. In the present study we investigated the anxiolytic potential of the recently synthesized 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate (PTMB) (10). The effects of this new benzodiazepine on spontaneous coordinated motor movements were also evaluated.Male albino mice (35-40 g) from our ...

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Possible anxiolytic effects of chrysin, a central benzodiazepine receptor ligand isolated from Passiflora Coerulea

Cited by 306 publications

References 14 publications

Experimental Paper. Intrapopulation variability of flavonoid content in roots of Baikal skullcap (Scutellaria baicalensis Georgi)

Experimental Paper. Intrapopulation variability of flavonoid content in roots of Baikal skullcap (Scutellaria baicalensis Georgi)

Behavioural Effects in Rodents of Methyl Angolensate: a Triterpenoid Isolated from *Entandrophragma angolense**

Anxiolytic-like effects of 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate in mice

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Possible anxiolytic effects of chrysin, a central benzodiazepine receptor ligand isolated from Passiflora Coerulea

Cited by 306 publications

References 14 publications

Experimental Paper. Intrapopulation variability of flavonoid content in roots of Baikal skullcap (Scutellaria baicalensis Georgi)

Experimental Paper. Intrapopulation variability of flavonoid content in roots of Baikal skullcap (Scutellaria baicalensis Georgi)

Behavioural Effects in Rodents of Methyl Angolensate: a Triterpenoid Isolated from Entandrophragma angolense*

Anxiolytic-like effects of 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate in mice

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Product

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Behavioural Effects in Rodents of Methyl Angolensate: a Triterpenoid Isolated from *Entandrophragma angolense**