Gastrodin

Gastrodin, a phenolic glycoside that chemically known as 4-hydroxybenzyl alcohol-4-O-β-D-glucopyranoside (figure 1), is the main active ingredient of gastrodia elata. Gastrodin is usually obtained by extraction from a plant or through chemical synthesis. However, the resources of wild gastrodia elata have become fewer and fewer due to over-exploitation. Moreover, both of the two methods have complicated procedures with high cost, produce too many by-products with serious pollution and waste natural resources as well. The novel approach to the production of gastrodin through biosynthesis and microbial transformation is drawing increasing attention.

Fig. 1 Gastrodia elata and chemical structure of gastrodin

Biosynthesis of Gastrodin

Generally, toluene is considered as a precursor of gastrodin. the catalytic pathway from toluene to 4-hydroxybenzyl alcohol has been reported to involve hydroxylation through monooxygenase of cytochrome P450, a member of a large enzyme family in plants that catalyzes most of the oxidation steps in plant secondary metabolism. Gastrodin production is derived from 4-hydroxybenzyl alcohol through a one-step glycosylation with different glucose donors, as shown in figure 2. In this process, the key enzyme in gastrodin biosynthesis is glucosyltransferase which is a large family identified in various plants^[1,2].

Fig. 2 Biosynthetic pathway of gastrodin

Compared to the extraction from a plant or through chemical synthesis, biosynthesis of gastrodin is extremely selective and highly reactive under a broad range of experimental conditions. Besides, it can use a wide array of complex molecules as substrates, yielding products with high selectivity and few by-products, therefore making it an environmentally friendly alternative to traditional extraction and chemical catalysts.

Applications

In recent decades, many experiments have been conducted on its pharmacological properties, and the results showed that gastrodin has various therapeutic effects including neuroprotective, anti-inflammatory, antioxidative, antiepileptic, anticonvulsive, antipsychotic, anxiolytic, antidepressant, circulatory system modulating, memory-improving effects, etc.

Among its various pharmacological properties, its strong actions in central nervous system (CNS) diseases appear to be particularly prominent. Considering its low toxicity and remarkable pharmacological performance, gastrodin may be a potential valuable therapeutic for the prevention and treatment of some CNS disorders^[3]. The underlying mechanism of gastrodin in preclinical models of CNS disorders including epilepsy, Alzheimer’s disease, Parkinson’s disease, affective disorders, cerebral ischemia/reperfusion, and cognitive impairment is summarized in figure 3.

Fig. 3 Mechanisms of action of gastrodin in CNS disorders

Our Gastrodin

Basic properties of our biosynthetic gastroin are listed as followings:

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References

1. Tsai, C.-C., Wu, K.-M., Chiang, T.-Y., et al. Comparative transcriptome analysis of Gastrodia elata (Orchidaceae) in response to fungus symbiosis to identify gastrodin biosynthesis-related genes. BMC Genomics, 2016, 17(1).
2. XU De-hong, CUI Pei-wu, LUO Huai-hao, et al. Research progress on biosynthesis of gastrodin. Chinese Traditional and Herbal Drugs, 2020, 51 (22).
3. Liu, Y., Gao, J., Peng, M., et al. A Review on Central Nervous System Effects of Gastrodin. Frontiers in Pharmacology, 2018, 9.

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