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Two new terpenoids from Reduning Injection.

Hai-Bo Li1,2, Biao Yang1,2, Wen Ge3

  • 1Jiangsu Kanion Pharmaceutical Co., Ltd., Lianyungang 222001, China.

Chinese Herbal Medicines
|September 19, 2022
PubMed
Summary

Researchers identified two new terpenoids from Reduning Injection, a traditional medicine. One compound demonstrated significant anti-inflammatory effects by inhibiting TNF-α production in cell-based assays, highlighting its therapeutic potential.

Keywords:
(1R,7R,8S,10R)-7,8,11-trihydroxy-4-guaien-3-oneReduning InjectionTNF-αanti-inflammationjasminoide A

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Area of Science:

  • Natural Product Chemistry
  • Pharmacology
  • Immunology

Background:

  • Reduning Injection (RDN) is a traditional medicine utilized for its antipyretic and anti-inflammatory properties.
  • Identifying the specific active constituents responsible for RDN's therapeutic effects is crucial for understanding its mechanism of action and potential pharmaceutical development.

Purpose of the Study:

  • To isolate and characterize the antipyretic and anti-inflammatory compounds present in the active fraction of Reduning Injection.
  • To evaluate the in vitro anti-inflammatory activity of the isolated compounds.

Main Methods:

  • The active fraction of Reduning Injection was identified using an LPS-induced mouse endotoxin shock model.
  • Chemical constituents were isolated using various chromatographic techniques, including HP-20 macroporous adsorptive resins, silica gel, ODS columns, and reverse-phase MPLC/HPLC.
  • Structural elucidation was performed using advanced spectroscopic methods (HR-ESI-MS, NMR, ECD) and chemical analyses. Anti-inflammatory activity was assessed by measuring TNF-α production in LPS-stimulated RAW 264.7 macrophages.

Main Results:

  • The 95% ethanol eluate of Reduning Injection was confirmed as the active fraction with antipyretic and anti-inflammatory properties.
  • Two novel terpenoids were isolated: a new iridoid, jasminoide A (1), and a new guaiane sesquiterpenoid, (1R,7R,8S,10R)-7,8,11-trihydroxy-4-guaien-3-one (2).
  • Compound 2 exhibited inhibitory activity against TNF-α production with an IC50 value of 72.24 µmol/L.

Conclusions:

  • This study successfully isolated and identified two new terpenoids from Reduning Injection.
  • Compound 2 demonstrated significant in vitro anti-inflammatory activity by inhibiting TNF-α production, suggesting its potential as a therapeutic agent.