Rhus parviflora and its biflavonoid constituent, rhusflavone, induce sleep through the positive allosteric modulation of GABAA-benzodiazepine receptors

Shrestha, Sabina; Park, Ji‐Hae; Lee, Dae-Young; Cho, Jin‐Gyeong; Cho, Suengmok; Yang, Hyejin; Yong, Hyeim; Yoon, Minseok; Han, Dongil; Baek, Nam‐In

doi:10.1016/j.jep.2012.04.047

Cited by 42 publications

(24 citation statements)

References 32 publications

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“…The present study demonstrates for the first time that leaves extracts prepared from R. parviflora display inhibitory effect on HIV-1 replication. Several phytochemicals such as gallic acid, myricetin, quercetin, kampferol and different glycosides have been reported to be present in R. parviflora [16,21]. Medicinally important compounds like gallic acid, quercetin, kampferol, glycosides etc.…”

Section: Resultsmentioning

confidence: 99%

“…(Anacardiaceae) is known as ‘Tintidika’ in Sanskrit language, widely distributed in Nepal, Northern India, Bhutan and Sri Lanka at the altitudinal range of 700–1100 m [15]. It is recorded in Ayurvedic pharmacopoeia as having therapeutic uses for Vāta vikāra, the complications related to neurological disorders including anxiety, insomnia, epilepsy, and rheumatoid arthritis [16]. In Nepal, fruits of R. parviflora are also used for human consumption and decoction of fruit or stem bark used to cure dysentery [17,18].…”

Section: Introductionmentioning

confidence: 99%

“…In some tribal areas, infusions of leaves were given in cholera [20]. Phytochemicals like gallic acid, some flavones viz., rutin, myricetin, quercetin, myricitrin, quercitrin, kampferol and some glycosides (isorhamnetin-3-α-L-arabinoside) have been isolated from the plant [16,21]. …”

Section: Introductionmentioning

confidence: 99%

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Anti-HIV-1 activity, protease inhibition and safety profile of extracts prepared from Rhus parviflora

Modi

Nutan

Pancholi

et al. 2013

BMC Complement Altern Med

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BackgroundIn the present study, extracts prepared from the leaves of Rhus parviflora Roxb. (Anacardiaceae) were evaluated for their anti-HIV activity, which have been traditionally used for the treatment of neurological disorders such as anxiety, insomnia and epilepsy.MethodsAqueous and 50% ethanolic extracts prepared from leaves of the plant were tested for their cytotoxicity and anti-HIV property using reporter gene based assays as well as human peripheral blood lymphocytes (PBLs). Further these extracts were evaluated for their ability to inhibit HIV-1 reverse transcriptase (RT) and protease activity. Safety profile of the extracts was determined on viability of Lactobacillus sp., secretion of pro-inflammatory cytokines by vaginal keratinocytes and transepithelial resistance.ResultsBoth aqueous (IC50 = 15 μg/ml) and 50% ethanolic (IC50 = 26 μg/ml) extracts prepared from leaves of R. parviflora showed anti-HIV activity in TZM-bl cells wherein the virus was treated with the extracts prior to infection. Further, both the extracts also inhibited virus load in HIV infected CEM-GFP cells and human PBLs. The anti-HIV activity is mediated through inhibition of HIV-1 protease activity. Both the extracts did not disturb the integrity of monolayer formed by intestinal epithelial Caco-2 cells. The extracts when tested up to 100 μg/ml did not significantly reduce the viability of L. plantarum, L. fermentum, L. rhamnosus and L. casei. The extracts (100 μg/ml) did not reveal any cytotoxic effect on vaginal keratinocytes (Vk2/E6E7). Levels of pro-inflammatory cytokines secreted by Vk2/E6E7 cells treated with both the plant extracts were within the non-inflammatory range.ConclusionsThe studies reported herein showed in vitro anti-HIV activity and preliminary safety profile of the extracts prepared from the leaves of R. parviflora.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Anti-HIV-1 activity, protease inhibition and safety profile of extracts prepared from Rhus parviflora

