Neuroprotective Principles from Gastrodia elata

• Published in: Journal of natural products (Washington, D.C.) Vol. 70; no. 4; pp. 571 - 574
• Main Authors: Huang, Nai-Kuei, Chern, Yijuang, Fang, Jim-Min, Lin, Chia-I, Chen, Wan-Ping, Lin, Yun-Lian
• Format: Journal Article
• Language: English
• Published: Washington, DC American Chemical Society 01-04-2007; Glendale, AZ American Society of Pharmacognosy
• Subjects: Adenosine - analogs & derivatives; Adenosine - chemistry; Adenosine - isolation & purification; Adenosine - pharmacology; Animals; apoptosis; Apoptosis - drug effects; Biological and medical sciences; bis(4-hydroxybenzyl)sulfide; chemical structure; cultured cells; Disease Models, Animal; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - isolation & purification; Drugs, Chinese Herbal - pharmacology; Gastrodia - chemistry; Gastrodia elata; General pharmacology; Medical sciences; medicinal plants; Molecular Structure; N-(4-hydroxybenzyl)adenine riboside; neurons; Neuroprotective Agents - chemistry; Neuroprotective Agents - isolation & purification; Neuroprotective Agents - pharmacology; neuroprotective effect; Oriental traditional medicine; PC12 Cells - drug effects; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; phytochemicals; Plants, Medicinal - chemistry; Rats; Receptor, Adenosine A2A - drug effects; Serum - metabolism; spectral analysis; Sulfides - chemistry; Sulfides - isolation & purification; Sulfides - pharmacology; Taiwan; Asia; China; Monocotyledones; Purine nucleoside; Rat; Adrenal glands; Ligand; Organic sulfide; Medicinal plant; Prevention; A2A adenosine receptor; Folk medicine; Orchidaceae; Angiospermae; Rhizome; Below ground plant part; Pharmacognosy; Rodentia; Neuroprotective agent; In vitro; Biological activity; Vertebrata; Biological fixation; Mammalia; Cell line; Neuron; Cytoprotector; Animal; Plant origin; Phenols; Affinity; Isolation; Spermatophyta; Ribonucleoside; Apoptosis
• ISSN: 0163-3864; 1520-6025
• DOI: 10.1021/np0605182

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 N 6-(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 μM and 3.7 × 10-8 M, respectively, and IC50 values of 42.90 μM (K i 24.10 μM) and 4.660 μM (K i 2.620 μM), respectively, in an adenosine A2A receptor binding assay.