• Korean Journal of Pharmacognosy
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• v.30 no.3
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• pp.284-289
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• 1999

In order to find active ingradients having an agonistic activity to benzodiazepine receptor from Gastrodia elata Blume (Orchidaceae) which has been used as an anticonvulsant in oriental medicine, one component and some fractions were separated from the butanol extract of the rhizomes of this plant and evaluated for their activities on GABA/benzodiazepine receptor in vitro. As a result, one crude mixture (F4f) obtained from the most active fraction (F4) inhibited significantly the binding of $[^3H]Ro15-1788$, a selective benzodiazepine receptor antagonist, to benzodiazepine receptor of rat cortices. GABA significantly enhanced the inhibition of $[^3H]flunitrazepam$ binding by F4f, and this positive GABA shift supported the strong possibility of the agonistic activity of F4f to benzodiazepine receptor.

• Biomolecules & Therapeutics
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• v.5 no.4
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• pp.325-330
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• 1997

Methanol extract of G. elata inhibited the binding of [/sup 3/H]Rol5-1788, a selective benzodiazepine receptor antagonest, to benzodiazepine receptor of rat cortices. Saturation experiments followed by Scatchard analysis of the results showed that the inhibition of [sub 3/H]Ro15-1788 binding by G. dlata. appeared to be com-petitive. These competitive inhibiton of the butanol fraction was observed to be higher than the methanol extract. Methanol extract of G. efara inhibited a [sub 3/H]flunitrazepam, a selective benzodiazepine receptor agonist, binding to benzodiazepine receptor. GABA significantly enhanced the inhibition of [/sub 3/H]flunitrazepam binding by G. elata, and these "positive GABA shift" supported the strong possibility of agonestic activity to benzodiazepine receptor Butanol fraction was observed to be higher than crude extract by methanol in an agonistic activity to benzodiazepine receptor, furthermore enhanced the binding of [sub 3/H]SR95531 to GABA receptor. Butanol fraction of G. elata significantly diminished the pentylenetetrazole-induced lethality of mice. From these results, it can be concluded that substance or substances with neurochemical properties characteri- stic of a benzodiazepine receptor agonist may be important components, and contribute to the anticonvulsant property of G. elata.