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<p>Guided by the MS/MS-based molecular networking, eight previously undescribed clerodane diterpenoid glycosides, designated tinospinosides F–M (<b>1</b>−<b>8</b>), along with 12 known analogues (<b>9</b>−<b>20</b>), were isolated from the tuberous roots of <i>Paratinospora sagittata</i>. Structural elucidation of the undescribed compounds was achieved through comprehensive spectroscopic analyses (NMR, HRESIMS), with their absolute configurations confirmed via single-crystal X-ray diffraction, TD-DFT/ECD computational analyses, and chemical degradation. Immunomodulation evaluation on all the isolates revealed that compounds <b>6</b> and <b>7</b> exerted significant promoting effect toward NO production in RAW264.7 macrophages. Further study demonstrated that <b>6</b> could enhance the release of immune cytokines (e.g., TNF-<i>α</i>) and upregulate the protein expression of iNOS and COX-2, which was potentially mediated through the activation of NF-κB signaling pathway.</p> Graphical Abstract <p></p>

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Clerodane diterpenoid glycosides from the tuberous roots of Paratinospora sagittata: targeted isolation, structure characterization and immunomodulatory properties

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年2月2日

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  • Jun-Sheng Zhang,
  • Rui Ao,
  • Yin-Bo Pan,
  • Xin-Cheng Zhuang,
  • Yi-Ke Yin,
  • Jie Bao,
  • Hua Zhang

摘要

Guided by the MS/MS-based molecular networking, eight previously undescribed clerodane diterpenoid glycosides, designated tinospinosides F–M (1−8), along with 12 known analogues (9−20), were isolated from the tuberous roots of Paratinospora sagittata. Structural elucidation of the undescribed compounds was achieved through comprehensive spectroscopic analyses (NMR, HRESIMS), with their absolute configurations confirmed via single-crystal X-ray diffraction, TD-DFT/ECD computational analyses, and chemical degradation. Immunomodulation evaluation on all the isolates revealed that compounds 6 and 7 exerted significant promoting effect toward NO production in RAW264.7 macrophages. Further study demonstrated that 6 could enhance the release of immune cytokines (e.g., TNF-α) and upregulate the protein expression of iNOS and COX-2, which was potentially mediated through the activation of NF-κB signaling pathway.

Graphical Abstract