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Antinociceptive activity of doliroside B
Xishan Bai1, Yanhong Li1, Yuxiao Li1
1Key Laboratory of Chemistry in Ethnic Medicinal Resources, State Ethnic Affairs Commission & Ministry of Education, School of Ethnic Medicine, Yunnan Minzu University, Kunming, China.
Pharmaceutical Biology
|January 11, 2023
Summary
Doliroside B disodium salt (DBDS) from Dolichos trilobus demonstrates significant pain relief by targeting multiple pathways, including COX-1 inhibition and modulation of GABA receptors. This natural compound shows promise as a novel analgesic agent.
Area of Science:
- Pharmacology
- Natural Products Chemistry
- Pain Management
Background:
- Dolichos trilobus Linn (Leguminosae) is utilized in traditional Yi ethnic medicine for treating pain, fractures, and rheumatism.
- Exploring the therapeutic potential of compounds derived from medicinal plants is crucial for novel drug discovery.
Purpose of the Study:
- To investigate the pain-relieving effects of doliroside B (DB) and its disodium salt (DBDS) from Dolichos trilobus.
- To elucidate the underlying mechanisms of DBDS-mediated analgesia.
Main Methods:
- DB and DBDS were administered orally to mice in writhing, hot plate, and formalin tests.
- In vitro studies utilized lipopolysaccharide-induced RAW264.7 macrophages to investigate the mechanism of action.
- Enzyme activity assays and receptor function modulation were assessed.
Main Results:
- DBDS (5 mg/kg) exhibited significant antinociceptive activity, inhibiting writhing by 80.2%.
- DBDS selectively inhibited COX-1 activity and reduced nitric oxide (NO), inducible nitric oxide synthase (iNOS), and interleukin-6 (IL-6) production.
- DBDS positively modulated GABAA1 receptor function.
Conclusions:
- DBDS possesses potent antinociceptive properties acting on both peripheral and central nervous systems.
- The multi-target action of DBDS suggests its potential as a novel therapeutic agent for pain management.
- Further research is recommended to develop DBDS into a viable drug for pain treatment.
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