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January 20, 20261 citations

Acanthospermum hispidum and Its Metabolite Stigmasterol Modulates Anti-Inflammatory Antagonism of COX-1 and TGF-β.

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OAOnome Mary AdeboyeASAbimbola SowemimoMFMuyiwa Samuel Fageyinbo

Key Points

  • To investigate the anti-inflammatory effects of Acanthospermum hispidum and its metabolite stigmasterol, and elucidate their mechanism of action.
  • Evaluated anti-inflammatory activity using carrageenan, histamine and serotonin-induced rat paw oedema
  • Conducted molecular docking studies on receptors related to inflammation
  • Tested various doses of AH extract (50-200 mg/kg)
  • Identified the most active fraction F1 and analyzed stigmasterol's binding affinities
  • AH extract significantly inhibited inflammation at doses of 100, 150, and 200 mg/kg
  • Peak inhibition occurred at 100 mg/kg with significant results (p < 0.01)
  • Dose-dependent increase in activity observed from T30 to T150
  • Stigmasterol showed strong antagonistic effects on COX-1 and COX-II with binding affinities of -8.9 kcal/mol

Abstract

Acanthospermum hispidum (AH) leaves have been widely used in traditional medicine for inflammation. In this study, the anti-inflammatory effect of AH was evaluated, and a possible mechanism was predicted using an in silico model. The in vivo anti-inflammatory activity of the AH extract was carried out using carrageenan, histamine and serotonin-induced rat paw oedema, whereas molecular docking was used against all receptors implicated with inflammation. AH extract showed significant (p < 0.01) inhibition at 50, 100, 150 and 200 mg/kg with all the models used (p ˂ 0.05 to ˂0.0001) with a non-significant decrease at T180; there were significances at some dose levels (e.g., 150 and 200 mg/kg). The peak percentage inhibition of the extract occurred at a dose of 100 mg/kg. A dose-dependent increase in anti-inflammatory activity was noted across the time examined T30-T150 with a non-significant decrease at T180. F1 was found to be the most active fraction. However, stigmasterol showed a potent antagonist influence on COX-1, COX-II, CAT and INF-gamma by showing binding affinities of -8.9, -8.9, -8.8 and -8.4 kcal/mol, respectively. Moreover, alkyl, carbon-hydrogen, conventional hydrogen and van der Waals interactions were noted. Stigmasterol was observed to obey the Lipinski rule of five except MLOGP. These findings justify the ethnomedicinal information of the usage of AH in the management of inflammation and related ailments.

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Cite This Study

Adeboye et al. (2026) studied this question.

synapsesocial.com/papers/696f1a239e64f732b51ee5b2https://doi.org/10.1002/cbdv.202501647
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