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Planta Med 2001; 67(9): 877-880
DOI: 10.1055/s-2001-18844
Letter

© Georg Thieme Verlag Stuttgart · New York

In vitro Effects of Hydroxybenzaldehydes from Gastrodia elata and their Analogues on GABAergic Neurotransmission, and a Structure-Activity Correlation

Jeoung-Hee Ha1 , Son-Moon Shin2 , Soo-Kwan Lee3 , Jin-Sook Kim4 , Uk-Seob Shin4 , Keun Huh4 , Jung-Ae Kim4 , Chul-Soon Yong4 , Nam-Jae Lee5 , Dong-Ung Lee5
  • 1 Department of Pharmacology, College of Medicine, Yeungnam University, Taegu, Korea
  • 2 Department of Pediatrics, Sungkyunkwan University, School of Medicine, Samsung Cheil Hospital, Korea
  • 3 Department of Pediatrics, College of Medicine, Yeungnam University, Taegu, Korea
  • 4 College of Pharmacy, Yeungnam University, Gyongsan, Korea
  • 5 Department of Biochemistry, College of Natural Science, Dongguk University, Kyongju, Korea
Further Information

Publication History

December 19, 2000

March 4, 2001

Publication Date:
06 December 2001 (online)

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Abstract

The present study was designed to characterize the modulatory effects of the constituents of Gastrodia elata and their analogues on the GABAergic neurotransmission. 4-Hydroxybenzaldehyde (1) and 4-hydroxy-3-methoxybenzaldehyde (4) inhibited potently the activity of GABA transaminase (IC50 = 4.1 and 5.4 μg/ml, respectively), while the activity of another constituent, 4-hydroxybenzyl alcohol (2), was very weak. Further investigation with 10 analogues revealed a structure-activity correlation, suggesting that the aldehyde group and the hydroxy group at C-4 are necessary for the inhibitory effect on the enzyme activity. Some potent enzyme inhibitors were examined for the effect on the radioligands to the GABAA receptor complexes of rat cerebral cortices. Among them, the component 4 dose-dependently increased (20 - 30 %) the binding of [3 H]flunitrazepam in the presence of GABA.

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Prof. Dr. Dong-Ung Lee

Department of Biochemistry

College of Natural Science

Dongguk University

Kyongju 780-714

Korea

Email: dulee@mail.dongguk.ac.kr

Fax: +82-54-742-9833

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