Abstract

Gastrodin (GAS), the main bioactive component of G. elata Blume, has important pharmaceutical and functional activities. The aim of this study is to produce GAS from p-2-hydroxybenzyl alcohol (HBA) through biotransformation. The conversion of exogenous HBA into GAS compound was conducted using cell suspension cultures of Armillaria luteo-virens Sacc. The bioconversion conditions were fully optimized with response surface methodology (RSM), turning out that the optimal transformation conditions composed of 3 mg/mL HBA, 6.5 g/30 mL inoculums level, 1.5% Tween 80, pH 4.5, and transformation temperature at 23°C. Under the optimized conditions, the conversion productivity of GAS reached the highest value (5.65 ± 0.45 mg/L). Verified experiments further validated that the optimized conditions were suitable for predicting the actual process of HBA transformation in the resting-cell system. The bioconversion kinetics model was as well simulated with Michaelis–Menten equation, which showing the suitability. The present study proposed the biotransformation pathway of HBA into GAS by resting cells transformation, indicating that the biotransformation process involved glucosylation reaction. Furthermore, Imprinting Control Region (ICR) mice in vivo demonstrated that the identified gastrodin possessed a significant anti-inflammatory activity. The fundamental data in the present work provides an efficient way to produce GAS through the whole-cells biocatalysis.

Highlights

  • Gastrodin, the bioactive component of G. elata Blume, has sedative and anticonvulsant functions, neuroprotective effect, facilitating memory consolidation, retrieval, antioxidant and free radical scavenging activities [1,2] Recent studies have focused mainly on the extraction, identification, quantification and pharmaceutical activity of functional compounds from Gastrodia elata Blume [3,4,5,6]

  • Biotransformation is a useful tool for modifying structures of biologically active compounds owing to its so many good advantages as high stereo- and region-selectivity, mild reaction condition, simple operation procedure [9] and more approached to examine the metabolism of natural products [10] compared with chemical synthesis

  • The optimization of GAS production was carried out using Box-Wilson Central composite design (CCD) with four star points and five replicates at center point for each of the four factors, with other factors fixed at suitable levels

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Summary

Introduction

The bioactive component of G. elata Blume, has sedative and anticonvulsant functions, neuroprotective effect, facilitating memory consolidation, retrieval, antioxidant and free radical scavenging activities [1,2] Recent studies have focused mainly on the extraction, identification, quantification and pharmaceutical activity of functional compounds from Gastrodia elata Blume [3,4,5,6]. There are still many researches focusing on obtaining GAS from p-2-hydroxybenzyl alcohol (HBA) or p-hydroxybenzaldehyde (HBD) through biotransformation. Biotransformation is a useful tool for modifying structures of biologically active compounds owing to its so many good advantages as high stereo- and region-selectivity, mild reaction condition, simple operation procedure [9] and more approached to examine the metabolism of natural products [10] compared with chemical synthesis. The characteristic of biocatalysts as converting exogenous substrates to region- and stereo- selectively useful substances under mild conditions is one of great interests, since some of the resulted products are not easy to prepare through biotransformation or synthetic chemical methods [11]. There have been literatures on the glycosylation of exogenously supplied phenolic compounds through the cultured plant cells [17,18,19]

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