Agonistic Activities to the Benzodiazepine Receptor by Extracts of Medicinal Plants(III) Activities of Composite Druge and Component Fractions

생약의 Benzodiazepine 수용체 효능활성 검색(III) 생약복합제제 추출물 및 성분분획의 활성

  • 이동웅 (동국대학교 자연과학대학 생화학과) ;
  • 하정희 (영남대학교 의과대학 약리학교실) ;
  • 강병수 (동국대학교 한의과대학 본초학교실) ;
  • 이갑득 (동국대학교 자연과학대학 화학과)
  • Published : 2000.08.01

Abstract

This study was attempted to evaluate an agonistic activity to benzodiazepine receptor of several medicinal pants, which have been used as sedatives in oriental medicine. The activities of the methanol extracts of composite preparation of oriental drugs were compared with those of the simple drugs, furthermore, the active fraction was found out from the simple preparation. Inhibitory effects of composite preparations, Cyperus rotundus/Acorus gramineus, Thuja orientalis/Euphoria longan, Thuja orientalis/Albizzia julibrissin, on the binding of ${[^3H]}$Ro15-1788, a selective benszodiazepine receptor antagonist to benzodiazepine receptor of rat cortices, were observed to be lower than those of corresponding simple preparations. These unexpected results suggest that some components of the composite druge may rather act as an obstacle, not to show the sinergistic effect. The methanol extracts of Cyperus rotundus having the highest activity were fractionated using polar and nonpolar solvents to give ethylacetate and hexane fractions, respectively. The ethylacetate fraction containing relatively polar components exhibited much higher activity than the hexane fraction, which consiste of nonpolar agonist, binding to benzodiazepine receptor. However, in the presence of GABA, this fraction inhibited ${[^3H]}$flunitrazepan binding, and these positive GABA shift supported the strong possibility of agonistic activity to benzodiazepine receptro. As a result, it may be concluded that the substance or substances with neurochemical properties as a benzodiazepine receptor agonist may contribute to the sedative property of Cyperus rotundus.

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