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ORIGINAL RESEARCH article

Front. Pharmacol.
Sec. Experimental Pharmacology and Drug Discovery
Volume 15 - 2024 | doi: 10.3389/fphar.2024.1437806

Design, synthesis and neuroprotective activity of compound derived from Gastrodia elata Blume and borneol

Provisionally accepted
Lijuan Zhi Lijuan Zhi 1Huan Li Huan Li 1Baimei Shi Baimei Shi 2Tao Yu Tao Yu 1*Xiaoni Jia Xiaoni Jia 1*Hui Zhang Hui Zhang 1*
  • 1 Center Laboratory, Xi’an Mental Health Center, Xi’an, China
  • 2 College of Chemical Engineering, Xi’an University, Xi’an, China

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

    Traditional Chinese medicine Gastrodia elata Blume (GEB) possesses properties that soothe the liver and dispel wind. Its constituents exhibit numerous pharmacological properties, including neuroprotective effects, analgesic properties for headache relief, memory enhancement, and others. Borneol enhances drug absorption by traversing the blood-brain barrier, thereby improving its bioavailability and therapeutic efficacy. This paper adopts the strategy of "compound Chinese medicine molecular chemistry" to integrate and fuse the effective substances of compound Chinese medicines, aiming to design innovative drug molecules and contribute to the beneficial exploration of compound Chinese medicine modernization. We designed and synthesized compounds TB-1 to TB-16. Following the evaluation of their safety, TB-1, TB-2, TB-12, and TB-16 were selected for further investigation of their neuroprotective properties. The compound designed in this study exhibits a dose-dependent protective effect on glutamate-damaged PC12 cells. Further network pharmacology and molecular docking analyses indicate that TB-2 possesses a potential therapeutic effect against cerebral ischemia, and its possible targets were SRC, MAPK1 and KDR.

    Keywords: Gastrodia elata Blume, Borneol, Neuroprotection, Glutamate, cerebral ischemia

    Received: 13 Jun 2024; Accepted: 10 Sep 2024.

    Copyright: © 2024 Zhi, Li, Shi, Yu, Jia and Zhang. 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:
    Tao Yu, Center Laboratory, Xi’an Mental Health Center, Xi’an, China
    Xiaoni Jia, Center Laboratory, Xi’an Mental Health Center, Xi’an, China
    Hui Zhang, Center Laboratory, Xi’an Mental Health Center, Xi’an, China

    Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.