Neuroprotective principles from Gastrodia elata.
Serum deprivation-induced neuronal-like PC12 cell apoptosis was used as an ischemic/hypoxic model to screen neuroprotective compounds from the rhizomes of Gastrodia elata, a traditional Chinese medicine. Two active compounds, bis(4-hydroxybenzyl)sulfide (1) and N6-(4-hydroxybenzyl)adenine riboside (2), together with 15 known compounds were obtained from the active fraction. Compound 2 was further elucidated by chemical synthesis. Compounds 1 and 2 potently prevented PC12 cell apoptosis in concentration-dependent manners with EC50 values of 7.20 microM and 3.7 x 10-8 M, respectively, and IC50 values of 42.90 microM (Ki 24.10 microM) and 4.660 microM (Ki 2.620 microM), respectively, in an adenosine A2A receptor binding assay.
Huang
Nai-Kuei
NK
National Research Institute of Chinese Medicine, Taipei 112, Taiwan, Republic of China, Institute of Biomedical Sciences, Academia Sinica, Nankang, Taipei 115, Taiwan, Republic of China.
Chern
Yijuang
Y
Fang
Jim-Min
JM
Lin
Chia-I
CI
Chen
Wan-Ping
WP
Lin
Yun-Lian
YL
D000241:Adenosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D004195:Disease Models, Animal; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D031668:Gastrodia / Q000737:chemistry*; D015394:Molecular Structure; D018696:Neuroprotective Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D016716:PC12 Cells / Q000187:drug effects; D010946:Plants, Medicinal / Q000737:chemistry*; D051381:Rats; D043705:Receptor, Adenosine A2A / Q000187:drug effects; D044967:Serum / Q000378:metabolism; D013440:Sulfides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
D004365:Drugs, Chinese Herbal; C519742:N6-(4-hydroxybenzyl)adenine riboside; D018696:Neuroprotective Agents; D043705:Receptor, Adenosine A2A; D013440:Sulfides; C477166:bis(4-hydroxybenzyl)sulfide; D000241:Adenosine