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ORIGINAL RESEARCH article

Front. Pharmacol.

Sec. Ethnopharmacology

Volume 16 - 2025 | doi: 10.3389/fphar.2025.1624576

This article is part of the Research TopicBioactive Metabolites in Traditional Medicine: Dual Pathways to Metabolic HealthView all 5 articles

Pharmacokinetics and brain tissue distribution of Gastrodia elata extract in normal and cerebral ischemic rats: A comparative study

Provisionally accepted
Ji  ShaoJi Shao1Yunyun  LuoYunyun Luo2Qi  XuQi Xu1Ting  DongTing Dong2Xue  HanXue Han1Bilian  ChenBilian Chen2Qiaojuan  ShiQiaojuan Shi1*Cuifen  FangCuifen Fang2*Huazhong  YingHuazhong Ying1*
  • 1Hangzhou Medical College, Hangzhou, China
  • 2Zhejiang lnstitute for Food and Drug Control, HangZhou, China

The final, formatted version of the article will be published soon.

Objective: This study systematically investigated the pharmacokinetic characteristics, cerebral distribution, and metabolic transformation of Gastrodia elata components in both healthy and cerebral ischemia rat models. Methods: Chemical profiling of Gastrodia elata was conducted using UPLC-Q-TOF-MS. Based on the systemically absorbed constituents identified in plasma and brain tissues of dosed rats, a validated UPLC-QQQ-MS method was established to quantitatively determine target compound levels in plasma and brain tissues of both normal and cerebral ischemic rats following 3-day oral administration. Subsequently, UPLC-Q-TOF-MS was reapplied to conduct identification and comparative analysis of xenobiotic metabolites in both in vivo systems and brain tissues. Results: Based on the established therapeutic efficacy of Gastrodia elata extract against cerebral ischemia-reperfusion injury, chemical profiling identified 53 constituents, among which six were simultaneously detected in plasma and brain tissue of dosed rats. The established simultaneous quantitative analytical method demonstrated reduced gastrointestinal absorption of parishin A, parishin B, parishin C, parishin E and gastrodin in ischemic model rats compared to healthy controls. Notably, brain accumulation of these compounds was significantly increased in ischemic models, attributable to compromised blood-brain barrier integrity. Xenobiotic metabolite analysis identified nine biotransformation products, four of which exhibited quantifiable exposure levels in brain tissues across all experimental groups. Conclusion: This study systematically revealed the bioactive components of Gastrodia elata and their cerebral distribution patterns. The pharmacokinetic characteristics of gastrodin and related bioactive compounds were also elucidated. These findings provide a valuable reference for pharmacological exploration, safety evaluation, and clinical application of Gastrodia elata in cerebrovascular disorders.

Keywords: Gastrodia elata, cerebral ischemia, pharmacokinetics, Brain tissue distribution, Xenobiotic metabolite identification

Received: 07 May 2025; Accepted: 07 Jul 2025.

Copyright: © 2025 Shao, Luo, Xu, Dong, Han, Chen, Shi, Fang and Ying. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

* Correspondence:
Qiaojuan Shi, Hangzhou Medical College, Hangzhou, China
Cuifen Fang, Zhejiang lnstitute for Food and Drug Control, HangZhou, China
Huazhong Ying, Hangzhou Medical College, Hangzhou, China

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