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Updated: Jun 14, 2025

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment
Published on: December 3, 2020
Study on the uptake of Gastrodin in the liver
Xing Wang1, Wenzhu Yang2, Jitong Lv2
1College of Medicine, Southwest Jiaotong University, No. 111, Chengdu North 2nd Ring Road, Chengdu, Sichuan, 610003, China.
Background:
Gastrodin is the active monomer of the Chinese herb Rhizoma Gastrodiae with the largest quantity of active components. Gastrodin is commonly used in the treatment of central nervous system disorders such as headaches and epilepsy due to its sedating and hypnotic properties. Its pharmacological mechanism and clinical application have been extensively explored due to its low toxicity.
Methods:
To investigate the molecular mechanism of hepatic uptake of Gastrodin in rats, animals were randomly assigned to three groups: control group, rifampicin (RIF) group, and adrenalone (ADR) group. Blood samples were collected through the cardiac puncture 90, 180, and 300 min after injection, respectively. Rats were sacrificed 300 min after administration, and liver tissue was collected. Gastrodin concentration was determined by HPLC, and the Kp value was calculated.
Results:
After administering the inhibitors of organic cation transporters (OCTs) and organic anion transporting polypeptides (OATPs), the KP values in the experimental groups were significantly lower compared to the blank control group (P < 0.05).
Conclusions:
These findings imply that Gastrodin may be a substrate for both OCTs and OATPs.
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