Modi

Nutan

Pancholi

et al. 2013

BMC Complement Altern Med

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“…In addition, the biflavonoids mesuaferrone B, rhusflavone, and agathisflavone, which were isolated from the ethyl acetate fraction, competitively blocked flumazenil binding with Ki values of 0.280, 0.045, and 0.091 μM. It was proposed that the conjugated ketone and C6-C8 biflavonoid linkage in rhusflavone decreased sleep latency and increased sleep duration by activating the BZD-site of GABA A [35]. However, these finding were only clinical manifestations without theory supporting, this hypothesis awaits confirmation in molecular biology studies to identify the target of rhusflavone.…”

Section: Resultsmentioning

confidence: 99%

Herbal Insomnia Medications that Target GABAergic Systems: A Review of the Psychopharmacological Evidence

Shi¹,

Dong²,

Zhao³

et al. 2014

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Insomnia is a common sleep disorder which is prevalent in women and the elderly. Current insomnia drugs mainly target the γ-aminobutyric acid (GABA) receptor, melatonin receptor, histamine receptor, orexin, and serotonin receptor. GABAA receptor modulators are ordinarily used to manage insomnia, but they are known to affect sleep maintenance, including residual effects, tolerance, and dependence. In an effort to discover new drugs that relieve insomnia symptoms while avoiding side effects, numerous studies focusing on the neurotransmitter GABA and herbal medicines have been conducted. Traditional herbal medicines, such as Piper methysticum and the seed of Zizyphus jujuba Mill var. spinosa, have been widely reported to improve sleep and other mental disorders. These herbal medicines have been applied for many years in folk medicine, and extracts of these medicines have been used to study their pharmacological actions and mechanisms. Although effective and relatively safe, natural plant products have some side effects, such as hepatotoxicity and skin reactions effects of Piper methysticum. In addition, there are insufficient evidences to certify the safety of most traditional herbal medicine. In this review, we provide an overview of the current state of knowledge regarding a variety of natural plant products that are commonly used to treat insomnia to facilitate future studies.

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“…All established antiepileptic drugs have anticonvulsant activity in at least maximal electroshock seizure (MES) model. [23] MES-induced seizure can be prevented either by drugs that inhibit voltage-dependent Na + channels such as phenytoin, valproate, felbamate and lamotrigine or by drugs that block glutamatergic receptor such as felbamate.…”

Section: Introductionmentioning

confidence: 99%

Potentiation of Antiepileptic Activity of Phenytoin Using Beta Carotene Against Maximal Electroshock Induced Convulsions in Mice

Jagannath¹

2017

WJPPS

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Phenytoin is the mostly used drug for the seizures. However question regarding safety and efficacy of this drug make it particularly compelling to identify adjunct therapy that could boost therapeutic benefit. Study found that one adjunct therapy is beta carotene. The main aim of present study was to evaluate potentiation of antiepileptic activity of Phenytoin by beta carotene in mice against maximal electroshock induced (MES) induced convulsions. In these methods all the animals were divided into sixteen groups & each group consists of six animals. Shock 50mA for 0.2 sec was applied for all groups of mice. Testing drugs doses were randomised within groups of animal in such way that each group was required during a given test series. The results revealed that beta carotene significantly potentiated efficacy of phenytoin but did not exert antiepileptic effect on its own. Alone beta carotene at the dose of 20mg/kg p.o. significantly reduced elevated MDA level in serum. Concurrent administration of phenytoin and beta carotene on serum MDA activity was not differed with alone beta carotene at the dose of 20mg/kg. It is concluded that beta carotene potentiates the antiepileptic activity of phenytoin.

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Rhus parviflora and its biflavonoid constituent, rhusflavone, induce sleep through the positive allosteric modulation of GABAA-benzodiazepine receptors

Cited by 42 publications

References 32 publications

Anti-HIV-1 activity, protease inhibition and safety profile of extracts prepared from Rhus parviflora

Anti-HIV-1 activity, protease inhibition and safety profile of extracts prepared from Rhus parviflora

Herbal Insomnia Medications that Target GABAergic Systems: A Review of the Psychopharmacological Evidence

Potentiation of Antiepileptic Activity of Phenytoin Using Beta Carotene Against Maximal Electroshock Induced Convulsions in Mice

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