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GABA-A receptor modulation and pharmacological effects of a flavo | 43378
Medicinal & Aromatic Plants

Medicinal & Aromatic Plants
Open Access

ISSN: 2167-0412

+44 1300 500008

GABA-A receptor modulation and pharmacological effects of a flavonoid isolated from Arenaria kansuensis (Traditional Tibetan Herb)


Joint Event on 4th World Congress on Medicinal Plants & Natural Products Research and 12th Global Ethnomedicine & Ethnopharmacology Conference

August 08-09, 2018 Osaka, Japan

Zenggen Liu, Yun Shao, Martin Wallner, Yanduo Tao and Richard Olsen

Chinese Academy of Sciences, China
Tibetan Medicine Research, China
University of California, USA

Scientific Tracks Abstracts: Medicinal & Aromatic Plants

Abstract :

It is very intense and significative in the search for novel neuro pharmacological activities devoid of undesirable side-effects typical of classical Benzodiazepines (BZDs) in recent years and flavonoids, as a relative new class of ligands, have been shown to possess some anxiolytic and anticonvulsant effects in vivo/vitro. The objective of the present work was to evaluated the pharmacological properties of a naturally occurring flavonoid (2�??, 4�??, 5, 7-tetrahydroxy-5�?? 6-dimethoxyflavone or DMB) at recombinant ã-aminobutyric acid-A (GABA-A) receptors and its anti-alcohol, anxiolytic and anticonvulsant activities were tested by the models of animal behavior. DMB isolated from traditional Tibetan herb (Arenaria kansuensis), positively modulated GABA-activated current at á1â2ã2 and á5â2ã2 GABA-A receptors expressed in HEK 293T cells. The behavioral studies showed that DMB at doses of 0.5-8.0 mg/kg (I.P.) exerted significant anti-alcohol effects in the loss of righting reflex assay (P<0.01). The anxiolytic activity was measured on an elevated plus maze and the results indicated that DMB can alleviated significantly anxiety at the doses of 2-8 mg/kg (P.O.). Both DMB anti-alcohol and anxiolytic effects on animal behavior were antagonized by flumazenil (5 mg/kg in vivo), the BZD antagonist. DMB competitively inhibited BZD-site [3H] flunitrazepam binding (IC50, 0.10 ìM), suggesting the neuro pharmacological activities of DMB were mediated via the BZD-sites on GABA-A receptors. In addition, DMB (0.5-8.0 mg/kg, I.P.) exerted dose-dependently anticonvulsant activity in pentylenetetrazole induced seizure paradigms (P<0.01). Furthermore, DMB did not cause myorelaxant effects in the rota rod test and horizontal wire test. Therefore, the results of the present study suggest that the pharmacological activities (anti-alcohol, anxiolytic and anticonvulsant) of DMB are probably mediated through positive allosteric modulation of the different GABA-A receptor subtypes via interaction at the BZD-site and these effects were not accompanied by myo-relaxant side-effects typical of BZDs.

Biography :

Zenggen Liu has his research interest is extraction, separation and identification of chemical composition from Traditional Tibetan Medicine, as well as activity screening of natural products and its derivatives.

E-mail: lzg@nwipb.cas.cn

 

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