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2000
Volume 25, Issue 8
  • ISSN: 1568-0266
  • E-ISSN: 1873-4294

Abstract

Background

In continuation of our chemical and biological work on we evaluated the antipyretic activity of its extract which on fractionation gives a pure alkaloid galegine. Galegine a bioprivileged compound, is a hemiterpene bearing a guanidine group, which holds significant importance in medicinal chemistry. Biological activities such as antimicrobial, antidiabetic, anti-inflammatory, cardiovascular, anticancer, and antihypertensive, are often associated with guanidine-containing molecules.

Objective

Given the biological importance of guanidine and in search of safe antipyretic agents from natural resources, an antipyretic activity of methanolic extract of and galegine was conducted to discover a potential hypothermic drug candidate from the plant.

Methods

the antipyretic activity of galegine (5, 25, and 50 mg/kg doses) and methanolic extract of (50, 100, and 200 mg/kg doses) was investigated by employing yeast-induced pyrexia in mice model. molecular docking analysis involving target enzymes cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), and microsomal prostaglandin E synthase-1 (mPGES-1) was conducted. Additionally, galegine underwent ADME/T profiling using SwissADME and Protox-II tools to evaluate its bioavailability and safety profiles.

Results

Both the extract and galegine showed a progressive dose-dependent reduction in body temperatures of the hyperthermic test animals. Moreover, molecular docking analysis revealed significant binding affinities ranging from -3.58 to -5.41 kcal/mol. ADME/T analyses of galegine predicted its high drug-likeness and good safety profile.

Conclusion

These biological and computational approaches supported in addressing pyrexia, with the isolated compound galegine emerging as a promising antipyretic agent.

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Galegine, a Bioprivileged Alkaloid from Tithonia tubaeformis: Antipyretic Activity Insights
Curr. Top. Med. Chem. 25, 943 (2025); https://doi.org/10.2174/0115680266333237241212071912
/content/journals/ctmc/10.2174/0115680266333237241212071912
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  • Article Type:     Research Article
Keyword(s): Galegine; guanidine derivative; hemiterpene; natural products; pyrexia; Tithonia tubaeformis

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