Flavones from Struthiola argentea with anthelmintic activity in vitro

Area of Science:

• Natural Product Chemistry
• Parasitology
• Medicinal Chemistry

Background:

• Helminth parasitic diseases pose significant threats to animal health and cause substantial economic losses.
• Existing anthelmintics face increasing resistance, necessitating the development of new drugs with novel mechanisms of action.

Purpose of the Study:

• To isolate and characterize bioactive compounds with anthelmintic properties from Struthiola argentea.
• To evaluate the in vitro and in vivo anthelmintic efficacy of isolated compounds.
• To investigate structure-activity relationships of isolated flavones.

Main Methods:

• Bioassay-guided fractionation of the methanol extract of Struthiola argentea.
• Structure elucidation of isolated compounds using 1D and 2D NMR and Mass Spectrometry (MS).
• In vitro assessment of larval motility inhibition and in vivo testing of anthelmintic activity.

Main Results:

• Three anthelmintic flavones (1-3) were isolated, including 5,6,2',5',6'-pentamethoxy-3',4'-methylenedioxyflavone (3).
• Compound 3 demonstrated potent in vitro activity, achieving 90% inhibition of larval motility at 3.1 microg/mL.
• Related flavones were tested, and compound 15 showed modest in vivo activity.

Conclusions:

• Struthiola argentea is a source of potent anthelmintic flavones.
• Compound 3 represents a promising candidate for further development as a novel anthelmintic agent.
• Structure-activity relationship studies provide insights for designing more effective anti-parasitic compounds.