2. Academic Validation
  3. Dissecting the antitumor effects of Scutellaria barbata: Initial insights into the metabolism of scutellarin and luteolin by gut microbiota

Dissecting the antitumor effects of Scutellaria barbata: Initial insights into the metabolism of scutellarin and luteolin by gut microbiota

  • J Pharm Biomed Anal. 2024 Sep 15:248:116325. doi: 10.1016/j.jpba.2024.116325.
Xianfeng Zhang 1,  Jingyue Wang 2,  Jie Fu 3,  Jiachun Hu 3,  Haojian Zhang 3,  Mengliang Ye 3,  Xinyu Yang 3,  Hang Yu 3,  Hui Xu 3,  Jinyue Lu 3,  Zhao Zhai 3,  Hengtong Zuo 3,  Xiang Hui 3,  Jianye Song 3,  Yi Zhao 3,  Qian Tong 4,  Yan Wang 5
Affiliations

Affiliations

  • 1 Department of Neurosurgery, The First Hospital of Jilin University, Changchun 130000, China.
  • 2 State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences/Peking Union Medical College, Beijing 100050, China; Department of Cardiovascular Medicine, The First Hospital of Jilin University, Changchun 130000, China.
  • 3 State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences/Peking Union Medical College, Beijing 100050, China.
  • 4 Department of Cardiovascular Medicine, The First Hospital of Jilin University, Changchun 130000, China. Electronic address: tongqian@jlu.edu.cn.
  • 5 State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences/Peking Union Medical College, Beijing 100050, China. Electronic address: wangyan@imm.ac.cn.
PMID: 38959755 DOI: 10.1016/j.jpba.2024.116325
Abstract

The high prevalence of Cancer and detrimental side effects associated with many Cancer treatments necessitate the search for effective alternative therapies. Natural Products are increasingly being recognized and investigated for their potential therapeutic benefits. Scutellaria barbata D. Don (SBD), a plant with potent antitumor properties, has attracted significant interest from oncology researchers. Its primary flavonoid components-scutellarin and luteolin-which have limited oral bioavailability due to poor absorption. This hinders its application for Cancer treatment. The gut microbiota, which is considered a metabolic organ, can modulate the biotransformation of compounds, thereby altering their bioavailability and efficacy. In this study, we employed liquid chromatography tandem mass spectrometry (LC-MS/MS 8060) and ion trap-time of flight (LC-MSn-IT-TOF) analysis to investigate the ex vivo metabolism of scutellarin and luteolin by the gut microbiota. Five metabolites and one potential metabolite were identified. We summarized previous studies on their antitumor effects and performed in vitro tumor cell line studies to prove their antitumor activities. The possible key pathway of gut microbiota metabolism in vitro was validated using molecular docking and pure Enzyme metabolic experiments. In addition, we explored the antitumor mechanisms of the two components of SBD through network pharmacology, providing a basis for subsequent target identification. These findings expand our understanding of the antitumor mechanisms of SBD. Notably, this study contributes to the existing body of knowledge regarding flavonoid biotransformation by the gut microbiota, highlighting the therapeutic potential of SBD in Cancer treatment. Moreover, our results provide a theoretical basis for future in vivo pharmacokinetic studies, aiming to optimize the clinical efficacy of SBD in oncological applications.

Keywords

Gut microbiota; LC/MS(n)-IT-TOF; LC‒MS/MS; Metabolism; Scutellaria barbata D. Don.

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